relugolix 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
gonadotropin releasing hormone (GnRH) antagonists	5432	737789-87-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: relugolix TAK-385 orgovyx relumina RVT 601	Relugolix is a nonpeptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby, reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and consequently testosterone. Molecular weight: 623.64 Formula: C29H27F2N7O5S CLOGP: 3.16 LIPINSKI: 2 HAC: 12 HDO: 2 TPSA: 129.23 ALOGS: -5.50 ROTB: 9 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

relugolix
TAK-385
orgovyx
relumina
RVT 601

Relugolix is a nonpeptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby, reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and consequently testosterone.

Molecular weight: 623.64
Formula: C29H27F2N7O5S
CLOGP: 3.16
LIPINSKI: 2
HAC: 12
HDO: 2
TPSA: 129.23
ALOGS: -5.50
ROTB: 9

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.04 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

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Date	Agency	Company
Aug. 1, 2019	PMDA	Takeda Pharmaceutical Company Limited
Dec. 18, 2020	FDA	MYOVANT SCIENCES
July 16, 2021	EMA	Gedeon Richter Plc.

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FDA Adverse Event Reporting System (Female)

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Therapy interrupted	827.89	56.46	161	806	13536	34942428
Hot flush	191.43	56.46	52	915	18014	34937950
Fatigue	59.40	56.46	61	906	370592	34585372

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Therapy interrupted	221.96	50.61	50	530	31291	79712517
Hot flush	132.17	50.61	37	543	54840	79688968
Intermenstrual bleeding	61.50	50.61	13	567	5871	79737937

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	H01CC54	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Anti-gonadotropin-releasing hormones
ATC	L02BX04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Other hormone antagonists and related agents
FDA EPC	N0000175839	Gonadotropin Releasing Hormone Receptor Antagonist
FDA MoA	N0000175084	Gonadotropin Releasing Hormone Receptor Antagonists
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000187064	Cytochrome P450 2B6 Inducers
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
FDA MoA	N0000190118	Cytochrome P450 3A Inducers
FDA PE	N0000008638	Decreased GnRH Secretion
MeSH PA	D000726	Androgen Antagonists

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Lower abdominal pain	indication	54586004
Uterine fibroids	indication	95315005	DOID:13223
Pain associated with endometriosis	indication	129103003
Menorrhagia	indication	386692008
Malignant tumor of prostate	indication	399068003	DOID:10283
Abnormal uterine bleeding due to uterine fibroid	indication	16754891000119106

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
120MG	ORGOVYX	MYOVANT SCIENCES	N214621	Dec. 18, 2020	RX	TABLET	ORAL	8735401	Feb. 4, 2024	TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER THAT IS SEX-HORMONE-DEPENDENT
120MG	ORGOVYX	MYOVANT SCIENCES	N214621	Dec. 18, 2020	RX	TABLET	ORAL	10449191	Sept. 29, 2037	TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER
120MG	ORGOVYX	MYOVANT SCIENCES	N214621	Dec. 18, 2020	RX	TABLET	ORAL	10786501	Sept. 29, 2037	TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER
120MG	ORGOVYX	MYOVANT SCIENCES	N214621	Dec. 18, 2020	RX	TABLET	ORAL	11583526	Sept. 29, 2037	TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER
1MG;0.5MG;40MG	MYFEMBREE	MYOVANT SCIENCES	N214846	May 26, 2021	RX	TABLET	ORAL	9346822	Feb. 17, 2024	MANAGEMENT OF HEAVY MENSTRUAL BLEEDING ASSOCIATED WITH UTERINE LEIOMYOMAS (FIBROIDS) IN PREMENOPAUSAL WOMEN
1MG;0.5MG;40MG	MYFEMBREE	MYOVANT SCIENCES	N214846	May 26, 2021	RX	TABLET	ORAL	11033551	Sept. 29, 2037	MANAGEMENT OF HEAVY MENSTRUAL BLEEDING ASSOCIATED WITH UTERINE LEIOMYOMAS (FIBROIDS) IN PREMENOPAUSAL WOMEN

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
120MG	ORGOVYX	MYOVANT SCIENCES	N214621	Dec. 18, 2020	RX	TABLET	ORAL	Dec. 18, 2025	NEW CHEMICAL ENTITY
1MG;0.5MG;40MG	MYFEMBREE	MYOVANT SCIENCES	N214846	May 26, 2021	RX	TABLET	ORAL	May 26, 2024	NEW PRODUCT
1MG;0.5MG;40MG	MYFEMBREE	MYOVANT SCIENCES	N214846	May 26, 2021	RX	TABLET	ORAL	Aug. 5, 2025	FOR THE MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS
1MG;0.5MG;40MG	MYFEMBREE	MYOVANT SCIENCES	N214846	May 26, 2021	RX	TABLET	ORAL	Dec. 18, 2025	NEW CHEMICAL ENTITY
1MG;0.5MG;40MG	MYFEMBREE	MYOVANT SCIENCES	N214846	May 26, 2021	RX	TABLET	ORAL	Jan. 27, 2026	INFORMATION ADDED TO THE LABELING TO DESCRIBE THE RESULTS OF MVT-601-035

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Gonadotropin-releasing hormone receptor	GPCR	P30968	GNRHR_HUMAN	ANTAGONIST	IC50	9.92		SCIENTIFIC LITERATURE	DRUG LABEL
Gonadotropin-releasing hormone receptor	GPCR		GNRHR_RAT	ANTAGONIST	IC50	9.48		IUPHAR

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External reference:

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ID	Source
018596	NDDF
10348973	PUBCHEM_CID
1144477009	SNOMEDCT_US
1144510001	SNOMEDCT_US
2472778	RXNORM
342118	MMSL
39104	MMSL
4039939	VANDF
5586	IUPHAR_LIGAND_ID
9628	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Myfembree	HUMAN PRESCRIPTION DRUG LABEL	3	72974-415	TABLET, FILM COATED	40 mg	ORAL	NDA	33 sections
Myfembree	HUMAN PRESCRIPTION DRUG LABEL	3	72974-415	TABLET, FILM COATED	40 mg	ORAL	NDA	33 sections
Myfembree	HUMAN PRESCRIPTION DRUG LABEL	3	72974-415	TABLET, FILM COATED	40 mg	ORAL	NDA	33 sections
Orgovyx	HUMAN PRESCRIPTION DRUG LABEL	1	72974-120	TABLET, FILM COATED	120 mg	ORAL	NDA	31 sections
Orgovyx	HUMAN PRESCRIPTION DRUG LABEL	1	72974-120	TABLET, FILM COATED	120 mg	ORAL	NDA	31 sections
Orgovyx	HUMAN PRESCRIPTION DRUG LABEL	1	72974-120	TABLET, FILM COATED	120 mg	ORAL	NDA	31 sections

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