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

Details

Stereochemistry ACHIRAL
Molecular Formula C24H25ClFN5O2.H2O
Molecular Weight 487.9551
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of DACOMITINIB

SMILES

COc1cc2c(cc1N=C(/C(/[H])=C(\[H])/CN3CCCCC3)O)c(ncn2)Nc4ccc(c(c4)Cl)F.O

InChI

InChIKey=BSPLGGCPNTZPIH-IPZCTEOASA-N
InChI=1S/C24H25ClFN5O2.H2O/c1-33-22-14-20-17(24(28-15-27-20)29-16-7-8-19(26)18(25)12-16)13-21(22)30-23(32)6-5-11-31-9-3-2-4-10-31;/h5-8,12-15H,2-4,9-11H2,1H3,(H,30,32)(H,27,28,29);1H2/b6-5+;

HIDE SMILES / InChI

Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C24H25ClFN5O2
Molecular Weight 469.9398
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Description
Curator's Comment:: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26768165 | http://www.ncbi.nlm.nih.gov/pubmed/22761403 | https://www.ncbi.nlm.nih.gov/pubmed/25939761

Dacomitinib is an oral, once-daily, pan-HER inhibitor. It is an irreversible inhibitor of HER-1 (EGFR), HER-2 and HER-4 tyrosine kinases. Dacomtinib is being evaluated in phase 3 clinical trials against nonsmall-cell lung cancer. Direct comparison with erlotinib did not show superiority of dacomtinib, but subgroup analysis have demonstrated that subgroup with exon 19 deletion had favorable outcomes with dacomitinib. In addition to nonsmall-cell lung cancer dacomtinib is being evaluated against esophagus, head and neck and other neoplasms. Due to its ability to pass through blood-brain barrier, dacomitinib can be used to treat brain tumors.

Originator

Curator's Comment:: # Pfizer

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
VIZIMPRO

Approved Use

VIZIMPRO is a kinase inhibitor indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 19 deletion or exon 21 L858R substitution mutations as detected by an FDA-approved test.

Launch Date

1.53791994E12
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
108 ng/mL
45 mg 1 times / day steady-state, oral
dose: 45 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DACOMITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
105 ng/mL
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DACOMITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
2213 ng × h/mL
45 mg 1 times / day steady-state, oral
dose: 45 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DACOMITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1720 ng × h/mL
60 mg 1 times / day steady-state, oral
dose: 60 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DACOMITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
70 h
45 mg 1 times / day steady-state, oral
dose: 45 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DACOMITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
2%
45 mg 1 times / day steady-state, oral
dose: 45 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DACOMITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Other AEs: Diarrhea, Diarrhea...
Other AEs:
Diarrhea (grade 1-2, 79%)
Diarrhea (grade 3-4, 8%)
Mucosal inflammation (grade 1-2, 40.6%)
Stomatitis (grade 1-2, 40.6%)
Mucosal inflammation (grade 3-4, 4.4%)
Stomatitis (grade 3-4, 4.4%)
Nausea (grade 1-2, 17.7%)
Nausea (grade 3-4, 1.3%)
Constipation (grade 1-2, 13%)
Mouth ulceration (grade 1-2, 12%)
Dermatitis acneiform (grade 1-2, 46%)
Rash (grade 1-2, 46%)
Rash maculo-papular (grade 1-2, 46%)
Dermatitis acneiform (grade 3-4, 23%)
Rash (grade 3-4, 23%)
Rash maculo-papular (grade 3-4, 23%)
Nail infection (grade 1-2, 56%)
Nail toxicity (grade 1-2, 56%)
Onychoclasis (grade 1-2, 56%)
Onycholysis (grade 1-2, 56%)
Onychomadesis (grade 1-2, 56%)
Paronychia (grade 1-2, 56%)
Nail infection (grade 3-4, 8%)
Nail toxicity (grade 3-4, 8%)
Onychoclasis (grade 3-4, 8%)
Onycholysis (grade 3-4, 8%)
Onychomadesis (grade 3-4, 8%)
Paronychia (grade 3-4, 8%)
Dry skin (grade 1-2, 28.2%)
Xerosis (grade 1-2, 28.2%)
Dry skin (grade 3-4, 1.8%)
Xerosis (grade 3-4, 1.8%)
Alopecia (grade 1-2, 22.6%)
Alopecia (grade 3-4, 0.4%)
Pruritus (grade 1-2, 20.1%)
Pruritus generalized (grade 1-2, 20.1%)
Rash pruritic (grade 1-2, 20.1%)
Pruritus (grade 3-4, 0.9%)
Pruritus generalized (grade 3-4, 0.9%)
Rash pruritic (grade 3-4, 0.9%)
Palmar-plantar erythrodysesthesia syndrome (grade 1-2, 14.1%)
Palmar-plantar erythrodysesthesia syndrome (grade 3-4, 0.9%)
Dermatitis (grade 1-2, 9.2%)
Dermatitis (grade 3-4, 1.8%)
Decreased appetite (grade 1-2, 27.9%)
Decreased appetite (grade 3-4, 3.1%)
Weight decreased (grade 1-2, 23.8%)
Weight decreased (grade 3-4, 2.2%)
Cough (grade 1-2, 21%)
Epistaxis (grade 1-2, 19%)
Nasal inflammation (grade 1-2, 19%)
Nasal mucosal disorder (grade 1-2, 19%)
Nasal mucosal ulcer (grade 1-2, 19%)
Rhinitis (grade 1-2, 19%)
Dyspnea (grade 1-2, 10.8%)
Dyspnea (grade 3-4, 2.2%)
Upper respiratory tract infection (grade 1-2, 10.7%)
Upper respiratory tract infection (grade 3-4, 1.3%)
Chest pain (grade 1-2, 10%)
Conjunctivitis (grade 1-2, 19%)
Pain in extremity (grade 1-2, 14%)
Musculoskeletal pain (grade 1-2, 11.1%)
Musculoskeletal pain (grade 3-4, 0.9%)
Asthenia (grade 1-2, 10.8%)
Asthenia (grade 3-4, 2.2%)
Insomnia (grade 1-2, 10.6%)
Insomnia (grade 3-4, 0.4%)
Fatigue (all grades, 9%)
Skin fissures (all grades, 9%)
Hypertrichosis (all grades, 1.3%)
Skin exfoliation (all grades, 3.5%)
Vomiting (all grades, 9%)
Dysgeusia (all grades, 7%)
Interstitial lung disease (all grades, 2.6%)
Keratitis (all grades, 1.8%)
Dehydration (all grades, 1.3%)
Anemia (grade 1-2, 43.1%)
Anemia (grade 3-4, 0.9%)
Lymphopenia (grade 1-2, 36%)
Lymphopenia (grade 3-4, 6%)
Hypoalbuminemia (grade 1-2, 44%)
ALT increased (grade 1-2, 38.6%)
ALT increased (grade 3-4, 1.4%)
Hyperglycemia (grade 1-2, 35%)
Hyperglycemia (grade 3-4, 1%)
AST increased (grade 1-2, 34.5%)
AST increased (grade 3-4, 0.5%)
Hypocalcemia (grade 1-2, 31.6%)
Hypocalcemia (grade 3-4, 1.4%)
Hypokalemia (grade 1-2, 22%)
Hypokalemia (grade 3-4, 7%)
Hyponatremia (grade 1-2, 23.1%)
Hyponatremia (grade 3-4, 2.9%)
Creatinine increased (grade 1-2, 24%)
Alkaline phosphatase increased (grade 1-2, 21.5%)
Alkaline phosphatase increased (grade 3-4, 0.5%)
Hypomagnesemia (grade 1-2, 21.5%)
Hypomagnesemia (grade 3-4, 0.5%)
Hyperbilirubinemia (grade 1-2, 15.5%)
Hyperbilirubinemia (grade 3-4, 0.5%)
Sources:
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Disc. AE: Maculopapular rash, Interstitial lung disease...
AEs leading to
discontinuation/dose reduction:
Maculopapular rash (1%)
Interstitial lung disease (1%)
Pneumonitis (2%)
Stomatitis (1%)
Diarrhea (1%)
Dermatitis acneiform (1%)
Bronchopulmonary aspergillosis (0.4%)
Cerebral infarction (0.4%)
Infection (0.4%)
Keratitis (0.4%)
Keratolysis exfoliativa acquired (0.4%)
Liver injury (0.4%)
Lung infection (0.4%)
Lymphocyte count decreased (0.4%)
Malaise (0.4%)
Malnutrition (0.4%)
Muscular weakness (0.4%)
Respiratory failure (0.4%)
Urinary tract infection (0.4%)
Sources:
60 mg 1 times / day steady, oral
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Condition: advanced solid tumors
Sources:
AEs

AEs

AESignificanceDosePopulation
Dehydration all grades, 1.3%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hypertrichosis all grades, 1.3%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Keratitis all grades, 1.8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Interstitial lung disease all grades, 2.6%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Skin exfoliation all grades, 3.5%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Dysgeusia all grades, 7%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Fatigue all grades, 9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Skin fissures all grades, 9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Vomiting all grades, 9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Chest pain grade 1-2, 10%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Insomnia grade 1-2, 10.6%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Upper respiratory tract infection grade 1-2, 10.7%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Asthenia grade 1-2, 10.8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Dyspnea grade 1-2, 10.8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Musculoskeletal pain grade 1-2, 11.1%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Mouth ulceration grade 1-2, 12%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Constipation grade 1-2, 13%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Pain in extremity grade 1-2, 14%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Palmar-plantar erythrodysesthesia syndrome grade 1-2, 14.1%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hyperbilirubinemia grade 1-2, 15.5%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Nausea grade 1-2, 17.7%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Conjunctivitis grade 1-2, 19%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Epistaxis grade 1-2, 19%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Nasal inflammation grade 1-2, 19%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Nasal mucosal disorder grade 1-2, 19%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Nasal mucosal ulcer grade 1-2, 19%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Rhinitis grade 1-2, 19%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Pruritus generalized grade 1-2, 20.1%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Pruritus grade 1-2, 20.1%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Rash pruritic grade 1-2, 20.1%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Cough grade 1-2, 21%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Alkaline phosphatase increased grade 1-2, 21.5%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hypomagnesemia grade 1-2, 21.5%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hypokalemia grade 1-2, 22%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Alopecia grade 1-2, 22.6%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hyponatremia grade 1-2, 23.1%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Weight decreased grade 1-2, 23.8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Creatinine increased grade 1-2, 24%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Decreased appetite grade 1-2, 27.9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Dry skin grade 1-2, 28.2%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Xerosis grade 1-2, 28.2%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hypocalcemia grade 1-2, 31.6%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
AST increased grade 1-2, 34.5%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hyperglycemia grade 1-2, 35%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Lymphopenia grade 1-2, 36%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
ALT increased grade 1-2, 38.6%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Mucosal inflammation grade 1-2, 40.6%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Stomatitis grade 1-2, 40.6%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Anemia grade 1-2, 43.1%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hypoalbuminemia grade 1-2, 44%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Dermatitis acneiform grade 1-2, 46%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Rash maculo-papular grade 1-2, 46%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Rash grade 1-2, 46%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Nail infection grade 1-2, 56%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Nail toxicity grade 1-2, 56%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Onychoclasis grade 1-2, 56%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Onycholysis grade 1-2, 56%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Onychomadesis grade 1-2, 56%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Paronychia grade 1-2, 56%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Diarrhea grade 1-2, 79%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Dermatitis grade 1-2, 9.2%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Alopecia grade 3-4, 0.4%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Insomnia grade 3-4, 0.4%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
AST increased grade 3-4, 0.5%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Alkaline phosphatase increased grade 3-4, 0.5%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hyperbilirubinemia grade 3-4, 0.5%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hypomagnesemia grade 3-4, 0.5%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Anemia grade 3-4, 0.9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Musculoskeletal pain grade 3-4, 0.9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Palmar-plantar erythrodysesthesia syndrome grade 3-4, 0.9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Pruritus generalized grade 3-4, 0.9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Pruritus grade 3-4, 0.9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Rash pruritic grade 3-4, 0.9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hyperglycemia grade 3-4, 1%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Nausea grade 3-4, 1.3%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Upper respiratory tract infection grade 3-4, 1.3%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
ALT increased grade 3-4, 1.4%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hypocalcemia grade 3-4, 1.4%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Dermatitis grade 3-4, 1.8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Dry skin grade 3-4, 1.8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Xerosis grade 3-4, 1.8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Asthenia grade 3-4, 2.2%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Dyspnea grade 3-4, 2.2%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Weight decreased grade 3-4, 2.2%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hyponatremia grade 3-4, 2.9%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Dermatitis acneiform grade 3-4, 23%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Rash maculo-papular grade 3-4, 23%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Rash grade 3-4, 23%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Decreased appetite grade 3-4, 3.1%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Mucosal inflammation grade 3-4, 4.4%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Stomatitis grade 3-4, 4.4%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Lymphopenia grade 3-4, 6%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Hypokalemia grade 3-4, 7%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Diarrhea grade 3-4, 8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Nail infection grade 3-4, 8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Nail toxicity grade 3-4, 8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Onychoclasis grade 3-4, 8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Onycholysis grade 3-4, 8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Onychomadesis grade 3-4, 8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Paronychia grade 3-4, 8%
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Bronchopulmonary aspergillosis 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Cerebral infarction 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Infection 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Keratitis 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Keratolysis exfoliativa acquired 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Liver injury 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Lung infection 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Lymphocyte count decreased 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Malaise 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Malnutrition 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Muscular weakness 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Respiratory failure 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Urinary tract infection 0.4%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Dermatitis acneiform 1%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Diarrhea 1%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Interstitial lung disease 1%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Maculopapular rash 1%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Stomatitis 1%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
Pneumonitis 2%
Disc. AE
45 mg 1 times / day multiple, oral
MTD
Dose: 45 mg, 1 times / day
Route: oral
Route: multiple
Dose: 45 mg, 1 times / day
Sources:
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: dacomitnib increased dextromethorphan AUC by 362% and Cmax by 973%
Page: 55.0
Drug as victimTox targets

Tox targets

Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Irreversible protein kinase inhibitors: balancing the benefits and risks.
2012 Jul 26
Patents

Sample Use Guides

In phase III study against non small cell lung cancer dacomitinib was administered orally at a dose 45 mg a day.
Route of Administration: Oral
Cells were seeded in duplicate at 5 × 103 to 5 × 104 cells per well in 24-well plates. A day after plating, dacomitinib was added at 10 μmol/L and 2-fold dilutions over 12 concentrations were carried out to generate a dose–response curve. Control wells without the drug were also seeded. The cells were counted on day 1 when the drug was added, as well as after 6 days when the experiment ended. After the trypsinization cells were placed in an Isotone solution and immediately counted using a Coulter Z1 particle counter (Beckman Coulter, Inc.). The suspension cultures were counted using a Coulter Vi-Cell counter (Beckman Coulter, Inc.). As a group, HER2-amplified cell lines were most sensitive to growth inhibition by dacomitinib (IC50 < 1 μmol/L in 14 of 16 lines).
Substance Class Chemical
Created
by admin
on Sat Jun 26 15:25:34 UTC 2021
Edited
by admin
on Sat Jun 26 15:25:34 UTC 2021
Record UNII
5092U85G58
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DACOMITINIB
USAN  
USAN  
Official Name English
DACOMITINIB MONOHYDRATE
Common Name English
DACOMITINIB [USAN]
Common Name English
DACOMITINIB HYDRATE [JAN]
Common Name English
DACOMITINIB [ORANGE BOOK]
Common Name English
2-BUTENAMIDE, N-(4-((3-CHLORO-4-FLUOROPHENYL)AMINO)-7-METHOXY-6-QUINAZOLINYL)-4-(1- PIPERIDINYL)-, HYDRATE (1:1), (2E)-
Common Name English
PF-00299804-03
Code English
VIZIMPRO
Brand Name English
(2E)-N-(4-(3-CHLORO-4-FLUOROPHENYL)AMINO)7-METHOXYQUINAZOLIN-6-YL)4-(PIPERIDIN-1-YL)BUT-2-ENAMIDE MONOHYDRATE
Common Name English
DACOMITINIB [MI]
Common Name English
Classification Tree Code System Code
WHO-ATC L01XE47
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
FDA ORPHAN DRUG 435114
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
NCI_THESAURUS C2167
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
Code System Code Type Description
EVMPD
SUB191069
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
LACTMED
Dacomitinib
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
CAS
1042385-75-0
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
EPA CompTox
1042385-75-0
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
RXCUI
2058849
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
NCI_THESAURUS
C53398
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
WIKIPEDIA
Dacomitinib
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
ChEMBL
CHEMBL2110732
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
MERCK INDEX
M12088
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
DRUG BANK
DB11963
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
FDA UNII
5092U85G58
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
PUBCHEM
70693519
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
DRUG CENTRAL
5297
Created by admin on Sat Jun 26 15:25:34 UTC 2021 , Edited by admin on Sat Jun 26 15:25:34 UTC 2021
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC INTRAVENOUS

DOSE

Tmax PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC SINGLE DOSE

ORAL