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Oprozomib

Oprozomib (codenamed ONX 0912 and PR-047) is an orally active second-generation proteasome inhibitor developed by Onyx Pharmaceuticals, an Amgen subsidiary. It is being investigated for the treatment of hematologic malignancies, specifically, multiple myeloma, with Phase 1b studies ongoing (as of February 16, 2016). Being an epoxyketone derivative, oprozomib is structurally related to carfilzomib and has the added benefit of being orally bioavailable. It selectively inhibits chymotrypsin-like activity of both the constitutive proteasome ( PSMB5) and immunoproteasome ( LMP7). Like carfilzomib, it is active against bortezomib-resistant multiple myeloma cells.