Relugolix
Highest phase reached
Approved
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Relugolix
- Molecular weight
- 623.64
- Structure (SMILES)
- CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nn2)c(=O)n3Cc2c(F)cccc2F)cc1
- orgovyx
- Orgovyx
- relugolix component of myfembree
- Relugolix component of myfembree
- 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
- CAS registry numbers
- 737789-87-6
- ChEMBL ID
- CHEMBL1800159
- InChIKey
- AOMXMOCNKJTRQP-UHFFFAOYSA-N
- PubChem compound IDs
- 10348973
- RxNorm IDs (RxCUI)
- 2472778
- FDA ingredient codes (UNII)
- P76B05O5V6
- L02BX
- L02BX04
Sources for recorded values
- Applicant
- SUMITOMO PHARMA AM
- Approval date
- 18 Dec 2020
- Application number
- NDA214621
- 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
- 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 name
- relugolix
- Type
- Synthetic organic
- Drug name stem
- -golix
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- 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
- 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
- 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
- Event
- hot flush
- Reports
- 7
- Reporting signal score
- 19.0229
- Event
- menstrual disorder
- Reports
- 2
- Reporting signal score
- 7.2197
- NCT01452659
- NCT02655224
- NCT02655237
- NCT01452685
- NCT01458301
- NCT03654274
- NCT03931915
- NCT02083185
- NCT02135445
- NCT02141659
- NCT03085095
- NCT05605964
- NCT05679388
- NCT06111313
- NCT06111781
- NCT06129851
- NCT06130995
- NCT06463457
- NCT03204318
- NCT06279195
- NCT04423211
- NCT04523207
- NCT05050084
- NCT05053152
- NCT05765500
And 3 more, listed on the interactive page.
- Dose
- 120mg
- Route
- Oral
- How often
- Once daily
- Swallow tablets whole, do not crush or chew
- Take with or without food
- 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
- 72974-120
- 72974-415
- Recorded assays
- 107
- Active assays
- 22
- Confirmatory
- Other
- Androgen Antagonists
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
- 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)
In development for (3)
- Endometriosis Phase 3
- Hypogonadism Phase 1
- Uterine corpus leiomyoma Phase 3
Other linked conditions (2)
- Anemia
- Leiomyoma
Targets (1)
- GNRHR Gonadotropin-releasing hormone receptor antagonist