Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C24H25ClFN5O3 |
Molecular Weight | 485.938 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)C\C=C\C(=O)NC1=CC2=C(C=C1O[C@H]3CCOC3)N=CN=C2NC4=CC(Cl)=C(F)C=C4
InChI
InChIKey=ULXXDDBFHOBEHA-CWDCEQMOSA-N
InChI=1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
Molecular Formula | C24H25ClFN5O3 |
Molecular Weight | 485.938 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 1 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/201292Orig1s000PharmR.pdf
Curator's Comment: description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/201292Orig1s000PharmR.pdf
Afatinib is a anilino-quinazoline derivative and irreversible antagonist of the receptor tyrosine kinase epidermal growth factor receptor family, with antineoplastic activity. Afatinib selectively and covalently binds to and inhibits the epidermal growth factor receptors 1 (ErbB1; EGFR), 2 (ErbB2; HER2), and 4 (ErbB4; HER4), and certain EGFR mutants, including those caused by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. This may result in the inhibition of tumor growth and angiogenesis in tumor cells overexpressing these kinases. Additionally, afatinib inhibits the EGFR T790M gatekeeper mutation which is resistant to treatment with first-generation EGFR inhibitors. EGFR, HER2 and HER4 are RTKs that belong to the EGFR superfamily; they play major roles in both tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types. Afatinib is a substrate and an inhibitor of P-gp and of the transporter BCRP. Co-administration of P-gp inhibitors can increase afatinib exposure while co-administration of chronic Pgp inducers can decrease afatinib exposure.
CNS Activity
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=25247337
Curator's Comment: Afatinib appears to penetrate into the CNS with concentrations high enough to have clinical effect on CNS metastases
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P00533|||Q9GZX1 Gene ID: 1956.0 Gene Symbol: EGFR Target Organism: Homo sapiens (Human) |
0.5 nM [IC50] | ||
Target ID: P04626 Gene ID: 2064.0 Gene Symbol: ERBB2 Target Organism: Homo sapiens (Human) |
14.0 nM [IC50] | ||
Target ID: Q15303 Gene ID: 2066.0 Gene Symbol: ERBB4 Target Organism: Homo sapiens (Human) |
0.7 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | GILOTRIF Approved UseIndicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test Launch Date2013 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
42.7 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29337963 |
40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
AFATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
33.7 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24906422 |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
AFATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
30.7 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24906422 |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
AFATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
683 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29337963 |
40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
AFATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
886 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24906422 |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
AFATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
956 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24906422 |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
AFATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
74.9 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24906422 |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
AFATINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
60.3 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/24906422 |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
AFATINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5% |
AFATINIB plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Other AEs: Diarrhoea, Rash... Other AEs: Diarrhoea (84.6%) Sources: Rash (72.3%) Dermatitis acneiform (13.6%) Stomatitis (58.2%) Nail disorder (38.5%) Decreased appetite (20.8%) Nausea (18.7%) Pruritus (17.7%) Epistaxis (14.6%) Dry skin (14.4%) Fatigue (14.4%) Vomiting (13.3%) Eye disorders NEC (9.2%) Palmar-plantar erythrodysaesthesia syndrome (7.7%) Diarrhoea (grade 3, 38.7%) Rash (grade 3, 13.3%) Dermatitis acneiform (grade 3, 1.3%) Stomatitis (grade 3, 2.8%) Nail disorder (grade 3, 4.9%) Decreased appetite (grade 3, 2.8%) Nausea (grade 3, 1.3%) Pruritus (grade 3, 0.3%) Dry skin (grade 3, 0.3%) Fatigue (grade 3, 3.1%) Vomiting (grade 3, 1.5%) Eye disorders NEC (grade 3, 0.5%) Palmar-plantar erythrodysaesthesia syndrome (grade 3, 1.3%) Diarrhoea (grade 4, 1%) |
50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Other AEs: ALT increased, AST increased... Other AEs: ALT increased (3.8%) Sources: AST increased (2.8%) Alkaline phosphatase increased (0.8%) Bilirubin increased (0.3%) GGT increased (0.3%) Hyperbilirubinaemia (1%) Hypoalbuminaemia (1.5%) Acute hepatic failure (0.3%) Anorectal varices (0.3%) Cytolytic hepatitis (0.3%) Hepatic pain (0.3%) Hepatitis acute (0.3%) |
360 mg 1 times / day single, oral Dose: 360 mg, 1 times / day Route: oral Route: single Dose: 360 mg, 1 times / day Sources: |
healthy, adolescents n = 2 Health Status: healthy Age Group: adolescents Population Size: 2 Sources: |
Other AEs: Nausea, Vomiting... Other AEs: Nausea Sources: Vomiting Asthenia Dizziness Headache Abdominal pain Amylase increased |
100 mg 1 times / day multiple, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 2 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 2 Sources: |
DLT: Skin rash, Diarrhoea... Dose limiting toxicities: Skin rash (grade 3, 50%) Sources: Diarrhoea (grade 3, 50%) |
70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 18 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 18 Sources: |
DLT: Fatigue, ALT increased... Dose limiting toxicities: Fatigue (grade 3, 5.6%) Sources: ALT increased (grade 3, 5.6%) |
70 mg 1 times / day multiple, oral Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 18 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 18 Sources: |
DLT: Diarrhoea... Dose limiting toxicities: Diarrhoea (grade 3, 11.1%) Sources: |
85 mg 1 times / day multiple, oral Dose: 85 mg, 1 times / day Route: oral Route: multiple Dose: 85 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 6 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 6 Sources: |
DLT: Diarrhoea, Diarrhoea... Dose limiting toxicities: Diarrhoea (grade 3, 16.7%) Sources: Diarrhoea (grade 2, 16.7%) |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Disc. AE: Diarrhea, Paronychia... AEs leading to discontinuation/dose reduction: Diarrhea (1.3%) Sources: Paronychia (0.9%) Interstitial lung disease (1%) |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Other AEs: Diarrhea, Stomatitis... Other AEs: Diarrhea (grade 3, 15%) Sources: Stomatitis (grade 3, 8%) |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Other AEs: Weight decreased, Nausea... Other AEs: Weight decreased (grade 3, 1%) Sources: Nausea (grade 3, 1%) Vomiting (grade 3, 4%) Dermatitis acneiform (grade 3, 3%) Hypokalaemia (grade 3, 2%) ALT increased (grade 3, 2%) AST increased (grade 3, 2%) Stomatitis (grade 4, <1%) Hypokalaemia (grade 4, 2%) |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: Page: 201292Orig1s000MedR.pdf - p.66 |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: Page: 201292Orig1s000MedR.pdf - p.66 |
Other AEs: Rash, Paronychia... Other AEs: Rash (grade 3, 16%) Sources: Page: 201292Orig1s000MedR.pdf - p.66Paronychia (grade 3, 11%) Cystitis (grade 3, 1%) Decreased appetite (grade 3, 4%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Vomiting | 13.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Dermatitis acneiform | 13.6% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Dry skin | 14.4% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Fatigue | 14.4% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Epistaxis | 14.6% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Pruritus | 17.7% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Nausea | 18.7% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Decreased appetite | 20.8% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Nail disorder | 38.5% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Stomatitis | 58.2% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Palmar-plantar erythrodysaesthesia syndrome | 7.7% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Rash | 72.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Diarrhoea | 84.6% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Eye disorders NEC | 9.2% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Dry skin | grade 3, 0.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Pruritus | grade 3, 0.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Eye disorders NEC | grade 3, 0.5% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Dermatitis acneiform | grade 3, 1.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Nausea | grade 3, 1.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Palmar-plantar erythrodysaesthesia syndrome | grade 3, 1.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Vomiting | grade 3, 1.5% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Rash | grade 3, 13.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Decreased appetite | grade 3, 2.8% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Stomatitis | grade 3, 2.8% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Fatigue | grade 3, 3.1% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Diarrhoea | grade 3, 38.7% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Nail disorder | grade 3, 4.9% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Diarrhoea | grade 4, 1% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Acute hepatic failure | 0.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Anorectal varices | 0.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Bilirubin increased | 0.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Cytolytic hepatitis | 0.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
GGT increased | 0.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Hepatic pain | 0.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Hepatitis acute | 0.3% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Alkaline phosphatase increased | 0.8% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Hyperbilirubinaemia | 1% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Hypoalbuminaemia | 1.5% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
AST increased | 2.8% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
ALT increased | 3.8% | 50 mg 1 times / day multiple, oral Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy, 32 to 82 years n = 390 Health Status: unhealthy Condition: non-small cell lung cancer Age Group: 32 to 82 years Sex: M+F Population Size: 390 Sources: |
Abdominal pain | 360 mg 1 times / day single, oral Dose: 360 mg, 1 times / day Route: oral Route: single Dose: 360 mg, 1 times / day Sources: |
healthy, adolescents n = 2 Health Status: healthy Age Group: adolescents Population Size: 2 Sources: |
|
Amylase increased | 360 mg 1 times / day single, oral Dose: 360 mg, 1 times / day Route: oral Route: single Dose: 360 mg, 1 times / day Sources: |
healthy, adolescents n = 2 Health Status: healthy Age Group: adolescents Population Size: 2 Sources: |
|
Asthenia | 360 mg 1 times / day single, oral Dose: 360 mg, 1 times / day Route: oral Route: single Dose: 360 mg, 1 times / day Sources: |
healthy, adolescents n = 2 Health Status: healthy Age Group: adolescents Population Size: 2 Sources: |
|
Dizziness | 360 mg 1 times / day single, oral Dose: 360 mg, 1 times / day Route: oral Route: single Dose: 360 mg, 1 times / day Sources: |
healthy, adolescents n = 2 Health Status: healthy Age Group: adolescents Population Size: 2 Sources: |
|
Headache | 360 mg 1 times / day single, oral Dose: 360 mg, 1 times / day Route: oral Route: single Dose: 360 mg, 1 times / day Sources: |
healthy, adolescents n = 2 Health Status: healthy Age Group: adolescents Population Size: 2 Sources: |
|
Nausea | 360 mg 1 times / day single, oral Dose: 360 mg, 1 times / day Route: oral Route: single Dose: 360 mg, 1 times / day Sources: |
healthy, adolescents n = 2 Health Status: healthy Age Group: adolescents Population Size: 2 Sources: |
|
Vomiting | 360 mg 1 times / day single, oral Dose: 360 mg, 1 times / day Route: oral Route: single Dose: 360 mg, 1 times / day Sources: |
healthy, adolescents n = 2 Health Status: healthy Age Group: adolescents Population Size: 2 Sources: |
|
Diarrhoea | grade 3, 50% DLT |
100 mg 1 times / day multiple, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 2 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 2 Sources: |
Skin rash | grade 3, 50% DLT |
100 mg 1 times / day multiple, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 2 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 2 Sources: |
ALT increased | grade 3, 5.6% DLT |
70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 18 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 18 Sources: |
Fatigue | grade 3, 5.6% DLT |
70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 18 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 18 Sources: |
Diarrhoea | grade 3, 11.1% DLT |
70 mg 1 times / day multiple, oral Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 18 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 18 Sources: |
Diarrhoea | grade 2, 16.7% DLT |
85 mg 1 times / day multiple, oral Dose: 85 mg, 1 times / day Route: oral Route: multiple Dose: 85 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 6 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 6 Sources: |
Diarrhoea | grade 3, 16.7% DLT |
85 mg 1 times / day multiple, oral Dose: 85 mg, 1 times / day Route: oral Route: multiple Dose: 85 mg, 1 times / day Sources: |
unhealthy, median age 58 years n = 6 Health Status: unhealthy Condition: solid tumours Age Group: median age 58 years Sex: M+F Population Size: 6 Sources: |
Paronychia | 0.9% Disc. AE |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Interstitial lung disease | 1% Disc. AE |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Diarrhea | 1.3% Disc. AE |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Diarrhea | grade 3, 15% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Stomatitis | grade 3, 8% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Nausea | grade 3, 1% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Weight decreased | grade 3, 1% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
ALT increased | grade 3, 2% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
AST increased | grade 3, 2% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Hypokalaemia | grade 3, 2% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Dermatitis acneiform | grade 3, 3% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Vomiting | grade 3, 4% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Hypokalaemia | grade 4, 2% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Stomatitis | grade 4, <1% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: |
Cystitis | grade 3, 1% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: Page: 201292Orig1s000MedR.pdf - p.66 |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: Page: 201292Orig1s000MedR.pdf - p.66 |
Paronychia | grade 3, 11% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: Page: 201292Orig1s000MedR.pdf - p.66 |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: Page: 201292Orig1s000MedR.pdf - p.66 |
Rash | grade 3, 16% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: Page: 201292Orig1s000MedR.pdf - p.66 |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: Page: 201292Orig1s000MedR.pdf - p.66 |
Decreased appetite | grade 3, 4% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: Page: 201292Orig1s000MedR.pdf - p.66 |
unhealthy, median age 61.5 years n = 229 Health Status: unhealthy Condition: adenocarcinoma of the lung Age Group: median age 61.5 years Sex: M+F Population Size: 229 Sources: Page: 201292Orig1s000MedR.pdf - p.66 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes [IC50 0.75 uM] | ||||
yes [Ki 3.4 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
minor | ||||
yes [Km 30 uM] | yes (co-administration study) Comment: Afatinib is a substrate and inhibitor (Ki=3.4 μM) for P-gp transporter and exposure to afatinib was changed when it was administered with a P-gp inhibitor, ritonavir (AUC increased by 48%) or with a P-gp inducer, rifampicin (AUC decreased by 34%). Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/201292Orig1s000ClinPharmR.pdf#page=15 Page: - |
|||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. | 2008 Aug 7 |
|
A phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumours. | 2008 Jan 15 |
|
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification. | 2010 Jul 8 |
|
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. | 2010 Nov 24 |
|
Phase I trial of the irreversible EGFR and HER2 kinase inhibitor BIBW 2992 in patients with advanced solid tumors. | 2010 Sep 1 |
|
Irreversible EGFR inhibitor EKB-569 targets low-LET γ-radiation-triggered rel orchestration and potentiates cell death in squamous cell carcinoma. | 2011 |
|
Afatinib (BIBW 2992) development in non-small-cell lung cancer. | 2011 Jul |
|
Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. | 2011 Mar 10 |
|
Genotype-driven therapies for non-small cell lung cancer: focus on EGFR, KRAS and ALK gene abnormalities. | 2011 May |
|
Comprehensive analysis of kinase inhibitor selectivity. | 2011 Oct 30 |
Sample Use Guides
In cellular in vitro assays, afatinib was able to inhibit phosphorylation and/or proliferation of multiple cell lines representing models of overexpression of wild type EGFR, constitutively active HER2, and EGFR exon 19 deletion mutations, including an exon 19/T790M double mutant. Concentrations of afatinib required for activity in these models ranged from approximately 10 to 100 nM; effects on exon 19/T790M double mutants typically occurred at the high end of this range.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 17:25:09 GMT 2023
by
admin
on
Fri Dec 15 17:25:09 GMT 2023
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Record UNII |
41UD74L59M
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Record Status |
Validated (UNII)
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Record Version |
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-
Download
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Official Name | English | ||
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Common Name | English | ||
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Brand Name | English | ||
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Brand Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
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NDF-RT |
N0000175605
Created by
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WHO-VATC |
QL01XE13
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WHO-ATC |
L01XE13
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FDA ORPHAN DRUG |
484115
Created by
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NCI_THESAURUS |
C2167
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EU-Orphan Drug |
EU/3/18/2110
Created by
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EMA ASSESSMENT REPORTS |
GIOTRIF(AUTHORIZED: CARCINOMA, NON-SMALL-CELL LUNG)
Created by
admin on Fri Dec 15 17:25:09 GMT 2023 , Edited by admin on Fri Dec 15 17:25:09 GMT 2023
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FDA ORPHAN DRUG |
375712
Created by
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FDA ORPHAN DRUG |
690419
Created by
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FDA ORPHAN DRUG |
433414
Created by
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FDA ORPHAN DRUG |
781420
Created by
admin on Fri Dec 15 17:25:09 GMT 2023 , Edited by admin on Fri Dec 15 17:25:09 GMT 2023
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NCI_THESAURUS |
C129825
Created by
admin on Fri Dec 15 17:25:09 GMT 2023 , Edited by admin on Fri Dec 15 17:25:09 GMT 2023
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Code System | Code | Type | Description | ||
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439081-18-2
Created by
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NON-SPECIFIC STEREOCHEMISTRY | |||
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AFATINIB
Created by
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PRIMARY | |||
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10184653
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PRIMARY | |||
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DB08916
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PRIMARY | |||
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750691
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PRIMARY | |||
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C66940
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PRIMARY | |||
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41UD74L59M
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PRIMARY | |||
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CHEMBL1173655
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PRIMARY | |||
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m1439
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PRIMARY | Merck Index | ||
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100000124505
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PRIMARY | |||
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61390
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PRIMARY | |||
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850140-72-6
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PRIMARY | |||
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41UD74L59M
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PRIMARY | |||
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1430438
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PRIMARY | RxNorm | ||
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9230
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PRIMARY | |||
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DTXSID20893451
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PRIMARY | |||
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SUB32268
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PRIMARY | |||
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4318
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PRIMARY | |||
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YY-16
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PRIMARY | |||
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5667
Created by
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PRIMARY | |||
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Afatinib
Created by
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PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
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TARGET -> INHIBITOR |
IRREVERSIBLE INHIBITOR
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TARGET -> INHIBITOR |
IRREVERSIBLE INHIBITOR
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BINDER->LIGAND |
BINDING
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TARGET -> INHIBITOR |
IRREVERSIBLE INHIBITOR
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TARGET -> INHIBITOR |
a case of successful treatment of a patient aged >80 years with lung adenocarcinoma positive for the uncommon EGFR L861Q mutation with low‐dose afatinib. An 83‐year‐old woman presented with cough and dyspnea. A chest computed tomography (CT) scan revealed tumors in the left upper lobe, left pleural effusion, and multiple lung metastases in both lungs. The patient was diagnosed with lung adenocarcinoma with an EGFR L861Q mutation based on cytological findings. The patient received 30 mg/day of afatinib and experienced no severe adverse events.
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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METABOLITE -> PARENT |
minor metabolite
MINOR
URINE
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METABOLITE -> PARENT | |||
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METABOLITE LESS ACTIVE -> PARENT | |||
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METABOLITE -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Cmax | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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