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Details

Stereochemistry ACHIRAL
Molecular Formula C22H24ClFN4O3
Molecular Weight 446.9031
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GEFITINIB

SMILES

COc1cc2c(cc1OCCCN3CCOCC3)c(ncn2)Nc4ccc(c(c4)Cl)F

InChI

InChIKey=XGALLCVXEZPNRQ-UHFFFAOYSA-N
InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27)

HIDE SMILES / InChI

Molecular Formula C22H24ClFN4O3
Molecular Weight 446.9031
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: https://www.drugs.com/cdi/gefitinib.html

Gefitinib is an anilinoquinazoline with antineoplastic activity. Gefitinib inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme. Thus the function of the EGFR tyrosine kinase in activating the Ras signal transduction cascade is inhibited; and malignant cells are inhibited. Gefitinib is the first selective inhibitor of the EGFR tyrosine kinase which is also referred to as Her1 or ErbB-1. EGFR is overexpressed in the cells of certain types of human carcinomas - for example in lung and breast cancers. Overexpression leads to inappropriate activation of the apoptotic Ras signal transduction cascade, eventually leading to uncontrolled cell proliferation. Gefitinib is used for the continued treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of either platinum-based or docetaxel chemotherapies.

CNS Activity

Curator's Comment:: low penetration in humans

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1 nM [IC50]
19.2699999999999996 µM [IC50]
1.22999999999999998 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Iressa

Approved Use

IRESSA is indicated as monotherapy for the continued treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of both platinum-based and docetaxel chemotherapies who are benefiting or have benefited from IRESSA.

Launch Date

1052006400000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
57.45 ng/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GEFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
724 ng/mL
250 mg 1 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GEFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
57.5 ng/mL
250 mg 1 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GEFITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
579 ng/mL
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
178 ng/mL
100 mg 1 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2160 ng/mL
700 mg 1 times / day multiple, oral
dose: 700 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
213 ng/mL
500 mg single, oral
dose: 500 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2210 ng/mL
400 mg/m² 1 times / day multiple, oral
dose: 400 mg/m²
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1415 ng × h/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GEFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
13103 ng × h/mL
250 mg 1 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GEFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1415 ng × h/mL
250 mg 1 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GEFITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
10026 ng × h/mL
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2985 ng × h/mL
100 mg 1 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
42314 ng × h/mL
700 mg 1 times / day multiple, oral
dose: 700 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
6181 ng × h/mL
500 mg single, oral
dose: 500 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
29.3 μg × h/mL
400 mg/m² 1 times / day multiple, oral
dose: 400 mg/m²
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
23.83 h
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GEFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
25 h
250 mg 1 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GEFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
21.2 h
250 mg 1 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GEFITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
38.1 h
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
55.2 h
100 mg 1 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
72.9 h
700 mg 1 times / day multiple, oral
dose: 700 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
28.2 h
500 mg single, oral
dose: 500 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
GEFITINIB unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
11.9 h
400 mg/m² 1 times / day multiple, oral
dose: 400 mg/m²
route of administration: Oral
experiment type: MULTIPLE
co-administered:
GEFITINIB plasma
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
9%
250 mg 1 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
GEFITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
10%
GEFITINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1000 mg 1 times / day steady, oral
Dose: 1000 mg, 1 times / day
Route: oral
Route: steady
Dose: 1000 mg, 1 times / day
Sources:
unhealthy, 51 years (range: 46 – 72 years)
Health Status: unhealthy
Age Group: 51 years (range: 46 – 72 years)
Sex: M+F
Sources:
DLT: Toxic epidermal necrolysis...
Dose limiting toxicities:
Toxic epidermal necrolysis (grade 4, 1 patient)
Sources:
1250 mg 1 times / day steady, oral
Dose: 1250 mg, 1 times / day
Route: oral
Route: steady
Dose: 1250 mg, 1 times / day
Sources:
unhealthy, 51 years (range: 46 – 72 years)
Health Status: unhealthy
Age Group: 51 years (range: 46 – 72 years)
Sex: M+F
Sources:
250 mg 1 times / day steady, oral
Recommended
Dose: 250 mg, 1 times / day
Route: oral
Route: steady
Dose: 250 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Asthenia...
AEs leading to
discontinuation/dose reduction:
Asthenia (grade 4, 1 patient)
Sources:
500 mg 1 times / day steady, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Acne, Rash...
AEs leading to
discontinuation/dose reduction:
Acne (grade 3, 2 patients)
Rash (grade 2-3, 2 patients)
Diarrhea (1 patient)
Abdominal pain (1 patient)
Headache (1 patient)
Epistaxis (1 patient)
Pruritus (1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Toxic epidermal necrolysis grade 4, 1 patient
DLT
1000 mg 1 times / day steady, oral
Dose: 1000 mg, 1 times / day
Route: oral
Route: steady
Dose: 1000 mg, 1 times / day
Sources:
unhealthy, 51 years (range: 46 – 72 years)
Health Status: unhealthy
Age Group: 51 years (range: 46 – 72 years)
Sex: M+F
Sources:
Asthenia grade 4, 1 patient
Disc. AE
250 mg 1 times / day steady, oral
Recommended
Dose: 250 mg, 1 times / day
Route: oral
Route: steady
Dose: 250 mg, 1 times / day
Sources:
unhealthy
Abdominal pain 1 patient
Disc. AE
500 mg 1 times / day steady, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy
Diarrhea 1 patient
Disc. AE
500 mg 1 times / day steady, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy
Epistaxis 1 patient
Disc. AE
500 mg 1 times / day steady, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy
Headache 1 patient
Disc. AE
500 mg 1 times / day steady, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy
Pruritus 1 patient
Disc. AE
500 mg 1 times / day steady, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy
Rash grade 2-3, 2 patients
Disc. AE
500 mg 1 times / day steady, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy
Acne grade 3, 2 patients
Disc. AE
500 mg 1 times / day steady, oral
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy
Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer






Drug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: itraconazole increased auc of gefitinib by 80%
major
yes (pharmacogenomic study)
Comment: CYP2D6 PMs have approximately 2-fold higher exposure to gefitinib than CYP2D6 EM
Page: 21
minor
no (pharmacogenomic study)
Comment: CYP3A5 genotype did not appear to impact gefitinib PK
Page: 21
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
New drugs in gynecologic cancer.
2001 Apr
Prospects for combining hormonal and nonhormonal growth factor inhibition.
2001 Dec
Inhibitors of HER2/neu (erbB-2) signal transduction.
2001 Dec
High levels of HER-2 expression alter the ability of epidermal growth factor receptor (EGFR) family tyrosine kinase inhibitors to inhibit EGFR phosphorylation in vivo.
2001 Dec
ZD1839 (Iressa), a novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, potently inhibits the growth of EGFR-positive cancer cell lines with or without erbB2 overexpression.
2001 Dec 15
OSI Pharmaceuticals, Genentech and Roche announce data from clinical studies of Tarceva.
2001 Jun
New drug targets for genomic cancer therapy: successes, limitations, opportunities and future challenges.
2001 May
[3rd National Congress of Medical Oncology. Issues in Gynecologic Oncology. Naples, November 7, 2000].
2001 Nov-Dec
Targeted Therapies in the Treatment of Breast Cancer. Proceedings of a meeting. Kailua-Kona, Hawaii, July 19-23, 2000.
2001 Oct
HER-targeted tyrosine-kinase inhibitors.
2002
Gefitinib.
2002
ZD1839 (Iressa): what's in it for the patient?
2002
Why the epidermal growth factor receptor? The rationale for cancer therapy.
2002
93rd Annual Meeting of the American Association for Cancer Research, San Francisco, CA, USA, 6-10 April 2002.
2002
Finding the needle in the haystack: why high-throughput screening is good for your health.
2002
ZD1839 (IRESSA): a selective EGFR-TK inhibitor.
2002 Apr
ZD1839 ('Iressa'), a specific oral epidermal growth factor receptor-tyrosine kinase inhibitor, potentiates radiotherapy in a human colorectal cancer xenograft model.
2002 Apr 8
A serum factor after intestinal resection stimulates epidermal growth factor receptor signaling and proliferation in intestinal epithelial cells.
2002 Aug
Epidermal growth factor receptor tyrosine kinase inhibitors.
2002 Aug
Inhibition of apoptosis by amphiregulin via an insulin-like growth factor-1 receptor-dependent pathway in non-small cell lung cancer cell lines.
2002 Dec 20
[Molecular target-based cancer therapy: epidermal growth factor receptor inhibitors].
2002 Feb
Combined anti-EGF receptor and anti-HER2 receptor therapy in breast cancer: a promising strategy ready for clinical testing.
2002 Jan
Selective inhibition of the epidermal growth factor receptor by ZD1839 decreases the growth and invasion of ovarian clear cell adenocarcinoma cells.
2002 Jul
Targeting epidermal growth factor receptor in lung cancer.
2002 Jul
Second/third/fourth line therapy with tyrosine kinase inhibitors in NSCLC.
2002 Jul-Aug
Tyrosine kinase signal transduction inhibitors. Clinical trials.
2002 Jul-Aug
The rational basis of using novel targeted biological agents in non-small cell lung cancer.
2002 Jul-Aug
Gateways to Clinical Trials. June 2002.
2002 Jun
HER (erbB) tyrosine kinase inhibitors in the treatment of breast cancer.
2002 Jun
Molecular mechanisms in signal transduction: new targets for the therapy of gynecologic malignancies.
2002 Jun
Local recurrence in head and neck cancer: relationship to radiation resistance and signal transduction.
2002 Mar
Antitumor activity of the selective epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) Iressa (ZD1839) in an EGFR-expressing multidrug-resistant cell line in vitro and in vivo.
2002 Mar 10
[Progress in diagnosis and treatment of lung cancer].
2002 Mar 20
ZD1839 (IRESSA), an EGFR-selective tyrosine kinase inhibitor, enhances taxane activity in bcl-2 overexpressing, multidrug-resistant MCF-7 ADR human breast cancer cells.
2002 Mar 20
[Future trends in anticancer chemotherapy].
2002 May
[Latest therapeutic strategy for stage IV non-small cell lung cancer].
2002 May
[New treatment strategy for stage III non-small-cell lung cancer].
2002 May
[ZD1839].
2002 May
ZD1839, a selective oral epidermal growth factor receptor-tyrosine kinase inhibitor, is well tolerated and active in patients with solid, malignant tumors: results of a phase I trial.
2002 May 1
Targeting the epidermal growth factor receptor with tyrosine kinase inhibitors: small molecules, big hopes.
2002 May 1
ZD1839 (Iressa) induces antiangiogenic effects through inhibition of epidermal growth factor receptor tyrosine kinase.
2002 May 1
Phase I safety, pharmacokinetic, and pharmacodynamic trial of ZD1839, a selective oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with five selected solid tumor types.
2002 Nov 1
The multifunctional, multi-institutional, and sometimes even global phase I study: a better life for phase I evaluations or just "living large"?
2002 Nov 1
Despite concerns, FDA panel backs EGFR inhibitor.
2002 Nov 6
Enhancement of antitumor activity of ionizing radiation by combined treatment with the selective epidermal growth factor receptor-tyrosine kinase inhibitor ZD1839 (Iressa).
2002 Oct
Surprise phase III failure for ZD1839.
2002 Oct
ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy.
2002 Oct 15
Cancer drugs. Smart weapons prove tough to design.
2002 Oct 18
Follicular and epidermal alterations in patients treated with ZD1839 (Iressa), an inhibitor of the epidermal growth factor receptor.
2002 Sep
Gefitinib (Iressa) for advanced non-small cell lung cancer.
2002 Sep 2
Patents

Sample Use Guides

250 mg orally once a day
Route of Administration: Oral
Gefitinib could inhibit highly expressed EGFR cell growth in a dose-dependent manner in the range of dose from 0.10 to 102.4 uM
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:08:51 UTC 2021
Edited
by admin
on Fri Jun 25 21:08:51 UTC 2021
Record UNII
S65743JHBS
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GEFITINIB
EMA EPAR   INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
GEFITINIB [INN]
Common Name English
GEFITINIB [USAN]
Common Name English
NSC-759856
Code English
4-QUINAZOLINAMINE, N-(3-CHLORO-4-FLUOROPHENYL)-7-METHOXY-6-(3-4-MORPHOLIN)PROPOXY)-
Common Name English
GEFITINIB [EMA EPAR]
Common Name English
ZD-1839
Code English
GEFITINIB [VANDF]
Common Name English
IRESSA
Brand Name English
GEFITINIB [JAN]
Common Name English
GEFITINIB [EP MONOGRAPH]
Common Name English
GEFITINIB [ORANGE BOOK]
Common Name English
GEFITINIB [MART.]
Common Name English
GEFITINIB [WHO-DD]
Common Name English
GEFITINIB [MI]
Common Name English
ZD1839
Code English
Classification Tree Code System Code
EU-Orphan Drug EU/3/18/2075
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
WHO-ATC L01XE02
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
NCI_THESAURUS C129825
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
WHO-VATC QL01XE02
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
EMA ASSESSMENT REPORTS IRESSA (AUTHORIZED: CARCINOMA, NON-SMALL-CELL LUNG)
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
NDF-RT N0000175605
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
NDF-RT N0000175076
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
NCI_THESAURUS C1967
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
FDA ORPHAN DRUG 443014
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
LIVERTOX 450
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
Code System Code Type Description
WIKIPEDIA
GEFITINIB
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
ChEMBL
CHEMBL939
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
EVMPD
SUB20637
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
DRUG BANK
DB00317
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
EPA CompTox
184475-35-2
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
FDA UNII
S65743JHBS
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
NCI_THESAURUS
C1855
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
MERCK INDEX
M5682
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY Merck Index
MESH
C419708
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
INN
8204
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
RXCUI
328134
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY RxNorm
IUPHAR
4941
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
CAS
184475-35-2
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
PUBCHEM
123631
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
DRUG CENTRAL
1282
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
LACTMED
Gefitinib
Created by admin on Fri Jun 25 21:08:51 UTC 2021 , Edited by admin on Fri Jun 25 21:08:51 UTC 2021
PRIMARY
Related Record Type Details
TRANSPORTER -> SUBSTRATE
OFF-TARGET->NON-INHIBITOR
Overall survival (OS) was significantly shorter among patients with uncommon EGFR mutations (G719X or L861Q) com-pared with OS of those with common EGFR mutations (12 versus 28.4 months; p = 0.002). In the gefitinib group (n = 114), patients with uncommon EGFR mutations had a significantly shorter OS (11.9 versus 29.3 months; p < 0.001). By contrast, OS was similar between patients with uncommon mutations and those with common mutations in the carboplatin-paclitaxel group (n = 111; 22.8 versus 28 months; p = 0.358)
TRANSPORTER -> INHIBITOR
TRANSPORTER -> SUBSTRATE
BINDER->LIGAND
In vitro binding of gefitinib to human plasma proteins (serum albumin and ?1-acid glycoprotein) is 90% and is independent of drug concentrations.
BINDING
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
TRANSPORTER -> SUBSTRATE
TRANSPORTER -> INHIBITOR
TRANSPORTER -> INDUCER
Related Record Type Details
METABOLITE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC AT STEADY-STATE

INTRAVENOUS ADMINISTRATION

ORAL BIOAVAILABILITY PHARMACOKINETIC