General Information of Drug (ID: DMK7IWL)

Drug Name
Relugolix Drug Info
Synonyms
737789-87-6; TAK-385; TAK 385; UNII-P76B05O5V6; CHEMBL1800159; TAK-385/TAK385; P76B05O5V6; 1-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea; Relugolix [USAN:INN]; TAK385; Relugolix (JAN/INN); SCHEMBL778416; GTPL5586; DTXSID40224167; MolPort-044-567-649; AOMXMOCNKJTRQP-UHFFFAOYSA-N; EX-A1083; BCP21587; ZINC43206033; BDBM50347982; AKOS027440398; SB16721; DB11853; CS-5917
Indication
Disease Entry ICD 11 Status REF
Prostate cancer 2C82.0 Approved [1]
Endometriosis GA10 Phase 3 [2]
Cross-matching ID
PubChem CID
10348973
CAS Number
CAS 737789-87-6
TTD Drug ID
DMK7IWL
VARIDT Drug ID
DR00186
ACDINA Drug ID
D01379

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Gonadorelin DMAQ469 Amenorrhea GA20.0 Approved [4]
Ganirelix DMGMB30 Ovulation dysfunction 5A80 Approved [5]
Abarelix DM5WFNP Prostate cancer 2C82.0 Approved [6]
Triptorelin DMTK4LS Infertility GB04 Approved [7]
Leuprorelin acetate DM15HAT Prostate cancer 2C82.0 Approved [8]
Nafarelin DMAHEFY Endometriosis GA10 Approved [9]
Cetrorelix DMFD9Q6 Ovarian stimulation LB45.1 Approved [10]
Elagolix sodium DMRDUC0 Endometriosis GA10 Approved [11]
Degarelix DM3O8QY Prostate cancer 2C82.0 Approved [12]
AEZS-108 DMAYO46 Acute lymphoblastic leukaemia 2A85 Phase 3 [13]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [14]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [15]
Methotrexate DM2TEOL Anterior urethra cancer Approved [16]
Folic Acid DMEMBJC Colorectal carcinoma Approved [17]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [16]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [16]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [18]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [16]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [19]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [20]
⏷ 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
Gonadotropin-releasing hormone receptor (GNRHR) TT8R70G GNRHR_HUMAN Antagonist [1]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [3]

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01665)
4 Use of cognitive behavior therapy for functional hypothalamic amenorrhea. Ann N Y Acad Sci. 2006 Dec;1092:114-29.
5 Age attenuates testosterone secretion driven by amplitude-varying pulses of recombinant human luteinizing hormone during acute gonadotrope inhibiti... J Clin Endocrinol Metab. 2007 Sep;92(9):3626-32.
6 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
7 Regulation of GnRH I receptor gene expression by the GnRH agonist triptorelin, estradiol, and progesterone in the gonadotroph-derived cell line alphaT3-1. Endocrine. 2006 Aug;30(1):139-44.
8 Clinical pipeline report, company report or official report of Takeda (2009).
9 Reversible downregulation of endocrine and germinative testicular function (hormonal castration) in the dog with the GnRH-agonist azagly-nafarelin ... Theriogenology. 2009 Apr 15;71(7):1037-45.
10 Gonadotropin releasing hormone analogs induce apoptosis by extrinsic pathway involving p53 phosphorylation in primary cell cultures of human prostatic adenocarcinomas. Prostate. 2009 Jul 1;69(10):1025-33.
11 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
12 Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II. J Med Chem. 2005 Jul 28;48(15):4851-60.
13 Stability of cytotoxic luteinizing hormone-releasing hormone conjugate (AN-152) containing doxorubicin 14-O-hemiglutarate in mouse and human serum in vitro: implications for the design of preclinicalstudies. Proc Natl Acad Sci U S A. 2000 Jan 18;97(2):829-34.
14 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
15 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
16 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
17 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
18 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
19 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
20 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.