Relugolix

Summary

Relugolix (CHEMBL1800159) is an approved small molecule (ATC L02BX04) targeting GNRHR; indicated across 8 conditions including prostate cancer and prostate adenocarcinoma.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L02BX04
• Targets: 1 (GNRHR)
• Indications: 8 conditions
• Clinical trials: 52
• Chemistry: 623.6 Da · C29H27F2N7O5S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1800159
Name	Relugolix
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	10348973
ATC	L02BX04
Molecular formula	C29H27F2N7O5S
Molecular weight	623.6
InChIKey	AOMXMOCNKJTRQP-UHFFFAOYSA-N

SMILES: CN(C)CC1=C(SC2=C1C(=O)N(C(=O)N2CC3=C(C=CC=C3F)F)C4=NN=C(C=C4)OC)C5=CC=C(C=C5)NC(=O)NOC

IUPAC name: 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea

Also known as: Orgovyx, Relugolix, Relugolix component of myfembree, Tak-385, TAK-385, RELUGOLIX, Relugolix; Orgovyx

Patent coverage: 414 distinct patent families (984 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 919 (93%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
GNRHR	GnRH1 receptor	Antagonist	9.48	0.1%	P30968

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Gonadotropin-releasing hormone receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Gonadotropin-releasing hormone receptor.

Bioactivity

ChEMBL activities: 12 potent at pChembl ≥ 5 of 12 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
GNRHR	10.1	IC50	0.08	nM	CHEMBL_ACT_6284340
GNRHR	9.6	IC50	0.25	nM	CHEMBL_ACT_25555595
P30969	9.49	IC50	0.32	nM	CHEMBL_ACT_6284369
P30969	9.49	IC50	0.32	nM	CHEMBL_ACT_6284389
GNRHR	9.48	IC50	0.33	nM	CHEMBL_ACT_6284268
GNRHR	9.48	IC50	0.33	nM	CHEMBL_ACT_6284298
GNRHR	9.43	Kd	0.37	nM	CHEMBL_ACT_22430573
GNRHR	9.09	IC50	0.82	nM	CHEMBL_ACT_6284250
GNRHR	9.08	Kd	0.84	nM	CHEMBL_ACT_22430577
GNRHR	8.39	IC50	4.05	nM	CHEMBL_ACT_25555571
GNRHR	7.75	IC50	18	nM	CHEMBL_ACT_6284386
KCNH2	5.38	IC50	4140	nM	CHEMBL_ACT_25555618

Target pathways

Aggregated over 1 target gene(s): GNRHR.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Hormone ligand-binding receptors	1	GNRHR
G alpha (q) signalling events	1	GNRHR

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	1
gonadotropin secretion	1
cellular response to hormone stimulus	1
signal transduction	1
cellular response to gonadotropin-releasing hormone	1

Indications & clinical

Indications

8 indications (4 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
prostate cancer	4	MONDO:0008315	MONDO:0008315
prostate adenocarcinoma	4	MONDO:0005082	EFO:0000673
metastatic prostate carcinoma	4	MONDO:0004956	EFO:0000196
neoplasm	4	MONDO:0005070	EFO:0000616
endometriosis	3	MONDO:0005133	EFO:0001065
uterine corpus leiomyoma	3	MONDO:0007886	EFO:0000731
hypogonadism	1	MONDO:0002146	MONDO:0002146

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 52.

Phase distribution

Phase	Trials
PHASE2	18
PHASE3	17
PHASE1	11
Not specified	4
PHASE2/PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04423211	PHASE3	RECRUITING	Treating Prostate Cancer That Has Come Back After Surgery With Apalutamide and Targeted Radiation Based on PET Imaging
NCT04513717	PHASE3	ACTIVE_NOT_RECRUITING	Two Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a High Gene Risk Score, The PREDICT-RT Trial
NCT04787744	PHASE2/PHASE3	RECRUITING	Veterans Affairs Seamless Phase II/III Randomized Trial of STAndard Systemic theRapy With or Without PET-directed Local Therapy for Oligometastatic pRosTate Cancer
NCT05050084	PHASE3	ACTIVE_NOT_RECRUITING	Two Studies for Patients With Unfavorable Intermediate Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a Higher Gene Risk Score, The Guidance Trial
NCT06650579	PHASE3	RECRUITING	REVELUTION-2: Relugolix+Abiraterone Acetate (AA) Versus Leuprolide+AA Cardiac Trial
NCT06671548	PHASE3	RECRUITING	Efficacy & Safety Study of Relugolix in Women With Heavy Menstrual Bleeding Associated With Uterine Fibroids
NCT02655224	PHASE3	COMPLETED	A Placebo-Controlled, Phase 3 Study of Relugolix (TAK-385) 40 mg in the Treatment of Pain Symptoms Associated With Uterine Fibroids
NCT02655237	PHASE3	COMPLETED	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
NCT03049735	PHASE3	COMPLETED	LIBERTY 1: Efficacy & Safety Study of Relugolix in Women With Heavy Menstrual Bleeding Associated With Uterine Fibroids
NCT03085095	PHASE3	COMPLETED	A Study to Evaluate the Safety and Efficacy of Relugolix in Men With Advanced Prostate Cancer
NCT03103087	PHASE3	COMPLETED	LIBERTY 2: Efficacy & Safety Study of Relugolix in Women With Heavy Menstrual Bleeding Associated With Uterine Fibroids
NCT03204318	PHASE3	COMPLETED	SPIRIT 1: Efficacy and Safety Study of Relugolix in Women With Endometriosis-Associated Pain
NCT03204331	PHASE3	COMPLETED	SPIRIT 2: Efficacy and Safety Study of Relugolix in Women With Endometriosis-Associated Pain
NCT03412890	PHASE3	COMPLETED	LIBERTY EXTENSION: Efficacy and Safety Extension Study of Relugolix in Women With Heavy Menstrual Bleeding Associated With Uterine Fibroids
NCT03654274	PHASE3	COMPLETED	SPIRIT EXTENSION: Efficacy and Safety Extension Study of Relugolix in Women With Endometriosis-Associated Pain
NCT03751124	PHASE3	COMPLETED	Study of Relugolix With Estradiol and Norethindrone Acetate in Women With Heavy Menstrual Bleeding Associated With Uterine Fibroids
NCT03931915	PHASE3	COMPLETED	Clinical Study to Evaluate Efficacy and Safety of TAK-385 40 mg Compared With Leuprorelin in Patients With Endometriosis
NCT05605964	PHASE3	COMPLETED	Randomized Study to Evaluate MACE in Patients With Prostate Cancer Treated With Relugolix or Leuprolide Acetate
NCT05053152	PHASE2	ACTIVE_NOT_RECRUITING	Testing the Addition of the Drug Relugolix to the Usual Radiation Therapy for Advanced-Stage Prostate Cancer, The NRG Promethean Study
NCT05320406	PHASE2	ACTIVE_NOT_RECRUITING	RElugolix VErsus LeUprolide Cardiac Trial
NCT05765500	PHASE2	RECRUITING	RecoverPC: Relugolix vs GnRH Agonist in Quality of Life
NCT06129851	PHASE2	NOT_YET_RECRUITING	Relugolix in Combination With Radiation Therapy for Treating Patients With High Risk Prostate Cancer
NCT06330805	PHASE2	RECRUITING	Effects of Relugolix vs Leuprolide on Cardiac Function in Patients With Prostate Cancer
NCT06378866	PHASE2	RECRUITING	Stereotactic Body Radiation Therapy Plus Immediate or Delayed Androgen Receptor Pathway Inhibitor and Androgen Deprivation Therapy or Salvage Radiation Therapy for the Treatment of Prostate Cancer, DIVINE Trial
NCT06463457	PHASE2	ACTIVE_NOT_RECRUITING	Comeback From Long coursE Androgen Deprivation Therapy (ADT) With RElugolix and Darolutamide (CLEARED)
NCT06499870	PHASE2	RECRUITING	Relugolix and Enzalutamide in Combination With Radiation Therapy for the Treatment of Very High Risk Prostate Cancer, OPTIMAL Trial
NCT07025369	PHASE2	RECRUITING	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
NCT07216248	PHASE2	RECRUITING	Optimal PSA Triggered Individual Management of Androgen Sensitive Prostate Cancer
NCT07455903	PHASE2	RECRUITING	Assessing Efficacy of Neoadjuvant ADT in Localized High-Risk Prostate Cancer Patients Utilizing 18F-Flotufolastat PSMA PET/CT
NCT01452659	PHASE2	COMPLETED	Efficacy and Safety of TAK-385 in the Treatment of Uterine Fibroids
NCT01452685	PHASE2	COMPLETED	A Long-term Extension Study of TAK-385 in the Treatment of Endometriosis
NCT01458301	PHASE2	COMPLETED	Efficacy and Safety of TAK-385 in the Treatment of Endometriosis
NCT02083185	PHASE2	COMPLETED	A Phase 2 Study to Evaluate the Safety and Efficacy of TAK-385, Together With a Leuprorelin Observational Cohort, in Participants With Prostate Cancer
NCT02135445	PHASE2	COMPLETED	Safety and Efficacy of TAK-385 for Patients With Localized Prostate Cancer
NCT04523207	PHASE2	COMPLETED	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
NCT06279195	PHASE2	WITHDRAWN	Phenotyping of Idiopathic Pelvic Pain With Real-time Uterine Imaging and Relugolix-Combination Therapy Treatment
NCT06130995	PHASE1	RECRUITING	Relugolix + Enzalutamide Study in High-Risk Prostate Cancer
NCT06631521	PHASE1	RECRUITING	Neoadjuvant Darolutamide and Relugolix Combination Preceding Radical Prostatectomy for Prostate Cancer
NCT02093390	PHASE1	COMPLETED	A Phase 1 Study to Evaluate the Effects of Fluconazole and Atorvastatin on the Pharmacokinetics of TAK-385 in Healthy Subjects
NCT02141659	PHASE1	COMPLETED	A Study of TAK-385 in Hormone Treatment-naïve Participants With Prostate Cancer

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

13 molecules share ≥1 primary target. Top 13 by shared-target count:

Molecule	Source	Status	Shared targets
CETRORELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
DEGARELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
ELAGOLIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
GANIRELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
ABARELIX	ChEMBL	Phase 4 (approved)	GNRHR
GONADORELIN	ChEMBL	Phase 4 (approved)	GNRHR
LEUPROLIDE	ChEMBL	Phase 4 (approved)	GNRHR
LINZAGOLIX	ChEMBL	Phase 4 (approved)	GNRHR
ACYLINE	ChEMBL	Phase 2	GNRHR
SUFUGOLIX	ChEMBL	Phase 2	GNRHR
Belzutifan	PubChem	Approved	GNRHR
Deslorelin	PubChem	Approved	GNRHR
Triptorelin	PubChem	Approved	GNRHR