General Information of Drug (ID: DM5GFIK)

Drug Name
Icotinib hydrochloride Drug Info
Synonyms Conmana; Conmanna; Icotinib; BPI-2009-H
Indication
Disease Entry ICD 11 Status REF
Non-small-cell lung cancer 2C25.Y Registered [1]
Cross-matching ID
PubChem CID
44609731
CAS Number
CAS 1204313-51-8
TTD Drug ID
DM5GFIK
INTEDE Drug ID
DR0851

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [4]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [5]
Gefitinib DM15F0X Colon adenocarcinoma Approved [6]
Erlotinib DMCMBHA Adrenal gland neoplasm Approved [7]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [8]
Dacomitinib DMOH8VY Non-small-cell lung cancer 2C25.Y Approved [9]
BIBW 2992 DMTKD7Q Non-small-cell lung cancer 2C25.Y Approved [10]
SKI-758 DMQ8E9R Ischemia 8B10-8B11 Approved [11]
Epidermal growth factor DMVONE6 Vulnerary ND56.Z Approved [9]
Merimepodib DM0HS92 Breast cancer 2C60-2C65 Approved [12]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [13]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [14]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [15]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [16]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [17]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [18]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [19]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [20]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [14]
Verapamil DMA7PEW Angina pectoris BA40 Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 1A2 (CYP1A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [22]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [23]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [24]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [25]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [26]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [27]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [19]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [28]
Verapamil DMA7PEW Angina pectoris BA40 Approved [29]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [30]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A5 (CYP3A5)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [31]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [32]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [33]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [34]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [35]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [36]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [37]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [38]
Verapamil DMA7PEW Angina pectoris BA40 Approved [39]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [34]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Antagonist [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [3]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [3]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [3]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7641).
2 Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors. Lung Cancer. 2011 Aug;73(2):195-202.
3 Metabolic pathway of icotinib in vitro: the differential roles of CYP3A4, CYP3A5, and CYP1A2 on potential pharmacokinetic drug-drug interaction. J Pharm Sci. 2018 Apr;107(4):979-983.
4 Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
5 Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
6 Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
7 Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
8 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
9 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1797).
10 Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
11 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
12 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
13 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
14 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
15 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
16 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
17 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
18 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
19 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
20 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
21 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
22 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
23 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
24 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
25 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
26 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
27 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
28 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
29 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
30 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
31 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
32 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
33 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
34 Drug Interactions Flockhart Table
35 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
36 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
37 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
38 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
39 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.