General Information of Drug (ID: DM702MU)

Drug Name
ITX-5061 Drug Info
Synonyms
ITX5061; UNII-J4RA8K2Q2A; J4RA8K2Q2A; ITX-5061; 1252679-52-9; ITX 5061; CHEMBL3402567; HY-19900; CS-0016951; 1-Naphthaleneacetamide, N-(5-(1,1-dimethylethyl)-2-methoxy-3- ((methylsulfonyl)amino)phenyl)-4-(2-(4-morpholinyl)ethoxy)-alpha-oxo-, hydrochloride (1:1)
Indication
Disease Entry ICD 11 Status REF
Human immunodeficiency virus-1 infection 1C62 Phase 1 [1]
Cross-matching ID
PubChem CID
56843466
CAS Number
CAS 1252679-52-9
TTD Drug ID
DM702MU
INTEDE Drug ID
DR1804

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DME
Drug Status:
Approved 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 [3]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [4]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [5]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [6]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [7]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [8]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [9]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [10]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [4]
Verapamil DMA7PEW Angina pectoris BA40 Approved [11]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [12]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [13]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [14]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [7]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [11]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [15]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [16]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [17]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [18]
Propranolol DM79NTF Angina pectoris BA40 Approved [19]
⏷ 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 [20]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [21]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [22]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [23]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [24]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [25]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [26]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [27]
Verapamil DMA7PEW Angina pectoris BA40 Approved [28]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [23]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Mephenytoin 4-hydroxylase (CYP2C19)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [29]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [30]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [31]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [32]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [33]
Verapamil DMA7PEW Angina pectoris BA40 Approved [34]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [35]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [36]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [37]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [38]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [2]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [2]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Substrate [2]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [2]

References

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3 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.
4 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
5 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.
6 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
7 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.
8 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.
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12 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
13 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
14 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
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16 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
17 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
18 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
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20 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.
21 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.
22 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.
23 Drug Interactions Flockhart Table
24 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.
25 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
26 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
27 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
28 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
29 High-dose rabeprazole/amoxicillin therapy as the second-line regimen after failure to eradicate H. pylori by triple therapy with the usual doses of a proton pump inhibitor, clarithromycin and amoxicillin. Hepatogastroenterology. 2003 Nov-Dec;50(54):2274-8.
30 Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9.
31 Cytochrome P450 pharmacogenetics and cancer. Oncogene. 2006 Mar 13;25(11):1679-91.
32 CYP2C19*17 is associated with decreased breast cancer risk. Breast Cancer Res Treat. 2009 May;115(2):391-6.
33 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
34 Cytochromes of the P450 2C subfamily are the major enzymes involved in the O-demethylation of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):116-21.
35 Diclofenac and its derivatives as tools for studying human cytochromes P450 active sites: particular efficiency and regioselectivity of P450 2Cs. Biochemistry. 1999 Oct 26;38(43):14264-70.
36 A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
37 Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33.
38 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.