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

General Information of Drug (ID: DMGMB30)

• Drug Name: Ganirelix Drug Info
• Synonyms: Ganirelixum; Orgalutran; Ganirelix acetate; Antagon (TN); Ganirelix (INN); Ganirelix [INN:BAN]; Ganirelixum [INN-Latin]; Orgalutran (TN); RS-26306

Indication

Disease Entry	ICD 11	Status	REF
Ovulation dysfunction	5A80	Approved	[1]

• Therapeutic Class: Abortifacient Agents
• Cross-matching ID:
  PubChem CID: 16130957
  ChEBI ID: CHEBI:135910
  CAS Number: CAS 124904-93-4
  TTD Drug ID: DMGMB30

Molecule-Related Drug Atlas

Drug(s) Targeting Gonadotropin-releasing hormone receptor (GNRHR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gonadorelin	DMAQ469	Amenorrhea	GA20.0	Approved	[4]
Relugolix	DMK7IWL	Prostate cancer	2C82.0	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]

Drug(s) Affected By Lutropin subunit beta (LHB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Leuprorelin acetate	DM15HAT	Prostate cancer	2C82.0	Approved	[14]
Levonorgestrel	DM1DP7T	Atypical endometrial hyperplasia		Approved	[15]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[16]
Naloxone	DM3FXMA	Narcotic depression	6A7Z	Approved	[17]
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[18]
Alprazolam	DMC7XDN	Anxiety		Approved	[19]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[20]
Norethindrone acetate	DMDGCQP	N. A.	N. A.	Approved	[15]
Metoclopramide	DMFA5MY	Nausea	MD90	Approved	[17]
Cetrorelix	DMFD9Q6	Ovarian stimulation	LB45.1	Approved	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Gonadotropin-releasing hormone receptor (GNRHR)	TT8R70G	GNRHR_HUMAN	Antagonist	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Lutropin subunit beta (LHB)	OT5GBOVJ	LSHB_HUMAN	Gene/Protein Processing	[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: 3877).
• [2] 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.
• [3] Progesterone rise on HCG day in GnRH antagonist/rFSH stimulated cycles affects endometrial gene expression. Reprod Biomed Online. 2011 Mar;22(3):263-71. doi: 10.1016/j.rbmo.2010.11.002. Epub 2010 Nov 13.
• [4] Use of cognitive behavior therapy for functional hypothalamic amenorrhea. Ann N Y Acad Sci. 2006 Dec;1092:114-29.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [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] Erectile function and nocturnal penile tumescence in patients with prostate cancer undergoing luteinizing hormone-releasing hormone agonist therapy. Int J Urol. 1999 Jan;6(1):19-23. doi: 10.1046/j.1442-2042.1999.06128.x.
• [15] Relative progestational and androgenic activity of four progestins used for male hormonal contraception assessed in vitro in relation to their ability to suppress LH secretion in the castrate male rat. Mol Cell Endocrinol. 2010 Oct 26;328(1-2):16-21. doi: 10.1016/j.mce.2010.06.010. Epub 2010 Jun 25.
• [16] Chronic senescent human mesenchymal stem cells as possible contributor to the wound healing disorder after exposure to the alkylating agent sulfur mustard. Arch Toxicol. 2021 Feb;95(2):727-747. doi: 10.1007/s00204-020-02946-5. Epub 2021 Jan 25.
• [17] Differences in the opioid control of luteinizing hormone secretion between pathological and iatrogenic hyperprolactinemic states. J Clin Endocrinol Metab. 1987 Mar;64(3):508-12. doi: 10.1210/jcem-64-3-508.
• [18] Rapid-onset hypogonadism secondary to crizotinib use in men with metastatic nonsmall cell lung cancer. Cancer. 2012 Nov 1;118(21):5302-9. doi: 10.1002/cncr.27450. Epub 2012 Apr 4.
• [19] The effect of alprazolam on serum cortisol and luteinizing hormone pulsatility in normal women and in women with stress-related anovulation. J Clin Endocrinol Metab. 1995 Mar;80(3):818-23. doi: 10.1210/jcem.80.3.7883836.
• [20] Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
• [21] Pharmacokinetics of new testosterone transdermal therapeutic systems in gonadotropin-releasing hormone antagonist-suppressed normal men. Exp Clin Endocrinol Diabetes. 1999;107(1):63-9. doi: 10.1055/s-0029-1212075.