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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

Molecular Formula C22H24BrFN4O2
Molecular Weight 475.3543
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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P00533|||Q9GZX1
Gene ID: 1956.0
Gene Symbol: EGFR
Target Organism: Homo sapiens (Human)
0.5 µM [IC50]
Target ID: P35968
Gene ID: 3791.0
Gene Symbol: KDR
Target Organism: Homo sapiens (Human)
0.04 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

1.30204801E12
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
n = 5
Other AEs: Rash, Blood pressure systolic increased...
300 mg 1 times / day single, oral
Recommended|MTD
healthy, mean age 34.4 years
n = 6
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
n = 6
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Population Size: 6
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
n = 6
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Population Size: 6
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 45.6 years
Sex: M+F
Population Size: 8
Sources:
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 50.6 years
Sex: M+F
Population Size: 8
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 51.6 years
Sex: M+F
Population Size: 8
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
n = 25
Health Status: unhealthy
Condition: cancer
Age Group: mean age 57.7 years
Sex: M+F
Population Size: 25
Sources:
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
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 50 years
Sex: M+F
Population Size: 3
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
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 52.5 years
Sex: M+F
Population Size: 6
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
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 53 years
Sex: M+F
Population Size: 3
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
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 55.5 years
Sex: M+F
Population Size: 6
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
Sources:
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
n = 5
Blood pressure systolic increased
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 34.4 years
n = 5
Rash
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 34.4 years
n = 5
Vomiting grade 2
Disc. AE
300 mg 1 times / day single, oral
Recommended|MTD
healthy, mean age 34.4 years
n = 6
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
n = 6
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Population Size: 6
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
n = 6
Health Status: healthy
Age Group: mean age 34.4 years
Sex: M
Population Size: 6
Sources:
Diarrhea grade 2, 12.5%
DLT
200 mg 1 times / day multiple, oral
Recommended|MTD
unhealthy, mean age 45.6 years
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 45.6 years
Sex: M+F
Population Size: 8
Sources:
Hypophosphatemia grade 3, 12.5%
DLT
200 mg 1 times / day multiple, oral
Recommended|MTD
unhealthy, mean age 45.6 years
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 45.6 years
Sex: M+F
Population Size: 8
Sources:
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 50.6 years
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 50.6 years
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 50.6 years
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 50.6 years
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 50.6 years
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 50.6 years
Sex: M+F
Population Size: 8
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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: Page: 022405Orig1s000MedR.pdf - p.71
unhealthy, mean age 50.7 years
n = 231
Health Status: unhealthy
Condition: medullary thyroid cancer
Age Group: mean age 50.7 years
Sex: M+F
Population Size: 231
Sources: Page: 022405Orig1s000MedR.pdf - p.71
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 51.6 years
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 51.6 years
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 51.6 years
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 51.6 years
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: cancer
Age Group: mean age 51.6 years
Sex: M+F
Population Size: 8
Sources:
Rash grade 2, 4%
DLT
300 mg 1 times / day multiple, oral
Recommended|MTD
unhealthy, mean age 57.7 years
n = 25
Health Status: unhealthy
Condition: cancer
Age Group: mean age 57.7 years
Sex: M+F
Population Size: 25
Sources:
Congestive cardiac failure grade 3, 4%
Disc. AE
300 mg 1 times / day multiple, oral
Recommended|MTD
unhealthy, mean age 57.7 years
n = 25
Health Status: unhealthy
Condition: cancer
Age Group: mean age 57.7 years
Sex: M+F
Population Size: 25
Sources:
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
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 50 years
Sex: M+F
Population Size: 3
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
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 52.5 years
Sex: M+F
Population Size: 6
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
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 52.5 years
Sex: M+F
Population Size: 6
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
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 53 years
Sex: M+F
Population Size: 3
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
n = 3
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 53 years
Sex: M+F
Population Size: 3
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
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 55.5 years
Sex: M+F
Population Size: 6
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
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 55.5 years
Sex: M+F
Population Size: 6
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
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 55.5 years
Sex: M+F
Population Size: 6
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
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: median age 55.5 years
Sex: M+F
Population Size: 6
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
Sources:
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
Sources:
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
n = 623
Health Status: unhealthy
Condition: non-small-cell lung cancer
Age Group: median age 61 years
Sex: M+F
Population Size: 623
Sources:
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
The VEGF receptor tyrosine kinase inhibitor, ZD6474, inhibits angiogenesis and affects microvascular architecture within an orthotopically implanted renal cell carcinoma.
2004
Clinical evaluation of ZD6474, an orally active inhibitor of VEGF and EGF receptor signaling, in patients with solid, malignant tumors.
2005 Aug
Cooperative antitumor effect of multitargeted kinase inhibitor ZD6474 and ionizing radiation in glioblastoma.
2005 Aug 1
The effects of ZD6474, an inhibitor of VEGF signaling, on cutaneous wound healing in mice.
2005 Dec
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
Sequence-dependent antiproliferative effects of cytotoxic drugs and epidermal growth factor receptor inhibitors.
2005 May
Molecule-kinase interaction map.
2005 Nov
Update on angiogenesis inhibitors.
2005 Nov
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
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
Clinical trials of antiangiogenic therapy in non-small cell lung cancer: focus on bevacizumab and ZD6474.
2006 Apr
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 Aug
Tissue distribution and metabolism of the tyrosine kinase inhibitor ZD6474 (Zactima) in tumor-bearing nude mice following oral dosing.
2006 Aug
A rapid method for the purification of wild-type and V804M mutant ret catalytic domain: A tool to study thyroid cancer.
2006 Aug 15
ZD6474 induces growth arrest and apoptosis of GIST-T1 cells, which is enhanced by concomitant use of sunitinib.
2006 Dec
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 Dec 1
Inhibitory effects of castration in an orthotopic model of androgen-independent prostate cancer can be mimicked and enhanced by angiogenesis inhibition.
2006 Dec 15
ZD6474, an inhibitor of VEGFR and EGFR tyrosine kinase activity in combination with radiotherapy.
2006 Jan 1
ZD6474 inhibits tumor growth and intraperitoneal dissemination in a highly metastatic orthotopic gastric cancer model.
2006 Jan 15
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 Jul
Epidermal growth factor receptor/angiogenesis dual targeting: preclinical experience.
2006 Jul
VEGF-associated tyrosine kinase inhibition increases the tumor response to single and fractionated dose radiotherapy.
2006 Jul 1
Tyrosine kinase inhibitors of vascular endothelial growth factor receptors in clinical trials: current status and future directions.
2006 Jul-Aug
Gateways to clinical trials.
2006 Mar
Antiangiogenic drugs in non-small cell lung cancer treatment.
2006 Mar
A phase I dose-escalation study of ZD6474 in Japanese patients with solid, malignant tumors.
2006 Nov
Second-line treatment of non-small cell lung cancer: big targets, small progress; small targets, big progress?
2006 Nov
Targeting the EGF/VEGF-R system by tyrosine-kinase inhibitors--a novel antiproliferative/antiangiogenic strategy in thyroid cancer.
2006 Nov
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 Nov
Vandetanib, a novel multitargeted kinase inhibitor, in cancer therapy.
2006 Oct
Gateways to clinical trials.
2006 Sep
New molecular targeted therapies in thyroid cancer.
2006 Sep
Gateways to clinical trials.
2007 Apr
The RET oncogene is a critical component of transcriptional programs associated with retinoic acid-induced differentiation in neuroblastoma.
2007 Apr
Angiogenic inhibition reduces germinal matrix hemorrhage.
2007 Apr
Micronodular transformation as a novel mechanism of VEGF-A-induced metastasis.
2007 Aug 23
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 Feb
Pharmacology of epidermal growth factor inhibitors.
2007 Jan-Mar
Novel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates.
2007 Jul 1
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 Jun
ZD6474 induces growth arrest and apoptosis of human leukemia cells, which is enhanced by concomitant use of a novel MEK inhibitor, AZD6244.
2007 Jun
Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer.
2007 Mar
Combination of target agents: challenges and opportunities.
2007 May
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 Feb
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 Jan
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.
Substance Class Chemical
Created
by admin
on Fri Jun 25 22:00:06 UTC 2021
Edited
by admin
on Fri Jun 25 22:00:06 UTC 2021
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
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
Related Record Type Details
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TARGET -> INHIBITOR
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
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
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
Related Record Type Details
METABOLITE INACTIVE -> PARENT
FECAL; PLASMA; URINE
METABOLITE ACTIVE -> PARENT
MAJOR
FECAL; PLASMA; URINE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC