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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

Molecular Formula C22H23N3O4
Molecular Weight 393.4366
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: 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

1100649600000
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

1100649600000
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
Health Status: unhealthy
Age Group: Median age 54 years
Sex: M+F
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
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
Health Status: unhealthy
Age Group: Median age 57 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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:
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
Sources:
Other AEs: Neutropenia...
Other AEs:
Neutropenia (grade 3, 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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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
Disc. AE: Diarrhoea, Rash...
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
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:
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
Health Status: unhealthy
Age Group: Median age 63 years
Sex: M+F
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
Disc. AE: Rash...
1000 mg 1 times / day single, oral
Highest studied dose
healthy
Other AEs: Erythematous rash...
200 mg 2 times / day multiple, oral
Highest studied dose
healthy
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
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
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
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
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
Health Status: unhealthy
Age Group: Median age 57 years
Sex: M+F
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
Health Status: unhealthy
Age Group: Median age 57 years
Sex: M+F
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
Health Status: unhealthy
Age Group: Median age 57 years
Sex: M+F
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
Health Status: unhealthy
Age Group: Median age 57 years
Sex: M+F
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
Health Status: unhealthy
Age Group: Median age 57 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
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
Sources:
unhealthy, Median age 62 years
Health Status: unhealthy
Age Group: Median age 62 years
Sex: M+F
Sources:
Diarrhoea 1%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Rash 1%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Rash 10%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Diarrhea 2%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Diarrhea 4%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Rash 7%
Disc. AE
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Constipation grade 3, 1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Headache grade 3, 1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Hemoptysis grade 3, 1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Fatigue grade 3, 14%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Dyspnea grade 3, 17%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Abdominal pain grade 3, 2%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Vomiting grade 3, 2%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Bone pain grade 3, 3%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Nausea grade 3, 3%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Neuropathy grade 3, 3%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Chest pain grade 3, 4%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Cough grade 3, 4%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Infection grade 3, 4%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Diarrhea grade 3, 6%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Anorexia grade 3, 8%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Rash grade 3, 8%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Conjunctivitis grade 3, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Insomnia grade 3, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Pruritus grade 3, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Stomatitis grade 3, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Anorexia grade 4, 1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Dyspnea grade 4, 11%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Fatigue grade 4, 4%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Abdominal pain grade 4, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Diarrhea grade 4, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Rash grade 4, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
Vomiting grade 4, <1%
150 mg 1 times / day multiple, oral
Recommended
unhealthy, Median age 62 years
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
Health Status: unhealthy
Age Group: Median age 63 years
Sex: M+F
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
Health Status: unhealthy
Age Group: Median age 63 years
Sex: M+F
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
Health Status: unhealthy
Age Group: Median age 63 years
Sex: M+F
Sources:
Rash grade 3, 100%
Disc. AE
200 mg 2 times / day multiple, oral
Highest studied dose
healthy, adult
Erythematous rash grade 1
1000 mg 1 times / day single, oral
Highest studied dose
healthy
Diarrhea
200 mg 2 times / day multiple, oral
Highest studied dose
healthy
Transaminases increased
200 mg 2 times / day multiple, oral
Highest studied dose
healthy
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
Small-molecule epidermal growth factor receptor tyrosine kinase inhibitors.
2003
Development of the epidermal growth factor receptor inhibitor Tarceva (OSI-774).
2003
3D-QSAR and docking studies on 4-anilinoquinazoline and 4-anilinoquinoline epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.
2003 Aug
Second-line chemotherapy for non-small cell lung cancer.
2003 Aug
Erlotinib: a new therapeutic approach for non-small cell lung cancer.
2003 Aug
The biological and biochemical effects of CP-654577, a selective erbB2 kinase inhibitor, on human breast cancer cells.
2003 Aug 1
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
[Non-small cell lung cancer: 1) Molecular-target therapy].
2003 Jul 10
Epidermal growth factor receptor inhibitors: an update on their development as cancer therapeutics.
2003 Jun
[Therapeutic implications of epidermal growth factor receptor in lung cancer].
2003 Nov
[Inhibitors of epidermal growth factor receptor and colorectal cancer].
2003 Nov
[Targeting of epidermal growth factor receptor and applications in ORL cancer].
2003 Nov
Identifying predictive and surrogate markers of erlotinib antitumor activity other than rash.
2003 Nov
Can rash associated with HER1/EGFR inhibition be used as a marker of treatment outcome?
2003 Nov
Clinical experience with the HER1/EGFR tyrosine kinase inhibitor erlotinib.
2003 Nov
Erlotinib: preclinical investigations.
2003 Nov
Targeting the HER1/EGFR receptor to improve outcomes in non-small-cell lung cancer.
2003 Nov
Defining the role of the epidermal growth factor receptor in pancreatic cancer grown in vitro.
2003 Nov
Pharmacology of oral chemotherapy agents.
2003 Nov-Dec
Molecular neuro-oncology and development of targeted therapeutic strategies for brain tumors. Part 1: Growth factor and Ras signaling pathways.
2003 Oct
New targeted therapies in gastrointestinal cancers.
2003 Oct
Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.
2003 Oct 23
Liquid-chromatographic determination of erlotinib (OSI-774), an epidermal growth factor receptor tyrosine kinase inhibitor.
2003 Oct 25
Epidermal growth factor receptor inhibitors, gefitinib and erlotinib (Tarceva , OSI-774), in the treatment of bronchioloalveolar carcinoma.
2003 Sep
Gateways to clinical trials.
2003 Sep
Distribution and function of EGFR in human tissue and the effect of EGFR tyrosine kinase inhibition.
2003 Sep-Oct
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
Emerging roles of targeted small molecule protein-tyrosine kinase inhibitors in cancer therapy.
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
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
Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors.
2004 Feb 9
Lung cancer: looking ahead in 2004.
2004 Jan
Multicenter phase II study of erlotinib, an oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with recurrent or metastatic squamous cell cancer of the head and neck.
2004 Jan 1
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.
2004 Jan 5
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
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
The role of EGFR inhibitors in nonsmall cell lung cancer.
2004 Mar
The HER receptor family: a rich target for therapeutic development.
2004 Mar 1
Patents

Sample Use Guides

The dose for NSCLC is 150 mg/day.
Route of Administration: Oral
Erlotinib (20 µM) inhibited 33.8% of the growth of T. gondii
Substance Class Chemical
Created
by admin
on Sat Jun 26 16:41:09 UTC 2021
Edited
by admin
on Sat Jun 26 16:41:09 UTC 2021
Record UNII
J4T82NDH7E
Record Status Validated (UNII)
Record Version
  • Download
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
Related Record Type Details
TRANSPORTER -> SUBSTRATE
TRANSPORTER -> INHIBITOR
TRANSPORTER -> SUBSTRATE
TRANSPORTER -> SUBSTRATE
TRANSPORTER -> INHIBITOR
SALT/SOLVATE -> PARENT
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
TRANSPORTER -> INHIBITOR
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MAJOR
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METABOLITE -> PARENT
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METABOLITE -> PARENT
METABOLITE -> PARENT
MAJOR
FECAL; URINE
METABOLITE -> PARENT
METABOLITE -> PARENT
MAJOR
URINE
METABOLITE -> PARENT
MINOR
FECAL; URINE
METABOLITE -> PARENT
MAJOR
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METABOLITE -> PARENT
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Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
CSF/PLASMA RATIO BIOLOGICAL SPECIES
BIOLOGICAL