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

Details

Stereochemistry ACHIRAL
Molecular Formula C22H23N3O4.ClH
Molecular Weight 429.897
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ERLOTINIB HYDROCHLORIDE

SMILES

Cl.COCCOC1=CC2=C(C=C1OCCOC)C(NC3=CC(=CC=C3)C#C)=NC=N2

InChI

InChIKey=GTTBEUCJPZQMDZ-UHFFFAOYSA-N
InChI=1S/C22H23N3O4.ClH/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);1H

HIDE SMILES / InChI

Molecular Formula C22H23N3O4
Molecular Weight 393.4357
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including 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
OSI-774 OSI Pharmaceuticals.
2001 Feb
HER-targeted tyrosine-kinase inhibitors.
2002
Gateways to clinical trials.
2002 Dec
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
The future of cytotoxic therapy: selective cytotoxicity based on biology is the key.
2003
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
Epidermal growth factor receptor tyrosine kinase inhibitors: application in non-small cell lung cancer.
2003 Dec
Tolerability of gefitinib in patients receiving treatment in everyday clinical practice.
2003 Dec
Targeting the epidermal growth factor receptor in non-small cell lung cancer.
2003 Dec 1
Epidermal growth factor receptor as a therapeutic target in colorectal cancer.
2003 Feb
Inhibitors of epidermal-growth-factor receptors: a review of clinical research with a focus on non-small-cell lung cancer.
2003 Jul
Challenges and opportunities for Erlotinib (Tarceva): what does the future hold?
2003 Jun
Erlotinib (Tarceva): an update on the clinical trial program.
2003 Jun
[Inhibitors of epidermal growth factor receptor and colorectal cancer].
2003 Nov
[Targeting of epidermal growth factor receptor and applications in ORL cancer].
2003 Nov
Can rash associated with HER1/EGFR inhibition be used as a marker of treatment outcome?
2003 Nov
Epidermal growth factor receptor tyrosine kinase inhibitors in late stage clinical trials.
2003 Nov
Pharmacology of oral chemotherapy agents.
2003 Nov-Dec
Gateways to clinical trials.
2003 Oct
Gateways to clinical trials.
2003 Sep
Review of epidermal growth factor receptor biology.
2004
Potential role for epidermal growth factor receptor inhibitors in combined-modality therapy for non-small-cell lung cancer.
2004
HER1/EGFR targeting: refining the strategy.
2004
Gateways to clinical trials.
2004 Apr
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
Rationale and clinical validation of epidermal growth factor receptor as a target in the treatment of head and neck cancer.
2004 Apr
Identification of epidermal growth factor receptor-derived peptides immunogenic for HLA-A2(+) cancer patients.
2004 Apr 19
Novel treatments in non-small cell lung cancer.
2004 Feb
Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors.
2004 Feb 9
Lung cancer: looking ahead in 2004.
2004 Jan
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
Targeting non-small cell lung cancer with epidermal growth factor tyrosine kinase inhibitors: where do we stand, where do we go.
2004 Jun
EGFR inhibitors square off at ASCO.
2004 Jun
Antitumor activity of erlotinib (OSI-774, Tarceva) alone or in combination in human non-small cell lung cancer tumor xenograft models.
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
[Bronchioloalveolar carcinoma (BAC)].
2004 Mar
Inverse correlation of epidermal growth factor receptor messenger RNA induction and suppression of anchorage-independent growth by OSI-774, an epidermal growth factor receptor tyrosine kinase inhibitor, in glioblastoma multiforme cell lines.
2004 Mar
Emerging role of epidermal growth factor receptor inhibition in therapy for advanced malignancy: focus on NSCLC.
2004 Mar 1
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
[Lung cancer: molecular targeting therapy].
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
Substance Class Chemical
Created
by admin
on Wed Jul 05 23:01:18 UTC 2023
Edited
by admin
on Wed Jul 05 23:01:18 UTC 2023
Record UNII
DA87705X9K
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ERLOTINIB HYDROCHLORIDE
JAN   MART.   MI   ORANGE BOOK   USAN   WHO-DD  
USAN  
Official Name English
4-(M-ETHYNYLANILINO)-6,7-BIS(2-METHOXYETHOXY)QUINAZOLINE MONOHYDROCHLORIDE
Systematic Name English
Erlotinib hydrochloride [WHO-DD]
Common Name English
ERLOTINIB HYDROCHLORIDE [MART.]
Common Name English
ERLOTINIB HYDROCHLORIDE [USP-RS]
Common Name English
OSI-774
Code English
N-(3-ETHENYLPHENYL)-6,7-BIS(2-METHOXYETHOXY)-4-QUINAZOLINAMINE HYDROCHLORIDE
Systematic Name English
TARCEVA
Brand Name English
ERLOTINIB HYDROCHLORIDE [MI]
Common Name English
ERLOTINIB HYDROCHLORIDE [ORANGE BOOK]
Common Name English
ERLOTINIB HYDROCHLORIDE [USAN]
Common Name English
ERLOTINIB HYDROCHLORIDE [JAN]
Common Name English
ERLOTINIB HCL
Common Name English
CP-358774-01
Code English
CP-358,774-01
Code English
4-QUINAZOLINAMINE, N-(3-ETHYNYLPHENYL)-6,7-BIS(2-METHOXYETHOXY)-, MONOHYDROCHLORIDE
Common Name English
CP-358
Code English
Classification Tree Code System Code
NCI_THESAURUS C2167
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
EMA ASSESSMENT REPORTS TARCEVA (AUTHORIZED: PANCREATIC NEOPLASMS)
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
NCI_THESAURUS C129825
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
FDA ORPHAN DRUG 172003
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
Code System Code Type Description
CHEBI
53509
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
ChEMBL
CHEMBL553
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
RXCUI
477320
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY RxNorm
MERCK INDEX
M5000
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY Merck Index
DRUG BANK
DBSALT000064
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
EVMPD
SUB21050
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
EPA CompTox
DTXSID10171412
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
DAILYMED
DA87705X9K
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
SMS_ID
100000092747
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
USAN
MM-14
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
CAS
183319-69-9
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
NCI_THESAURUS
C2693
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
PUBCHEM
176871
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
FDA UNII
DA87705X9K
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
RS_ITEM_NUM
1241608
Created by admin on Wed Jul 05 23:01:18 UTC 2023 , Edited by admin on Wed Jul 05 23:01:18 UTC 2023
PRIMARY
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