Beloranib

Summary

Beloranib (CHEMBL4297504) is a phase-3 clinical-stage small molecule targeting METAP2; indicated across 2 conditions including obesity disorder and prader-willi syndrome.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (METAP2)
• Indications: 2 conditions
• Clinical trials: 4
• Chemistry: 499.6 Da · C29H41NO6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297504
Name	Beloranib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	6918502
Molecular formula	C29H41NO6
Molecular weight	499.6
InChIKey	ZEZFKUBILQRZCK-MJSCXXSSSA-N

SMILES: CC(=CC[C@@H]1[C@@](O1)(C)[C@H]2[C@@H]([C@@H](CC[C@]23CO3)OC(=O)/C=C/C4=CC=C(C=C4)OCCN(C)C)OC)C

IUPAC name: [(3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl] (E)-3-[4-[2-(dimethylamino)ethoxy]phenyl]prop-2-enoate

Also known as: Beloranib, Zgn-433, ZGN-433, Zgn-440, ZGN-440, BELORANIB, US9682965, Compound A

Patent coverage: 140 distinct patent families (430 SureChEMBL compound mentions), from 1 matched compound structure(s). 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
METAP2	Methionyl aminopeptidase 2	Inhibition		68.1%	P50579

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Methionine aminopeptidase 2.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
METAP2	6.56	IC50	275	nM	CHEMBL_ACT_26707952

Target pathways

Aggregated over 1 target gene(s): METAP2.

Top Reactome pathways

4 total, by targets touching each:

Pathway	Targets	Genes
Visual phototransduction	1	METAP2
The phototransduction cascade	1	METAP2
Inactivation, recovery and regulation of the phototransduction cascade	1	METAP2
Sensory Perception	1	METAP2

Dominant GO biological processes

GO term	Targets
regulation of translational initiation	1
protein processing	1
proteolysis	1

Indications & clinical

Indications

2 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
obesity disorder	3	MONDO:0011122	EFO:0001073
Prader-Willi syndrome	3	MONDO:0008300	MONDO:0008300

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE1	3
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01666691	PHASE2	COMPLETED	An Efficacy, Safety and Pharmacokinetics Study of Beloranib (ZGN-440 for Injectable Suspension) in Obese Subjects
NCT01028261	PHASE1	COMPLETED	Safety, Tolerability and Pharmacokinetics of Multiple Doses of ZGN-433 in Obese Female Volunteers
NCT01372761	PHASE1	COMPLETED	Pharmacokinetics, Safety, Tolerability and Efficacy of Intravenous Doses of ZGN-433 in Obese Female Volunteers
NCT01507077	PHASE1	COMPLETED	ZGN-440 (Beloranib for Subcutaneous Injection) for Treatment of Obesity

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
CLIOQUINOL	ChEMBL	Phase 4 (approved)	METAP2
NITROXOLINE	ChEMBL	Phase 4 (approved)	METAP2
THIABENDAZOLE	ChEMBL	Phase 4 (approved)	METAP2
EBSELEN	ChEMBL	Phase 3	METAP2
BENZOXIQUINE	ChEMBL	Phase 2	METAP2
CLOXYQUIN	ChEMBL	Phase 2	METAP2
FUMAGILLIN	ChEMBL	Phase 2	METAP2
O-CHLOROACETYLCARBAMOYLFUMAGILLOL	ChEMBL	Phase 2	METAP2
Albendazole	PubChem	Approved	METAP2
Anthralin	PubChem	Approved	METAP2
Fenbendazole	PubChem	Approved	METAP2
Fosfomycin	PubChem	Approved	METAP2
Mebendazole	PubChem	Approved	METAP2
oxyquinoline	PubChem	Approved	METAP2