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

Stem definitionDrug idCAS RN
5432 737789-87-6

Description:

MoleculeDescription

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:

None

Approvals:

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

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Therapy interrupted 470.92 56.70 84 299 10512 31686449
Hot flush 92.37 56.70 24 359 16172 31680789

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Therapy interrupted 116.68 57.71 24 184 24778 70903458
Prostate cancer 67.36 57.71 16 192 31147 70897089

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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 PE N0000008638 Decreased GnRH Secretion
FDA MoA N0000175084 Gonadotropin Releasing Hormone Receptor Antagonists
MeSH PA D000726 Androgen Antagonists
MeSH PA D006727 Hormone Antagonists
FDA EPC N0000175839 Gonadotropin Releasing Hormone Receptor Antagonist
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

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

DiseaseRelationSNOMED_IDDOID
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




🐢 Veterinary Drug Use

None

🐢 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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
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
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
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

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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
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 Dec. 18, 2025 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Gonadotropin-releasing hormone receptor GPCR ANTAGONIST IC50 9.92 SCIENTIFIC LITERATURE DRUG LABEL
Gonadotropin-releasing hormone receptor GPCR ANTAGONIST IC50 9.48 IUPHAR

External reference:

IDSource
D10888 KEGG_DRUG
P76B05O5V6 UNII
C3896936 UMLSCUI
CHEMBL1800159 ChEMBL_ID
10348973 PUBCHEM_CID
DB11853 DRUGBANK_ID
5586 IUPHAR_LIGAND_ID
342118 MMSL
39104 MMSL
d09698 MMSL
4039939 VANDF
018596 NDDF
1144477009 SNOMEDCT_US
1144510001 SNOMEDCT_US
C561634 MESH_SUPPLEMENTAL_RECORD_UI
9628 INN_ID
2472778 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Orgovyx HUMAN PRESCRIPTION DRUG LABEL 1 72974-120 TABLET, FILM COATED 120 mg ORAL NDA 30 sections
Orgovyx HUMAN PRESCRIPTION DRUG LABEL 1 72974-120 TABLET, FILM COATED 120 mg ORAL NDA 30 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