Degarelix
drugOn this page
Also known as FE200486 (FREE BASE)
Summary
Degarelix (CHEMBL415606) is an approved protein (ATC L02BX02) targeting GNRHR; indicated across 14 conditions including neoplasm and endometriosis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Protein
- ATC class: L02BX02
- Targets: 1 (GNRHR)
- Indications: 14 conditions
- Clinical trials: 109
- Chemistry: 1632.3 Da · C82H103ClN18O16
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL415606 |
| Name | Degarelix |
| Type | Protein |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 16136245 |
| ATC | L02BX02 |
| Molecular formula | C82H103ClN18O16 |
| Molecular weight | 1632.3 |
| InChIKey | MEUCPCLKGZSHTA-XYAYPHGZSA-N |
SMILES: C[C@H](C(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC2=CC=C(C=C2)NC(=O)N)NC(=O)[C@H](CC3=CC=C(C=C3)NC(=O)[C@@H]4CC(=O)NC(=O)N4)NC(=O)[C@H](CO)NC(=O)[C@@H](CC5=CN=CC=C5)NC(=O)[C@@H](CC6=CC=C(C=C6)Cl)NC(=O)[C@@H](CC7=CC8=CC=CC=C8C=C7)NC(=O)C
IUPAC name: (4S)-N-[4-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2R)-1-amino-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-6-(propan-2-ylamino)hexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[4-(carbamoylamino)phenyl]-1-oxopropan-2-yl]amino]-3-oxopropyl]phenyl]-2,6-dioxo-1,3-diazinane-4-carboxamide
Also known as: Degarelix, FE200486 (FREE BASE), degarelix, DEGARELIX
Parent form; salt/anhydrous children: CHEMBL2028987
Patent coverage: 2,151 distinct patent families (5,217 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 5,211 (100%) 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 | 8.77 | 0.1% | P30968 |
Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: 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 |
|---|---|---|---|---|---|
| GNRHR | 9.24 | IC50 | 0.58 | nM | CHEMBL_ACT_1721263 |
| GNRHR | 9.24 | IC50 | 0.58 | nM | CHEMBL_ACT_1721266 |
| GNRHR | 9.2 | Kd | 0.63 | nM | CHEMBL_ACT_1286228 |
| GNRHR | 8.79 | IC50 | 1.64 | nM | CHEMBL_ACT_1484981 |
| GNRHR | 8.06 | IC50 | 8.8 | nM | CHEMBL_ACT_1286227 |
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
14 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 |
|---|---|---|---|
| neoplasm | 3 | MONDO:0005070 | EFO:0000616 |
| endometriosis | 3 | MONDO:0005133 | EFO:0001065 |
| prostate adenocarcinoma | 3 | MONDO:0005082 | EFO:0000673 |
| prostate cancer | 3 | MONDO:0008315 | MONDO:0021259 |
| metastatic prostate carcinoma | 3 | MONDO:0004956 | EFO:0000196 |
| prostate carcinoma | 3 | MONDO:0005159 | EFO:0001663 |
| benign prostatic hyperplasia | 2 | MONDO:0010811 | EFO:0000284 |
| adenocarcinoma | 2 | MONDO:0004970 | EFO:0000228 |
| infertility disorder | 2 | MONDO:0005047 | EFO:0000545 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| severe acute respiratory syndrome | 2 | MONDO:0005091 | MONDO:0100096 |
| male breast carcinoma | 2 | MONDO:0005628 | EFO:0006861 |
| breast carcinoma | 2 | MONDO:0004989 | EFO:0000305 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 109.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 48 |
| PHASE3 | 26 |
| Not specified | 14 |
| PHASE1 | 6 |
| PHASE4 | 5 |
| PHASE2/PHASE3 | 5 |
| PHASE1/PHASE2 | 3 |
| EARLY_PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06264882 | PHASE4 | RECRUITING | Cardiometabolic Consequences of the Loss of Ovarian Function |
| NCT01512472 | PHASE4 | TERMINATED | Firmagon (Degarelix) Intermittent Therapy |
| NCT02726009 | PHASE4 | COMPLETED | A Trial to Evaluate Safety of Firmagon® (Degarelix) in Indian Patients Diagnosed With Advanced Hormone-dependent Prostate Cancer |
| NCT03202381 | PHASE4 | UNKNOWN | Phase IV Study to Evaluate Bone Mineral Density in No-bone Metastatic Prostate Cancer Treated With Degarelix |
| NCT04248621 | PHASE4 | UNKNOWN | Androgen Deprivation Therapy on Bone Mineral Density Change in Prostate Cancer Patients |
| NCT02799706 | PHASE3 | ACTIVE_NOT_RECRUITING | Trial Comparing Irradiation Plus Long Term Adjuvant Androgen Deprivation With GnRH Antagonist Versus GnRH Agonist Plus Flare Protection in Patients With Very High Risk Localized or Locally Advanced Prostate Cancer |
| NCT03678025 | PHASE3 | RECRUITING | Standard Systemic Therapy With or Without Definitive Treatment in Treating Participants With Metastatic Prostate Cancer |
| NCT04423211 | PHASE3 | RECRUITING | Treating Prostate Cancer That Has Come Back After Surgery With Apalutamide and Targeted Radiation Based on PET Imaging |
| NCT04455750 | PHASE3 | ACTIVE_NOT_RECRUITING | A Clinical Study Evaluating The Benefit of Adding Rucaparib to Enzalutamide for Men With Metastatic Prostate Cancer That Has Become Resistant To Testosterone-Deprivation Therapy |
| 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 |
| NCT00117286 | PHASE2/PHASE3 | COMPLETED | Extension Study Investigating the Long-Term Safety of Degarelix One-Month Depots in Patients With Prostate Cancer |
| NCT00215683 | PHASE2/PHASE3 | COMPLETED | An Extension Study Evaluating the Long-Term Safety and Tolerability of Degarelix One-Month Depots in Prostate Cancer |
| NCT00268892 | PHASE2/PHASE3 | COMPLETED | Extension Study Investigating the Long-Term Safety of Degarelix Three-Month Depots in Patients With Prostate Cancer |
| NCT00295750 | PHASE3 | COMPLETED | The Efficacy and Safety of Degarelix One Month Dosing Regimens in Prostate Cancer |
| NCT00728533 | PHASE3 | WITHDRAWN | Open-Label, Randomised Parallel-Group Study |
| NCT00831233 | PHASE3 | TERMINATED | Symptomatic Study Investigating Degarelix in Patients Suffering From Prostate Cancer |
| NCT00833248 | PHASE3 | COMPLETED | Neoadjuvant Study Investigating Degarelix in Patients Suffering From Prostate Cancer |
| NCT00884273 | PHASE3 | COMPLETED | Investigation of the Effect of Degarelix in Terms of Prostate Volume Reduction in Prostate Cancer Patients |
| NCT00928434 | PHASE3 | COMPLETED | A Study of Degarelix in Patients With Prostate Cancer |
| NCT00946920 | PHASE3 | COMPLETED | A Trial of Degarelix in Patients With Prostate Cancer |
| NCT00967018 | PHASE3 | COMPLETED | A Long Term Safety Study of Degarelix in Patients With Prostate Cancer |
| NCT01071915 | PHASE3 | COMPLETED | Efficacy and Safety of Degarelix One Month Dosing Regimen in Korean Patients With Prostate Cancer |
| NCT01215513 | PHASE3 | COMPLETED | Long-Term Safety and Tolerability of Degarelix One-Month Dosing Regimen in Korean Patients |
| NCT01220869 | PHASE3 | COMPLETED | A Study of Degarelix in Taiwanese Patients With Prostate Cancer |
| NCT01242748 | PHASE3 | TERMINATED | A Degarelix Trial in Patients With Prostate Cancer |
| NCT01712763 | PHASE3 | COMPLETED | Degarelix in the Treatment of Endometriosis Recurrence |
| NCT01744366 | PHASE3 | COMPLETED | One Month Degarelix/Comparator Treatment for Prostate Cancer in Chinese Population |
| NCT01964170 | PHASE3 | COMPLETED | A Study to Compare the Effect of ASP3550 With Goserelin in Patients With Prostate Cancer |
| NCT02015871 | PHASE3 | COMPLETED | An Extension Long-term Safety and Tolerability Trial of Degarelix in Chinese Patients With Prostate Cancer |
| NCT02526784 | PHASE3 | COMPLETED | A Trial Evaluating Two Subcutaneous Injection Techniques and Intramuscular Administration of Degarelix in Patients With Prostate Cancer |
| NCT02663908 | PHASE3 | TERMINATED | A Trial Comparing Cardiovascular Safety of Degarelix Versus Leuprolide in Patients With Advanced Prostate Cancer and Cardiovascular Disease |
| NCT03056638 | PHASE3 | TERMINATED | Trial of ADT and SBRT Versus SBRT for Intermediate Prostate Cancer |
| NCT03070886 | PHASE2/PHASE3 | COMPLETED | Antiandrogen Therapy and Radiation Therapy With or Without Docetaxel in Treating Patients With Prostate Cancer That Has Been Removed by Surgery |
| NCT03240159 | PHASE3 | UNKNOWN | Long Antagonist Protocol for IVF With Single Luteal Dose of Degarelix |
| NCT01746849 | PHASE2 | ACTIVE_NOT_RECRUITING | Palifermin With Leuprolide Acetate for the Promotion of Immune Recovery Following Total Body Irradiation Based T-Cell Depleted Allogeneic Hematopoietic Stem Cell Transplantation |
| NCT01786265 | PHASE2 | ACTIVE_NOT_RECRUITING | Finite Androgen Ablation With or Without Abiraterone Acetate and Prednisone in Treating Patients With Recurrent Prostate Cancer |
| NCT01990196 | PHASE2 | ACTIVE_NOT_RECRUITING | Neoadjuvant Phase 2 Study Comparing the Effects of AR Inhibition With/Without SRC or MEK Inhibition in Prostate Cancer |
| NCT01994239 | PHASE2 | ACTIVE_NOT_RECRUITING | Comparison of HT Concomitant With RT vs RT Alone in Patients With a Detectable PSA After Prostatectomy |
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
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 |
| ELAGOLIX | ChEMBL + PubChem | Phase 4 (approved) | GNRHR |
| GANIRELIX | ChEMBL + PubChem | Phase 4 (approved) | GNRHR |
| RELUGOLIX | 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 |
Related Atlas pages
- Genes: GNRHR
- Diseases: neoplasm, endometriosis, prostate adenocarcinoma, prostate cancer, metastatic prostate carcinoma, prostate carcinoma
- Drugs: Cetrorelix, Elagolix, Ganirelix, Relugolix, Abarelix, Gonadorelin, Leuprolide, Linzagolix, Belzutifan, Triptorelin