Oprozomib
Also known as: ONX 0912, Oprozomib, PR-047
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Summary
Oral second‑generation proteasome inhibitor under clinical investigation for multiple myeloma and related hematologic cancers.
Mechanism of Action
Irreversible covalent inhibition of the 20S proteasome chymotrypsin‑like activity, leading to accumulation of poly‑ubiquitinated proteins and apoptosis of malignant plasma cells
Routes of Administration
Goals & Uses
- Mantle Cell LymphomaOncologyLow
- Multiple MyelomaOncologyModerate
- Proteasome inhibitor resistance circumventionOncologyLow
- Multiple myeloma treatmentOncologyModerate
- Non-Hodgkin lymphoma treatmentOncologyLow
- Waldenström's macroglobulinemia treatmentOncologyLow
Contraindications
- Severe hepatic impairment (Child‑Pugh C)Liver DiseaseModerate
- Severe hepatic impairmentOrganHighLiver function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Hypersensitivity to oprozomib or related epoxyketone inhibitorsAllergyHigh
- Known hypersensitivity to oprozomib or excipientsAllergyHigh
Adverse Effects
- Peripheral neuropathyNeurologicalUncommon
- ThrombocytopeniaHematologicCommonLow platelet count
- Gastrointestinal toxicity (nausea, vomiting, diarrhea)GastrointestinalCommon
- AnemiaHematologicCommonLow red blood cell count or hemoglobin
- NeutropeniaHematologicCommonLow neutrophil count
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- FatigueGeneralCommonLow energy or tiredness
- Cardiac adverse eventsCardiovascularUncommon
- DiarrheaGastrointestinalCommonLoose or frequent stools
Drug Interactions
- Anticoagulants (e.g., warfarin)Moderate
- CYP3A4 inducers (e.g., rifampin)Moderate
- CYP3A4 inducers (e.g., rifampin, carbamazepine)Moderate
- CYP3A4 inhibitors (e.g., ketoconazole)Moderate
- DexamethasoneLow
- CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin)Moderate
Population Constraints
- PregnancyReproductive SafetyAbsolute
- Severe renal impairmentOrgan ImpairmentRelative
- Pediatric patientsAgeRelative
- Pregnant or breastfeeding womenReproductiveRelative
- Patients with pre-existing cardiac diseaseCardiovascularRelative
Regulatory Status
- European UnionInvestigationalUnder clinical evaluation
- United StatesInvestigationalPhase I/II trials ongoing
- United KingdomInvestigationalNo marketing authorisation
Not approved in any jurisdiction; ongoing Phase I/II trials as of 2024.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Oprozomib?
Oral second‑generation proteasome inhibitor under clinical investigation for multiple myeloma and related hematologic cancers.
What is Oprozomib used for?
Oprozomib is educationally associated with: Mantle Cell Lymphoma, Multiple Myeloma, Proteasome inhibitor resistance circumvention, Multiple myeloma treatment, Non-Hodgkin lymphoma treatment, Waldenström's macroglobulinemia treatment. Educational only — not medical advice.
How is Oprozomib administered?
Recorded routes of administration: Oral.
What are the potential side effects of Oprozomib?
Reported adverse effects include: Peripheral neuropathy, Thrombocytopenia, Gastrointestinal toxicity (nausea, vomiting, diarrhea), Anemia, Neutropenia, Nausea, Fatigue, Cardiac adverse events, Diarrhea. This list is not exhaustive — consult a qualified clinician.
Who should avoid Oprozomib?
Recorded contraindications: Severe hepatic impairment (Child‑Pugh C), Severe hepatic impairment, Pregnancy, Hypersensitivity to oprozomib or related epoxyketone inhibitors, Known hypersensitivity to oprozomib or excipients. Consult a qualified clinician before use.