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Details

Stereochemistry ACHIRAL
Molecular Formula C22H24BrFN4O2
Molecular Weight 475.3543
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VANDETANIB

SMILES

CN1CCC(CC1)COc2cc3c(cc2OC)c(ncn3)Nc4ccc(cc4F)Br

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

Description
Curator's Comment:: 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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P00533|||Q9GZX1
Gene ID: 1956
Gene Symbol: EGFR
Target Organism: Homo sapiens (Human)
0.5 µM [IC50]
Target ID: P35968
Gene ID: 3791
Gene Symbol: KDR
Target Organism: Homo sapiens (Human)
0.0400000000000000008 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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

1302048000000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2024 ng/mL
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
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
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
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
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
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%
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 1 times / day single, oral
Highest studied dose
healthy, mean age 34.4 years
Other AEs: Rash, Blood pressure systolic increased...
300 mg 1 times / day single, oral
Recommended|MTD
healthy, mean age 34.4 years
Disc. AE: Vomiting...
400 mg 1 times / day single, oral
Dose: 400 mg, 1 times / day
Route: oral
Route: single
Dose: 400 mg, 1 times / day
Sources:
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
Disc. AE: Eczema...
AEs leading to
discontinuation/dose reduction:
Eczema (grade 1)
Sources:
800 mg 1 times / day single, oral
Dose: 800 mg, 1 times / day
Route: oral
Route: single
Dose: 800 mg, 1 times / day
Sources:
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
Disc. AE: Folliculitis...
AEs leading to
discontinuation/dose reduction:
Folliculitis (grade 2)
Sources:
200 mg 1 times / day multiple, oral
Recommended|MTD
unhealthy, mean age 45.6 years
DLT: Hypophosphatemia, Diarrhea...
600 mg 1 times / day multiple, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
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:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
500 mg 1 times / day multiple, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
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:
300 mg 1 times / day multiple, oral
Recommended|MTD
unhealthy, mean age 57.7 years
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:
100 mg 1 times / day multiple, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, median age 50 years
Health Status: unhealthy
Age Group: median age 50 years
Sex: M+F
Sources:
Other AEs: Lymphopenia...
Other AEs:
Lymphopenia (grade 3, 33.3%)
Sources:
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:
unhealthy, median age 52.5 years
Health Status: unhealthy
Age Group: median age 52.5 years
Sex: M+F
Sources:
DLT: Hypertension...
Other AEs: Fatigue...
Dose limiting toxicities:
Hypertension (grade 3, 33.3%)
Other AEs:
Fatigue (grade 3, 16.7%)
Sources:
400 mg 1 times / day multiple, oral
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, median age 53 years
Health Status: unhealthy
Age Group: median age 53 years
Sex: M+F
Sources:
DLT: Hypertension, Alanine aminotransferase increased...
Dose limiting toxicities:
Hypertension (grade 3, 33.3%)
Alanine aminotransferase increased (grade 3, 33.3%)
Sources:
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:
unhealthy, median age 55.5 years
Health Status: unhealthy
Age Group: median age 55.5 years
Sex: M+F
Sources:
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:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
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:
unhealthy, median age 61 years
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:
AEs

AEs

AESignificanceDosePopulation
Blood pressure diastolic increased
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 34.4 years
Blood pressure systolic increased
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 34.4 years
Rash
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 34.4 years
Vomiting grade 2
Disc. AE
300 mg 1 times / day single, oral
Recommended|MTD
healthy, mean age 34.4 years
Eczema grade 1
Disc. AE
400 mg 1 times / day single, oral
Dose: 400 mg, 1 times / day
Route: oral
Route: single
Dose: 400 mg, 1 times / day
Sources:
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
Folliculitis grade 2
Disc. AE
800 mg 1 times / day single, oral
Dose: 800 mg, 1 times / day
Route: oral
Route: single
Dose: 800 mg, 1 times / day
Sources:
healthy, mean age 34.4 years
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Sources:
Diarrhea grade 2, 12.5%
DLT
200 mg 1 times / day multiple, oral
Recommended|MTD
unhealthy, mean age 45.6 years
Hypophosphatemia grade 3, 12.5%
DLT
200 mg 1 times / day multiple, oral
Recommended|MTD
unhealthy, mean age 45.6 years
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:
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.6 years
Health Status: unhealthy
Age Group: mean age 50.6 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 50.7 years
Health Status: unhealthy
Age Group: mean age 50.7 years
Sex: M+F
Sources:
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:
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
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:
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
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:
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
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:
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
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:
unhealthy, mean age 51.6 years
Health Status: unhealthy
Age Group: mean age 51.6 years
Sex: M+F
Sources:
Rash grade 2, 4%
DLT
300 mg 1 times / day multiple, oral
Recommended|MTD
unhealthy, mean age 57.7 years
Congestive cardiac failure grade 3, 4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
unhealthy, mean age 57.7 years
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:
unhealthy, median age 50 years
Health Status: unhealthy
Age Group: median age 50 years
Sex: M+F
Sources:
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:
unhealthy, median age 52.5 years
Health Status: unhealthy
Age Group: median age 52.5 years
Sex: M+F
Sources:
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:
unhealthy, median age 52.5 years
Health Status: unhealthy
Age Group: median age 52.5 years
Sex: M+F
Sources:
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:
unhealthy, median age 53 years
Health Status: unhealthy
Age Group: median age 53 years
Sex: M+F
Sources:
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:
unhealthy, median age 53 years
Health Status: unhealthy
Age Group: median age 53 years
Sex: M+F
Sources:
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:
unhealthy, median age 55.5 years
Health Status: unhealthy
Age Group: median age 55.5 years
Sex: M+F
Sources:
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:
unhealthy, median age 55.5 years
Health Status: unhealthy
Age Group: median age 55.5 years
Sex: M+F
Sources:
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:
unhealthy, median age 55.5 years
Health Status: unhealthy
Age Group: median age 55.5 years
Sex: M+F
Sources:
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:
unhealthy, median age 55.5 years
Health Status: unhealthy
Age Group: median age 55.5 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
Health Status: unhealthy
Age Group: median age 61 years
Sex: M+F
Sources:
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:
unhealthy, median age 61 years
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:
unhealthy, median age 61 years
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:
unhealthy, median age 61 years
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
weak [IC50 52 uM]
weak
unlikely
weak
unlikely
weak
unlikely
yes [IC50 18.3 uM]
yes [IC50 5.5 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
minor
minor
minor
minor
minor
no
no
yes
yes
yes
yes
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

PubMed

PubMed

TitleDatePubMed
In vivo videomicroscopy reveals differential effects of the vascular-targeting agent ZD6126 and the anti-angiogenic agent ZD6474 on vascular function in a liver metastasis model.
2004
Disease associated mutations at valine 804 in the RET receptor tyrosine kinase confer resistance to selective kinase inhibitors.
2004 Aug 12
Anticancer effects of ZD6474, a VEGF receptor tyrosine kinase inhibitor, in gefitinib ("Iressa")-sensitive and resistant xenograft models.
2004 Dec
Combination antiangiogenic and androgen deprivation therapy for prostate cancer: a promising therapeutic approach.
2004 Dec 15
ZD6474, a potent inhibitor of vascular endothelial growth factor signaling, combined with radiotherapy: schedule-dependent enhancement of antitumor activity.
2004 Dec 15
Small in-frame deletion in the epidermal growth factor receptor as a target for ZD6474.
2004 Dec 15
Regulation of p27Kip1 protein levels contributes to mitogenic effects of the RET/PTC kinase in thyroid carcinoma cells.
2004 Jun 1
Identification of RET kinase inhibitors as potential new treatment for sporadic and inherited thyroid cancer.
2004 Nov
Efficacy of combined antiangiogenic and vascular disrupting agents in treatment of solid tumors.
2004 Nov 15
ZD6474, a vascular endothelial growth factor receptor tyrosine kinase inhibitor with additional activity against epidermal growth factor receptor tyrosine kinase, inhibits orthotopic growth and angiogenesis of gastric cancer.
2004 Sep
The tyrosine kinase inhibitor ZD6474 inhibits tumour growth in an intracerebral rat glioma model.
2004 Sep 13
Antiangiogenic therapy of cerebral melanoma metastases results in sustained tumor progression via vessel co-option.
2004 Sep 15
ZD6474 headed for phase III trials in the fall.
2005 Aug
Cooperative antitumor effect of multitargeted kinase inhibitor ZD6474 and ionizing radiation in glioblastoma.
2005 Aug 1
Gateways to clinical trials.
2005 Dec
The effects of ZD6474, an inhibitor of VEGF signaling, on cutaneous wound healing in mice.
2005 Dec
Antitumor activity of ZD6474, a vascular endothelial growth factor-2 and epidermal growth factor receptor small molecule tyrosine kinase inhibitor, in combination with SC-236, a cyclooxygenase-2 inhibitor.
2005 Feb 1
ZD6474--a novel inhibitor of VEGFR and EGFR tyrosine kinase activity.
2005 Jun
ZD6474--clinical experience to date.
2005 Jun
In vitro procoagulant activity induced in endothelial cells by chemotherapy and antiangiogenic drug combinations: modulation by lower-dose chemotherapy.
2005 Jun 15
Gateways to clinical trials.
2005 Mar
Sequence-dependent antiproliferative effects of cytotoxic drugs and epidermal growth factor receptor inhibitors.
2005 May
ZD6474 suppresses oncogenic RET isoforms in a Drosophila model for type 2 multiple endocrine neoplasia syndromes and papillary thyroid carcinoma.
2005 May 1
A multicenter phase II trial of ZD6474, a vascular endothelial growth factor receptor-2 and epidermal growth factor receptor tyrosine kinase inhibitor, in patients with previously treated metastatic breast cancer.
2005 May 1
Angiogenesis and lung cancer: prognostic and therapeutic implications.
2005 May 10
Molecule-kinase interaction map.
2005 Nov
Update on angiogenesis inhibitors.
2005 Nov
ZD6474, a novel tyrosine kinase inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor, inhibits tumor growth of multiple nervous system tumors.
2005 Nov 15
Targeting the tumor vasculature: enhancing antitumor efficacy through combination treatment with ZD6126 and ZD6474.
2005 Nov-Dec
Gateways to clinical trials.
2005 Oct
Phase II data with ZD6474, a small-molecule kinase inhibitor of epidermal growth factor receptor and vascular endothelial growth factor receptor, in previously treated advanced non-small-cell lung cancer.
2005 Sep
Rapid and sensitive LC/MS/MS analysis of the novel tyrosine kinase inhibitor ZD6474 in mouse plasma and tissues.
2005 Sep 15
A rapid method for the purification of wild-type and V804M mutant ret catalytic domain: A tool to study thyroid cancer.
2006 Aug 15
Two targets, one drug for new EGFR inhibitors.
2006 Aug 16
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 Aug 28
Toxicities of antiangiogenic therapy in non-small-cell lung cancer.
2006 Dec
ZD6474 inhibits proliferation and invasion of human hepatocellular carcinoma cells.
2006 Feb 14
ZD6474 inhibits tumor growth and intraperitoneal dissemination in a highly metastatic orthotopic gastric cancer model.
2006 Jan 15
Multi-target inhibitors in non-small cell lung cancer (NSCLC).
2006 Mar
Antiangiogenic drugs in non-small cell lung cancer treatment.
2006 Mar
Gateways to clinical trials.
2006 Nov
American Society of Clinical Oncology--43rd annual meeting. Research into therapeutics: Part 3.
2007 Aug
Micronodular transformation as a novel mechanism of VEGF-A-induced metastasis.
2007 Aug 23
Role of anti-angiogenesis agents in treating NSCLC: focus on bevacizumab and VEGFR tyrosine kinase inhibitors.
2007 Feb
Vandetanib (ZD6474): an orally available receptor tyrosine kinase inhibitor that selectively targets pathways critical for tumor growth and angiogenesis.
2007 Feb
Antitumor effects of ZD6474 on head and neck squamous cell carcinoma.
2007 Feb
A transplantable human medullary thyroid carcinoma as a model for RET tyrosine kinase-driven tumorigenesis.
2007 Jun
1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2.
2007 May
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 Nov 1
Patents

Sample Use Guides

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
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.
Name Type Language
VANDETANIB
DASH   INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
GNF-PF-2188
Code English
VANDETANIB [VANDF]
Common Name English
VANDETANIB [MART.]
Common Name English
NSC-744325
Code English
CAPRELSA
Brand Name English
VANDETANIB [INN]
Common Name English
NSC-760766
Code English
ZD6474
Code English
VANDETANIB [WHO-DD]
Common Name 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
Classification Tree Code System Code
EMA ASSESSMENT REPORTS CAPRELSA (AUTHORIZED: THYROID NEOPLASMS)
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
LIVERTOX 1021
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
NDF-RT N0000175605
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
NCI_THESAURUS C1742
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
NCI_THESAURUS C2167
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
EU-Orphan Drug EU/3/05/344
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
WHO-ATC L01XE12
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
NCI_THESAURUS C93259
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
FDA ORPHAN DRUG 211005
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
WHO-VATC QL01XE12
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
Code System Code Type Description
IUPHAR
5717
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
NDF-RT
N0000185503
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY P-Glycoprotein Inhibitors [MoA]
EVMPD
SUB29174
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
ChEMBL
CHEMBL24828
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
DRUG CENTRAL
4178
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
NDF-RT
N0000187061
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY Organic Cation Transporter 2 Inhibitors [MoA]
NCI_THESAURUS
C2737
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
CAS
443913-73-3
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
HSDB
8198
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
INN
8365
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
EPA CompTox
443913-73-3
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
MERCK INDEX
M11387
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY Merck Index
LACTMED
Vandetanib
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
DRUG BANK
DB05294
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
PUBCHEM
3081361
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
FDA UNII
YO460OQ37K
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY
RXCUI
1098413
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY RxNorm
MESH
C452423
Created by admin on Fri Jun 25 22:00:06 UTC 2021 , Edited by admin on Fri Jun 25 22:00:06 UTC 2021
PRIMARY