Abarelix

Summary

Abarelix (CHEMBL1252) is an approved protein hormone antagonist (ATC L02BX01) targeting GNRHR; indicated across 2 conditions including neoplasm.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: L02BX01
• Targets: 1 (GNRHR)
• Indications: 2 conditions
• Clinical trials: 3
• Chemistry: 1416.1 Da · C72H95ClN14O14

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1252
Name	Abarelix
Type	Protein
Max phase	4
FDA approved	no
PubChem CID	16131215
ChEBI	CHEBI:337298
ATC	L02BX01
Molecular formula	C72H95ClN14O14
Molecular weight	1416.1
InChIKey	AIWRTTMUVOZGPW-HSPKUQOVSA-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](CC(=O)N)NC(=O)[C@H](CC2=CC=C(C=C2)O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](CC3=CN=CC=C3)NC(=O)[C@@H](CC4=CC=C(C=C4)Cl)NC(=O)[C@@H](CC5=CC6=CC=CC=C6C=C5)NC(=O)C

IUPAC name: (2R)-2-[[(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]-methylamino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[(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]butanediamide

ChEBI definition: A polypeptide compound composed of ten natural and non-natural amino acid resiudes in a linear sequence.

Pharmacological roles (ChEBI): hormone antagonist, antineoplastic agent.

Also known as: Abarelix, Plenaxis, PPI-149, R-382, R-3827, R382, R3827, ABARELIX

Patent coverage: 5,713 distinct patent families (25,996 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 25,841 (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	Antagonist	9.49	0.1%	P30968

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Gonadotropin-releasing hormone receptor.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
GNRHR	9.1	Kd	0.79	nM	CHEMBL_ACT_1291628
GNRHR	8.46	IC50	3.5	nM	CHEMBL_ACT_1291627

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

2 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

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

Clinical trials

Total trials: 3.

Phase distribution

Phase	Trials
PHASE4	1
PHASE3	1
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00103623	PHASE4	SUSPENDED	The Plenaxis® Experience Study
NCT00841113	PHASE3	COMPLETED	Abarelix Versus Goserelin Plus Bicalutamide in Patients With Advanced or Metastatic Prostate Cancer
NCT00100243	PHASE2	COMPLETED	Study of Abarelix in Androgen-Independent Prostate Cancer Progressing After Agonist Therapy

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
RELUGOLIX	ChEMBL + PubChem	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