Peringatan Keamanan

The most common toxicities reported are skin-related events and diarrhea.

Icotinib

DB11737

small molecule experimental investigational

Deskripsi

Icotinib is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI)
Icotinib was approved in China by the SFDA in June, 2011 and in January 2014, Beta Pharma, Inc. was given a “May Proceed” from the US FDA to conduct a Phase I study for the evaluation of icotinib as a treatment of EGFR+ Non-Small Cell Lung Cancer (NSCLC).

Struktur Molekul 2D

Berat 391.427
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 5.5 hrs
Volume Distribusi the volume of distribution was calculated as Vz/F = 115.00 ± 63.26 l
Klirens (Clearance) the clearance was calculated as CL/F = 13.30 ± 4.78 l/h

Absorpsi

Bioavailability = 52%

Metabolisme

Hepatic (mainly CYP3A4, less CYP1A2)

Rute Eliminasi

>90% via faeces, 9% via urine

Interaksi Obat

391 Data
Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Icotinib.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Icotinib.
Pitolisant The serum concentration of Icotinib can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Icotinib can be increased when combined with Metreleptin.
Diltiazem The metabolism of Icotinib can be decreased when combined with Diltiazem.
Cimetidine The metabolism of Icotinib can be decreased when combined with Cimetidine.
Ciprofloxacin The metabolism of Icotinib can be decreased when combined with Ciprofloxacin.
Verapamil The metabolism of Icotinib can be decreased when combined with Verapamil.
Isavuconazole The metabolism of Icotinib can be decreased when combined with Isavuconazole.
Erythromycin The serum concentration of Icotinib can be increased when it is combined with Erythromycin.
Gestodene The metabolism of Icotinib can be decreased when combined with Gestodene.
Rucaparib The metabolism of Icotinib can be decreased when combined with Rucaparib.
Nabiximols The metabolism of Icotinib can be decreased when combined with Nabiximols.
Troglitazone The metabolism of Icotinib can be decreased when combined with Troglitazone.
Chloramphenicol The metabolism of Icotinib can be decreased when combined with Chloramphenicol.
Fluticasone propionate The metabolism of Icotinib can be decreased when combined with Fluticasone propionate.
Imatinib The metabolism of Icotinib can be decreased when combined with Imatinib.
Aprepitant The metabolism of Icotinib can be decreased when combined with Aprepitant.
Mibefradil The metabolism of Icotinib can be decreased when combined with Mibefradil.
Seproxetine The metabolism of Icotinib can be decreased when combined with Seproxetine.
Fluticasone furoate The metabolism of Fluticasone furoate can be increased when combined with Icotinib.
Letermovir The metabolism of Icotinib can be decreased when combined with Letermovir.
Fluticasone The metabolism of Icotinib can be decreased when combined with Fluticasone.
Medical Cannabis The metabolism of Icotinib can be decreased when combined with Medical Cannabis.
Curcumin sulfate The metabolism of Icotinib can be decreased when combined with Curcumin sulfate.
Methylene blue The metabolism of Icotinib can be decreased when combined with Methylene blue.
Clofazimine The metabolism of Icotinib can be decreased when combined with Clofazimine.
Pralsetinib The metabolism of Icotinib can be decreased when combined with Pralsetinib.
Levoketoconazole The metabolism of Icotinib can be decreased when combined with Levoketoconazole.
Acalabrutinib The metabolism of Icotinib can be decreased when combined with Acalabrutinib.
Osilodrostat The metabolism of Icotinib can be decreased when combined with Osilodrostat.
Modafinil The metabolism of Icotinib can be increased when combined with Modafinil.
Dapsone The metabolism of Dapsone can be increased when combined with Icotinib.
Lidocaine The risk or severity of methemoglobinemia can be increased when Icotinib is combined with Lidocaine.
Oxycodone The metabolism of Oxycodone can be increased when combined with Icotinib.
Flutamide The metabolism of Flutamide can be increased when combined with Icotinib.
Dextromethorphan The metabolism of Dextromethorphan can be increased when combined with Icotinib.
Propranolol The metabolism of Propranolol can be increased when combined with Icotinib.
Chloroquine The metabolism of Chloroquine can be increased when combined with Icotinib.
Trazodone The metabolism of Trazodone can be increased when combined with Icotinib.
Mycophenolate mofetil The metabolism of Mycophenolate mofetil can be increased when combined with Icotinib.
Norethisterone The metabolism of Norethisterone can be increased when combined with Icotinib.
Nateglinide The metabolism of Nateglinide can be increased when combined with Icotinib.
Pentamidine The metabolism of Pentamidine can be increased when combined with Icotinib.
Tretinoin The metabolism of Tretinoin can be increased when combined with Icotinib.
Clopidogrel The metabolism of Clopidogrel can be increased when combined with Icotinib.
Irinotecan The metabolism of Irinotecan can be increased when combined with Icotinib.
Disulfiram The metabolism of Disulfiram can be increased when combined with Icotinib.
Ondansetron The metabolism of Ondansetron can be increased when combined with Icotinib.
Zonisamide The metabolism of Zonisamide can be increased when combined with Icotinib.
Buprenorphine The metabolism of Buprenorphine can be increased when combined with Icotinib.
Salmeterol The metabolism of Salmeterol can be increased when combined with Icotinib.
Zaleplon The metabolism of Zaleplon can be increased when combined with Icotinib.
Azelastine The metabolism of Azelastine can be increased when combined with Icotinib.
Nitrendipine The metabolism of Nitrendipine can be increased when combined with Icotinib.
Praziquantel The metabolism of Praziquantel can be increased when combined with Icotinib.
Atorvastatin The metabolism of Atorvastatin can be increased when combined with Icotinib.
Quinacrine The metabolism of Quinacrine can be increased when combined with Icotinib.
Chlorpheniramine The metabolism of Chlorpheniramine can be increased when combined with Icotinib.
Dutasteride The metabolism of Dutasteride can be increased when combined with Icotinib.
Cilostazol The metabolism of Cilostazol can be increased when combined with Icotinib.
Domperidone The metabolism of Domperidone can be increased when combined with Icotinib.
Finasteride The metabolism of Finasteride can be increased when combined with Icotinib.
Halofantrine The metabolism of Halofantrine can be increased when combined with Icotinib.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Icotinib.
Lapatinib The metabolism of Lapatinib can be increased when combined with Icotinib.
Paliperidone The metabolism of Paliperidone can be increased when combined with Icotinib.
Romidepsin The metabolism of Romidepsin can be increased when combined with Icotinib.
Udenafil The metabolism of Udenafil can be increased when combined with Icotinib.
Saxagliptin The metabolism of Saxagliptin can be increased when combined with Icotinib.
Ambrisentan The metabolism of Ambrisentan can be increased when combined with Icotinib.
Apixaban The metabolism of Apixaban can be increased when combined with Icotinib.
Vicriviroc The metabolism of Vicriviroc can be increased when combined with Icotinib.
Hydroxyprogesterone caproate The metabolism of Hydroxyprogesterone caproate can be increased when combined with Icotinib.
Ivacaftor The serum concentration of Icotinib can be increased when it is combined with Ivacaftor.
Vortioxetine The metabolism of Vortioxetine can be increased when combined with Icotinib.
Daclatasvir The metabolism of Daclatasvir can be increased when combined with Icotinib.
Paritaprevir The metabolism of Paritaprevir can be increased when combined with Icotinib.
Asunaprevir The metabolism of Asunaprevir can be increased when combined with Icotinib.
Tezacaftor The metabolism of Tezacaftor can be increased when combined with Icotinib.
Valbenazine The metabolism of Valbenazine can be increased when combined with Icotinib.
Lorlatinib The metabolism of Lorlatinib can be increased when combined with Icotinib.
Deutetrabenazine The metabolism of Deutetrabenazine can be increased when combined with Icotinib.
Doravirine The metabolism of Doravirine can be increased when combined with Icotinib.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Icotinib.
Hydrocortisone cypionate The metabolism of Hydrocortisone cypionate can be increased when combined with Icotinib.
Levonorgestrel The metabolism of Levonorgestrel can be increased when combined with Icotinib.
Glyburide The metabolism of Glyburide can be increased when combined with Icotinib.
Istradefylline The metabolism of Istradefylline can be increased when combined with Icotinib.
Risperidone The metabolism of Risperidone can be increased when combined with Icotinib.
Lercanidipine The metabolism of Lercanidipine can be increased when combined with Icotinib.
Dexloxiglumide The metabolism of Dexloxiglumide can be increased when combined with Icotinib.
Azimilide The metabolism of Azimilide can be increased when combined with Icotinib.
Budesonide The metabolism of Icotinib can be increased when combined with Budesonide.
Sildenafil The metabolism of Sildenafil can be increased when combined with Icotinib.
Lovastatin The metabolism of Lovastatin can be increased when combined with Icotinib.
Nevirapine The metabolism of Nevirapine can be increased when combined with Icotinib.
Ziprasidone The metabolism of Icotinib can be decreased when combined with Ziprasidone.
Gefitinib The metabolism of Gefitinib can be increased when combined with Icotinib.
Progesterone The metabolism of Progesterone can be increased when combined with Icotinib.

Target Protein

Epidermal growth factor receptor EGFR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25675121
    Tan F, Shi Y, Wang Y, Ding L, Yuan X, Sun Y: Icotinib, a selective EGF receptor tyrosine kinase inhibitor, for the treatment of non-small-cell lung cancer. Future Oncol. 2015;11(3):385-97. doi: 10.2217/fon.14.249.
  • PMID: 22112293
    Tan F, Shen X, Wang D, Xie G, Zhang X, Ding L, Hu Y, He W, Wang Y, Wang Y: Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer. 2012 May;76(2):177-82. doi: 10.1016/j.lungcan.2011.10.023. Epub 2011 Nov 22.
  • PMID: 21732454
    Liu D, Jiang J, Zhang L, Tan F, Wang Y, Hu P: Metabolite characterization of a novel anti-cancer agent, icotinib, in humans through liquid chromatography/quadrupole time-of-flight tandem mass spectrometry. Rapid Commun Mass Spectrom. 2011 Aug 15;25(15):2131-40. doi: 10.1002/rcm.5061.
  • PMID: 24588695
    Guan YS, He Q, Li M: Icotinib: activity and clinical application in Chinese patients with lung cancer. Expert Opin Pharmacother. 2014 Apr;15(5):717-28. doi: 10.1517/14656566.2014.890183. Epub 2014 Mar 4.
  • PMID: 26963729
    Zhang HX, Xiong HX, Li LW: Investigation on the protein-binding properties of icotinib by spectroscopic and molecular modeling method. Spectrochim Acta A Mol Biomol Spectrosc. 2016 May 15;161:88-94. doi: 10.1016/j.saa.2016.02.014. Epub 2016 Feb 23.

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Sekuens Gen/Protein (FASTA)

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