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

Details

Stereochemistry ACHIRAL
Molecular Formula C22H24ClFN4O3
Molecular Weight 446.902
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GEFITINIB

SMILES

COC1=C(OCCCN2CCOCC2)C=C3C(NC4=CC(Cl)=C(F)C=C4)=NC=NC3=C1

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 446.902
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 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
1.0 nM [IC50]
19.27 µM [IC50]
1.23 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

2003
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)
n = 4
Health Status: unhealthy
Condition: NSCLC
Age Group: 51 years (range: 46 – 72 years)
Sex: M+F
Population Size: 4
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)
n = 3
Health Status: unhealthy
Condition: NSCLC
Age Group: 51 years (range: 46 – 72 years)
Sex: M+F
Population Size: 3
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
n = 102
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
n = 114
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)
n = 4
Health Status: unhealthy
Condition: NSCLC
Age Group: 51 years (range: 46 – 72 years)
Sex: M+F
Population Size: 4
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
n = 102
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
n = 114
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
n = 114
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
n = 114
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
n = 114
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
n = 114
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
n = 114
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
n = 114
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: 21.0
minor
no (pharmacogenomic study)
Comment: CYP3A5 genotype did not appear to impact gefitinib PK
Page: 21.0
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Pharmacokinetics and tolerability of the orally active selective epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 in healthy volunteers.
2001
Growth factors and their receptors: new targets for prostate cancer therapy.
2001 Aug
Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo.
2001 Dec 15
Enhanced epidermal growth factor receptor signaling in MCF7 breast cancer cells after long-term culture in the presence of the pure antiestrogen ICI 182,780 (Faslodex).
2001 Jul
Blockade of growth factor receptors in ductal carcinoma in situ inhibits epithelial proliferation.
2001 Mar
New drug targets for genomic cancer therapy: successes, limitations, opportunities and future challenges.
2001 May
[Tyrosine kinase inhibitors--solid cancers].
2001 May
[Tumor angiogenesis and tumor angiogenesis inhibitors].
2001 May
[3rd National Congress of Medical Oncology. Issues in Gynecologic Oncology. Naples, November 7, 2000].
2001 Nov-Dec
Epidermal growth factor receptor tyrosine kinase inhibitors.
2002 Aug
Modulation of radiation response and tumor-induced angiogenesis after epidermal growth factor receptor inhibition by ZD1839 (Iressa).
2002 Aug 1
Activation of BAD by therapeutic inhibition of epidermal growth factor receptor and transactivation by insulin-like growth factor receptor.
2002 Aug 2
Combined anti-EGF receptor and anti-HER2 receptor therapy in breast cancer: a promising strategy ready for clinical testing.
2002 Jan
Cooperative inhibitory effect of ZD1839 (Iressa) in combination with trastuzumab (Herceptin) on human breast cancer cell growth.
2002 Jan
ZD1839 (Iressa): preclinical studies and pharmacology.
2002 Jan-Feb
Second/third/fourth line therapy with tyrosine kinase inhibitors in NSCLC.
2002 Jul-Aug
HER (erbB) tyrosine kinase inhibitors in the treatment of breast cancer.
2002 Jun
[Progress in diagnosis and treatment of lung cancer].
2002 Mar 20
Bradykinin antagonist dimer, CU201, inhibits the growth of human lung cancer cell lines in vitro and in vivo and produces synergistic growth inhibition in combination with other antitumor agents.
2002 May
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
Molecular characterization as a target for cancer therapy in relation to orphan status disorders (Review).
2002 Nov-Dec
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.
2002 Oct 21
Follicular and epidermal alterations in patients treated with ZD1839 (Iressa), an inhibitor of the epidermal growth factor receptor.
2002 Sep
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 Dec 15 15:42:15 GMT 2023
Edited
by admin
on Fri Dec 15 15:42:15 GMT 2023
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 [WHO-DD]
Common 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 [MI]
Common Name English
ZD1839
Code English
Classification Tree Code System Code
EU-Orphan Drug EU/3/18/2075
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
WHO-ATC L01XE02
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
NCI_THESAURUS C129825
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
WHO-VATC QL01XE02
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
EMA ASSESSMENT REPORTS IRESSA (AUTHORIZED: CARCINOMA, NON-SMALL-CELL LUNG)
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
NDF-RT N0000175605
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
NDF-RT N0000175076
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
NCI_THESAURUS C1967
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
FDA ORPHAN DRUG 443014
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
LIVERTOX NBK548839
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
Code System Code Type Description
SMS_ID
100000091738
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
WIKIPEDIA
GEFITINIB
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
ChEMBL
CHEMBL939
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
DAILYMED
S65743JHBS
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
EVMPD
SUB20637
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
DRUG BANK
DB00317
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
EPA CompTox
DTXSID8041034
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
FDA UNII
S65743JHBS
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
NCI_THESAURUS
C1855
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
MERCK INDEX
m5682
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY Merck Index
MESH
C419708
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
INN
8204
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
RXCUI
328134
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY RxNorm
IUPHAR
4941
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
CHEBI
49668
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
USAN
NN-73
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
CAS
184475-35-2
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
NSC
759856
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
PUBCHEM
123631
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
DRUG CENTRAL
1282
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
LACTMED
Gefitinib
Created by admin on Fri Dec 15 15:42:15 GMT 2023 , Edited by admin on Fri Dec 15 15:42:15 GMT 2023
PRIMARY
Related Record Type Details
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 -> SUBSTRATE
TRANSPORTER -> SUBSTRATE
BINDER->LIGAND
In vitro binding of gefitinib to human plasma proteins (serum albumin and α1-acid glycoprotein) is 90% and is independent of drug concentrations.
BINDING
TRANSPORTER -> INHIBITOR
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
TRANSPORTER -> INDUCER
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
Ki
TRANSPORTER -> SUBSTRATE
Related Record Type Details
IMPURITY -> 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