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Drug intelligence / Profile preview
oprozomib (gastro-retentive formulation)
- Development stage
- Unknown
- Lead developer
- Amgen
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
The Gastro-Retentive (GR) Formulation of oprozomib is an investigational, extended-release, gastro-retentive oral tablet formulation of oprozomib, a synthetic small molecule proteasome inhibitor. Developed by Amgen (following its acquisition of Onyx Pharmaceuticals), this formulation was designed to improve the gastrointestinal tolerability and pharmacokinetic variability of oprozomib compared to its immediate-release counterpart. Oprozomib is a tripeptide epoxyketone analog of carfilzomib that selectively and irreversibly inhibits the chymotrypsin-like activity of the 20S proteasome, leading to the accumulation of protein substrates and induction of apoptosis in cancer cells. The GR formulation was evaluated in the INTREPID-1 Phase 1b clinical trial (NCT02939183) in combination with pomalidomide and dexamethasone for the treatment of relapsed or refractory multiple myeloma.
- Other names
- Gastro-Retentive (GR) FormulationGR oprozomibextended-release gastroretentive oprozomiboprozomib GRoprozomib GR formulationoprozomib gastro-retentive formulation
02
Targets
PSMB5 (Proteasome subunit beta Type-5)PSMB8 (Immunoproteasome)
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