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 |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.04 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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 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 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| 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 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|
| 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 |
🐶 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 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 |
| 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 |
| 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 | 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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 |
| 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 |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| D10888 | KEGG_DRUG |
| P76B05O5V6 | UNII |
| C3896936 | UMLSCUI |
| CHEMBL1800159 | ChEMBL_ID |
| 10348973 | PUBCHEM_CID |
| DB11853 | DRUGBANK_ID |
| 5586 | IUPHAR_LIGAND_ID |
| 018596 | NDDF |
| 1144477009 | SNOMEDCT_US |
| 1144510001 | SNOMEDCT_US |
| 4039939 | VANDF |
| 2472778 | RXNORM |
| 342118 | MMSL |
| 39104 | MMSL |
| d09698 | MMSL |
| C561634 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9628 | INN_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |
| 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 |