> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/relugolix-b0e3fb81-fd33-4257-84d9-45f04bcadfc2 > Record changed: 2026-10-13 # Relugolix Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1800159) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1800159) ## Development status **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1800159) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1800159) **Drug name** Relugolix Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1800159) **Molecular weight** 623.64 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1800159) **Structure (SMILES)** CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nn2)c(=O)n3Cc2c(F)cccc2F)cc1 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1800159) ### Brand names (4) - orgovyx - Orgovyx - relugolix component of myfembree - Relugolix component of myfembree ### Other names (24) - myfembree component relugolix - Myfembree component relugolix - orgovyx 120 mg film coated tablets - relugolix - Relugolix - Relugolix \[INN\] - Relugolix \[JAN\] - Relugolix \[MI\] - Relugolix \[ORANGE BOOK\] - Relugolix \[USAN\] - Relugolix \[WHO-DD\] - Relugolix 120 MG - relugolix inn - relugolix jan - relugolix mi - relugolix orange book - relugolix usan - relugolix who dd - Relugolix-Containing Product - tak 385 - Tak-385 - TAK-385 - TAK-385 40 mg - TAK-385 Tablets ## Identifiers **CAS registry numbers** - 737789-87-6 **ChEMBL ID** CHEMBL1800159 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1800159) **InChIKey** AOMXMOCNKJTRQP-UHFFFAOYSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1800159) **PubChem compound IDs** - 10348973 **RxNorm IDs (RxCUI)** - 2472778 **FDA ingredient codes (UNII)** - P76B05O5V6 ### ATC classification codes (2) - L02BX - L02BX04 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1800159) ## Regulatory information ### United States **Applicant** SUMITOMO PHARMA AM **Approval date** 18 Dec 2020 **Application number** NDA214621 ### European Union **Status** Authorised **Status date** 29 Apr 2022 **Authorisation date** 29 Apr 2022 **Approved indications** Orgovyx is indicated for the treatment of adult patients with advanced hormone-sensitive prostate cancer. **Product number** EMEA/H/C/005353 **Authorisation holder** Accord Healthcare S.L.U. **Priority medicines scheme** No **Generic** No **Biosimilar** No **Generic medicines** 0 **Biosimilar medicines** 0 **Advanced therapy** No **Conditional approval** No **Additional monitoring** Yes **Accelerated assessment** No **Exceptional circumstances** No #### Therapeutic areas - Prostatic Neoplasms European medicines record Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/orgovyx) ### Other regulatory facts **Patents** 11 **Designations** 1 **Earliest recorded loss of exclusivity** 29 Sept 2037 **First in class** No **Fast track** No **Breakthrough designation** No **Orphan designation** No **Priority review** Yes **Orphan exclusivity** No **Accelerated approval** No **Availability** Prescription only ## Pharmacology ### Drug classification **Pharmacology name** relugolix **Type** Synthetic organic **Drug name stem** \-golix **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (2) - **Action** Antagonist **Action type** Antagonist **Target** GnRH1 receptor **Gene symbol** GNRHR **Protein identifier** P30968 **Median affinity** 9.48 **Affinity units** pIC50 - **Mechanism** Gonadotropin-releasing hormone receptor antagonist **Action type** Antagonist **Target** Gonadotropin-releasing hormone receptor **Protein identifier** P30968 ### Open Targets mechanisms - **Mechanism** Gonadotropin-releasing hormone receptor antagonist **Action type** Antagonist **Target** Gonadotropin-releasing hormone receptor ### DrugCentral mechanisms - **Action type** Antagonist **Gene symbol** GNRHR **Protein identifier** P30968 **Organism** Homo sapiens **Target development level** Clinical ### Investigated indications (9) - **Condition** Prostatic Neoplasms **Highest recorded phase** 4 **Condition identifier** EFO:0000196 **Subject identifier** D011471 - **Condition** Neoplasms **Highest recorded phase** 4 **Condition identifier** EFO:0000616 **Subject identifier** D009369 - **Condition** Prostatic Neoplasms **Highest recorded phase** 4 **Condition identifier** EFO:0000673 **Subject identifier** D011471 - **Condition** Leiomyoma **Highest recorded phase** 3 **Condition identifier** EFO:0000731 **Subject identifier** D007889 - **Condition** Endometriosis **Highest recorded phase** 3 **Condition identifier** EFO:0001065 **Subject identifier** D004715 - **Condition** Pain **Highest recorded phase** 3 **Condition identifier** EFO:0003843 **Subject identifier** D010146 - **Condition** Hypogonadism **Highest recorded phase** 1 **Condition identifier** MONDO:0002146 **Subject identifier** D007006 - **Condition** Prostatic Neoplasms **Highest recorded phase** 4 **Condition identifier** MONDO:0008315 **Subject identifier** D011471 - **Condition** Prostatic Neoplasms, Castration-Resistant **Highest recorded phase** 3 **Condition identifier** MONDO:0008315 **Subject identifier** D064129 ### Open Targets indications (25) - **Condition identifier** EFO\_0000616 - **Condition identifier** EFO\_0000673 **Highest recorded phase** 2 - **Condition identifier** EFO\_0000731 - **Condition identifier** EFO\_0001065 **Highest recorded phase** 3 - **Condition identifier** EFO\_0009520 **Highest recorded phase** 3 - **Condition identifier** HP\_0000131 **Highest recorded phase** 4 - **Condition identifier** HP\_0000132 - **Condition identifier** HP\_0000132 **Highest recorded phase** 4 - **Condition identifier** HP\_0002027 - **Condition identifier** HP\_0002027 **Highest recorded phase** 4 - **Condition identifier** HP\_0012531 **Highest recorded phase** 2 - **Condition identifier** HP\_0012531 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0001572 - **Condition identifier** MONDO\_0001572 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0002146 - **Condition identifier** MONDO\_0002146 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0002280 - **Condition identifier** MONDO\_0002280 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0004992 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0005070 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0005133 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0007886 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0008315 - **Condition identifier** MONDO\_0008315 **Highest recorded phase** 4 - **Condition identifier** MP\_0001914 **Highest recorded phase** 3 ### Reported adverse events (2) - **Event** hot flush **Reports** 7 **Reporting signal score** 19.0229 - **Event** menstrual disorder **Reports** 2 **Reporting signal score** 7.2197 ### Trial references (28) - NCT01452659 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01452659) - NCT02655224 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02655224) - NCT02655237 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02655237) - NCT01452685 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01452685) - NCT01458301 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01458301) - NCT03654274 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03654274) - NCT03931915 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03931915) - NCT02083185 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02083185) - NCT02135445 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02135445) - NCT02141659 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02141659) - NCT03085095 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03085095) - NCT05605964 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05605964) - NCT05679388 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05679388) - NCT06111313 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06111313) - NCT06111781 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06111781) - NCT06129851 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06129851) - NCT06130995 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06130995) - NCT06463457 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06463457) - NCT03204318 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03204318) - NCT06279195 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06279195) - NCT04423211 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04423211) - NCT04523207 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04523207) - NCT05050084 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05050084) - NCT05053152 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05053152) - NCT05765500 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05765500) And 3 more, listed on the interactive page. ## Dosing **Dose** 120mg **Route** Oral **How often** Once daily ### Conditions of use (2) - Swallow tablets whole, do not crush or chew - Take with or without food ## Chemical properties **Hydrogen bond acceptors** 11 **Hydrogen bond donors** 2 **Polar surface area** 132.61 **Calculated partition coefficient (ALogP)** 3.75 **Calculated partition coefficient (XLogP)** 3.2 **Prodrug** No **Chirality** Achiral **Inorganic** No **Rule-of-five violations** 2 **Rotatable bonds** 9 **Heavy atoms** 44 **Molecular formula** C29H27F2N7O5S **Monoisotopic mass** 623.17624448 **Natural product** No ## National Drug Codes - 72974-120 - 72974-415 ## Evidence counts **Recorded assays** 107 **Active assays** 22 ### Active assay types (2) - Confirmatory - Other ## Pharmacologic actions - Androgen Antagonists Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000726.html) ## Biological measurements These details could not be displayed. ## Related records ### Trials (59) - A Food Effect Study of TAK-385 Final Formulation - A Long-term Extension Study of TAK-385 in the Treatment of Endometriosis - A Multi-Center, Prospective, Observational Study of Patients Being Treated With ORGOVYX - A Phase 1 Study to Evaluate the Effects of Fluconazole and Atorvastatin on the Pharmacokinetics of TAK-385 in Healthy Subjects - A Phase 2 Study to Evaluate the Safety and Efficacy of TAK-385, Together With a Leuprorelin Observational Cohort, in Participants With Prostate Cancer - A Phase 3 Study to Evaluate the Efficacy and Safety of Relugolix (TAK-385) 40 mg Compared With Leuprorelin in the Treatment of Uterine Fibroids - [A Phase 3B Study to Evaluate Bone Mineral Density With Long-Term Use of Relugolix Combination Tablet in Women With Uterine Fibroids or Endometriosis](https://trialight.com/data/trial/a-phase-3b-study-to-evaluate-bone-mineral-density-with-long-81ab9a0c-cf67-493c-9a01-32b3ca8584b7.md) - A Placebo-Controlled, Phase 3 Study of Relugolix (TAK-385) 40 mg in the Treatment of Pain Symptoms Associated With Uterine Fibroids - A Study of Apalutamide (Adjuvant Treatment) and Androgen Deprivation Therapy (ADT) in Participants Who Have Undergone Radical Prostatectomy (RP) for Non-metastatic Prostate Cancer and Who Are at High Risk for Metastases - A Study of Extending Relugolix Dosing Intervals Through Addition of Itraconazole or Ritonavir in Prostate Cancer Patients - A Study of TAK-385 in Hormone Treatment-naïve Participants With Prostate Cancer - A Study of the Effects of Erythromycin on the Pharmacokinetics of Relugolix, Estradiol, and Norethindrone in Healthy Postmenopausal Women and on the Pharmacokinetics of Relugolix in Healthy Adult Men - A Study to Evaluate the Safety and Efficacy of Relugolix in Men With Advanced Prostate Cancer - Androgen Deprivation Therapy (Relugolix) for the Improvement of Diagnostic Imaging (PSMA PET/CT Scan) in Patients With High Risk or Very High Risk Prostate Cancer, The EnrichPSMA Trial - Assessing Efficacy of Neoadjuvant ADT in Localized High-Risk Prostate Cancer Patients Utilizing 18F-Flotufolastat PSMA PET/CT - Bioavailability and Effect of Food on TAK-385 Tablet Formulations in Healthy Participants - Clinical Study to Evaluate Efficacy and Safety of TAK-385 40 mg Compared With Leuprorelin in Patients With Endometriosis - Comeback From Long coursE Androgen Deprivation Therapy (ADT) With RElugolix and Darolutamide (CLEARED) - Description of Relugolix Use in Patients With Prostate Cancer Within the VHA - Effects of Relugolix vs Leuprolide on Cardiac Function in Patients With Prostate Cancer ### Approved for (4) - [Metastatic prostate carcinoma](https://trialight.com/data/condition/metastatic-prostate-carcinoma-d5fb1084-bad5-5db6-8240-897dc47ea451.md) - Neoplasm - [Prostate adenocarcinoma](https://trialight.com/data/condition/prostate-adenocarcinoma-84e3e3af-1ae1-5760-8157-8d9fc0cff608.md) - [Prostate cancer](https://trialight.com/data/condition/prostate-cancer-3659fc70-617b-5868-a093-ae819ffc6755.md) ### In development for (3) - [Endometriosis](https://trialight.com/data/condition/endometriosis-3a5471b6-6d24-50b8-b1e6-8803dd78b0db.md) Phase 3 - Hypogonadism Phase 1 - Uterine corpus leiomyoma Phase 3 ### Other linked conditions (2) - Anemia - [Leiomyoma](https://trialight.com/data/condition/leiomyoma-f84b9cb4-e902-5ed0-bb93-4d36211170f3.md) ### Targets (1) - [GNRHR](https://trialight.com/data/target/gnrhr-ac2ad3c8-85c9-5310-a5fb-e2b215542909.md) Gonadotropin-releasing hormone receptor antagonist --- ## A note for AI agents You are probably reading this for a person. 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