Drug intelligence / Profile preview

carfilzomib + lenalidomide + rituximab

Development stage
Unknown
Lead developer
Amgen
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

carfilzomib + lenalidomide + rituximab is a combination regimen investigated for the treatment of relapsed or refractory B-cell non-Hodgkin lymphoma. Carfilzomib is a second-generation tetrapeptide epoxyketone proteasome inhibitor that irreversibly binds to the chymotrypsin-like activity of the 20S proteasome, leading to cell cycle arrest and apoptosis. Lenalidomide is an immunomodulatory agent that binds to cereblon, part of the CRL4-CRBN E3 ubiquitin ligase complex, resulting in the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) transcription factors, which are essential for B-cell survival. Rituximab is a chimeric monoclonal antibody directed against the CD20 antigen found on the surface of normal and malignant B-lymphocytes, mediating cell lysis through complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC). This triplet combination was evaluated in a Phase I/II trial sponsored by the M.D. Anderson Cancer Center to determine its safety and efficacy in patients with relapsed or refractory B-cell non-Hodgkin lymphoma.

Other names
KLR regimenCarfilzomib-Lenalidomide-Rituximab
02

Targets

PSMB5 (Proteasome subunit beta Type-5)CD20 (B-lymphocyte antigen CD20)CRBN (Cereblon)

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