Drug intelligence / Profile preview

lenalidomide + bortezomib + rituximab + dexamethasone

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Oral, Intravenous, Subcutaneous
01

Overview

This is a four-drug combination regimen consisting of lenalidomide (an immunomodulatory agent), bortezomib (a proteasome inhibitor), rituximab (a monoclonal antibody targeting CD20), and dexamethasone (a synthetic glucocorticoid corticosteroid). The combination is used primarily in the treatment of hematologic malignancies such as Waldenström macroglobulinemia and mantle cell lymphoma. Each component has a distinct mechanism of action: - Lenalidomide modulates the immune system and inhibits angiogenesis. - Bortezomib inhibits the 26S proteasome, disrupting protein degradation in cancer cells. - Rituximab targets CD20 on B lymphocytes, leading to cell lysis via immune-mediated mechanisms. - Dexamethasone exerts anti-inflammatory and immunosuppressive effects by binding to glucocorticoid receptors. The regimen has demonstrated efficacy in clinical trials for patients with relapsed or refractory lymphomas and other B-cell malignancies[1][3][7]. It is typically administered in cycles with specific dosing schedules for each drug.

Other names
lenalidomide, bortezomib, rituximab, dexamethasoneR-VRD
02

Targets

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

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