U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C22H24BrFN4O2
Molecular Weight 475.354
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VANDETANIB

SMILES

COC1=CC2=C(NC3=CC=C(Br)C=C3F)N=CN=C2C=C1OCC4CCN(C)CC4

InChI

InChIKey=UHTHHESEBZOYNR-UHFFFAOYSA-N
InChI=1S/C22H24BrFN4O2/c1-28-7-5-14(6-8-28)12-30-21-11-19-16(10-20(21)29-2)22(26-13-25-19)27-18-4-3-15(23)9-17(18)24/h3-4,9-11,13-14H,5-8,12H2,1-2H3,(H,25,26,27)

HIDE SMILES / InChI
Molecular Formula C22H24BrFN4O2
Molecular Weight 475.354
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/25982012

Vandetanib, 4-anilinoquinazoline, is an anti-cancer drug that with the potential for use in a broad range of tumour types. In 2011 vandetanib (trade name Caprelsa) was approved by the FDA to treat nonresectable, locally advanced, or metastatic medullary thyroid cancer in adult patients. In vitro studies have shown that vandetanib inhibits the tyrosine kinase activity of the EGFR and VEGFR families, RET, BRK, TIE2, and members of the EPH receptor and Src kinase families. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, and maintenance of the tumor microenvironment. Vandetanib was shown to inhibit epidermal growth factor (EGF)-stimulated receptor tyrosine kinase phosphorylation in tumor cells and endothelial cells and VEGF-stimulated tyrosine kinase phosphorylation in endothelial cells. Vandetanib administration reduced tumor cell-induced angiogenesis, tumor vessel permeability, and inhibited tumor growth and metastasis in mouse models of cancer.

CNS Activity

Originator

Approval Year

2011
587
Targets

Targets

Primary TargetPharmacologyConditionPotency
Epidermal growth factor receptor
49
Target ID: P00533|||Q9GZX1
Gene ID: 1956.0
Gene Symbol: EGFR
Target Organism: Homo sapiens (Human)
Inhibitor
8504
 0.5 µM [IC50]
Vascular endothelial growth factor receptor 2
112
Target ID: P35968
Gene ID: 3791.0
Gene Symbol: KDR
Target Organism: Homo sapiens (Human)
Inhibitor
8504
 0.04 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
CAPRELSA

Approved Use

Indicated for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease. Use CAPRELSA in patients with indolent, asymptomatic or slowly progressing disease only after careful consideration of the treatment related risks of CAPRELSA.

Launch Date

2011
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2024 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000ClinPharmR.pdf
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VANDETANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
130 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000ClinPharmR.pdf
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VANDETANIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
38611 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000ClinPharmR.pdf
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VANDETANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
22030 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000ClinPharmR.pdf
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VANDETANIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7.6 day
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000ClinPharmR.pdf
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VANDETANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
204 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000ClinPharmR.pdf
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VANDETANIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
6%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000ClinPharmR.pdf
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VANDETANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1200 mg single, oral
Highest studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
https://pubmed.ncbi.nlm.nih.gov/22206795/
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
https://pubmed.ncbi.nlm.nih.gov/22206795/
Other AEs: Rash, Blood pressure systolic increased...
Other AEs:
Rash
Blood pressure systolic increased
Blood pressure diastolic increased
Sources:
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
https://pubmed.ncbi.nlm.nih.gov/22206795/
300 mg single, oral
Studied dose
Dose: 300 mg
Route: oral
Route: single
Dose: 300 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
Disc. AE: Vomiting...
AEs leading to
discontinuation/dose reduction:
Vomiting (grade 2)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
400 mg single, oral
Dose: 400 mg
Route: oral
Route: single
Dose: 400 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/22206795/
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/22206795/
Disc. AE: Eczema...
AEs leading to
discontinuation/dose reduction:
Eczema (grade 1)
Sources:
https://pubmed.ncbi.nlm.nih.gov/22206795/
800 mg single, oral
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/22206795/
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/22206795/
Disc. AE: Folliculitis...
AEs leading to
discontinuation/dose reduction:
Folliculitis (grade 2)
Sources:
https://pubmed.ncbi.nlm.nih.gov/22206795/
200 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
unhealthy, mean age 45.6 years
Health Status: unhealthy
Age Group: mean age 45.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
DLT: Hypophosphatemia, Diarrhea...
Dose limiting toxicities:
Hypophosphatemia (grade 3, 12.5%)
Diarrhea (grade 2, 12.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
600 mg 1 times / day multiple, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
DLT: Intestinal obstruction, Diarrhea...
Dose limiting toxicities:
Intestinal obstruction (grade 3, 12.5%)
Diarrhea (grade 3, 25%)
Colitis (grade 3, 12.5%)
Hypertension (grade 3, 12.5%)
Fatigue (grade 3, 12.5%)
Thrombocytopenia (grade 3, 12.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Disc. AE: Skin disorder, Asthenia...
Other AEs: Rash, Acneiform dermatitis...
AEs leading to
discontinuation/dose reduction:
Skin disorder (2.5%)
Asthenia (1.7%)
Fatigue (0.9%)
Pyrexia (0.9%)
Diarrhea (0.9%)
Creatinine increased (0.9%)
Electrocardiogram QTc interval prolonged (0.9%)
Hypertension (0.9%)
General physical health deterioration (0.4%)
Dysphagia (0.4%)
Nausea (0.4%)
Pancreatitis (0.4%)
Peritonitis (0.4%)
Small intestinal perforation (0.4%)
Vomiting (0.4%)
Systolic dysfunction (0.4%)
Chylothorax (0.4%)
Cough (0.4%)
Dysphonia (0.4%)
Dyspnea (0.4%)
Pneumonitis (0.4%)
Peripheral ischemia (0.4%)
Peripheral sensorimotor neuropathy (0.4%)
Vision blurred (0.4%)
Arthralgia (0.4%)
Germ cell cancer (0.4%)
Other AEs:
Rash (grade 3, 3.9%)
Acneiform dermatitis (grade 3, 0.9%)
Photosensitivity reaction (grade 3, 1.7%)
Generalized erythema (grade 3, 1.3%)
Skin exfoliation (grade 3, 0.4%)
Palmar-plantar erythrodysaesth. (grade 3, 0.4%)
Dermatitis bullous (grade 3, 0.4%)
Skin candida (grade 3, 0.4%)
Erysipelas (grade 3, 0.4%)
Pneumonitis (grade 3, 0.4%)
Dyspnea (grade 3, 1.7%)
Respiratory failure (grade 3, 0.8%)
Diarrhea (grade 3, 3%)
Nausea (grade 3, 1%)
Hypertension (grade 3, 6%)
Headache (grade 3, 1%)
Fatigue (grade 3, 6%)
Decreased appetite (grade 3, 4%)
Dermatitis acneiform (grade 3, <1%)
Vomiting (grade 3, 1%)
Asthenia (grade 3, 3%)
Abdominal pain (grade 3, 2%)
QT interval prolonged (grade 3, 8%)
Photosensitivity reaction (grade 3, 2%)
Hypocalcaemia (grade 3, 2%)
Pruritus (grade 3, 1%)
Weight decreased (grade 3, 1%)
Depression (grade 3, 2%)
ALT increased (grade 3, 2%)
Calcium decreased (grade 3, 6%)
Calcium increased (grade 3, 9%)
Glucose increased (grade 3, 2%)
Magnesium decreased (grade 3, <1%)
Potassium decreased (grade 3, <1%)
Potassium increased (grade 3, <1%)
Hemoglobin decreased (grade 3, <1%)
Neutrophil count decreased (grade 3, <1%)
WBC decreased (grade 3, <1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
500 mg 1 times / day multiple, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
DLT: Diarrhea, Folliculitis...
Disc. AE: Folliculitis...
Dose limiting toxicities:
Diarrhea (grade 2, 12.5%)
Folliculitis (grade 2, 12.5%)
ALT increased (grade 3, 12.5%)
Rash (grade 3, 12.5%)
AEs leading to
discontinuation/dose reduction:
Folliculitis (grade 3, 12.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
unhealthy, mean age 57.7 years
Health Status: unhealthy
Age Group: mean age 57.7 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
DLT: Rash...
Disc. AE: Congestive cardiac failure...
Dose limiting toxicities:
Rash (grade 2, 4%)
AEs leading to
discontinuation/dose reduction:
Congestive cardiac failure (grade 3, 4%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
100 mg 1 times / day multiple, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 50 years
Health Status: unhealthy
Age Group: median age 50 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
Other AEs: Lymphopenia...
Other AEs:
Lymphopenia (grade 3, 33.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
200 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 52.5 years
Health Status: unhealthy
Age Group: median age 52.5 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
DLT: Hypertension...
Other AEs: Fatigue...
Dose limiting toxicities:
Hypertension (grade 3, 33.3%)
Other AEs:
Fatigue (grade 3, 16.7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
400 mg 1 times / day multiple, oral
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 53 years
Health Status: unhealthy
Age Group: median age 53 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
DLT: Hypertension, Alanine aminotransferase increased...
Dose limiting toxicities:
Hypertension (grade 3, 33.3%)
Alanine aminotransferase increased (grade 3, 33.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 55.5 years
Health Status: unhealthy
Age Group: median age 55.5 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
DLT: Hypertension, Diarrhea...
Dose limiting toxicities:
Hypertension (grade 3, 33.3%)
Diarrhea (grade 3, 33.3%)
Headache (grade 3, 33.3%)
Toxic skin eruption (grade 2, 33.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Disc. AE: Rash, Dyspnea...
Other AEs: Diarrhea, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Rash (1.3%)
Dyspnea (1%)
Pneumonia (1.1%)
Other AEs:
Diarrhea (50%)
Diarrhea (grade 3-4, 5%)
Rash (28%)
Rash (grade 3-4, 3%)
Nausea (23%)
Nausea (grade 3-4, 1%)
Anorexia (20%)
Anorexia (grade 3-4, 2%)
Fatigue (20%)
Fatigue (grade 3-4, 4%)
Dyspnea (15%)
Dyspnea (grade 3-4, 4%)
Cough (13%)
Cough (grade 3-4, 0.8%)
Dermatitis acneiform (12%)
Dermatitis acneiform (grade 3-4, 0.6%)
Vomiting (14%)
Vomiting (grade 3-4, 2%)
Constipation (9%)
Dry skin (10%)
Dry skin (grade 3-4, 0.3%)
Hypertension (16%)
Hypertension (grade 3-4, 4%)
Pruritus (6%)
Pruritus (grade 3-4, 0.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022405s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022405s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/21282542/
Other AEs: QT interval prolonged, Torsades de pointes...
Other AEs:
QT interval prolonged (5.1%)
Torsades de pointes (0.2%)
Sudden death (grade 5, 0.2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022405s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/21282542/
AEs

AEs

AESignificanceDosePopulation
Blood pressure diastolic increased
1200 mg single, oral
Highest studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
https://pubmed.ncbi.nlm.nih.gov/22206795/
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
https://pubmed.ncbi.nlm.nih.gov/22206795/
Blood pressure systolic increased
1200 mg single, oral
Highest studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
https://pubmed.ncbi.nlm.nih.gov/22206795/
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
https://pubmed.ncbi.nlm.nih.gov/22206795/
Rash
1200 mg single, oral
Highest studied dose
Dose: 1200 mg
Route: oral
Route: single
Dose: 1200 mg
Sources:
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
https://pubmed.ncbi.nlm.nih.gov/22206795/
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
https://pubmed.ncbi.nlm.nih.gov/22206795/
Vomiting grade 2
Disc. AE
300 mg single, oral
Studied dose
Dose: 300 mg
Route: oral
Route: single
Dose: 300 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
Eczema grade 1
Disc. AE
400 mg single, oral
Dose: 400 mg
Route: oral
Route: single
Dose: 400 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/22206795/
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/22206795/
Folliculitis grade 2
Disc. AE
800 mg single, oral
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/22206795/
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/22206795/
Diarrhea grade 2, 12.5%
DLT
200 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
unhealthy, mean age 45.6 years
Health Status: unhealthy
Age Group: mean age 45.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
Hypophosphatemia grade 3, 12.5%
DLT
200 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
unhealthy, mean age 45.6 years
Health Status: unhealthy
Age Group: mean age 45.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
Colitis grade 3, 12.5%
DLT
600 mg 1 times / day multiple, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
Fatigue grade 3, 12.5%
DLT
600 mg 1 times / day multiple, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
Hypertension grade 3, 12.5%
DLT
600 mg 1 times / day multiple, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
Intestinal obstruction grade 3, 12.5%
DLT
600 mg 1 times / day multiple, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
Thrombocytopenia grade 3, 12.5%
DLT
600 mg 1 times / day multiple, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
Diarrhea grade 3, 25%
DLT
600 mg 1 times / day multiple, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
Arthralgia 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Chylothorax 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Cough 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Dysphagia 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Dysphonia 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Dyspnea 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
General physical health deterioration 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Germ cell cancer 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Nausea 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Pancreatitis 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Peripheral ischemia 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Peripheral sensorimotor neuropathy 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Peritonitis 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Pneumonitis 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Small intestinal perforation 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Systolic dysfunction 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Vision blurred 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Vomiting 0.4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Creatinine increased 0.9%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Diarrhea 0.9%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Electrocardiogram QTc interval prolonged 0.9%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Fatigue 0.9%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Hypertension 0.9%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Pyrexia 0.9%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Asthenia 1.7%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Skin disorder 2.5%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Dermatitis bullous grade 3, 0.4%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Erysipelas grade 3, 0.4%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Palmar-plantar erythrodysaesth. grade 3, 0.4%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Pneumonitis grade 3, 0.4%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Skin candida grade 3, 0.4%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Skin exfoliation grade 3, 0.4%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Respiratory failure grade 3, 0.8%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Acneiform dermatitis grade 3, 0.9%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Headache grade 3, 1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Nausea grade 3, 1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Pruritus grade 3, 1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Vomiting grade 3, 1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Weight decreased grade 3, 1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Generalized erythema grade 3, 1.3%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Dyspnea grade 3, 1.7%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Photosensitivity reaction grade 3, 1.7%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
ALT increased grade 3, 2%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Abdominal pain grade 3, 2%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Depression grade 3, 2%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Glucose increased grade 3, 2%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Hypocalcaemia grade 3, 2%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Photosensitivity reaction grade 3, 2%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Asthenia grade 3, 3%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Diarrhea grade 3, 3%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Rash grade 3, 3.9%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Decreased appetite grade 3, 4%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Calcium decreased grade 3, 6%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Fatigue grade 3, 6%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Hypertension grade 3, 6%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
QT interval prolonged grade 3, 8%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Calcium increased grade 3, 9%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Dermatitis acneiform grade 3, <1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Hemoglobin decreased grade 3, <1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Magnesium decreased grade 3, <1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Neutrophil count decreased grade 3, <1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Potassium decreased grade 3, <1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Potassium increased grade 3, <1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
WBC decreased grade 3, <1%
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022405Orig1s000MedR.pdf
Diarrhea grade 2, 12.5%
DLT
500 mg 1 times / day multiple, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
Folliculitis grade 2, 12.5%
DLT
500 mg 1 times / day multiple, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
ALT increased grade 3, 12.5%
DLT
500 mg 1 times / day multiple, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
Rash grade 3, 12.5%
DLT
500 mg 1 times / day multiple, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
Folliculitis grade 3, 12.5%
Disc. AE
500 mg 1 times / day multiple, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
Rash grade 2, 4%
DLT
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
unhealthy, mean age 57.7 years
Health Status: unhealthy
Age Group: mean age 57.7 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
Congestive cardiac failure grade 3, 4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
unhealthy, mean age 57.7 years
Health Status: unhealthy
Age Group: mean age 57.7 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/15905307/
https://www.ema.europa.eu/en/documents/assessment-report/caprelsa-epar-public-assessment-report_en.pdf
Lymphopenia grade 3, 33.3%
100 mg 1 times / day multiple, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 50 years
Health Status: unhealthy
Age Group: median age 50 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
Fatigue grade 3, 16.7%
200 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 52.5 years
Health Status: unhealthy
Age Group: median age 52.5 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
Hypertension grade 3, 33.3%
DLT
200 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 52.5 years
Health Status: unhealthy
Age Group: median age 52.5 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
Alanine aminotransferase increased grade 3, 33.3%
DLT
400 mg 1 times / day multiple, oral
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 53 years
Health Status: unhealthy
Age Group: median age 53 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
Hypertension grade 3, 33.3%
DLT
400 mg 1 times / day multiple, oral
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 53 years
Health Status: unhealthy
Age Group: median age 53 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
Toxic skin eruption grade 2, 33.3%
DLT
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 55.5 years
Health Status: unhealthy
Age Group: median age 55.5 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
Diarrhea grade 3, 33.3%
DLT
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 55.5 years
Health Status: unhealthy
Age Group: median age 55.5 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
Headache grade 3, 33.3%
DLT
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 55.5 years
Health Status: unhealthy
Age Group: median age 55.5 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
Hypertension grade 3, 33.3%
DLT
300 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
unhealthy, median age 55.5 years
Health Status: unhealthy
Age Group: median age 55.5 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/17409986/
Dyspnea 1%
Disc. AE
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Pneumonia 1.1%
Disc. AE
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Rash 1.3%
Disc. AE
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Dry skin 10%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Dermatitis acneiform 12%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Cough 13%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Vomiting 14%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Dyspnea 15%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Hypertension 16%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Anorexia 20%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Fatigue 20%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Nausea 23%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Rash 28%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Diarrhea 50%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Pruritus 6%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Constipation 9%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Dry skin grade 3-4, 0.3%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Pruritus grade 3-4, 0.5%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Dermatitis acneiform grade 3-4, 0.6%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Cough grade 3-4, 0.8%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Nausea grade 3-4, 1%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Anorexia grade 3-4, 2%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Vomiting grade 3-4, 2%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Rash grade 3-4, 3%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Dyspnea grade 3-4, 4%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Fatigue grade 3-4, 4%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Hypertension grade 3-4, 4%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Diarrhea grade 3-4, 5%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21282542/
Torsades de pointes 0.2%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022405s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022405s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/21282542/
QT interval prolonged 5.1%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022405s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022405s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/21282542/
Sudden death grade 5, 0.2%
300 mg/day 1 times / day multiple, oral
Recommended
Dose: 300 mg/day, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg/day, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022405s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/21282542/
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022405s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/21282542/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inducer
1087
inducer
440

inhibitor
2438
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1741

OATP1B1
1079

OATP1B3
961

CYP1A2
2153

CYP2A6
879

CYP2B6
926

CYP2C8
1057

CYP2E1
1060

CYP3A4/5
296

OCT2
779
FMO1
25

FMO3
77

UGT1A1
479

UGT1A3
470

UGT1A9
423

UGT1A4
399

UGT2B4
278

P-gp
2052

OATP1B1
503

OATP1B3
435

OCT2
434
CYP1A2
832
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
2333
 no
CYP2A6
911
 no
CYP2B6
1160
 no
CYP2C8
1117
 no
CYP2C9
2497
 no
CYP2E1
1146
 no
CYP3A4/5
357
 no
OATP1B1
1095
 no
P-gp
1932
 no
CYP2D6
2546
 weak [IC50 52 uM]
CYP1A2
2333
 weak
unlikely
Comment: less than 40% effect at 2uM in vitro
CYP2C9
2497
 weak
unlikely
Comment: less than 40% effect at 2uM in vitro
CYP3A4
2633
 weak
unlikely
Comment: less than 40% effect at 2uM in vitro
OATP1B3
970
 yes [IC50 18.3 uM]
OCT2
782
 yes [IC50 5.5 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
UGT1A1
479
 minor
UGT1A3
470
 minor
UGT1A4
399
 minor
UGT1A9
423
 minor
UGT2B4
278
 minor
OCT2
434
 no
P-gp
2052
 no
FMO1
25
 yes
FMO3
77
 yes
OATP1B1
503
 yes
OATP1B3
435
 yes
CYP3A4
1946
 yes
yes (co-administration study)
Comment: Itraconazole does not increased exposure to vandetanib; rifampicin reduced exposure to vandetanib by 48% but increased exposure to the active N-desmethyl metabolite
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:49960
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:49960
ChemicalBook
CB01011762
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB01011762
eMolecules
10778617
https://www.emolecules.com/cgi-bin/more?vid=10778617
MolPort
MolPort-005-942-399
https://www.molport.com/shop/molecule-link/MolPort-005-942-399
Selleck Chemicals
Vandetanib
http://www.selleckchem.com/products/Vandetanib.html
ZINC
ZINC000053683345
http://zinc15.docking.org/substances/ZINC000053683345
PubMed

PubMed

TitleDatePubMed
Dose scheduling of the dual VEGFR and EGFR tyrosine kinase inhibitor vandetanib (ZD6474, Zactima) in combination with radiotherapy in EGFR-positive and EGFR-null human head and neck tumor xenografts.
2008-02
Effects of AZD2171 and vandetanib (ZD6474, Zactima) on haemodynamic variables in an SW620 human colon tumour model: an investigation using dynamic contrast-enhanced MRI and the rapid clearance blood pool contrast agent, P792 (gadomelitol).
2008-01
Induction of cell cycle arrest and apoptosis in human nasopharyngeal carcinoma cells by ZD6474, an inhibitor of VEGFR tyrosine kinase with additional activity against EGFR tyrosine kinase.
2007-11-01
Micronodular transformation as a novel mechanism of VEGF-A-induced metastasis.
2007-08-23
American Society of Clinical Oncology--43rd annual meeting. Research into therapeutics: Part 3.
2007-08
Novel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates.
2007-07-01
A transplantable human medullary thyroid carcinoma as a model for RET tyrosine kinase-driven tumorigenesis.
2007-06
Antiangiogenic and antitumor activity of a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor ZD6474 in a metastatic human pancreatic tumor model.
2007-06
ZD6474 induces growth arrest and apoptosis of human leukemia cells, which is enhanced by concomitant use of a novel MEK inhibitor, AZD6244.
2007-06
Rationale and clinical results of multi-target treatments in oncology.
2007-05-24
Pharmacology of epidermal growth factor inhibitors.
2007-05-24
1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2.
2007-05
Combination of target agents: challenges and opportunities.
2007-05
Gateways to clinical trials.
2007-04
The RET oncogene is a critical component of transcriptional programs associated with retinoic acid-induced differentiation in neuroblastoma.
2007-04
Angiogenic inhibition reduces germinal matrix hemorrhage.
2007-04
Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer.
2007-03
Drug insight: VEGF as a therapeutic target for breast cancer.
2007-03
Role of anti-angiogenesis agents in treating NSCLC: focus on bevacizumab and VEGFR tyrosine kinase inhibitors.
2007-02
Dual targeting of the vascular endothelial growth factor and epidermal growth factor receptor pathways: rationale and clinical applications for non-small-cell lung cancer.
2007-02
Targeted therapy of orthotopic human lung cancer by combined vascular endothelial growth factor and epidermal growth factor receptor signaling blockade.
2007-02
Vandetanib (ZD6474): an orally available receptor tyrosine kinase inhibitor that selectively targets pathways critical for tumor growth and angiogenesis.
2007-02
Antitumor effects of ZD6474 on head and neck squamous cell carcinoma.
2007-02
Inhibitory effects of castration in an orthotopic model of androgen-independent prostate cancer can be mimicked and enhanced by angiogenesis inhibition.
2006-12-15
Synergistic antitumor activity of ZD6474, an inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling, with gemcitabine and ionizing radiation against pancreatic cancer.
2006-12-01
Toxicities of antiangiogenic therapy in non-small-cell lung cancer.
2006-12
ZD6474 induces growth arrest and apoptosis of GIST-T1 cells, which is enhanced by concomitant use of sunitinib.
2006-12
A phase I dose-escalation study of ZD6474 in Japanese patients with solid, malignant tumors.
2006-11
Second-line treatment of non-small cell lung cancer: big targets, small progress; small targets, big progress?
2006-11
Gateways to clinical trials.
2006-11
Targeting the EGF/VEGF-R system by tyrosine-kinase inhibitors--a novel antiproliferative/antiangiogenic strategy in thyroid cancer.
2006-11
A phase II study of ZD6474 (Zactima, a selective inhibitor of VEGFR and EGFR tyrosine kinase in patients with relapsed multiple myeloma--NCIC CTG IND.145.
2006-11
Vandetanib, a novel multitargeted kinase inhibitor, in cancer therapy.
2006-10
Gateways to clinical trials.
2006-09
New molecular targeted therapies in thyroid cancer.
2006-09
Prolonged exposure of colon cancer cells to the epidermal growth factor receptor inhibitor gefitinib (Iressa(TM)) and to the antiangiogenic agent ZD6474: Cytotoxic and biomolecular effects.
2006-08-28
Two targets, one drug for new EGFR inhibitors.
2006-08-16
A rapid method for the purification of wild-type and V804M mutant ret catalytic domain: A tool to study thyroid cancer.
2006-08-15
Tyrosine kinase inhibitors of vascular endothelial growth factor receptors in clinical trials: current status and future directions.
2006-08-02
Anti-tumor activity of the combination of cetuximab, an anti-EGFR blocking monoclonal antibody and ZD6474, an inhibitor of VEGFR and EGFR tyrosine kinases.
2006-08
Tissue distribution and metabolism of the tyrosine kinase inhibitor ZD6474 (Zactima) in tumor-bearing nude mice following oral dosing.
2006-08
VEGF-associated tyrosine kinase inhibition increases the tumor response to single and fractionated dose radiotherapy.
2006-07-01
Sequence-dependent inhibition of human colon cancer cell growth and of prosurvival pathways by oxaliplatin in combination with ZD6474 (Zactima), an inhibitor of VEGFR and EGFR tyrosine kinases.
2006-07
Epidermal growth factor receptor/angiogenesis dual targeting: preclinical experience.
2006-07
Clinical trials of antiangiogenic therapy in non-small cell lung cancer: focus on bevacizumab and ZD6474.
2006-04
Gateways to clinical trials.
2006-03
Multi-target inhibitors in non-small cell lung cancer (NSCLC).
2006-03
Antiangiogenic drugs in non-small cell lung cancer treatment.
2006-03
ZD6474, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, inhibits growth of experimental lung metastasis and production of malignant pleural effusions in a non-small cell lung cancer model.
2006
ZD6474 headed for phase III trials in the fall.
2005-08
Patents

Patents

07173038
1
08163926
1
08642608
2
20030144298
5
JP2006524634A
46
JP2011513364A
6
JP2011529067A
37
JP4701159B2
91

Sample Use Guides

In Vivo Use Guide
300 mg once daily may be taken with or without food. Dosage reduction may be necessary in the event of severe toxicities or QTc interval prolongation. The starting dose is 200 mg in patients with moderate to severe renal impairment.
Route of Administration: Oral
In Vitro Use Guide
Used in in vitro co-culture tubule formation model consisting of HUVECs and human fibroblasts vandetanib potently inhibited each of the tubule growth parameters measured (number of branch points [IC50 = 33.23 nM], total vessel length [IC50 = 60.97 nM], tubule area [IC50 = 92.70 nM]), at potencies consistent with the potency of vandetanib for inhibition of VEGF-stimulated proliferation of HUVECs.
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:16:51 GMT 2025
Edited
by admin
on Mon Mar 31 18:16:51 GMT 2025
Record UNII
YO460OQ37K
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
VANDETANIB
DASH   INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
CAPRELSA
Preferred Name English
GNF-PF-2188
Code English
VANDETANIB [VANDF]
Common Name English
VANDETANIB [MART.]
Common Name English
NSC-744325
Code English
vandetanib [INN]
Common Name English
NSC-760766
Code English
ZD6474
Code English
N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
Systematic Name English
VANDETANIB [USAN]
Common Name English
VANDETANIB [JAN]
Common Name English
VANDETANIB [MI]
Common Name English
VANDETANIB [ORANGE BOOK]
Common Name English
4-QUINAZOLINAMINE, N-(4-BROMO-2-FLUOROPHENYL)-6-METHOXY-7-((1-METHYL-4- PIPERIDINYL)METHOXY)-
Systematic Name English
ZD-64
Code English
ZACTIMA
Brand Name English
ZD-6474
Code English
Vandetanib [WHO-DD]
Common Name English
Classification Tree Code System Code
EMA ASSESSMENT REPORTS CAPRELSA (AUTHORIZED: THYROID NEOPLASMS)
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
LIVERTOX NBK548169
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
NDF-RT N0000175605
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
NCI_THESAURUS C1742
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
NCI_THESAURUS C2167
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
EU-Orphan Drug EU/3/05/344
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
WHO-ATC L01XE12
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
NCI_THESAURUS C93259
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
FDA ORPHAN DRUG 211005
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
WHO-VATC QL01XE12
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
Code System Code Type Description
IUPHAR
5717
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
NDF-RT
N0000185503
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY P-Glycoprotein Inhibitors [MoA]
EVMPD
SUB29174
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
ChEMBL
CHEMBL24828
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
NSC
744325
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
USAN
SS-07
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
DRUG CENTRAL
4178
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
NDF-RT
N0000187061
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY Organic Cation Transporter 2 Inhibitors [MoA]
NCI_THESAURUS
C2737
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
CAS
443913-73-3
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
HSDB
8198
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
DAILYMED
YO460OQ37K
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
WIKIPEDIA
Vandetanib
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
NSC
760766
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
INN
8365
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY
EPA CompTox
DTXSID1046681
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
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MERCK INDEX
m11387
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY Merck Index
LACTMED
Vandetanib
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
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DRUG BANK
DB05294
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
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PUBCHEM
3081361
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
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SMS_ID
100000090715
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
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CHEBI
49960
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
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FDA UNII
YO460OQ37K
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
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RXCUI
1098413
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
PRIMARY RxNorm
MESH
C452423
Created by admin on Mon Mar 31 18:16:51 GMT 2025 , Edited by admin on Mon Mar 31 18:16:51 GMT 2025
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Related Record Type Details
EPHRIN TYPE-A RECEPTOR 3
TARGET -> INHIBITOR
EPHRIN TYPE-A RECEPTOR 8
TARGET -> INHIBITOR
FETAL HEPATIC FLAVIN-CONTAINING MONOOXYGENASE 1 (HUMAN)
METABOLIC ENZYME -> SUBSTRATE
FETAL HEPATIC FLAVIN-CONTAINING MONOOXYGENASE 3 (HUMAN)
METABOLIC ENZYME -> SUBSTRATE
OCT-2
TRANSPORTER -> INHIBITOR
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> INHIBITOR
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2
TARGET -> INHIBITOR
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET M918T
TARGET -> INHIBITOR
IC50
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET V804L
TARGET -> INHIBITOR RESISTANT
IC50
OATP-8
TRANSPORTER -> SUBSTRATE
Structure of VANDETANIB
EXCRETED UNCHANGED
Within a 21-day collection period after a single dose of 14C-vandetanib, approximately 69% was recovered with 44% in feces and 25% in urine.
FECAL
Structure of VANDETANIB
EXCRETED UNCHANGED
Within a 21-day collection period after a single dose of 14C-vandetanib, approximately 69% was recovered with 44% in feces and 25% in urine.
URINE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET V804M
TARGET -> INHIBITOR RESISTANT
IC50
EPIDERMAL GROWTH FACTOR RECEPTOR
TARGET -> INHIBITOR
EPHRIN TYPE-B RECEPTOR 2
TARGET -> INHIBITOR
Related Record Type Details
Structure of N-OXIDE VANDETANIB
METABOLITE INACTIVE -> PARENT
FECAL; PLASMA; URINE
Structure of N-DESMETHYL VANDETANIB
METABOLITE ACTIVE -> PARENT
MAJOR
FECAL; PLASMA; URINE
Related Record Type Details
Structure of VANDETANIB
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
NIH
NCATS
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