Marizomib

Summary

Marizomib (CHEMBL371405) is a phase-3 clinical-stage small-molecule antineoplastic agent; indicated across 7 conditions including glioblastoma and plasma cell myeloma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 7 conditions
• Clinical trials: 7
• Chemistry: 313.77 Da · C15H20ClNO4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL371405
Name	Marizomib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	11347535
ChEBI	CHEBI:48045
Molecular formula	C15H20ClNO4
Molecular weight	313.77
InChIKey	NGWSFRIPKNWYAO-SHTIJGAHSA-N

SMILES: C[C@]12[C@H](C(=O)N[C@]1(C(=O)O2)[C@H]([C@H]3CCCC=C3)O)CCCl

IUPAC name: (1R,4R,5S)-4-(2-chloroethyl)-1-[(S)-[(1S)-cyclohex-2-en-1-yl]-hydroxymethyl]-5-methyl-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dione

ChEBI definition: A salinosporamide in which the core (1R)-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dione skeleton is substituted at positions 1, 4, and 5 by (1S)-cyclohex-2-en-1-yl(hydroxy)methyl, 2-chloroethyl, and methyl groups, respectively (the 1R,4R,5S diastereoisomer). A potent proteasome inhibitor, it has attracted interest for potential use in the treatment of various cancers.

Pharmacological roles (ChEBI): antineoplastic agent, proteasome inhibitor.

Also known as: Marizomib, NPI-0052, Salinosporamide a, Salinosporamide A, salinosporamide A, salinisporamide A, MARIZOMIB

Patent coverage: 1,945 distinct patent families (7,332 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

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Proteasome Macropain subunit, 20S proteasome, Proteasome component C5, Proteasome Macropain subunit MB1.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PSMB1	9.22	IC50	0.6	nM	CHEMBL_ACT_19258337
PSMB11	8.89	IC50	1.3	nM	CHEMBL_ACT_24706196
PSMB5	8.46	IC50	3.5	nM	CHEMBL_ACT_12135822
PSMB5	8.46	IC50	3.5	nM	CHEMBL_ACT_19258358
PSMB5	7.66	IC50	22	nM	CHEMBL_ACT_13849746
PSMB2	7.55	IC50	28	nM	CHEMBL_ACT_12135818
PSMB1	6.37	IC50	430	nM	CHEMBL_ACT_12135815

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

7 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
glioblastoma	3	MONDO:0018177	EFO:0000519
plasma cell myeloma	2	MONDO:0009693	EFO:0001378
ependymoma	2	MONDO:0016698	EFO:1000028
paraganglioma	2	MONDO:0000448	EFO:1000453
lymphoma	1	MONDO:0005062	EFO:0000574
neoplasm	1	MONDO:0005070	MONDO:0004992

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

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE1	3
PHASE2	2
PHASE3	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03345095	PHASE3	COMPLETED	A Phase III Trial of With Marizomib in Patients With Newly Diagnosed Glioblastoma
NCT03727841	PHASE2	TERMINATED	Marizomib for Recurrent Low-Grade and Anaplastic Supratentorial, Infratentorial, and Spinal Cord Ependymoma
NCT05050305	PHASE2	WITHDRAWN	Marizomib Central Nervous System (CNS)
NCT00396864	PHASE1	COMPLETED	Phase 1 Clinical Trial of NPI-0052 in Patients With Advanced Solid Tumor Malignancies or Refractory Lymphoma
NCT02103335	PHASE1	COMPLETED	Combination Study of Pomalidomide, Marizomib, and Low-Dose Dexamethasone in Relapsed and Refractory Multiple Myeloma
NCT04341311	PHASE1	TERMINATED	Phase I Study of Marizomib + Panobinostat for Children With DIPG
NCT04644107	Not specified	NO_LONGER_AVAILABLE	Expanded Access for Marizomib

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).