Gonadorelin
drugOn this page
Also known as Fertiral lh-rhGonadorelin decapeptideGonadorelinaGonadorelineGonadotropin-releasing hormoneRelefact lh-rhGonadotropin-releasing hormone (GnRH)LHRHGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-GlySID124893762Gonadorelin (acetate)
Summary
Gonadorelin (CHEMBL1007) is an approved protein gonadotropin releasing hormone agonist (ATC H01CA01); indicated across 4 conditions including osteoporosis and breast neoplasm.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Protein
- ATC class: H01CA01 (+1 more)
- Indications: 4 conditions
- Clinical trials: 40
- Chemistry: 1182.3 Da · C55H75N17O13
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1007 |
| Name | Gonadorelin |
| Type | Protein |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 638793 |
| ChEBI | CHEBI:5520 |
| ATC | H01CA01, V04CM01 |
| Molecular formula | C55H75N17O13 |
| Molecular weight | 1182.3 |
| InChIKey | XLXSAKCOAKORKW-AQJXLSMYSA-N |
SMILES: CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)CNC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC3=CNC4=CC=CC=C43)NC(=O)[C@H](CC5=CN=CN5)NC(=O)[C@@H]6CCC(=O)N6
IUPAC name: (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
ChEBI definition: A ten-membered synthetic oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, glycyl, leucyl, arginyl, prolyl and glycinamide residues joined in sequence.
Pharmacological roles (ChEBI): gonadotropin releasing hormone agonist.
Also known as: Fertiral lh-rh, Gonadorelin, Gonadorelin decapeptide, Gonadorelina, Gonadoreline, Gonadotropin-releasing hormone, Relefact lh-rh, Gonadotropin-releasing hormone (GnRH), LHRH, Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly, SID124893762, GONADORELIN
Parent form; salt/anhydrous children: CHEMBL1200511, CHEMBL1200516
Patent coverage: 3,863 distinct patent families (8,578 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 8,245 (96%) 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
Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Gonadotropin-releasing hormone receptor, Lutropin-choriogonadotropic hormone receptor, Gonadotropin-releasing hormone receptor.
Bioactivity
ChEMBL activities: 5 potent at pChembl ≥ 5 of 5 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P16235 | 8.9 | Ki | 1.26 | nM | CHEMBL_ACT_784036 |
| P30969 | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_900132 |
| P30969 | 8.22 | IC50 | 6 | nM | CHEMBL_ACT_1106662 |
| P30969 | 8.15 | IC50 | 7 | nM | CHEMBL_ACT_1106663 |
| GNRHR | 8 | IC50 | 10 | nM | CHEMBL_ACT_1106661 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
4 indications (0 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 |
|---|---|---|---|
| osteoporosis | 3 | MONDO:0005298 | EFO:0003882 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| cocaine dependence | 1 | MONDO:0005186 | EFO:0002610 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 40.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 14 |
| PHASE2 | 14 |
| Not specified | 5 |
| PHASE1 | 3 |
| PHASE4 | 2 |
| PHASE2/PHASE3 | 1 |
| PHASE1/PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT02475057 | PHASE4 | COMPLETED | Endothelial Function in Prostate Cancer Patients on Degarelix vs. Luteinizing Hormone-Releasing Hormone Agonists |
| NCT03989024 | PHASE4 | UNKNOWN | Pulsatile Gonadotropin-releasing Hormone for Infertility in Non-obese Patients With Polycystic Ovary Syndrome |
| NCT00430183 | PHASE3 | ACTIVE_NOT_RECRUITING | Surgery With or Without Docetaxel and Leuprolide or Goserelin in Treating Patients With High-Risk Localized Prostate Cancer |
| NCT00567580 | PHASE3 | ACTIVE_NOT_RECRUITING | Prostate Radiation Therapy or Short-Term Androgen Deprivation Therapy and Pelvic Lymph Node Radiation Therapy With or Without Prostate Radiation Therapy in Treating Patients With a Rising Prostate Specific Antigen (PSA) After Surgery for Prostate Cancer |
| NCT04390646 | PHASE2/PHASE3 | RECRUITING | GnRH Therapy on Cognition in Down Syndrome |
| NCT04546009 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study Evaluating the Efficacy and Safety of Giredestrant Combined With Palbociclib Compared With Letrozole Combined With Palbociclib in Participants With Estrogen Receptor-Positive, HER2-Negative Locally Advanced or Metastatic Breast Cancer (persevERA Breast Cancer) |
| NCT04961996 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study Evaluating the Efficacy and Safety of Adjuvant Giredestrant Compared With Physician’s Choice of Adjuvant Endocrine Monotherapy in Participants With Estrogen Receptor-Positive, HER2-Negative Early Breast Cancer (lidERA Breast Cancer) |
| NCT05296798 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Evaluate the Efficacy and Safety of Giredestrant in Combination With Phesgo (Pertuzumab, Trastuzumab, and Hyaluronidase-zzxf) Versus Phesgo in Participants With Locally Advanced or Metastatic Breast Cancer (heredERA Breast Cancer) |
| NCT05306340 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study Evaluating the Efficacy and Safety of Giredestrant Plus Everolimus Compared With the Physician’s Choice of Endocrine Therapy Plus Everolimus in Participants With Estrogen Receptor-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer (evERA Breast Cancer) |
| NCT05891093 | PHASE3 | RECRUITING | Efficacy and Safety of Fluzoparib Combined With Adjuvant Endocrine Therapy for HR+/HER2- SNF3-subtype Early Breast Cancer (BCTOP-L-A01) |
| NCT06065748 | PHASE3 | RECRUITING | A Study to Evaluate Efficacy and Safety of Giredestrant Compared With Fulvestrant (Plus a CDK4/6 Inhibitor), in Participants With ER-Positive, HER2-Negative Advanced Breast Cancer Resistant to Adjuvant Endocrine Therapy (pionERA Breast Cancer) |
| NCT00005044 | PHASE3 | COMPLETED | Hormone Therapy and Radiation Therapy in Treating Patients With Prostate Cancer |
| NCT00288080 | PHASE3 | COMPLETED | Hormone Therapy and Radiation Therapy or Hormone Therapy and Radiation Therapy Followed by Docetaxel and Prednisone in Treating Patients With Localized Prostate Cancer |
| NCT00329797 | PHASE3 | COMPLETED | Zoledronate in Preventing Osteoporosis and Bone Fractures in Patients With Locally Advanced Nonmetastatic Prostate Cancer Undergoing Radiation Therapy and Hormone Therapy |
| NCT01278290 | PHASE3 | COMPLETED | Comparative Validation of the Triptorelin Test for the Diagnosis of CPP in Girls |
| NCT01976728 | PHASE3 | COMPLETED | LutrePulse Hypogonadotropic Hypogonadism |
| NCT03009981 | PHASE3 | COMPLETED | A Study of Androgen Annihilation in High-Risk Biochemically Relapsed Prostate Cancer |
| NCT00329043 | PHASE2 | ACTIVE_NOT_RECRUITING | Sunitinib Malate With Hormonal Ablation for Patients Who Will Have Prostatectomy |
| NCT03879577 | PHASE2 | ACTIVE_NOT_RECRUITING | Assessing the Response Rate of Neo-adjuvant Taxotere and Trastuzumab in Nigerian Women With Breast Cancer |
| NCT03944434 | PHASE2 | ACTIVE_NOT_RECRUITING | FACILE: FeAsibility of First-line RiboCIclib in OLdEr Patients with Advanced Breast Cancer |
| NCT04293393 | PHASE2 | ACTIVE_NOT_RECRUITING | Neoadjuvant Study Chemotherapy vs Letrozole + Abemaciclib in HR+/HER2- High/Intermediate Risk Breast Cancer Patients |
| NCT04576455 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study Evaluating the Efficacy and Safety of Giredestrant Compared With Physician’s Choice of Endocrine Monotherapy in Participants With Previously Treated Estrogen Receptor-Positive, HER2-Negative Locally Advanced or Metastatic Breast Cancer (acelERA Breast Cancer) |
| NCT05498272 | PHASE2 | RECRUITING | Study of Neoadjuvant PARP Inhibition Followed by Radical Prostatectomy in Patients With Unfavorable Intermediate-Risk or High-Risk Prostate Cancer With Select HRR Gene Alterations |
| NCT06001762 | PHASE2 | ACTIVE_NOT_RECRUITING | TRADE: Dose Escalation Tolerability of Abemaciclib in HR+ HER2- Early Stage Breast Cancer |
| NCT00006359 | PHASE2 | COMPLETED | Androgen Suppression Plus Radiation Therapy in Treating Patients With Prostate Cancer |
| NCT00528866 | PHASE2 | COMPLETED | Radiation Therapy, Androgen Suppression, and Docetaxel in Treating Patients With High-Risk Prostate Cancer Who Have Undergone Radical Prostatectomy |
| NCT00666666 | PHASE2 | COMPLETED | R-(-)-Gossypol and Androgen Ablation Therapy in Treating Patients With Newly Diagnosed Metastatic Prostate Cancer |
| NCT01674270 | PHASE2 | COMPLETED | Degarelix Neo-Adjuvant Radical Prostatectomy Trial |
| NCT01790126 | PHASE2 | COMPLETED | The Role of Highly Selective Androgen Receptor (AR) Targeted Therapy in Men With Biochemically Relapsed Hormone Sensitive Prostate Cancer |
| NCT01823835 | PHASE1/PHASE2 | TERMINATED | A Study of GDC-0810 Single Agent or in Combination With Palbociclib and/or a Luteinizing Hormone-Releasing Hormone (LHRH) Agonist in Women With Locally Advanced or Metastatic Estrogen Receptor Positive Breast Cancer |
| NCT03058939 | PHASE2 | WITHDRAWN | Assessing the Response Rate of Neo-adjuvant Paclitaxel (Taxol) in Nigerian Women With Breast Cancer |
| NCT03380806 | PHASE2 | UNKNOWN | Prostate Boost Irradiation With Stereotactic Body RT (SBRT) |
| NCT03142893 | PHASE1 | ACTIVE_NOT_RECRUITING | Hormonal Mechanisms of Sleep Restriction - Axis Study |
| NCT03332797 | PHASE1 | ACTIVE_NOT_RECRUITING | A Study of GDC-9545 Alone or in Combination With Palbociclib and/or Luteinizing Hormone-Releasing Hormone (LHRH) Agonist in Locally Advanced or Metastatic Estrogen Receptor-Positive Breast Cancer |
| NCT00000325 | PHASE1 | COMPLETED | Psychostimulant Abuse - Novel Treatment Approaches - 1 |
| NCT01381016 | Not specified | COMPLETED | Estrogen Sensitivity and Ovulatory Dysfunction in Obesity |
| NCT02588404 | Not specified | WITHDRAWN | The Predictive Value of TMPRSS2-ERG Fusion in High Risk Prostate Cancer Patient |
| NCT02705014 | Not specified | UNKNOWN | Efficacy of Pulsatile GnRH Therapy on Male Patients With Pituitary Stalk Interruption Syndrome |
| NCT03017313 | Not specified | COMPLETED | To Evaluate the Criteria for Renewal of Luteinizing Hormone-Releasing Hormone (LHRH) Analogue Treatment in Prostate Cancer Patients |
| NCT05184374 | Not specified | UNKNOWN | Efficacy of Prolonged GnRH Test in Male Adolescents With Postoperative HH |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Diseases: osteoporosis