Drug intelligence / Profile preview

carfilzomib + methylprednisolone

Development stage
Preclinical
Lead developer
Amgen
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a **combination therapy** consisting of carfilzomib, a proteasome inhibitor, and methylprednisolone, a synthetic glucocorticoid corticosteroid. Carfilzomib selectively and irreversibly inhibits the 20S proteasome's chymotrypsin-like activity, resulting in disruption of protein homeostasis and induction of apoptosis in multiple myeloma cells. Methylprednisolone acts as an anti-inflammatory and immunosuppressant, frequently used to manage symptoms or as part of chemotherapy regimens for hematologic malignancies. The combination has been clinically investigated for use in the treatment of multiple myeloma, especially in relapsed or refractory settings.

02

Targets

GR (Glucocorticoid receptor)PSMB1 (26S Proteasome (β1-Subunit))PSMB5 (Proteasome subunit beta Type-5)PSMB2 (Proteasome subunit beta type-2)

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