Drug intelligence / Profile preview

oprozomib + cyclophosphamide + dexamethasone

Development stage
Unknown
Lead developer
Amgen
Modality
Small Molecules
Administration
Oral
01

Overview

Oprozomib + cyclophosphamide + dexamethasone is an investigational **three-drug oral combination regimen** targeting relapsed/refractory multiple myeloma (RRMM). **Oprozomib** is a potent, orally available irreversible **proteasome inhibitor** structurally related to carfilzomib, developed for oncology settings, particularly hematological malignancies. **Cyclophosphamide** is an alkylating agent that inhibits DNA replication, and **dexamethasone** is a synthetic corticosteroid with anti-inflammatory and immunosuppressive effects. The regimen exploits synergistic antineoplastic mechanisms—proteasome inhibition disrupts protein homeostasis in malignant cells, cyclophosphamide induces DNA damage, and dexamethasone represses inflammatory cytokines—to target myeloma cells. Trials in RRMM have explored this combination's dose, efficacy, and safety, noting adverse events typical of chemotherapy and proteasome inhibition, but showing preliminary antitumor activity. The combination is being evaluated in phase 1b clinical development; studies to date have not advanced to phase 2 due to sponsor termination decisions[2][1].

02

Targets

PSMB6 (Proteasome 20S subunit beta 6)PSMB7 (Proteasome subunit beta type-7)DNAGR (Glucocorticoid receptor)PSMB5 (Proteasome subunit beta Type-5)

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