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

Details

Stereochemistry ACHIRAL
Molecular Formula C24H25ClFN5O2
Molecular Weight 469.939
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of DACOMITINIB ANHYDROUS

SMILES

COC1=C(NC(=O)\C=C\CN2CCCCC2)C=C3C(NC4=CC=C(F)C(Cl)=C4)=NC=NC3=C1

InChI

InChIKey=LVXJQMNHJWSHET-AATRIKPKSA-N
InChI=1S/C24H25ClFN5O2/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)/b6-5+

HIDE SMILES / InChI
Molecular Formula C24H25ClFN5O2
Molecular Weight 469.939
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.

CNS Activity

Originator

Pfizer
420
Curator's Comment: # Pfizer

Approval Year

2018
436
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 6.0 nM [IC50]
Inhibitor
8297
 45.7 nM [IC50]
Inhibitor
8297
 73.7 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
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
Phase II
1132
Unknown

Approved Use

Unknown
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
108 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
60 mg 1 times / day steady, oral
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
Health Status: unhealthy
Condition: advanced solid tumors
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211288s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
unhealthy
n = 227
Health Status: unhealthy
Condition: non-small cell lung cancer
Population Size: 227
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211288Orig1s000MultidisciplineR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inducer
781
inhibitor
1767
substrate
1217

inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP3A4/5
278

UGT1A1
204

UGT1A4
77

UGT1A6
108

UGT1A9
116

UGT2B7
146

UGT2B15
64

P-gp
1461

BCRP
699

OCT1
512

OAT1
599

OAT3
642

OCT2
647

OATP1B1
788

OATP1B3
706

BSEP
402
P-gp
1537

BCRP
561
CYP1A2
701

CYP2B6
547
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BSEP
403
 no
CYP1A2
1692
 no
CYP1A2
1692
 no
CYP2B6
1001
 no
CYP2B6
1001
 no
CYP2C19
1553
 no
CYP2C8
965
 no
CYP2C9
1819
 no
CYP3A4
1925
 no
CYP3A4/5
335
 no
OAT1
603
 no
OAT3
644
 no
OATP1B1
803
 no
OATP1B3
715
 no
OCT2
648
 no
UGT1A4
80
 no
UGT1A6
141
 no
UGT1A9
121
 no
UGT2B15
64
 no
UGT2B7
157
 no
BCRP
773
 yes
OCT1
543
 yes
P-gp
1650
 yes
UGT1A1
254
 yes
CYP2D6
1891
 yes
yes (co-administration study)
Comment: dacomitnib increased dextromethorphan AUC by 362% and Cmax by 973%
Page: 55.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
561
 yes
CYP3A4
1737
 yes
P-gp
1537
 yes
CYP2D6
1217
 yes
no (co-administration study)
Comment: paroxetine increased dacaomitnib AUC by 37%
Page: 55.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
AA Blocks
AA008TCL
https://www.aablocks.com/goods/Goods/detail?id=AA008TCL
AK Scientific, Inc. (AKSCI)
Y0338
http://www.aksci.com/item_detail.php?cat=Y0338
Aaron Chemicals
AR008U4D
http://www.aaronchem.com/1110813-31-4
AbMole Bioscience
M1869
http://www.abmole.com/products/dacomitinib.html
Acadechem
ACDS-068047
http://www.acadechemical.com/product/142746
Aceschem
ACF023368
https://www.aceschem.com/catalog/1110813-31-4.html
Achemtek
0102-012372
http://www.achemtek.com/1110813-31-4
Acorn PharmaTech
ACN-031538
http://www.acornpharmatech.com/
Acorn PharmaTech
ACN-039804
http://www.acornpharmatech.com/
Active Biopharma
ABP000126
http://www.activebiopharma.com/1110813-31-4
Adooq BioScience
PF299804
http://www.adooq.com/pf299804.html
Adooq BioScience
A11051
https://www.adooq.com/pf299804.html
Allbio Pharm Co., Ltd
AF10236
http://www.allbiopharm.com/product/n/AF10236
Alsachim
4710
http://www.alsachim.com/product-C6058-glo.bal-view.html
Ambinter
Amb22170031
http://www.ambinter.com/reference/22170031
ApexBio Technology
A8319
http://www.apexbt.com/dacomitinib-pf299804-pf299.html
Aurora Fine Chemicals LLC
A24.092.577
http://online.aurorafinechemicals.com/info?ID=A24.092.577
Aurora Fine Chemicals LLC
K16.647.345
http://online.aurorafinechemicals.com/info?ID=K16.647.345
Aurum Pharmatech LLC
Q-4059
http://www.Aurumpharmatech.com/Product/ProductDetails/Q_4059
Axon MedChem
3235
https://www.axonmedchem.com/product/3235
BioChemPartner
BCP02530
http://www.biochempartner.com/1110813-31-4-BCP02530
BioCrick
BCC3683
http://www.biocrick.com/Dacomitinib-PF299804-PF299-BCC3683.html
BioSynth
J-500784
https://www.biosynth.com/en/products/all-products/products/J-500784.html
Boerchem
BC261945
http://www.boerchem.com/?product_43053.html
Chem Scene
CS-0500
http://www.chemscene.com/1110813-31-4.html
ChemWise
AR60114
http://www.chemwisellc.com/product/dacomitinib-pf299804/
Chemspace
CSSB00016996156
https://chem-space.com/CSSB00016996156
DC Chemicals
DC1091
http://www.dcchemicals.com/product_show-PF_299804_Dacomitinib_PF_00299804_.html
Excenen
EX-A030
http://www.excenen.com/searchresultlist.php?id=1110813-31-4
Glentham Life Sciences
GP3436
http://www.glentham.com/products/product/GP3436/
Hairui
HR144463
http://www.hairuichem.com/en/product/1110813-31-4.html
Matrix Scientific
125377
https://www.matrixscientific.com/125377.html
MedChem Express
HY-13272
https://www.medchemexpress.com/Dacomitinib.html
Renno Tech
RL00451
http://www.rennotech.com/product_show.asp?id=1197
Sinfoo Biotech
S052390
http://www.sinfoobiotech.com/product/1055788
Smolecule
S547934
http://www.smolecule.com/products/s547934
Smolecule
S785416
https://www.smolecule.com/products/s785416
Synblock Inc
SB21754
http://www.synblock.com/product/1110813-31-4.html
TCI (Tokyo Chemical Industry)
D5450
http://www.tcichemicals.com/eshop/en/us/commodity/D5450/index.html
THE BioTek
bt-287214
https://www.thebiotek.com/product/inhibitors/bt-287214
Tocris
6231
https://www.tocris.com/products/dacomitinib_6231
VladaChem
VL263938-10MG
https://www.vladachem.com/product.php?products=1110813-31-4
Yuhao Chemical
YH65989
http://www.chemyuhao.com/1110813-31-4.html
abcr GmbH
AB447090
http://www.abcr.com/shop/en/AB447090
eNovation Chemicals
K13827
https://www.enovationchem.com/ProductDetails.asp?ProductID=K13827
eNovation Chemicals
Y0974039
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0974039
PubMed

PubMed

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

Patents

20050250761
2
20100190977
2
7772243
2
8623883
2

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
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 Fri Dec 15 16:26:48 UTC 2023
Edited
by admin
on Fri Dec 15 16:26:48 UTC 2023
Record UNII
2XJX250C20
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DACOMITINIB ANHYDROUS
Common Name English
(2E)-N-(4-((3-CHLORO-4-FLUOROPHENYL)AMINO)-7-METHOXYQUINAZOLIN-6-YL)-4-PIPERIDIN-1-YLBUT-2-ENAMIDE
Systematic Name English
PF-00299804
Code English
dacomitinib [INN]
Common Name English
Dacomitinib [WHO-DD]
Common Name English
Code System Code Type Description
INN
9314
Created by admin on Fri Dec 15 16:26:48 UTC 2023 , Edited by admin on Fri Dec 15 16:26:48 UTC 2023
PRIMARY
CAS
1110813-31-4
Created by admin on Fri Dec 15 16:26:48 UTC 2023 , Edited by admin on Fri Dec 15 16:26:48 UTC 2023
PRIMARY
RXCUI
2058848
Created by admin on Fri Dec 15 16:26:48 UTC 2023 , Edited by admin on Fri Dec 15 16:26:48 UTC 2023
PRIMARY
EPA CompTox
DTXSID50149493
Created by admin on Fri Dec 15 16:26:48 UTC 2023 , Edited by admin on Fri Dec 15 16:26:48 UTC 2023
PRIMARY
NCI_THESAURUS
C171723
Created by admin on Fri Dec 15 16:26:48 UTC 2023 , Edited by admin on Fri Dec 15 16:26:48 UTC 2023
PRIMARY
FDA UNII
2XJX250C20
Created by admin on Fri Dec 15 16:26:48 UTC 2023 , Edited by admin on Fri Dec 15 16:26:48 UTC 2023
PRIMARY
PUBCHEM
11511120
Created by admin on Fri Dec 15 16:26:48 UTC 2023 , Edited by admin on Fri Dec 15 16:26:48 UTC 2023
PRIMARY
CHEBI
132268
Created by admin on Fri Dec 15 16:26:48 UTC 2023 , Edited by admin on Fri Dec 15 16:26:48 UTC 2023
PRIMARY
SMS_ID
100000175266
Created by admin on Fri Dec 15 16:26:48 UTC 2023 , Edited by admin on Fri Dec 15 16:26:48 UTC 2023
PRIMARY
DAILYMED
2XJX250C20
Created by admin on Fri Dec 15 16:26:48 UTC 2023 , Edited by admin on Fri Dec 15 16:26:48 UTC 2023
PRIMARY
Related Record Type Details
ATP-BINDING CASSETTE SUB-FAMILY G MEMBER 2
TRANSPORTER -> INHIBITOR
The reversal effect on ABCB1-overexpressing cells is more potent than that on ABCG2-overexpressing cells. Dacomitinib at 1.0 μM significantly reversed drug resistance mediated by ABCB1 and ABCG2, but not ABCC1, doing so by antagonizing the drug efflux function in ABCB1- and ABCG2-overexpressing cell lines.
BINDING
MAY BE CLINICALLY SIGNIFICANT
Structure of DACOMITINIB
SOLVATE->ANHYDROUS
EPIDERMAL GROWTH FACTOR RECEPTOR
TARGET -> INHIBITOR
IRREVERSIBLE INHIBITOR
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> INHIBITOR
The reversal effect on ABCB1-overexpressing cells is more potent than that on ABCG2-overexpressing cells. Dacomitinib at 1.0 μM significantly reversed drug resistance mediated by ABCB1 and ABCG2, but not ABCC1, doing so by antagonizing the drug efflux function in ABCB1- and ABCG2-overexpressing cell lines.
BINDING
MAY BE CLINICALLY SIGNIFICANT
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
IN-VITRO
CYTOCHROME P450 2D6
METABOLIC ENZYME -> SUBSTRATE
IN-VITRO
Structure of DACOMITINIB
SALT/SOLVATE -> PARENT
Related Record Type Details
Structure of N-(4-(3-CHLORO-4-FLUORO-ANILINO)-7-METHOXY-QUINAZOLIN-6-YL)-4-(2-OXO-1-PIPERIDYL)BUT-2-ENAMIDE
METABOLITE -> PARENT
MINOR
FECAL
Structure of 2-AMINO-3-(3-((4-(3-CHLORO-4-FLUORO-ANILINO)-7-METHOXY-QUINAZOLIN-6-YL)AMINO)-3-OXO-1-(1-PIPERIDYLMETHYL)PROPYL)SULFANYL-PROPANOIC ACID, (2R)-
METABOLITE -> PARENT
In addition, it is likely that dacomitinib underwent glutathione conjugation with subsequent hydrolysis to form the cysteine conjugate (M2).
MAJOR
FECAL
Structure of 5-((4-((4-((3-CHLORO-4-FLUOROPHENYL)AMINO)-7-METHOXYQUINAZOLIN-6-YL)AMINO)-4-OXOBUT-2-EN-1-YL)AMINO)PENTANOIC ACID
METABOLITE -> PARENT
MINOR
FECAL
Structure of O-DESMETHYL DACOMITINIB
METABOLITE ACTIVE -> PARENT
Concentrations of PF-05199265 peaked at 6 h post-dose.
MAJOR
PLASMA
Structure of O-DESMETHYL DACOMITINIB
METABOLITE ACTIVE -> PARENT
MAJOR
FECAL; PLASMA
Structure of O-DESMETHYL DACOMITINIB
METABOLITE ACTIVE -> PARENT
Fecal homogenate extracts indicated that metabolism of [14C] dacomitinib was similar and extensive in all the 6 subjects. The four most abundant drugrelated components were dacomitinib (20 %), PF-05199265 (20 %), a cysteine conjugate (M2; 9.5 %), and a monooxygenated metabolite (M7; 5.1 %)
MAJOR
FECAL
Related Record Type Details
Structure of DACOMITINIB ANHYDROUS
ACTIVE MOIETY
NIH
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