Peringatan Keamanan

Symptoms of overdose include diarrhea, rash, and liver transaminase elevation. The most common adverse reactions (>50%) in NSCLC are rash, diarrhea, anorexia and fatigue. The most common adverse reactions (>50%) in pancreatic cancer are fatigue, rash, nausea and anorexia.

Erlotinib

DB00530

small molecule approved investigational

Deskripsi

Erlotinib is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase that is used in the treatment of non-small cell lung cancer, pancreatic cancer and several other types of cancer. It is typically marketed under the trade name Tarceva. Erlotinib binds to the epidermal growth factor receptor (EGFR) tyrosine kinase in a reversible fashion at the adenosine triphosphate (ATP) binding site of the receptor. Recent studies demonstrate that erlotinib is also a potent inhibitor of JAK2V617F, which is a mutant form of tyrosine kinase JAK2 found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. This finding introduces the potential use of erlotinib in the treatment of JAK2V617F-positive PV and other myeloproliferative disorders.

Struktur Molekul 2D

Berat 393.4357
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Median half-life of 36.2 hours.
Volume Distribusi Apparent volume of distribution = 232 L
Klirens (Clearance) Smokers have a 24% higher rate of erlotinib clearance.

Absorpsi

Erlotinib is about 60% absorbed after oral administration and its bioavailability is substantially increased by food to almost 100%. Peak plasma levels occur 4 hours after dosing. The solubility of erlotinib is pH dependent. Solubility decreases pH increases. Smoking also decrease the exposure of erlotinib.

Metabolisme

Metabolism occurs in the liver. In vitro assays of cytochrome P450 metabolism showed that erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2, and the extrahepatic isoform CYP1A1.

Rute Eliminasi

Following a 100 mg oral dose, 91% of the dose was recovered in which 83% was in feces (1% of the dose as unchanged parent compound) and 8% in urine (0.3% of the dose as unchanged parent compound).

Farmakogenomik

3 Varian
EGFR (rs28929495)

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

EGFR (rs121913444)

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

EGFR (rs121434568)

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

Interaksi Makanan

3 Data
  • 1. Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of erlotinib.
  • 2. Exercise caution with St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of erlotinib.
  • 3. Take on an empty stomach. Food increases erlotinib bioavailability, therefore administer at least 1 hour before or 2 hours after meals.

Interaksi Obat

1297 Data
Peginterferon alfa-2b The serum concentration of Erlotinib can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Erlotinib can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Erlotinib can be decreased when it is combined with Teriflunomide.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Erlotinib.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Erlotinib.
Cimetidine Cimetidine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nizatidine Nizatidine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ranitidine Ranitidine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Famotidine Famotidine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methantheline Methantheline can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium oxide Magnesium oxide can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium bicarbonate Sodium bicarbonate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonate Calcium carbonate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Metiamide Metiamide can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Roxatidine acetate Roxatidine acetate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magaldrate Magaldrate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium hydroxide Magnesium hydroxide can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium trisilicate Magnesium trisilicate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium carbonate Magnesium carbonate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lafutidine Lafutidine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lavoltidine Lavoltidine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bismuth subnitrate Bismuth subnitrate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium silicate Magnesium silicate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium acetoacetate Aluminium acetoacetate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hydrotalcite Hydrotalcite can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium peroxide Magnesium peroxide can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Almasilate Almasilate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium glycinate Aluminium glycinate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aloglutamol Aloglutamol can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Niperotidine Niperotidine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium silicate Calcium silicate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pantoprazole Pantoprazole can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Esomeprazole Esomeprazole can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rabeprazole Rabeprazole can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Omeprazole Omeprazole can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lansoprazole Lansoprazole can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexlansoprazole Dexlansoprazole can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexrabeprazole Dexrabeprazole can cause a decrease in the absorption of Erlotinib 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 Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Vonoprazan Vonoprazan can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Erlotinib.
Colchicine The metabolism of Colchicine can be decreased when combined with Erlotinib.
Iloperidone The risk or severity of QTc prolongation can be increased when Erlotinib is combined with Iloperidone.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Erlotinib.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Erlotinib.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Erlotinib.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Erlotinib.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Erlotinib.
Irinotecan The risk or severity of neutropenia can be increased when Erlotinib is combined with Irinotecan.
Metreleptin The metabolism of Erlotinib can be increased when combined with Metreleptin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Erlotinib.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Erlotinib.
Olanzapine Olanzapine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Promethazine Promethazine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Doxepin Doxepin can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Asenapine Asenapine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Epinastine Epinastine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Enzalutamide The metabolism of Erlotinib can be increased when combined with Enzalutamide.
Pioglitazone The serum concentration of Pioglitazone can be increased when it is combined with Erlotinib.
Treprostinil The serum concentration of Treprostinil can be increased when it is combined with Erlotinib.
Dicoumarol The serum concentration of Dicoumarol can be increased when it is combined with Erlotinib.
Phenindione The serum concentration of Phenindione can be increased when it is combined with Erlotinib.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Erlotinib.
Phenprocoumon The serum concentration of Phenprocoumon can be increased when it is combined with Erlotinib.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Erlotinib.
4-hydroxycoumarin The serum concentration of 4-hydroxycoumarin can be increased when it is combined with Erlotinib.
Coumarin The serum concentration of Coumarin can be increased when it is combined with Erlotinib.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Erlotinib.
Ethyl biscoumacetate The serum concentration of Ethyl biscoumacetate can be increased when it is combined with Erlotinib.
Fluindione The serum concentration of Fluindione can be increased when it is combined with Erlotinib.
Clorindione The serum concentration of Clorindione can be increased when it is combined with Erlotinib.
Diphenadione The serum concentration of Diphenadione can be increased when it is combined with Erlotinib.
Tioclomarol The serum concentration of Tioclomarol can be increased when it is combined with Erlotinib.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Erlotinib.
Ciprofloxacin The serum concentration of Erlotinib can be increased when it is combined with Ciprofloxacin.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Erlotinib.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Erlotinib.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Erlotinib.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Erlotinib.
Crizotinib The metabolism of Erlotinib can be decreased when combined with Crizotinib.
Mirabegron The serum concentration of Erlotinib can be increased when it is combined with Mirabegron.
Abiraterone The metabolism of Erlotinib can be decreased when combined with Abiraterone.
Cyproterone acetate The metabolism of Erlotinib can be increased when combined with Cyproterone acetate.
Chlorpromazine The serum concentration of Erlotinib can be decreased when it is combined with Chlorpromazine.
Lorlatinib The serum concentration of Erlotinib can be decreased when it is combined with Lorlatinib.
Pegvisomant The serum concentration of Erlotinib can be decreased when it is combined with Pegvisomant.
Calcitriol The serum concentration of Erlotinib can be decreased when it is combined with Calcitriol.
Flunisolide The serum concentration of Erlotinib can be decreased when it is combined with Flunisolide.
Troglitazone The serum concentration of Erlotinib can be decreased when it is combined with Troglitazone.
Butalbital The serum concentration of Erlotinib can be decreased when it is combined with Butalbital.
Flucloxacillin The serum concentration of Erlotinib can be decreased when it is combined with Flucloxacillin.
Bexarotene The serum concentration of Erlotinib can be decreased when it is combined with Bexarotene.
Acetaminophen The serum concentration of Erlotinib can be decreased when it is combined with Acetaminophen.
Aminoglutethimide The serum concentration of Erlotinib can be decreased when it is combined with Aminoglutethimide.
Clozapine The serum concentration of Erlotinib can be decreased when it is combined with Clozapine.
Beclomethasone dipropionate The serum concentration of Erlotinib can be decreased when it is combined with Beclomethasone dipropionate.
Progesterone The serum concentration of Erlotinib can be decreased when it is combined with Progesterone.
Griseofulvin The serum concentration of Erlotinib can be decreased when it is combined with Griseofulvin.

Target Protein

Nuclear receptor subfamily 1 group I member 2 NR1I2
Epidermal growth factor receptor EGFR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11129168
    Raymond E, Faivre S, Armand JP: Epidermal growth factor receptor tyrosine kinase as a target for anticancer therapy. Drugs. 2000;60 Suppl 1:15-23; discussion 41-2.
  • PMID: 17178722
    Li Z, Xu M, Xing S, Ho WT, Ishii T, Li Q, Fu X, Zhao ZJ: Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth. J Biol Chem. 2007 Feb 9;282(6):3428-32. Epub 2006 Dec 18.
  • PMID: 16290256
    Dudek AZ, Kmak KL, Koopmeiners J, Keshtgarpour M: Skin rash and bronchoalveolar histology correlates with clinical benefit in patients treated with gefitinib as a therapy for previously treated advanced or metastatic non-small cell lung cancer. Lung Cancer. 2006 Jan;51(1):89-96. Epub 2005 Nov 14.
  • PMID: 15613453
    Jones HE, Goddard L, Gee JM, Hiscox S, Rubini M, Barrow D, Knowlden JM, Williams S, Wakeling AE, Nicholson RI: Insulin-like growth factor-I receptor signalling and acquired resistance to gefitinib (ZD1839; Iressa) in human breast and prostate cancer cells. Endocr Relat Cancer. 2004 Dec;11(4):793-814.
  • PMID: 11123895
    Blum G, Gazit A, Levitzki A: Substrate competitive inhibitors of IGF-1 receptor kinase. Biochemistry. 2000 Dec 26;39(51):15705-12.

Contoh Produk & Brand

Produk: 69 • International brands: 0
Produk
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    Tablet • 25 mg • Oral • Canada • Generic • Approved
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    Tablet • 100 mg • Oral • Canada • Generic • Approved
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    Tablet • 150 mg • Oral • Canada • Generic • Approved
  • Erlotinib
    Tablet, film coated • 100 mg/1 • Oral • US • Generic • Approved
  • Erlotinib
    Tablet, film coated • 150 mg/1 • Oral • US • Generic • Approved
  • Erlotinib
    Tablet, film coated • 25 mg/1 • Oral • US • Generic • Approved
  • Erlotinib
    Tablet, film coated • 100 mg/1 • Oral • US • Generic • Approved
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    Tablet, film coated • 150 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 69 produk.

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