oprozomib immediate-release formulation

The Immediate Release (IR) Formulation of oprozomib is an oral, small-molecule, second-generation proteasome inhibitor developed by Amgen (originally through its subsidiary Onyx Pharmaceuticals, which acquired the originator Proteolix). Oprozomib is a tripeptide epoxyketone structurally analogous to carfilzomib that selectively and irreversibly inhibits the chymotrypsin-like activity of the 20S proteasome (specifically the PSMB5 and PSMB8/LMP7 subunits). This inhibition prevents the degradation of pro-apoptotic proteins, leading to accumulation of misfolded proteins and induction of apoptosis in cancer cells. The IR formulation was developed as a tablet to improve gastrointestinal tolerability and reduce pharmacokinetic variability compared to earlier modified-release formulations. It was evaluated in the Phase 1b INTREPID-1 trial (NCT02939183) in combination with pomalidomide and dexamethasone for the treatment of relapsed or refractory multiple myeloma, but clinical development of oprozomib has since been terminated.

Other names

Immediate Release (IR) Formulationoprozomib IRoprozomib IR formulationoprozomib IR tabletoprozomib immediate-release tablet