Peringatan Keamanan

The acute toxicity of gefitinib up to 500 mg in clinical studies has been low. In non-clinical studies, a single dose of 12,000 mg/m2 (about 80 times the recommended clinical dose on a mg/m2 basis) was lethal to rats. Half this dose caused no mortality in mice. Symptoms of overdose include diarrhea and skin rash.

Gefitinib

DB00317

small molecule approved investigational

Deskripsi

Gefitinib (originally coded ZD1839) is a drug used in the treatment of certain types of cancer. Acting in a similar manner to erlotinib (marketed as Tarceva), gefitinib selectively targets the mutant proteins in malignant cells. It is marketed by AstraZeneca under the trade name Iressa.

Struktur Molekul 2D

Berat 446.902
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 48 hours [IV administration]
Volume Distribusi * 1400 L [IV administration]
Klirens (Clearance) * 595 mL/min [IV administration]

Absorpsi

Absorbed slowly after oral administration with a mean bioavailability of 60%. Peak plasma levels occurs 3-7 hours post-administration. Food does not affect the bioavailability of gefitinib.

Metabolisme

Primarily hepatic via CYP3A4. Three sites of biotransformation have been identified: metabolism of the N-propoxymorpholino-group, demethylation of the methoxy-substituent on the quinazoline, and oxidative defluorination of the halogenated phenyl group.

Rute Eliminasi

Elimination is by metabolism (primarily CYP3A4) and excretion in feces. Excretion is predominantly via the feces (86%), with renal elimination of drug and metabolites accounting for less than 4% of the administered dose.

Farmakogenomik

4 Varian
EGFR (rs121434568)

The presence of this polymorphism in EGFR is associated with a higher response rate to gefitinib.

EGFR (rs28929495)

The presence of this polymorphism in EGFR is associated with a higher response rate to gefitinib.

EGFR (rs121913444)

The presence of this polymorphism in EGFR is associated with a higher response rate to gefitinib.

ABCG2 (rs2231142)

Patients with this genotype have an increased risk of diarrhea with gefitinib.

Interaksi Makanan

2 Data
  • 1. Exercise caution with grapefruit products. Grapefruit is an inhibitor of CYP3A4, the enzyme primarily responsible for metabolizing gefitinib. Coadministration with grapefruit products may decrease gefitinib metabolism and increase plasma concentrations.
  • 2. Take with or without food.

Interaksi Obat

779 Data
Magnesium oxide Magnesium oxide can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium bicarbonate Sodium bicarbonate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonate Calcium carbonate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magaldrate Magaldrate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium hydroxide Magnesium hydroxide can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium trisilicate Magnesium trisilicate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium carbonate Magnesium carbonate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bismuth subnitrate Bismuth subnitrate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium silicate Magnesium silicate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium acetoacetate Aluminium acetoacetate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hydrotalcite Hydrotalcite can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium peroxide Magnesium peroxide can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Almasilate Almasilate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium glycinate Aluminium glycinate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aloglutamol Aloglutamol can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium silicate Calcium silicate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexlansoprazole Dexlansoprazole can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexrabeprazole Dexrabeprazole can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pantoprazole Pantoprazole can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Omeprazole Omeprazole can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lansoprazole Lansoprazole can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rabeprazole Rabeprazole can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Esomeprazole Esomeprazole can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium zirconium cyclosilicate Sodium zirconium cyclosilicate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Vonoprazan Vonoprazan can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Gefitinib.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Gefitinib.
Vinorelbine Gefitinib may increase the neutropenic activities of Vinorelbine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Gefitinib.
Olanzapine Olanzapine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cimetidine Cimetidine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nizatidine Nizatidine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ranitidine Ranitidine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Famotidine Famotidine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methantheline Methantheline can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Promethazine Promethazine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Doxepin Doxepin can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Asenapine Asenapine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Metiamide Metiamide can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Roxatidine acetate Roxatidine acetate can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lafutidine Lafutidine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lavoltidine Lavoltidine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Niperotidine Niperotidine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Epinastine Epinastine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dicoumarol Gefitinib may increase the anticoagulant activities of Dicoumarol.
Phenindione Gefitinib may increase the anticoagulant activities of Phenindione.
Warfarin Gefitinib may increase the anticoagulant activities of Warfarin.
Phenprocoumon Gefitinib may increase the anticoagulant activities of Phenprocoumon.
Acenocoumarol Gefitinib may increase the anticoagulant activities of Acenocoumarol.
4-hydroxycoumarin Gefitinib may increase the anticoagulant activities of 4-hydroxycoumarin.
Coumarin Gefitinib may increase the anticoagulant activities of Coumarin.
(R)-warfarin Gefitinib may increase the anticoagulant activities of (R)-warfarin.
Ethyl biscoumacetate Gefitinib may increase the anticoagulant activities of Ethyl biscoumacetate.
Fluindione Gefitinib may increase the anticoagulant activities of Fluindione.
Clorindione Gefitinib may increase the anticoagulant activities of Clorindione.
Diphenadione Gefitinib may increase the anticoagulant activities of Diphenadione.
Tioclomarol Gefitinib may increase the anticoagulant activities of Tioclomarol.
(S)-Warfarin Gefitinib may increase the anticoagulant activities of (S)-Warfarin.
Mirabegron The serum concentration of Gefitinib can be increased when it is combined with Mirabegron.
Cyclosporine The metabolism of Gefitinib can be decreased when combined with Cyclosporine.
Imipramine The metabolism of Gefitinib can be decreased when combined with Imipramine.
Rucaparib The metabolism of Gefitinib can be decreased when combined with Rucaparib.
Rolapitant The metabolism of Gefitinib can be decreased when combined with Rolapitant.
Venlafaxine Venlafaxine may increase the excretion rate of Gefitinib which could result in a lower serum level and potentially a reduction in efficacy.
Metoprolol The metabolism of Gefitinib can be decreased when combined with Metoprolol.
Clobazam The serum concentration of Gefitinib can be increased when it is combined with Clobazam.
Clozapine The serum concentration of Clozapine can be increased when it is combined with Gefitinib.
Quinine The metabolism of Gefitinib can be decreased when combined with Quinine.
Chlorpromazine The metabolism of Gefitinib can be decreased when combined with Chlorpromazine.
Chloroquine The metabolism of Gefitinib can be decreased when combined with Chloroquine.
Nicardipine The metabolism of Gefitinib can be decreased when combined with Nicardipine.
Panobinostat The metabolism of Gefitinib can be decreased when combined with Panobinostat.
Asunaprevir The metabolism of Gefitinib can be decreased when combined with Asunaprevir.
Duloxetine The metabolism of Gefitinib can be decreased when combined with Duloxetine.
Primaquine The metabolism of Gefitinib can be decreased when combined with Primaquine.
Celecoxib The metabolism of Gefitinib can be decreased when combined with Celecoxib.
Fluvoxamine The metabolism of Gefitinib can be decreased when combined with Fluvoxamine.
Fusidic acid The metabolism of Gefitinib can be decreased when combined with Fusidic acid.
Cholecalciferol The metabolism of Gefitinib can be decreased when combined with Cholecalciferol.
Tranylcypromine The metabolism of Gefitinib can be decreased when combined with Tranylcypromine.
Perhexiline The metabolism of Gefitinib can be decreased when combined with Perhexiline.
Tegaserod The metabolism of Gefitinib can be decreased when combined with Tegaserod.
Abiraterone The metabolism of Gefitinib can be decreased when combined with Abiraterone.
Vilazodone The metabolism of Gefitinib can be decreased when combined with Vilazodone.
Sulfaphenazole The metabolism of Gefitinib can be decreased when combined with Sulfaphenazole.
Phenylbutyric acid The metabolism of Gefitinib can be decreased when combined with Phenylbutyric acid.
Manidipine The metabolism of Gefitinib can be decreased when combined with Manidipine.
Ritanserin The metabolism of Gefitinib can be decreased when combined with Ritanserin.
Rhein The metabolism of Gefitinib can be decreased when combined with Rhein.
Terbinafine The metabolism of Gefitinib can be decreased when combined with Terbinafine.
Lumefantrine The metabolism of Gefitinib can be decreased when combined with Lumefantrine.
Darifenacin The metabolism of Gefitinib can be decreased when combined with Darifenacin.
Desipramine The metabolism of Gefitinib can be decreased when combined with Desipramine.
Dosulepin The metabolism of Gefitinib can be decreased when combined with Dosulepin.
Lorcaserin The metabolism of Gefitinib can be decreased when combined with Lorcaserin.
Thioridazine The metabolism of Gefitinib can be decreased when combined with Thioridazine.
Paroxetine The metabolism of Gefitinib can be decreased when combined with Paroxetine.
Cinacalcet The metabolism of Gefitinib can be decreased when combined with Cinacalcet.

Target Protein

Epidermal growth factor receptor EGFR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15329413
    Pao W, Miller V, Zakowski M, Doherty J, Politi K, Sarkaria I, Singh B, Heelan R, Rusch V, Fulton L, Mardis E, Kupfer D, Wilson R, Kris M, Varmus H: EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci U S A. 2004 Sep 7;101(36):13306-11. Epub 2004 Aug 25.
  • PMID: 15284455
    Sordella R, Bell DW, Haber DA, Settleman J: Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science. 2004 Aug 20;305(5687):1163-7. Epub 2004 Jul 29.

Contoh Produk & Brand

Produk: 17 • International brands: 0
Produk
  • Apo-gefitinib
    Tablet • 250 mg • Oral • Canada • Generic • Approved
  • Auro-gefitinib
    Tablet • 250 mg • Oral • Canada • Generic • Approved
  • Eugia-gefitinib
    Tablet • 250 mg • Oral • Canada • Approved
  • Gefitinib
    Tablet, coated • 250 mg/1 • Oral • US • Generic • Approved
  • Gefitinib
    Tablet, coated • 250 mg/1 • Oral • US • Generic • Approved
  • Gefitinib
    Tablet, film coated • 250 mg/1 • Oral • US • Generic • Approved
  • Gefitinib
    Tablet, film coated • 250 mg/1 • Oral • US • Generic • Approved
  • Gefitinib
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 17 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul