Clinical Trials

Multiple clinical trials, predominantly sponsored by Amgen, have evaluated oprozomib as monotherapy or combined with agents such as dexamethasone, pomalidomide, or melphalan across Phase 1 and Phase 1/2 studies. These investigations focused on hematologic malignancies—including multiple myeloma, relapsed or refractory multiple myeloma, and Waldenström macroglobulinemia—as well as solid tumors and advanced hepatocellular carcinoma to assess safety, pharmacokinetics, and therapeutic efficacy. Across these patient cohorts, recorded study statuses include completed, terminated, and withdrawn trials.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02939183 COMPLETED
Relapsed or Refractory Multiple Myeloma
Amgen
 2017-01-17 PHASE1
NCT01881789 TERMINATED
Multiple Myeloma
Amgen
 2013-10-28 PHASE1; PHASE2
NCT01832727 TERMINATED
Multiple Myeloma
Amgen
 2013-07-02 PHASE1; PHASE2
NCT01999335 TERMINATED
Multiple Myeloma
Amgen
 2014-07-30 PHASE1
NCT01416428 TERMINATED
Multiple Myeloma; Waldenstrom Macroglobulinemia
Amgen
 2011-10-15 PHASE1; PHASE2
NCT02244112 TERMINATED
Advanced Non-Central Nervous System (CNS) Malignancies
Amgen
 2014-08 PHASE1
NCT02227914 WITHDRAWN
Advanced Hepatocellular Carcinoma
Amgen
 2014-12 PHASE1; PHASE2
NCT02072863 COMPLETED
Multiple Myeloma
Amgen
 2014-01 PHASE1; PHASE2
NCT01999335 Terminated
Multiple Myeloma
Amgen
 2014-07-30 Phase 1
NCT01832727 Terminated
Multiple Myeloma
Amgen
 2013-07-02 Phase 1|Phase 2
NCT01129349 COMPLETED
Solid Tumors
Amgen
 2010-04 PHASE1
NCT01416428 Terminated
Multiple Myeloma|Waldenstrom Macroglobulinemia
Amgen
 2011-10-15 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2024-09-26)

Check the Oprozomib product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Oprozomib is an orally bioavailable small molecule that selectively binds to and inhibits the chymotrypsin-like activity of the 20S proteasome β5 subunit and LMP7, thereby blocking proteasomal protein clearance and causing intracellular accumulation of polyubiquitinated proteins. This accumulation triggers cytotoxic unfolded protein response stress and programmed cell death, providing the mechanistic rationale for targeting proteasome-dependent hematologic malignancies such as multiple myeloma and Waldenstrom macroglobulinemia.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.