Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMAQ469)

Drug Name
Gonadorelin Drug Info
Synonyms
Dirigestran; Factrel; Fertagyl; Gonadorelina; Gonadorelinum; Hypocrine; Kryptocur; LFRH; LHFSHRH; Luforan; Luliberin; Lutal; Lutamin; Lutrefact; Relefact; Relisorm; Dirigestran Spofa; Gonadoliberin I; Gonadotropin releasing hormone; LHFSH Releasing Hormone; LUTEINIZING HORMONE; Lutrepulse KIT; MammalianGnRH; Relisorm l; Synthetic LRF; Synthetic gonadoliberin; HOE 471; AY-24031; FSH-Releasing Hormone; Fertagyl (TN); GnRH-I; Gonadorelin (INN); Gonadorelin [INN:BAN]; Gonadorelina [INN-Spanish]; Gonadorelinum [INN-Latin]; Gonadotropin-releasing factor; Gonadotropin-releasing hormone; Gonadotropin-releasing hormone I; Human LH-RH; LH-FSH Releasing Hormone; LH-Releasing hormone; Luteinizing hormone-releasing hormone; Mammalian LH-RH; Mammalian gonadotropin-releasing hormone; Ovine LH-RH; Ovine gonadotropin-releasing hormone; Porchine LH-RH; Porcine LH-releasing factor; Synthetic Gn-RH; Synthetic LH-FSH releasing hormone; Synthetic LH-RF; Synthetic LH-RH; Synthetic LH-releasing factor; Synthetic LH-releasing hormone; Synthetic gonadotropic hormone-releasing hormone; Synthetic gonadotropin-releasing hormone; LH-RH (swine); LH-Releasing factor (pig); LH-Releasing hormone (porcine); Luteinizing hormone-releasing factor (human); Luteinizing hormone-releasing factor (pig); Luteinizing hormone-releasing factor (rat); Luteinizing hormone-releasing factor (sheep); Luteinizing hormone-releasing factor (swine); Luteinizing hormone-releasing hormone (swin); Synthetic LH-FSH-RH; Synthetic decapeptide FSH/LH-RH; Follicle-stimulating hormone-releasing factor (pig); Gonadotropin, luteinizing hormone-releasing hormone, synthetic; Synthetic LH-RH/FSH-RH; Synthetic LH-releasing hormone/FSH-releasing hormone; PyroGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2
Indication
Disease Entry ICD 11 Status REF
Amenorrhea GA20.0 Approved [1]
Hypothalamic hypogonadism 5A61.2 Approved [2]
Therapeutic Class
Fertility Agents
Cross-matching ID
PubChem CID
638793
ChEBI ID
CHEBI:5520
CAS Number
CAS 9034-40-6
TTD Drug ID
DMAQ469
INTEDE Drug ID
DR1929

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Gonadotropin-releasing hormone receptor (GNRHR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Relugolix DMK7IWL Prostate cancer 2C82.0 Approved [7]
Ganirelix DMGMB30 Ovulation dysfunction 5A80 Approved [8]
Abarelix DM5WFNP Prostate cancer 2C82.0 Approved [9]
Triptorelin DMTK4LS Infertility GB04 Approved [10]
Leuprorelin acetate DM15HAT Prostate cancer 2C82.0 Approved [11]
Nafarelin DMAHEFY Endometriosis GA10 Approved [12]
Cetrorelix DMFD9Q6 Ovarian stimulation LB45.1 Approved [13]
Elagolix sodium DMRDUC0 Endometriosis GA10 Approved [14]
Degarelix DM3O8QY Prostate cancer 2C82.0 Approved [15]
AEZS-108 DMAYO46 Acute lymphoblastic leukaemia 2A85 Phase 3 [16]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Prolyl endopeptidase (PREP)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BRADYKININ DM4R6UV N. A. N. A. Phase 1 [17]
Drug(s) Metabolized By Thimet oligopeptidase (THOP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BRADYKININ DM4R6UV N. A. N. A. Phase 1 [18]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Gonadotropin-releasing hormone receptor (GNRHR) TT8R70G GNRHR_HUMAN Agonist [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Metallo-endopeptidase-like 1 (MMEL1) DEYCUQ2 MMEL1_HUMAN Substrate [4]
Prolyl endopeptidase (PREP) DEVSCNZ PPCE_HUMAN Substrate [5]
Thimet oligopeptidase (THOP1) DE95LJC THOP1_HUMAN Substrate [6]

References

1 Gonadorelin FDA Label
2 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: 4391).
3 Use of cognitive behavior therapy for functional hypothalamic amenorrhea. Ann N Y Acad Sci. 2006 Dec;1092:114-29.
4 Cell-specific activity of neprilysin 2 isoforms and enzymic specificity compared with neprilysin. Biochem J. 2002 May 1;363(Pt 3):697-705.
5 Ion-exchange chromatography: basic principles and application to the partial purification of soluble mammalian prolyl oligopeptidase. Methods Mol Biol. 2011;681:215-28.
6 Sleep deprivation changes thimet oligopeptidase (THOP1) expression and activity in rat brain. Heliyon. 2019 Nov 26;5(11):e02896.
7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
8 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.
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
10 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.
11 Clinical pipeline report, company report or official report of Takeda (2009).
12 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.
13 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.
14 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
15 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.
16 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.
17 Bradykinin release and inactivation in brain of rats submitted to an experimental model of Alzheimer's disease. Peptides. 2006 Dec;27(12):3363-9.
18 Expression and activity of thimet oligopeptidase (TOP) are modified in the hippocampus of subjects with temporal lobe epilepsy (TLE). Epilepsia. 2014 May;55(5):754-62.