Drug intelligence / Profile preview

oprozomib + melphalan + prednisone

Development stage
Discontinued
Lead developer
Amgen
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Oprozomib + melphalan + prednisone is a pharmaceutical combination regimen developed for the treatment of multiple myeloma, particularly in newly diagnosed patients who are ineligible for autologous stem cell transplant. Oprozomib is an oral, irreversible proteasome inhibitor structurally related to carfilzomib, targeting the chymotrypsin-like activity of the 20S proteasome, leading to the accumulation of ubiquitinated proteins and apoptosis in malignant plasma cells. Melphalan is an alkylating agent that crosslinks DNA, thereby disrupting replication and transcription in cancer cells, while prednisone is a synthetic glucocorticoid that exerts anti-inflammatory and immunosuppressive effects, supporting cytotoxicity and symptom management. The combination has been primarily developed and investigated by Amgen, with phase 1b/2 studies exploring its efficacy and safety in multiple myeloma. Development has been discontinued before marketing approval due to formulation and toxicity challenges[1][3][5][7].

Other names
OMPoprozomib + melphalan + prednisone
02

Targets

GR (Glucocorticoid receptor)26S proteasomeDNA

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