Drug intelligence / Profile preview

oprozomib

Development stage
Phase 2
Lead developer
Amgen
Modality
Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Oprozomib is an orally bioavailable, second-generation proteasome inhibitor structurally related to carfilzomib. It selectively inhibits the chymotrypsin-like activity of both the constitutive proteasome (PSMB5) and immunoproteasome (LMP7), leading to apoptosis in cancer cells. Oprozomib is being developed primarily for hematologic malignancies such as multiple myeloma and Waldenström macroglobulinemia. It has demonstrated preclinical and early clinical efficacy against bortezomib-resistant multiple myeloma cells and has been granted orphan drug status for multiple myeloma and Waldenström macroglobulinemia[2][4][6]. The drug was originally developed by Proteolix, later acquired by Onyx Pharmaceuticals (an Amgen subsidiary)[2].

Other names
oprozomib
02

Targets

PSMB8 (Immunoproteasome)PSMB5 (Proteasome subunit beta Type-5)

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