OncoSignal
Live from Open Targets Platform, fetched 2026-11-12 09:27 UTC. Every row links to its source record.

GNRHR gonadotropin releasing hormone receptor

ENSG00000109163 · protein coding · Open Targets profile

Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G- proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling.

25 of the 32 drugs recorded against GNRHR are approved, and 2 more reached Phase 3

Each band is a group of drugs. It runs from the kind of drug on the left to the furthest stage that drug has reached in any disease on the right. Thicker bands mean more drugs.

21 protein drugs at Approved: HISTRELIN, TRIPTORELIN PAMOATE, HISTRELIN ACETATE, GOSERELIN ACETATE, NAFARELIN ACETATE, ABARELIX, LEUPROLIDE MESYLATE, DEGARELIX ACETATE, GONADORELIN, BUSERELIN, DEGARELIX, GOSERELIN…1 protein drug at Phase 3: ZOPTARELIN DOXORUBICIN3 protein drugs at Phase 2: ACYLINE, OZARELIX, ONVITRELIN UCALONTIDE4 small molecule drugs at Approved: LINZAGOLIX CHOLINE, ELAGOLIX SODIUM, RELUGOLIX, ELAGOLIX1 small molecule drug at Phase 3: LINZAGOLIX2 small molecule drugs at Phase 2: SUFUGOLIX, OPIGOLIXProtein 25Small molecule 7Approved 25Phase 3 2Phase 2 5

Approved bands are highlighted. Withdrawn means the drug was pulled from the market or from development. A combined phase counts as the later one (Phase 1/2 is shown as Phase 2). Hover a band for the drug names. Source: Open Targets Platform, fetched live.

GNRHR: inherited and tumour-mutation evidence across 15 cancers

Each row is a cancer, strongest overall evidence first. The two dots show how strong the inherited (germline) and tumour-mutation (somatic) evidence is; the line between them is the gap.

Inherited (germline) variantsMutations in tumours (somatic)
00.250.50.751prostate cancerprostate cancerprostate carcinomaprostate carcinomabreast cancerbreast canceruterine corpus leiomyomauterine corpus leiomyomaprostate neoplasmprostate neoplasmleiomyomaleiomyomabreast carcinomabreast carcinomaprostate adenocarcinomaprostate adenocarcinomaendometrial cancerendometrial cancerbenign prostatic hyperplasiabenign prostatic hyperplasiaatypical endometrial hyperplasiaatypical endometrial hyperplasiaendometrial carcinomaendometrial carcinomaadenomyomaadenomyomatriple-negative breast carcinomatriple-negative breast carcinomaovarian cancerovarian cancer

Scores run from 0 (no evidence) to 1 (strongest). A missing dot at 0 means Open Targets holds no evidence of that kind. Source: Open Targets Platform, fetched live.

Tractability

Small molecule
Approved Drug, Structure with Ligand, High-Quality Ligand, Druggable Family
Antibody
GO CC high conf, UniProt loc med conf, UniProt SigP or TMHMM
PROTAC
Small Molecule Binder
Other modalities
Approved Drug

gnomAD loss of function constraint: o/e 0.49838000535964966 (upper bound 0.7791299819946289). Low values mean loss of function is poorly tolerated, a safety flag for inhibition.

Who runs trials of these drugs

Principal investigators and study chairs on 400 registry trials, updated in the last three years, of the most advanced drugs against GNRHR (linzagolix choline, histrelin, triptorelin pamoate, elagolix, goserelin, nafarelin, abarelix, leuprolide, degarelix, gonadorelin, relugolix, buserelin), ranked by Phase 2+ trials. Live from ClinicalTrials.gov.

156 of 386 trials of drugs against GNRHR have sites only in United States

Registry trials of linzagolix choline, histrelin, triptorelin pamoate, elagolix, goserelin, nafarelin, abarelix, leuprolide, degarelix, gonadorelin, relugolix, buserelin updated in the last three years, counted by the country group of their listed sites. A trial with sites in several groups counts in each; 304 of 386 have all sites in one country.

Sites only in this groupSites here and elsewhere
United StatesUnited States: 156 trials with sites only hereUnited States: 66 trials with sites here and elsewhere222ChinaChina: 50 trials with sites only hereChina: 22 trials with sites here and elsewhere72EuropeEurope: 66 trials with sites only hereEurope: 46 trials with sites here and elsewhere112JapanJapan: 7 trials with sites only hereJapan: 18 trials with sites here and elsewhere25OtherOther: 38 trials with sites only hereOther: 63 trials with sites here and elsewhere101

Site counts are not patients per country, and trials registered only outside ClinicalTrials.gov are not covered. Where sites are is a fact about the record, not a judgement of its quality. Europe is the EU and EEA, the UK and Switzerland. 14 trials list no sites and are left out. Source: ClinicalTrials.gov, fetched live.

172 trials of drugs against GNRHR were stopped early; 22 give no reason

Terminated, withdrawn and suspended interventional trials of linzagolix choline, histrelin, triptorelin pamoate, elagolix, goserelin, nafarelin, abarelix, leuprolide, degarelix, gonadorelin, relugolix, buserelin, newest update first, live from ClinicalTrials.gov. Each reason is quoted exactly as the registry gives it; we do not sort reasons into safety, efficacy or business. Dates are the last registry update. Showing the 25 most recent of 172.

  • terminated · 2026-10-28 · Institut National de la Santé Et de la Recherche Médicale, France · matched by the registry's drug synonyms
    “This decision is based on the stop-rule established in Amendment N°.2 to the protocol, which called for halting the study if the number of participants enrolled was less than 12 by March 31, 2009 : 6 out of 48 participants were enrolled”
  • terminated · 2026-10-15 · Spanish Breast Cancer Research Group · matched by the registry's drug synonyms
    “Study prematurely terminated due to recruitment challenges, low incidence of the target population, evolving treatment landscape, ethical considerations, and inability to ensure funding through study completion.”
  • terminated · 2026-10-15 · Praful Ravi, MB BCHir, MRCP · GNRH-A Leuprolide Acetate, GNRH-A Goserelin, Degarelix
    “The trial was intended to be Phase 1/2 but did not move forward to Phase 2 since the company providing drug and funding (Lilly) withdrew support for the trial based on data relating to abemaciclib in advanced prostate cancer.”
  • terminated · 2026-10-14 · UNICANCER · matched by the registry's drug synonyms
    “poor accrual”
  • withdrawn · 2026-10-01 · British Columbia Cancer Agency · Degarelix
    “Site did not proceed with this study”
  • terminated · 2026-09-28 · Merck Sharp & Dohme LLC · matched by the registry's drug synonyms
    “The study stopped due to futility”
  • terminated · 2026-09-02 · University of Colorado, Denver · matched by the registry's drug synonyms
    “Study completed”
  • terminated · 2026-06-26 · National Cancer Institute (NCI) · matched by the registry's drug synonyms
    “Slow/insufficient accrual”
  • terminated · 2026-06-26 · Eli Lilly and Company · matched by the registry's drug synonyms
    “The study was terminated early as related study I3Y-MC-JPCM (NCT03706365) did not meet its primary endpoint.”
  • terminated · 2026-06-25 · SOLTI Breast Cancer Research Group · matched by the registry's drug synonyms
    “The study was prematurely halted because enrollment was significantly delayed compared with the original projections due to the evolving therapeutic landscape.”
  • withdrawn · 2026-06-05 · University of Chicago · matched by the registry's drug synonyms
    “Data not collected and analyzed; withdrawn due to lack of bandwidth.”
  • terminated · 2026-05-14 · EQRx, Inc. · matched by the registry's drug synonyms
    “The study is being closed based on corporate changes at EQRx and is not related to any efficacy or safety issues with lerociclib.”
  • terminated · 2026-04-03 · Jiangsu HengRui Medicine Co., Ltd. · matched by the registry's drug synonyms
    “Due to the adjustment of the sponsor's development plan, after discussion with leading PI, sponsor has decided to terminate this study.”
  • terminated · 2026-04-03 · Amy DiVasta, MD · matched by the registry's drug synonyms
    “Funding was terminated.”
  • terminated · 2026-04-02 · Brown University · Degarelix
    “Principal Investigator left institution”
  • terminated · 2026-03-30 · Ferring Pharmaceuticals · matched by the registry's drug synonyms
    “This is a company decision made not related to safety concerns. Rather, it reflects a broader portfolio assessment and the desire to focus on programs that can bring timely and meaningful benefit to patients.”
  • terminated · 2026-03-30 · Ferring Pharmaceuticals · matched by the registry's drug synonyms
    “This is a company decision made not related to safety concerns. Rather, it reflects a broader portfolio assessment and the desire to focus on programs that can bring timely and meaningful benefit to patients.”
  • terminated · 2026-03-06 · Stephanie B. Seminara, MD · matched by the registry's drug synonyms
    “The study team no longer has access to GnRH. The study has been altered to account for this change and is no longer a clinical trial.”
  • terminated · 2026-01-29 · Loyola University · matched by the registry's drug synonyms
    “The study was stopped for feasibility”
  • withdrawn · 2025-11-14 · Ferring Pharmaceuticals · matched by the registry's drug synonyms
    “The decision to terminate development activities was based on business needs and unrelated to any safety or efficacy concerns.”
  • terminated · 2025-11-14 · Pfizer · matched by the registry's drug synonyms
    “Per business decision, but not due to safety concerns or regulatory request.”
  • withdrawn · 2025-10-22 · Northwestern University · matched by the registry's drug synonyms
    “PI left institution”
  • withdrawn · 2025-09-23 · OHSU Knight Cancer Institute · matched by the registry's drug synonyms
    “Loss of funding”
  • terminated · 2025-09-11 · Sanofi · Goserelin
    “The study was terminated based on the review by an independent data monitoring committee of the prespecified interim analysis of the Phase 3 AMEERA-5 efficacy data. No new safety signals were observed.”
  • withdrawn · 2025-08-28 · Endeavor Health · Relugolix (40 mg) /estradiol (1 mg)/norethisterone acetate (0.5 mg) oral tablet
    “Could not obtain approval for the planned study with available funding”
Paediatric incentives and obligations for GNRHR's drugs

For linzagolix choline, histrelin, triptorelin pamoate, elagolix, goserelin, nafarelin, abarelix, leuprolide, degarelix, gonadorelin, relugolix, buserelin: what EMA and FDA publish about paediatric plans, orphan status and pediatric approvals, and how many registered studies take children. Each line is a yes, no or not published fact from the record linked under it; none of it is a forecast.

  • EU paediatric investigation plan: yes · EMEA-002428-PIP02-18 (relugolix;estradiol;norethisterone acetate, Treatment of endometriosis): RP: decision refers to a refusal on a proposed Paediatric Investigation Plan, 16 Aug 2019; EMEA-002428-PIP01-18 (relugolix;estradiol;norethisterone acetate, Treatment of leiomyoma of uterus): W: decision granting a waiver in all age groups for all conditions or indications, 22 Mar 2019; EMEA-001323-PIP02-12 (Elagolix, Treatment of endometriosis): W: decision granting a waiver in all age groups for all conditions or indications, 18 Dec 2012; EMEA-001323-PIP01-12 (Elagolix, Treatment of uterine leiomyoma): W: decision granting a waiver in all age groups for all conditions or indications, 18 Dec 2012
    Rule: An EMA PIP decision (agreement, modification or waiver) lists the drug as its active substance, exact name. Source: EMA data download (dated snapshot), 2026-11-11
  • EU orphan designation: yes · EU/3/10/771 withdrawn 20 Sept 2010: Treatment of low-flow priapism
    Rule: An EU orphan designation lists the drug as its active substance (exact name) or belongs to a medicine that does; withdrawn and expired designations are listed with their status. Source: EMA EU/3/10/771, 2026-11-11
  • Authorised in the EU: yes · Degarelix Accord: authorised since 29 Sept 2023; Firmagon: authorised since 17 Feb 2009; Orgovyx: authorised since 29 Apr 2022; Ryeqo: authorised since 16 Jul 2021; +1 more
    Rule: An EMA medicine record lists the drug as its active substance or INN, exact name; national-only authorisations are not in this file. Source: EMA data download (dated snapshot), 2026-11-11
  • FDA orphan designation: not published · FDA's orphan designation database turns away automated requests, so this app does not read it; search it by hand at the link
    Rule: Would be: an FDA orphan designation names the drug. Source: FDA orphan designations search
  • FDA pediatric oncology approval: no · FDA's table lists no pediatric approval of linzagolix choline, histrelin, triptorelin pamoate, elagolix, goserelin, nafarelin, abarelix, leuprolide, degarelix, gonadorelin, relugolix, buserelin
    Rule: FDA's Pediatric Oncology Drug Approvals table names the drug. Source: FDA Pediatric Oncology Drug Approvals (content current as of 2026-03-03), 2026-11-12
  • Registered studies open to children: yes · 143 interventional studies of linzagolix choline, histrelin, triptorelin pamoate, elagolix, goserelin, nafarelin, abarelix, leuprolide, degarelix, gonadorelin, relugolix, buserelin include patients under 18; 15 are recruiting, not yet recruiting or active
    Rule: The registry's age group includes Child (birth to 17 years), which also counts studies that set no minimum age. Source: ClinicalTrials.gov search, 2026-11-12

Rare pediatric disease voucher. FDA, content current as of 29 Apr 2026: “As of February 3, 2026, enactment of the Consolidated Appropriations Act, 2026, the rare pediatric disease PRV program will sunset after September 30, 2029. FDA may not award any PRVs under this program after September 30, 2029.” Voucher sale prices are not shown here; they appear only as company-reported news. FDA: Rare Pediatric Disease Designation and Priority Review Voucher Programs

All 32 drugs and clinical candidates as a table

Each drug, stage and indication links to its Open Targets record, where the trials and approvals behind it are listed. Salt forms (for example a mesylate) are listed as Open Targets records them, as separate entries.

DrugTypeHighest stageIndicationsSource records
LINZAGOLIX CHOLINESmall moleculeapprovalleiomyoma, uterine corpus leiomyoma, endometriosisOpen Targets · ChEMBL
HISTRELINProteinapprovalcentral precocious puberty, endometriosis, polycystic ovary syndrome, neoplasm, prostate cancer, cancerOpen Targets · ChEMBL
TRIPTORELIN PAMOATEProteinapprovalprostate carcinoma, precocious puberty, prostate cancer, infertility disorder, endometriosis, Infertility, central precocious puberty, breast cancer, +1 moreOpen Targets · ChEMBL
HISTRELIN ACETATEProteinapprovalprostate cancerOpen Targets · ChEMBL
ELAGOLIX SODIUMSmall moleculeapprovalendometriosisOpen Targets · ChEMBL
GOSERELIN ACETATEProteinapprovalbreast carcinoma, carcinoma, breast cancer, prostate cancer, prostate adenocarcinoma, prostate carcinoma, estrogen-receptor positive breast cancer, salivary gland carcinoma, +5 moreOpen Targets · ChEMBL
NAFARELIN ACETATEProteinapprovalendometriosis, InfertilityOpen Targets · ChEMBL
ABARELIXProteinapprovalprostate cancer, neoplasmOpen Targets · ChEMBL
LEUPROLIDE MESYLATEProteinapprovalprostate cancer, prostate carcinoma, central precocious pubertyOpen Targets · ChEMBL
DEGARELIX ACETATEProteinapprovalprostate cancer, prostate carcinomaOpen Targets · ChEMBL
GONADORELINProteinphase 4endometriosis, infertility disorder, breast cancer, pregnancy, Infertility, adenomyosis, polycystic ovary syndrome, menopause, +30 moreOpen Targets · ChEMBL
RELUGOLIXSmall moleculephase 4uterine corpus leiomyoma, prostate cancer, anemia, Abdominal pain, Menorrhagia, leiomyoma, prostate neoplasm, neoplasm, +5 moreOpen Targets · ChEMBL
BUSERELINProteinphase 4neoplasm, prostate adenocarcinoma, prostate cancer, InfertilityOpen Targets · ChEMBL
DEGARELIXProteinphase 4prostate cancer, prostate neoplasm, neoplasm, lower urinary tract symptom, endometriosis, Infertility, cancer, benign prostatic hyperplasia, +10 moreOpen Targets · ChEMBL
GOSERELINProteinphase 4breast cancer, neoplasm, prostate adenocarcinoma, prostate cancer, lower urinary tract symptom, uterine corpus leiomyoma, adenomyoma, adenomyosis, +15 moreOpen Targets · ChEMBL
CETRORELIXProteinphase 4ovulation, benign prostatic hyperplasia, ovarian hyperstimulation syndrome, polycystic ovary syndrome, Infertility, endometriosis, rheumatoid arthritis, heart disorder, +5 moreOpen Targets · ChEMBL
GONADORELIN ACETATEProteinphase 4female infertility, endometriosis, Infertility, infertility disorder, breast cancer, pregnancy, Primary amenorrhea, prostate cancer, +35 moreOpen Targets · ChEMBL
ELAGOLIXSmall moleculephase 4uterine corpus leiomyoma, hemorrhage, endometriosis, Infertility, Dysmenorrhea, polycystic ovary syndrome, ovarian reserve, ovulationOpen Targets · ChEMBL
GANIRELIXProteinphase 4female infertility, Infertility, precocious puberty, Delayed puberty, polycystic ovary syndrome, pregnancyOpen Targets · ChEMBL
GANIRELIX ACETATEProteinphase 4Infertility, infertility disorder, postural orthostatic tachycardia syndrome due to NET deficiency, heart disorder, hypertensive disorder, cardiovascular disorder, arterial stiffness measurementOpen Targets · ChEMBL
LEUPROLIDEProteinphase 4prostate cancer, prostate neoplasm, neoplasm, breast cancer, prostate adenocarcinoma, Short stature, prostate carcinoma, uterine corpus leiomyoma, +25 moreOpen Targets · ChEMBL
CETRORELIX ACETATEProteinphase 4polycystic ovary syndrome, Infertility, heart disorder, hypertensive disorder, cardiovascular disorder, ovarian hyperstimulation syndromeOpen Targets · ChEMBL
LEUPROLIDE ACETATEProteinphase 4prostate cancer, precocious puberty, prostate carcinoma, breast cancer, Alzheimer disease, prostate adenocarcinoma, central precocious puberty, uterine corpus leiomyoma, +26 moreOpen Targets · ChEMBL
TRIPTORELINProteinphase 4neoplasm, prostate cancer, breast cancer, precocious puberty, Infertility, central precocious puberty, endometriosis, infertility disorder, +10 moreOpen Targets · ChEMBL
NAFARELINProteinphase 4endometriosis, Infertility, pregnancyOpen Targets · ChEMBL
LINZAGOLIXSmall moleculephase 3uterine corpus leiomyoma, Menorrhagia, Pain, endometriosisOpen Targets · ChEMBL
ZOPTARELIN DOXORUBICINProteinphase 3endometrial cancer, ovarian cancer, breast cancer, urothelial carcinoma, prostate cancerOpen Targets · ChEMBL
ACYLINEProteinphase 2prostate cancer, cardiovascular disorder, Azoospermia, hypogonadismOpen Targets · ChEMBL
SUFUGOLIXSmall moleculephase 2uterine corpus leiomyomaOpen Targets · ChEMBL
OPIGOLIXSmall moleculephase 2endometriosis, rheumatoid arthritisOpen Targets · ChEMBL
OZARELIXProteinphase 2prostate disorder, prostatitis, lower urinary tract symptom, benign prostatic hyperplasia, prostate cancerOpen Targets · ChEMBL
ONVITRELIN UCALONTIDEProteinphase 2ovarian cancer, neoplasmOpen Targets · ChEMBL