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

Details

Stereochemistry ACHIRAL
Molecular Formula C22H23N3O4
Molecular Weight 393.4366
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ERLOTINIB

SMILES

C#Cc1cccc(c1)Nc2c3cc(c(cc3ncn2)OCCOC)OCCOC

InChI

InChIKey=AAKJLRGGTJKAMG-UHFFFAOYSA-N
InChI=1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25)

HIDE SMILES / InChI

Description
Curator's Comment:: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021743s14s16lbl.pdf

Erlotinib hydrochloride (trade name Tarceva, Genentech/OSIP, originally coded as OSI-774) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer. Similar to gefitinib, erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. Erlotinib has recently been shown to be a potent inhibitor of JAK2V617F activity. JAK2V617F is a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders. The mechanism of clinical antitumor action of erlotinib is not fully characterized. Erlotinib inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor (EGFR). Specificity of inhibition with regard to other tyrosine kinase receptors has not been fully characterized. EGFR is expressed on the cell surface of normal cells and cancer cells.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TARCEVA

Approved Use

TARCEVA is a kinase inhibitor indicated for: Maintenance treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) whose disease has not progressed after four cycles of platinum-based first-line chemotherapy. Treatment of locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.

Launch Date

1.10064959E12
Primary
TARCEVA

Approved Use

TARCEVA is a kinase inhibitor indicated for: Maintenance treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) whose disease has not progressed after four cycles of platinum-based first-line chemotherapy. Treatment of locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.

Launch Date

1.10064959E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.25 μg/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ERLOTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
4.07 μg/mL
100 mg single, intravenous
dose: 100 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
ERLOTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1969.5 ng/mL
85 mg/m^2 1 times / day steady, oral
dose: 85 mg/m^2
route of administration: oral
experiment type: steady
co-administered:
ERLOTINIB plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
29.9 μg × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ERLOTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
32 μg × h/mL
100 mg single, intravenous
dose: 100 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
ERLOTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
26716.7 ng*h/mL
85 mg/m^2 1 times / day steady, oral
dose: 85 mg/m^2
route of administration: oral
experiment type: steady
co-administered:
ERLOTINIB plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
14.4 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ERLOTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
12.4 h
100 mg single, intravenous
dose: 100 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
ERLOTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
7%
ERLOTINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
100 mg 1 times / day single, intravenous
Highest studied dose
Dose: 100 mg, 1 times / day
Route: intravenous
Route: single
Dose: 100 mg, 1 times / day
Sources:
unhealthy, Median age 54 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 54 years
Sex: M+F
Population Size: 6
Sources:
150 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 7
Sources:
Other AEs: Mucositis, Diarrhea...
Other AEs:
Mucositis (grade 1-2, 28.6%)
Diarrhea (grade 1-2, 85.7%)
Hyperbilirubinemia (grade 1-2, 14.3%)
Skin toxicity (grade 1-2, 28.6%)
Sources:
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 6
Sources:
Other AEs: Diarrhea, Hyperbilirubinemia...
Other AEs:
Diarrhea (grade 1-2, 66.7%)
Hyperbilirubinemia (grade 1-2, 33.3%)
Skin toxicity (grade 1-2, 83.3%)
Headache (grade 1-2, 33.3%)
Diarrhea (grade 4, 33.3%)
Sources:
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Co-administed with::
Amrubicin(30 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Other AEs: Neutropenia...
Other AEs:
Neutropenia (grade 3, 33.3%)
Sources:
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Co-administed with::
Amrubicin(35 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Other AEs: Neutropenia, Neutropenia...
Other AEs:
Neutropenia (grade 3, 33.3%)
Neutropenia (grade 4, 66.7%)
Leukopenia (grade 3, 33.3%)
Leukopenia (grade 4, 33.3%)
Sources:
150 mg 1 times / day multiple, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Co-administed with::
Amrubicin(30 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Disc. AE: Leukopenia...
Other AEs: Erysipelas, Leukopenia...
AEs leading to
discontinuation/dose reduction:
Leukopenia (grade 3, 33.3%)
Other AEs:
Erysipelas (grade 3, 33.3%)
Leukopenia (grade 4, 33.3%)
Neutropenia (grade 3, 33.3%)
Neutropenia (grade 4, 33.3%)
Sources:
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Disc. AE: Rash, Diarrhea...
Other AEs: Rash, Pruritus...
AEs leading to
discontinuation/dose reduction:
Rash (10%)
Diarrhea (4%)
Rash (7%)
Diarrhea (2%)
Other AEs:
Rash (grade 3, 8%)
Pruritus (grade 3, <1%)
Diarrhea (grade 3, 6%)
Nausea (grade 3, 3%)
Vomiting (grade 3, 2%)
Stomatitis (grade 3, <1%)
Constipation (grade 3, 1%)
Abdominal pain (grade 3, 2%)
Fatigue (grade 3, 14%)
Chest pain (grade 3, 4%)
Dyspnea (grade 3, 17%)
Cough (grade 3, 4%)
Hemoptysis (grade 3, 1%)
Anorexia (grade 3, 8%)
Headache (grade 3, 1%)
Neuropathy (grade 3, 3%)
Bone pain (grade 3, 3%)
Infection (grade 3, 4%)
Conjunctivitis (grade 3, <1%)
Insomnia (grade 3, <1%)
Rash (grade 4, <1%)
Diarrhea (grade 4, <1%)
Anorexia (grade 4, 1%)
Fatigue (grade 4, 4%)
Dyspnea (grade 4, 11%)
Vomiting (grade 4, <1%)
Abdominal pain (grade 4, <1%)
Sources:
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Disc. AE: Diarrhoea, Rash...
2000 mg 1 times / week multiple, oral
Highest studied dose
Dose: 2000 mg, 1 times / week
Route: oral
Route: multiple
Dose: 2000 mg, 1 times / week
Sources:
unhealthy, Median age 63 years
n = 19
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 63 years
Sex: M+F
Population Size: 19
Sources:
Other AEs: Fatigue, Dehydration...
Other AEs:
Fatigue (grade 3, 5.3%)
Dehydration (grade 3, 5.3%)
Pneumonitis (grade 3, 5.3%)
Sources:
200 mg 2 times / day multiple, oral
Highest studied dose
healthy, adult
n = 6
Disc. AE: Rash...
1000 mg 1 times / day single, oral
Highest studied dose
healthy
n = 4
Other AEs: Erythematous rash...
200 mg 2 times / day multiple, oral
Highest studied dose
healthy
n = 5
Other AEs: Diarrhea, Transaminases increased...
AEs

AEs

AESignificanceDosePopulation
Hyperbilirubinemia grade 1-2, 14.3%
150 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 7
Sources:
Mucositis grade 1-2, 28.6%
150 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 7
Sources:
Skin toxicity grade 1-2, 28.6%
150 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 7
Sources:
Diarrhea grade 1-2, 85.7%
150 mg 1 times / day multiple, oral
Recommended|MTD
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 7
Sources:
Headache grade 1-2, 33.3%
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 6
Sources:
Hyperbilirubinemia grade 1-2, 33.3%
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 6
Sources:
Diarrhea grade 1-2, 66.7%
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 6
Sources:
Skin toxicity grade 1-2, 83.3%
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 6
Sources:
Diarrhea grade 4, 33.3%
200 mg 1 times / day multiple, oral
Studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, Median age 57 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: Median age 57 years
Sex: M+F
Population Size: 6
Sources:
Neutropenia grade 3, 33.3%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Co-administed with::
Amrubicin(30 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Leukopenia grade 3, 33.3%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Co-administed with::
Amrubicin(35 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Neutropenia grade 3, 33.3%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Co-administed with::
Amrubicin(35 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Leukopenia grade 4, 33.3%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Co-administed with::
Amrubicin(35 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Neutropenia grade 4, 66.7%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Co-administed with::
Amrubicin(35 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Erysipelas grade 3, 33.3%
150 mg 1 times / day multiple, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Co-administed with::
Amrubicin(30 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Neutropenia grade 3, 33.3%
150 mg 1 times / day multiple, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Co-administed with::
Amrubicin(30 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Leukopenia grade 3, 33.3%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Co-administed with::
Amrubicin(30 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Leukopenia grade 4, 33.3%
150 mg 1 times / day multiple, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Co-administed with::
Amrubicin(30 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Neutropenia grade 4, 33.3%
150 mg 1 times / day multiple, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Co-administed with::
Amrubicin(30 mg/m2; Days 1-3)
Sources:
unhealthy, Median age 62 years
n = 3
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 3
Sources:
Rash 10%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Diarrhea 2%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Diarrhea 4%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Rash 7%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Constipation grade 3, 1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Headache grade 3, 1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Hemoptysis grade 3, 1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Fatigue grade 3, 14%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Dyspnea grade 3, 17%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Abdominal pain grade 3, 2%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Vomiting grade 3, 2%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Bone pain grade 3, 3%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Nausea grade 3, 3%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Neuropathy grade 3, 3%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Chest pain grade 3, 4%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Cough grade 3, 4%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Infection grade 3, 4%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Diarrhea grade 3, 6%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Anorexia grade 3, 8%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Rash grade 3, 8%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Conjunctivitis grade 3, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Insomnia grade 3, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Pruritus grade 3, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Stomatitis grade 3, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Anorexia grade 4, 1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Dyspnea grade 4, 11%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Fatigue grade 4, 4%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Abdominal pain grade 4, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Diarrhea grade 4, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Rash grade 4, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Vomiting grade 4, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Diarrhoea 1%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Rash 1%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
n = 485
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 62 years
Sex: M+F
Population Size: 485
Sources:
Dehydration grade 3, 5.3%
2000 mg 1 times / week multiple, oral
Highest studied dose
Dose: 2000 mg, 1 times / week
Route: oral
Route: multiple
Dose: 2000 mg, 1 times / week
Sources:
unhealthy, Median age 63 years
n = 19
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 63 years
Sex: M+F
Population Size: 19
Sources:
Fatigue grade 3, 5.3%
2000 mg 1 times / week multiple, oral
Highest studied dose
Dose: 2000 mg, 1 times / week
Route: oral
Route: multiple
Dose: 2000 mg, 1 times / week
Sources:
unhealthy, Median age 63 years
n = 19
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 63 years
Sex: M+F
Population Size: 19
Sources:
Pneumonitis grade 3, 5.3%
2000 mg 1 times / week multiple, oral
Highest studied dose
Dose: 2000 mg, 1 times / week
Route: oral
Route: multiple
Dose: 2000 mg, 1 times / week
Sources:
unhealthy, Median age 63 years
n = 19
Health Status: unhealthy
Condition: nonsmall cell lung cance
Age Group: Median age 63 years
Sex: M+F
Population Size: 19
Sources:
Rash grade 3, 100%
Disc. AE
200 mg 2 times / day multiple, oral
Highest studied dose
healthy, adult
n = 6
Erythematous rash grade 1
1000 mg 1 times / day single, oral
Highest studied dose
healthy
n = 4
Diarrhea
200 mg 2 times / day multiple, oral
Highest studied dose
healthy
n = 5
Transaminases increased
200 mg 2 times / day multiple, oral
Highest studied dose
healthy
n = 5
OverviewDrug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major [Km 5.9 uM]
yes (co-administration study)
Comment: Coadministration of erlotinib with ketoconazole, a potent inhibitor of CYP3A4, resulted in a significant (67%) increase in erlotinib exposure (Study NP16612). The CYP3A4 inducer rifampicin has been demonstrated to impact the exposure to erlotinib; in Study NP16638 co-administration led to a 64% reduction in erlotinib AUC.
Page: -
minor
no
no
no
yes [Km 24 uM]
yes
yes
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Effects of the epidermal growth factor receptor inhibitor OSI-774, Tarceva, on downstream signaling pathways and apoptosis in human pancreatic adenocarcinoma.
2002 Aug
Cancer drugs. Smart weapons prove tough to design.
2002 Oct 18
Erlotinib OSI/Roche/Genentech.
2002 Sep
Small-molecule epidermal growth factor receptor tyrosine kinase inhibitors.
2003
Development of the epidermal growth factor receptor inhibitor Tarceva (OSI-774).
2003
Erlotinib: CP 358774, NSC 718781, OSI 774, R 1415.
2003
Second-line chemotherapy for non-small cell lung cancer.
2003 Aug
Erlotinib: a new therapeutic approach for non-small cell lung cancer.
2003 Aug
Clinical studies with non-iressa EGFR tyrosine kinase inhibitors.
2003 Aug
Specific method for determination of OSI-774 and its metabolite OSI-420 in human plasma by using liquid chromatography-tandem mass spectrometry.
2003 Aug 15
Targeting the epidermal growth factor receptor in non-small cell lung cancer.
2003 Dec 1
For investigational targeted drugs, combination trials pose challenges.
2003 Dec 3
Clinical Trials in Cancer-SMi Conference. 11-12 June 2003, London, UK.
2003 Jul
Pharmacodynamic evaluation of the epidermal growth factor receptor inhibitor OSI-774 in human epidermis of cancer patients.
2003 Jul
Inhibitors of epidermal-growth-factor receptors: a review of clinical research with a focus on non-small-cell lung cancer.
2003 Jul
Research retreat: Pfizer eliminates Sugen, shrinks cancer infrastructure.
2003 Jul 16
Epidermal growth factor receptor inhibitors: an update on their development as cancer therapeutics.
2003 Jun
Challenges and opportunities for Erlotinib (Tarceva): what does the future hold?
2003 Jun
Erlotinib (Tarceva): an update on the clinical trial program.
2003 Jun
Pharmacokinetics and pharmacodynamics: maximizing the clinical potential of Erlotinib (Tarceva).
2003 Jun
[Inhibitors of epidermal growth factor receptor and colorectal cancer].
2003 Nov
Clinical experience with the HER1/EGFR tyrosine kinase inhibitor erlotinib.
2003 Nov
Epidermal growth factor receptor tyrosine kinase inhibitors in late stage clinical trials.
2003 Nov
Molecular neuro-oncology and development of targeted therapeutic strategies for brain tumors. Part 1: Growth factor and Ras signaling pathways.
2003 Oct
Epidermal growth factor receptor inhibitors, gefitinib and erlotinib (Tarceva , OSI-774), in the treatment of bronchioloalveolar carcinoma.
2003 Sep
Distribution and function of EGFR in human tissue and the effect of EGFR tyrosine kinase inhibition.
2003 Sep-Oct
Potential role for epidermal growth factor receptor inhibitors in combined-modality therapy for non-small-cell lung cancer.
2004
Emerging roles of targeted small molecule protein-tyrosine kinase inhibitors in cancer therapy.
2004
Epidermal growth factor receptor inhibitors for the treatment of colorectal cancer: a promise fulfilled?
2004 Apr
Epidermal growth factor receptor tyrosine kinase inhibitors: evolving role in the treatment of solid tumors.
2004 Apr
Identification of epidermal growth factor receptor-derived peptides immunogenic for HLA-A2(+) cancer patients.
2004 Apr 19
Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors.
2004 Feb 9
Gateways to clinical trials.
2004 Jan-Feb
Emerging treatments in oncology: focus on tyrosine kinase (erbB) receptor inhibitors.
2004 Jan-Feb
Benzamides and benzamidines as specific inhibitors of epidermal growth factor receptor and v-Src protein tyrosine kinases.
2004 Jul 1
EGFR inhibitors square off at ASCO.
2004 Jun
Epidermal growth factor receptor tyrosine kinase inhibitors.
2004 Jun 14
The role of erlotinib (Tarceva, OSI 774) in the treatment of non-small cell lung cancer.
2004 Jun 15
The role of EGFR inhibitors in nonsmall cell lung cancer.
2004 Mar
[Bronchioloalveolar carcinoma (BAC)].
2004 Mar
The HER receptor family: a rich target for therapeutic development.
2004 Mar 1
Current data and ongoing trials in patients with recurrent non-small-cell lung cancer.
2004 May
New cytotoxic and molecular-targeted therapies of head and neck tumors.
2004 May
Combination treatment of glioblastoma multiforme cell lines with the anti-malarial artesunate and the epidermal growth factor receptor tyrosine kinase inhibitor OSI-774.
2004 May 1
Patents

Sample Use Guides

The dose for NSCLC is 150 mg/day. The dose for pancreatic cancer is 100 mg/day. All doses of TARCEVA should be taken on an empty stomach at least one hour before or two hours after food
Route of Administration: Oral
Erlotinib (20 µM) inhibited 33.8% of the growth of T. gondii
Name Type Language
ERLOTINIB
EMA EPAR   INN   MI   VANDF   WHO-DD  
INN  
Official Name English
N-(3-ETHYNYLPHENYL)-6,7-BIS(2-METHOXYETHOXY)QUINAZOLIN-4-AMINE
Systematic Name English
CP-358774
Code English
RG-1415
Code English
ERLOTINIB [EMA EPAR]
Common Name English
R-1415
Code English
CP-35877401
Code English
ERLOTINIB [MI]
Common Name English
ERLOTINIB [INN]
Common Name English
ERLOTINIB [VANDF]
Common Name English
4-QUINAZOLINAMINE, N-(3-ETHYNYLPHENYL)-6,7-BIS(2-METHOXYETHOXY)-
Systematic Name English
CP-358,774
Code English
ERLOTINIB [WHO-DD]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C2167
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
WHO-VATC QL01XE03
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
WHO-ATC L01XE03
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
LIVERTOX 365
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
NDF-RT N0000175076
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
EMA ASSESSMENT REPORTS TARCEVA (AUTHORIZED: PANCREATIC NEOPLASMS)
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
EMA ASSESSMENT REPORTS TARCEVA (AUTHORISED: CARCINOMA, NON-SMALL-CELL LUNG)
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
Code System Code Type Description
DRUG BANK
DB00530
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
CAS
183321-74-6
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
ChEMBL
CHEMBL553
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
IUPHAR
4920
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
NCI_THESAURUS
C65530
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
INN
8133
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
DRUG CENTRAL
1045
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
MERCK INDEX
M5000
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY Merck Index
EPA CompTox
183321-74-6
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
HSDB
8082
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
MESH
C400278
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
LACTMED
Erlotinib
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
WIKIPEDIA
ERLOTINIB
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
FDA UNII
J4T82NDH7E
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
RXCUI
337525
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY RxNorm
EVMPD
SUB16423MIG
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY
PUBCHEM
176870
Created by admin on Sat Jun 26 16:41:09 UTC 2021 , Edited by admin on Sat Jun 26 16:41:09 UTC 2021
PRIMARY