marizomib
Salinosporamide A (Marizomib) is a potent proteasome inhibitor being studied as a potential anticancer agent. It entered phase I human clinical trials for the treatment of multiple myeloma, only three years after its discovery in 2003. This marine natural product is produced by the obligate marine bacteria Salinispora tropica and Salinispora arenicola, which are found in ocean sediment. Salinosporamide A belongs to a family of compounds, known collectively as salinosporamides, which possess a densely functionalized γ-lactam-β-lactone bicyclic core. — Wikipedia
Clinical trial activity
13 trials · 9 clinical orgs · 0 marketing orgs
Earliest trial started May 1, 2006 (NCT00396864)
Timeline
Indications
Studied for
Mechanism of action
- 20S proteosomeINHIBITOR
20S proteosome inhibitor
Irreversible proteasome inhibitor. Inhibits all three proteolytic chymotrypsin-like (CT-L, b5), trypsin-like (T-L, b2) and caspase-like (C-L, b1) activities.
- Proteasome subunit beta type-2 (PSMB2) ↗
- Proteasome subunit beta type-1 (PSMB1) ↗
- Proteasome subunit beta type-5 (PSMB5) ↗
- Proteasome subunit beta type-8 (PSMB8) ↗
- Proteasome subunit beta type-9 (PSMB9) ↗
- Proteasome subunit beta type-6 (PSMB6) ↗
- Proteasome subunit alpha-type 8 (PSMA8) ↗
- Proteasome subunit alpha type-1 (PSMA1) ↗
- Proteasome subunit alpha type-2 (PSMA2) ↗
- Proteasome subunit alpha type-3 (PSMA3) ↗
- Proteasome subunit alpha type-4 (PSMA4) ↗
- Proteasome subunit alpha type-5 (PSMA5) ↗
- Proteasome subunit alpha type-6 (PSMA6) ↗
- Proteasome subunit alpha type-7 (PSMA7) ↗
- Proteasome subunit beta type-10 (PSMB10) ↗
- Proteasome subunit beta type-11 (PSMB11) ↗
- Proteasome subunit beta type-3 (PSMB3) ↗
- Proteasome subunit beta type-4 (PSMB4) ↗
- Proteasome subunit beta type-7 (PSMB7) ↗
- Proteasome Macropain subunit
- Proteasome Macropain subunit MB1
- Proteasome component C5
- Proteasome subunit beta type-8
- Proteasome subunit beta type-9
- Proteasome subunit beta type-6
- Proteasome subunit beta type-3
- Proteasome subunit beta type-10
- Proteasome subunit beta type-7
- Proteasome subunit beta type-1/beta type-5
- Proteasome subunit alpha type-1
- Proteasome subunit beta type-4
- Proteasome subunit alpha type-7
- Proteasome subunit alpha type-6
- Proteasome subunit alpha type-5
- Proteasome subunit alpha type-3
- Proteasome subunit alpha type-4
- Proteasome subunit alpha type-2
Chemistry & pharmacology
SMILES
C[C@@]12OC(=O)[C@]1([C@@H](O)[C@@H]1C=CCCC1)NC(=O)[C@@H]2CCCl- Mol. weight
- 313.78 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Availability
- Prescription Only
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaSalinosporamide A ↗
- ChEMBLCHEMBL98 ↗
- ChEMBLCHEMBL371405 ↗
Also known as
- hdac inhibitor
- homosalinosporamide a
- marizomib
- marizomib
- marizomib
- marizomib
- marizomib
- marizomib vorinostat
- npi 0052
- npi-0052
- npi-0052
- npi-0052
- npi-0052
- salinosporamide a
- zolinza
- zolinza
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05050305 | Phase 2 | Mar 31, 2022 | Bristol-Myers Squibb, Harvard University |
| NCT04341311 | Phase 1 | May 31, 2020 | Celgene, Harvard University, Secura |
| NCT03727841 | Phase 2 | Jul 5, 2019 | National Cancer Institute (NCI) |
| NCT03463265 | Phase 2 | Aug 1, 2018 | Aadi, LLC |
| NCT03345095 | Phase 3 | Jul 26, 2018 | Canadian Cancer Trials Group, Celgene, European Organisation for Research and Treatment of Cancer |
| NCT02903069 | Phase 1 | Aug 1, 2016 | Triphase Research and Development Corporation |
| NCT02330562 | Phase 1/Phase 2 (Phase 2) | Mar 1, 2015 | Triphase Research and Development Corporation |
| NCT02103335 | Phase 1 | Jun 5, 2014 | Celgene, Triphase Research and Development Corporation |
| NCT00667082 | Phase 1 | Mar 1, 2008 | Triphase Research and Development Corporation |
| NCT00629473 | Phase 1 | Jul 1, 2007 | Triphase Research and Development Corporation |
| NCT00461045 | Phase 1/Phase 2 (Phase 2) | Mar 1, 2007 | Triphase Research and Development Corporation |
| NCT00396864 | Phase 1 | May 1, 2006 | Triphase Research and Development Corporation |
| NCT04644107 | N/A | — | Celgene |
Organizations
Research & Development (9)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Triphase Research and Development Corporation | For profit | 7 | 7 | 2 | 2006 |
| Celgene | For profit | 4 | 1 | 3 | 2014 |
| Harvard University | Academic/Hospital | 2 | 2 | 2 | 2020 |
| Aadi, LLC | For profit | 1 | 1 | 1 | 2018 |
| Bristol-Myers Squibb | For profit | 1 | 0 | 1 | 2022 |
| Canadian Cancer Trials Group | Academic/Hospital | 1 | 0 | 1 | 2018 |
| European Organisation for Research and Treatment of Cancer | Academic/Hospital | 1 | 1 | 1 | 2018 |
| National Cancer Institute (NCI) | Government | 1 | 1 | 1 | 2019 |
| Secura | For profit | 1 | 0 | 1 | 2020 |