Buserelin

Summary

Buserelin (CHEMBL2110824) is an approved protein (ATC L02AE01) targeting GNRHR; indicated across 4 conditions including neoplasm and prostate adenocarcinoma.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: L02AE01
• Targets: 1 (GNRHR)
• Indications: 4 conditions
• Clinical trials: 11
• Chemistry: 1239.4 Da · C60H86N16O13

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2110824
Name	Buserelin
Type	Protein
Max phase	4
FDA approved	yes
PubChem CID	50225
ATC	L02AE01
Molecular formula	C60H86N16O13
Molecular weight	1239.4
InChIKey	CUWODFFVMXJOKD-UVLQAERKSA-N

SMILES: CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](COC(C)(C)C)NC(=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-[[(2R)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]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

Also known as: Buserelin, Buserelina, Busereline, buserelin, BUSERELIN

Parent form; salt/anhydrous children: CHEMBL2106198

Patent coverage: 8,636 distinct patent families (36,723 SureChEMBL compound mentions), from 6 matched compound structure(s). One matched structure accounts for 36,454 (99%) 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	Full agonist	10	0.1%	P30968

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

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

4 indications (1 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	4	MONDO:0005070	EFO:0000616
prostate adenocarcinoma	3	MONDO:0005082	EFO:0000673
infertility disorder	1	MONDO:0005047	EFO:0000545

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

Clinical trials

Total trials: 11.

Phase distribution

Phase	Trials
PHASE3	5
PHASE4	4
PHASE1/PHASE2	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00627406	PHASE4	COMPLETED	Triggering of Final Oocyte Maturation With GnRHa (Buserelin) in GnRH Antagonist Cycles
NCT00830492	PHASE4	COMPLETED	Clomiphene Citrate (CC)/Gonadotropin/Gonadotropin Releasing Hormone (GnRH) Antagonist Versus Gonadotropin/GnRH Agonist
NCT01213147	PHASE4	COMPLETED	Mild Stimulation Protocol Versus Microdose Gonadotropin-releasing Hormone Agonist Flare up Protocol in Poor Responders
NCT01816789	PHASE4	TERMINATED	Age Versus Ovarian Reserve Markers Based Therapy in IVF (IVF)/Intracytoplasmic Sperm Injection (ICSI) Cycles
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
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
NCT00002633	PHASE3	COMPLETED	Hormone Therapy With or Without Surgery or Radiation Therapy in Treating Patients With Prostate Cancer
NCT00003653	PHASE3	COMPLETED	Hormone Therapy in Treating Patients With Rising PSA Levels Following Radiation Therapy for Prostate Cancer
NCT00651326	PHASE3	TERMINATED	Androgen Suppression and Radiation With/Out Docetaxel in High-Risk Localized Prostate Cancer
NCT00823121	PHASE1/PHASE2	UNKNOWN	Replacement of Fresh Embryo Transfers (ETs) by Frozen Embryo Transfers (FETs) Using Vitrification
NCT00054106	PHASE1	COMPLETED	Hormone Therapy and OGX-011 Before Radical Prostatectomy in Treating Patients With Prostate Cancer

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.

14 molecules share ≥1 primary target. Top 14 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
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