oprozomib
Small moleculeexperimental
Oprozomib is an orally active second-generation proteasome inhibitor developed by Proteolix, which was acquired by Onyx Pharmaceuticals, an Amgen subsidiary, in 2009. It selectively inhibits chymotrypsin-like activity of both the constitutive proteasome (PSMB5) and immunoproteasome (LMP7). — Wikipedia
Clinical trial activity
9 trials · 1 clinical orgs · 0 marketing orgs
Phase 1
9
Phase 2
5
Phase 3
0
Phase 4
0
Earliest trial started Apr 1, 2010 (NCT01129349)
Timeline
2010s
- Jan 1, 2010
Earliest Phase 1 Sponsor(trial)
Indications
Mechanism of action
- 26S proteosomeINHIBITOR
26S proteosome inhibitor
Irreversible binding
- 26S proteasome non-ATPase regulatory subunit 1 (PSMD1) ↗
- 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) ↗
- 26S proteasome non-ATPase regulatory subunit 14 (PSMD14) ↗
- 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) ↗
- Proteasomal ubiquitin receptor ADRM1 (ADRM1) ↗
- 26S proteasome non-ATPase regulatory subunit 3 (PSMD3) ↗
- 26S proteasome regulatory subunit 7 (PSMC2) ↗
- 26S proteasome regulatory subunit 4 (PSMC1) ↗
- 26S proteasome regulatory subunit 6B (PSMC4) ↗
- 26S proteasome regulatory subunit 10B (PSMC6) ↗
- 26S proteasome regulatory subunit 6A (PSMC3) ↗
- 26S proteasome regulatory subunit 8 (PSMC5) ↗
- 26S proteasome non-ATPase regulatory subunit 2 (PSMD2) ↗
- 26S proteasome non-ATPase regulatory subunit 12 (PSMD12) ↗
- 26S proteasome non-ATPase regulatory subunit 11 (PSMD11) ↗
- 26S proteasome non-ATPase regulatory subunit 6 (PSMD6) ↗
- 26S proteasome non-ATPase regulatory subunit 7 (PSMD7) ↗
- 26S proteasome non-ATPase regulatory subunit 13 (PSMD13) ↗
- 26S proteasome non-ATPase regulatory subunit 4 (PSMD4) ↗
- 26S proteasome non-ATPase regulatory subunit 8 (PSMD8) ↗
- 26S proteasome complex subunit SEM1 (SEM1) ↗
- 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
- 26S proteasome non-ATPase regulatory subunit 14
- Proteasome subunit beta type-3
- Proteasome subunit beta type-10
- Proteasome subunit beta type-7
- 20S proteosome
- 26S protease regulatory subunit 6B
- Proteasome subunit beta type-1/beta type-5
- Proteasome subunit alpha type-1
- Proteasome subunit beta type-4
- 26S proteasome non-ATPase regulatory subunit 11
- Proteasomal ubiquitin receptor ADRM1
- 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
- 26S protease regulatory subunit 7
- 26S protease regulatory subunit 4
- 26S protease regulatory subunit 6A
- 26S protease regulatory subunit 10B
- 26S proteasome non-ATPase regulatory subunit 2
- 26S protease regulatory subunit 8
- 26S proteasome non-ATPase regulatory subunit 12
- 26S proteasome non-ATPase regulatory subunit 3
- 26S proteasome non-ATPase regulatory subunit 6
- 26S proteasome non-ATPase regulatory subunit 13
- 26S proteasome non-ATPase regulatory subunit 7
- 26S proteasome non-ATPase regulatory subunit 8
- 26S proteasome regulatory subunit S1
Chemistry & pharmacology
Loading structure…
SMILES
COC[C@H](NC(=O)c1cnc(C)s1)C(=O)N[C@@H](COC)C(=O)N[C@@H](Cc1ccccc1)C(=O)[C@@]1(C)CO1- Mol. weight
- 532.62 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaOprozomib ↗
- ChEMBLCHEMBL2103884 ↗
Also known as
- onx 0912
- onx-0912
- onx-0912
- oprozomib
- oprozomib
- oprozomib
- oprozomib
- oprozomib
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02939183 | Phase 1 | Jan 17, 2017 | Amgen |
| NCT02227914 | Phase 1/Phase 2 (Phase 2) | Dec 1, 2014 | Amgen |
| NCT02244112 | Phase 1 | Aug 1, 2014 | Amgen |
| NCT02072863 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2014 | Amgen |
| NCT01999335 | Phase 1 | Nov 1, 2013 | Amgen |
| NCT01881789 | Phase 1/Phase 2 (Phase 2) | Aug 1, 2013 | Amgen |
| NCT01832727 | Phase 1/Phase 2 (Phase 2) | May 1, 2013 | Amgen |
| NCT01416428 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2011 | Amgen |
| NCT01129349 | Phase 1 | Apr 1, 2010 | Amgen |
Showing 9 of 9 trials
Page 1 / 1
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Amgen | For profit | 9 | 9 | 2 | 2010 |
1 organizations
Page 1 / 1