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Details

Stereochemistry ACHIRAL
Molecular Formula C28H33N7O2
Molecular Weight 499.6084
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of OSIMERTINIB

SMILES

C=CC(=Nc1cc(c(cc1N(C)CCN(C)C)OC)Nc2nccc(-c3cn(C)c4ccccc34)n2)O

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 499.6084
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: 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.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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

1447286400000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
660.7 nM
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
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
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
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
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%
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
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:
unhealthy, 71 years
Health Status: unhealthy
Age Group: 71 years
Sex: F
Sources:
Other AEs: Nausea, Vomiting...
Other AEs:
Nausea
Vomiting
Diarrhea
Sources:
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:
unhealthy
Other AEs: Rash, Diarrhea...
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 63 years
Health Status: unhealthy
Age Group: 63 years
Sex: M+F
Sources:
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:
unhealthy, 71 years
Health Status: unhealthy
Age Group: 71 years
Sex: F
Sources:
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:
unhealthy, 71 years
Health Status: unhealthy
Age Group: 71 years
Sex: F
Sources:
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:
unhealthy, 71 years
Health Status: unhealthy
Age Group: 71 years
Sex: F
Sources:
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:
unhealthy
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:
unhealthy
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 22 uM]
no [IC50 22.8 uM]
no [IC50 23 uM]
no [IC50 31.91 uM]
no [IC50 4.63 uM]
no [IC50 52.5 uM]
no [IC50 7.98 uM]
no [IC50 >100 uM]
no [Inhibition 33 uM]
no
no
no
no
no
no
no
no
no
weak [IC50 5.1 uM]
yes
yes
yes
yes
yes
yes
Drug as victimTox targets
PubMed

PubMed

TitleDatePubMed
Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed.
2015 Dec
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

Sample Use Guides

80 mg orally once daily, with or without food
Route of Administration: Oral
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 Jun 26 13:54:58 UTC 2021
Edited
by admin
on Sat Jun 26 13:54:58 UTC 2021
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 [WHO-DD]
Common Name English
OSIMERTINIB [MI]
Common Name English
OSIMERTINIB [INN]
Common Name English
MERELETINIB
INN  
Official 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 Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
FDA ORPHAN DRUG 445214
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
NCI_THESAURUS C2167
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
WHO-ATC L01XE35
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
Code System Code Type Description
ChEMBL
CHEMBL3353410
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
FDA UNII
3C06JJ0Z2O
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
DRUG BANK
DB09330
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
RXCUI
1721560
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY RxNorm
NDF-RT
N0000191266
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY Cytochrome P450 1A2 Inducers [MoA]
INN
10043
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
NDF-RT
N0000175082
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY Kinase Inhibitors [MoA]
LACTMED
Osimertinib
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
NDF-RT
N0000190114
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY Cytochrome P450 3A Inhibitors [MoA]
NDF-RT
N0000185506
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY Cytochrome P450 3A4 Inducers [MoA]
CAS
1421373-65-0
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
WIKIPEDIA
OSIMERTINIB
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
DRUG CENTRAL
5062
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
NDF-RT
N0000190113
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY Breast Cancer Resistance Protein Inhibitors [MoA]
MERCK INDEX
M11906
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
NCI_THESAURUS
C116377
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
EVMPD
SUB176340
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
PUBCHEM
71496458
Created by admin on Sat Jun 26 13:54:59 UTC 2021 , Edited by admin on Sat Jun 26 13:54:59 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
MAJOR
EXCRETED UNCHANGED
FECAL; URINE
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TARGET -> INHIBITOR
BINDER->LIGAND
BINDING
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC