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Details

Stereochemistry ACHIRAL
Molecular Formula C28H33N7O2
Molecular Weight 499.6073
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of OSIMERTINIB

SMILES

COC1=C(NC2=NC=CC(=N2)C3=CN(C)C4=CC=CC=C34)C=C(NC(=O)C=C)C(=C1)N(C)CCN(C)C

InChI

InChIKey=DUYJMQONPNNFPI-UHFFFAOYSA-N
InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32)

HIDE SMILES / InChI
Molecular Formula C28H33N7O2
Molecular Weight 499.6073
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB09330

Osimertinib is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug developed by AstraZeneca Pharmaceuticals. Its use is indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) in cases where tumour EGFR expression is positive for the T790M mutation as detected by FDA-approved testing and which has progressed following therapy with a first-generation EGFR tyrosine kinase inhibitor. Approximately 10% of patients with NSCLC have a rapid and clinically effective response to EGFR-TKIs due to the presence of specific activating EGFR mutations within the tumour cells. More specifically, deletions around the LREA motif in exon 19 and exon 21 L858R point mutations are correlated with response to therapy. Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that binds to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) that predominate in non-small cell lung cancer (NSCLC) tumours following treatment with first-line EGFR-TKIs. As a third-generation tyrosine kinase inhibitor, osimertinib is specific for the gate-keeper T790M mutation which increases ATP binding activity to EGFR and results in poor prognosis for late-stage disease. Furthermore, osimertinib has been shown to spare wild-type EGFR during therapy, thereby reducing non-specific binding and limiting toxicity. Osimertinib is marketed under the brand name Tagrisso.

CNS Activity

Originator

Approval Year

2015
471
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 12.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
TAGRISSO

Approved Use

TAGRISSO is a kinase inhibitor indicated for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation positive non-small cell lung cancer (NSCLC), as detected by an FDA approved test, who have progressed on or after EGFR TKI therapy.

Launch Date

2015
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
660.7 nM
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5891183/pdf/CAS-109-1177.pdf
80 mg 1 times / day steady-state, oral
dose: 80 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OSIMERTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
118 nM
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/29683562
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSIMERTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
12670 nM × h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5891183/pdf/CAS-109-1177.pdf
80 mg 1 times / day steady-state, oral
dose: 80 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OSIMERTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6770 nM × h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/29683562
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSIMERTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
59.7 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/29683562
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSIMERTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
5%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s008lbl.pdf
OSIMERTINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Disc. AE: Electrocardiogram QT prolonged, Neutropenia...
Other AEs: Diarrhea, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Electrocardiogram QT prolonged (2.2%)
Neutropenia (1.9%)
Pneumonitis (grade 5, 1%)
Pneumonia (grade 5, 4 patients)
Cerebral hemorrhage (grade 5, 2 patients)
Other AEs:
Diarrhea (grade 1-2, 41%)
Diarrhea (grade 3-4, 1%)
Nausea (grade 1-2, 16.5%)
Nausea (grade 3-4, 0.5%)
Decreased appetite (grade 1-2, 15.3%)
Decreased appetite (grade 3-4, 0.7%)
Constipation (grade 1-2, 14.8%)
Constipation (grade 3-4, 0.2%)
Stomatitis (grade 1-2, 12%)
Rash (grade 1-2, 40.5%)
Generalized rash (grade 1-2, 40.5%)
Rash erythematous (grade 1-2, 40.5%)
Rash macular (grade 1-2, 40.5%)
Rash maculo-papular (grade 1-2, 40.5%)
Rash papular (grade 1-2, 40.5%)
Rash pustular (grade 1-2, 40.5%)
Erythema (grade 1-2, 40.5%)
Folliculitis (grade 1-2, 40.5%)
Acne (grade 1-2, 40.5%)
Dermatitis (grade 1-2, 40.5%)
Acneiform dermatitis (grade 1-2, 40.5%)
Rash (grade 3-4, 0.5%)
Generalized rash (grade 3-4, 0.5%)
Rash erythematous (grade 3-4, 0.5%)
Rash macular (grade 3-4, 0.5%)
Rash maculo-papular (grade 3-4, 0.5%)
Rash papular (grade 3-4, 0.5%)
Rash pustular (grade 3-4, 0.5%)
Erythema (grade 3-4, 0.5%)
Folliculitis (grade 3-4, 0.5%)
Acne (grade 3-4, 0.5%)
Dermatitis (grade 3-4, 0.5%)
Acneiform dermatitis (grade 3-4, 0.5%)
Dry skin (grade 1-2, 31%)
Eczema (grade 1-2, 31%)
Skin fissures (grade 1-2, 31%)
Xerosis (grade 1-2, 31%)
Disorder nail (grade 1-2, 25%)
Nail bed disorder (grade 1-2, 25%)
Nail bed inflammation (grade 1-2, 25%)
Nail bed tenderness (grade 1-2, 25%)
Nail discoloration (grade 1-2, 25%)
Nail dystrophy (grade 1-2, 25%)
Nail infection (grade 1-2, 25%)
Nail ridging (grade 1-2, 25%)
Onychoclasis (grade 1-2, 25%)
Onycholysis (grade 1-2, 25%)
Onychomadesis (grade 1-2, 25%)
Paronychia (grade 1-2, 25%)
Pruritus (grade 1-2, 14%)
Cough (grade 1-2, 13.8%)
Cough (grade 3-4, 0.2%)
Fatigue (grade 1-2, 13.5%)
Fatigue (grade 3-4, 0.5%)
Back pain (grade 1-2, 12.3%)
Back pain (grade 3-4, 0.7%)
Headache (grade 1-2, 9.8%)
Headache (grade 3-4, 0.2%)
Pneumonia (grade 1-2, 1.8%)
Pneumonia (grade 3-4, 2.2%)
Deep vein thrombosis (grade 1-2, 4.6%)
Jugular vein thrombosis (grade 1-2, 4.6%)
Pulmonary embolism (grade 1-2, 4.6%)
Deep vein thrombosis (grade 3-4, 2.4%)
Jugular vein thrombosis (grade 3-4, 2.4%)
Pulmonary embolism (grade 3-4, 2.4%)
Cerebrovascular accident (2.7%)
Hyponatremia (grade 1-2, 22.6%)
Hyponatremia (grade 3-4, 3.4%)
Hypermagnesemia (grade 1-2, 19.3%)
Hypermagnesemia (grade 3-4, 0.7%)
Lymphopenia (grade 1-2, 59.7%)
Lymphopenia (grade 3-4, 3.3%)
Thrombocytopenia (grade 1-2, 52.8%)
Thrombocytopenia (grade 3-4, 1.2%)
Anemia (grade 1-2, 43.8%)
Anemia (grade 3-4, 0.2%)
Neutropenia (grade 1-2, 29.6%)
Neutropenia (grade 3-4, 3.4%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
240 mg 1 times / day multiple, oral
Highest studied dose
Dose: 240 mg, 1 times / day
Route: oral
Route: multiple
Dose: 240 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29074213
unhealthy, 71 years
n = 1
Health Status: unhealthy
Condition: EGFR L858R–mutant metastatic lung adenocarcinoma
Age Group: 71 years
Sex: F
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/29074213
Other AEs: Nausea, Vomiting...
Other AEs:
Nausea
Vomiting
Diarrhea
Sources:
https://pubmed.ncbi.nlm.nih.gov/29074213
240 mg 1 times / day steady, oral
Highest studied dose
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208065Orig1s000ClinPharmR.pdf
Page: 53
unhealthy
n = 13
Health Status: unhealthy
Condition: NSCLC
Sex: M+F
Population Size: 13
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208065Orig1s000ClinPharmR.pdf
Page: 53
Other AEs: Rash, Diarrhea...
Other AEs:
Rash (60%)
Diarrhea (58%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208065Orig1s000ClinPharmR.pdf
Page: 53
AEs

AEs

AESignificanceDosePopulation
Neutropenia 1.9%
Disc. AE
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Electrocardiogram QT prolonged 2.2%
Disc. AE
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Cerebrovascular accident 2.7%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Pneumonia grade 1-2, 1.8%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Stomatitis grade 1-2, 12%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Back pain grade 1-2, 12.3%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Fatigue grade 1-2, 13.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Cough grade 1-2, 13.8%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Pruritus grade 1-2, 14%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Constipation grade 1-2, 14.8%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Decreased appetite grade 1-2, 15.3%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Nausea grade 1-2, 16.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Hypermagnesemia grade 1-2, 19.3%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Hyponatremia grade 1-2, 22.6%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Disorder nail grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Nail bed disorder grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Nail bed inflammation grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Nail bed tenderness grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Nail discoloration grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Nail dystrophy grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Nail infection grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Nail ridging grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Onychoclasis grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Onycholysis grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Onychomadesis grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Paronychia grade 1-2, 25%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Neutropenia grade 1-2, 29.6%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Dry skin grade 1-2, 31%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Eczema grade 1-2, 31%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Skin fissures grade 1-2, 31%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Xerosis grade 1-2, 31%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Deep vein thrombosis grade 1-2, 4.6%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Jugular vein thrombosis grade 1-2, 4.6%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Pulmonary embolism grade 1-2, 4.6%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Acne grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Acneiform dermatitis grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Dermatitis grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Erythema grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Folliculitis grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Generalized rash grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash erythematous grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash macular grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash maculo-papular grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash papular grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash pustular grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash grade 1-2, 40.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Diarrhea grade 1-2, 41%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Anemia grade 1-2, 43.8%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Thrombocytopenia grade 1-2, 52.8%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Lymphopenia grade 1-2, 59.7%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Headache grade 1-2, 9.8%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Anemia grade 3-4, 0.2%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Constipation grade 3-4, 0.2%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Cough grade 3-4, 0.2%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Headache grade 3-4, 0.2%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Acne grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Acneiform dermatitis grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Dermatitis grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Erythema grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Fatigue grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Folliculitis grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Generalized rash grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Nausea grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash erythematous grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash macular grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash maculo-papular grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash papular grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash pustular grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Rash grade 3-4, 0.5%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Back pain grade 3-4, 0.7%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Decreased appetite grade 3-4, 0.7%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Hypermagnesemia grade 3-4, 0.7%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Diarrhea grade 3-4, 1%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Thrombocytopenia grade 3-4, 1.2%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Pneumonia grade 3-4, 2.2%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Deep vein thrombosis grade 3-4, 2.4%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Jugular vein thrombosis grade 3-4, 2.4%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Pulmonary embolism grade 3-4, 2.4%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Lymphopenia grade 3-4, 3.3%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Hyponatremia grade 3-4, 3.4%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Neutropenia grade 3-4, 3.4%
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Pneumonitis grade 5, 1%
Disc. AE
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Cerebral hemorrhage grade 5, 2 patients
Disc. AE
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Pneumonia grade 5, 4 patients
Disc. AE
80 mg 1 times / day steady, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: steady
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
unhealthy, 63 years
n = 411
Health Status: unhealthy
Condition: EGFR T790M mutation-positive non-small cell lung cancer
Age Group: 63 years
Sex: M+F
Population Size: 411
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208065s000lbl.pdf
Diarrhea
240 mg 1 times / day multiple, oral
Highest studied dose
Dose: 240 mg, 1 times / day
Route: oral
Route: multiple
Dose: 240 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29074213
unhealthy, 71 years
n = 1
Health Status: unhealthy
Condition: EGFR L858R–mutant metastatic lung adenocarcinoma
Age Group: 71 years
Sex: F
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/29074213
Nausea
240 mg 1 times / day multiple, oral
Highest studied dose
Dose: 240 mg, 1 times / day
Route: oral
Route: multiple
Dose: 240 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29074213
unhealthy, 71 years
n = 1
Health Status: unhealthy
Condition: EGFR L858R–mutant metastatic lung adenocarcinoma
Age Group: 71 years
Sex: F
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/29074213
Vomiting
240 mg 1 times / day multiple, oral
Highest studied dose
Dose: 240 mg, 1 times / day
Route: oral
Route: multiple
Dose: 240 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29074213
unhealthy, 71 years
n = 1
Health Status: unhealthy
Condition: EGFR L858R–mutant metastatic lung adenocarcinoma
Age Group: 71 years
Sex: F
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/29074213
Diarrhea 58%
240 mg 1 times / day steady, oral
Highest studied dose
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208065Orig1s000ClinPharmR.pdf
Page: 53
unhealthy
n = 13
Health Status: unhealthy
Condition: NSCLC
Sex: M+F
Population Size: 13
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208065Orig1s000ClinPharmR.pdf
Page: 53
Rash 60%
240 mg 1 times / day steady, oral
Highest studied dose
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208065Orig1s000ClinPharmR.pdf
Page: 53
unhealthy
n = 13
Health Status: unhealthy
Condition: NSCLC
Sex: M+F
Population Size: 13
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/208065Orig1s000ClinPharmR.pdf
Page: 53
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
781
inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP3A
214

BCRP
699

CYP1A2
1524

CYP2A6
707

CYP2B6
810

CYP2E1
882

P-gp
1461

OAT1
599

OAT3
642

OATP1B1
788

OATP1B3
706

MATE1
306

MATE2
263

OCT2
647

CYP2C8
911

CYP3A4/5
278

Cav1.2
45

Kv4.3
16

Kv1.5
26

Cav3.2
12
CYP3A
191

P-gp
1537

BCRP
561

OATP1B1
406

OATP1B3
350
CYP2C
15

P-gp
257

CYP1A2
701
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OATP1B1
803
 no [IC50 22 uM]
CYP2C8
965
 no [IC50 22.8 uM]
MATE2
263
 no [IC50 23 uM]
Cav3.2
12
 no [IC50 31.91 uM]
MATE1
308
 no [IC50 4.63 uM]
OATP1B3
715
 no [IC50 52.5 uM]
OCT2
648
 no [IC50 7.98 uM]
Kv1.5
41
 no [IC50 >100 uM]
Kv4.3
16
 no [Inhibition 33 uM]
CYP1A2
1692
 no
CYP2A6
739
 no
CYP2B6
1001
 no
CYP2C9
1819
 no
CYP2D6
1891
 no
CYP2E1
970
 no
OAT1
603
 no
OAT3
644
 no
P-gp
1650
 no
CYP3A4/5
335
 weak [IC50 5.1 uM]
BCRP
773
 yes
CYP1A2
1692
 yes
CYP2C
34
 yes
CYP3A
298
 yes
CYP3A4
1925
 yes
P-gp
1650
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A
191
 major
OATP1B1
406
 no
OATP1B3
350
 no
BCRP
561
 yes
P-gp
1537
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Cav1.2
49
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:90943
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:90943
ChemicalBook
CB02677059
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB02677059
MolPort
MolPort-035-395-886
https://www.molport.com/shop/molecule-link/MolPort-035-395-886
ZINC
ZINC000098023177
http://zinc15.docking.org/substances/ZINC000098023177
PubMed

PubMed

TitleDatePubMed
Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib.
2004 May 20
AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
2014 Sep
Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed.
2015 Dec
Second and third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer.
2015 Mar
The latest therapeutic strategies after resistance to first generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) in patients with non-small cell lung cancer (NSCLC).
2015 May
Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer.
2015 Sep
Emerging Agents and New Mutations in EGFR-Mutant Lung Cancer.
2015 Sep 1
Management of advanced non-small cell lung cancers with known mutations or rearrangements: latest evidence and treatment approaches.
2016 Apr
Osimertinib: First Global Approval.
2016 Feb
Patents

Patents

20130053409
2

Sample Use Guides

In Vivo Use Guide
80 mg orally once daily, with or without food
Route of Administration: Oral
In Vitro Use Guide
Osimertinib inhibited cell lines harboring classic EGFR mutations, exon 19 deletions (PC-9) and L858R (H3255) with IC50 values 17 nM and 4 nM, respectively
Substance Class Chemical
Created
by admin
on Sat Dec 16 08:50:58 GMT 2023
Edited
by admin
on Sat Dec 16 08:50:58 GMT 2023
Record UNII
3C06JJ0Z2O
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
OSIMERTINIB
DASH   INN   USAN   WHO-DD  
USAN   INN  
Official Name English
OSIMERTINIB [MI]
Common Name English
osimertinib [INN]
Common Name English
MERELETINIB
INN  
Official Name English
Osimertinib [WHO-DD]
Common Name English
OSIMERTINIB [USAN]
Common Name English
2-PROPENAMIDE, N-(2-((2-(DIMETHYLAMINO)ETHYL)METHYLAMINO)-4-METHOXY-5-((4-(1-METHYL-1H-INDOL-3-YL)-2-PYRIMIDINYL)AMINO)PHENYL)-
Systematic Name English
AZD9291
Code English
AZD-9291
Code English
AZD-9291 FREE BASE
Code English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
NDF-RT N0000175605
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
FDA ORPHAN DRUG 445214
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
NCI_THESAURUS C2167
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
WHO-ATC L01XE35
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
Code System Code Type Description
ChEMBL
CHEMBL3353410
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
FDA UNII
3C06JJ0Z2O
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
DRUG BANK
DB09330
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
RXCUI
1721560
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY RxNorm
NDF-RT
N0000191266
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY Cytochrome P450 1A2 Inducers [MoA]
USAN
CD-52
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
INN
10043
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
NDF-RT
N0000175082
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY Kinase Inhibitors [MoA]
LACTMED
Osimertinib
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
NDF-RT
N0000190114
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY Cytochrome P450 3A Inhibitors [MoA]
NDF-RT
N0000185506
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY Cytochrome P450 3A4 Inducers [MoA]
CAS
1421373-65-0
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
WIKIPEDIA
OSIMERTINIB
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
DRUG CENTRAL
5062
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
CHEBI
90943
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
SMS_ID
100000162510
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
DAILYMED
3C06JJ0Z2O
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
NDF-RT
N0000190113
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY Breast Cancer Resistance Protein Inhibitors [MoA]
MERCK INDEX
m11906
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
NCI_THESAURUS
C116377
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
EPA CompTox
DTXSID501025961
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
EVMPD
SUB176340
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
PUBCHEM
71496458
Created by admin on Sat Dec 16 08:50:58 GMT 2023 , Edited by admin on Sat Dec 16 08:50:58 GMT 2023
PRIMARY
Related Record Type Details
CYTOCHROME P450 1A1
METABOLIC ENZYME -> SUBSTRATE
EPIDERMAL GROWTH FACTOR RECEPTOR (EXON 19 DELETION/T790M/C797S MUTANT)
TARGET -> INHIBITOR RESISTANT
CYTOCHROME P450 1A1
METABOLIC ENZYME -> INDUCER
Modulation of CYP1A1/CYP1A2 levels markedly reduced parent drug concentrations, significantly altering metabolite pharmacokinetics (PK) in humanized mice in vivo. Produces three hydroxy impurities where site is not specified.
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
MAJOR
Structure of OSIMERTINIB
EXCRETED UNCHANGED
FECAL; URINE
CYTOCHROME P450 3A5
METABOLIC ENZYME -> SUBSTRATE
MAJOR
EPIDERMAL GROWTH FACTOR RECEPTOR T790M MUTANT
TARGET -> INHIBITOR
EPIDERMAL GROWTH FACTOR RECEPTOR (EXON 19 DELETION/T790M MUTANT)
TARGET -> INHIBITOR
Structure of OSIMERTINIB MESYLATE
SALT/SOLVATE -> PARENT
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Related Record Type Details
Structure of 2-PROPENAMIDE, N-(2-((2-(DIMETHYLOXIDOAMINO)ETHYL)METHYLAMINO)-4-METHOXY-5-((4-(1-METHYL-1H-INDOL-3-YL)-2-PYRIMIDINYL)AMINO)PHENYL)-
METABOLITE -> PARENT
URINE
Structure of N-Hydroxy-osimertinib
METABOLITE -> PARENT
Structure of N-(4-METHOXY-2-(METHYLAMINO)-5-((4-(1-METHYLINDOL-3-YL)PYRIMIDIN-2-YL)AMINO)PHENYL)PROP-2-ENAMIDE
METABOLITE -> PARENT
This metabolite was detected in human hepatocytes.
Structure of AZ-5104
METABOLITE -> PARENT
PLASMA
Structure of AZ-7550
METABOLITE ACTIVE -> PARENT
FECAL; URINE
Structure of (2R)-2-AMINO-3-(3-(2-(2-DIMETHYLAMINOETHYL(METHYL)AMINO)-4-METHOXY-5-((4-(1-METHYLINDOL-3-YL)PYRIMIDIN-2-YL)AMINO)ANILINO)-3-OXO-PROPYL)SULFANYL-PROPANOIC ACID
METABOLITE -> PARENT
Structure of AZ-5104
METABOLITE ACTIVE -> PARENT
FECAL; URINE
Structure of N-Hydroxy-osimertinib
METABOLITE -> PARENT
Related Record Type Details
Structure of OSIMERTINIB
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
NIH
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