Drug intelligence / Profile preview

acalabrutinib + rituximab + lenalidomide

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

Overview

Acalabrutinib + rituximab + lenalidomide is a combination regimen for treating relapsed or refractory B-cell non-Hodgkin lymphoma, including diffuse large B-cell lymphoma (DLBCL) and follicular lymphoma (FL)[1][3][4][5]. - **Acalabrutinib** is a second-generation Bruton tyrosine kinase (BTK) inhibitor that selectively inhibits BTK, blocking B-cell receptor signaling and downstream pathways critical for lymphoma cell survival and proliferation. - **Rituximab** is a monoclonal antibody targeting CD20 on B cells, inducing cell death via direct apoptosis, antibody-dependent cell-mediated cytotoxicity (ADCC), and complement-dependent cytotoxicity (CDC). - **Lenalidomide** is an immunomodulatory drug that exerts antitumor activity by enhancing immune responses, inhibiting angiogenesis, and direct cytotoxic effects on lymphoma cells. This combination, sometimes referred to as the R2A regimen, has shown potential synergism by combining complementary mechanisms: BTK pathway blockade, CD20-directed immunotherapy, and immunomodulation, with clinical studies reporting promising efficacy and manageable toxicity, particularly in relapsed/refractory aggressive B-cell lymphomas[1][3].

Other names
R2AR-2AR 2A
02

Targets

CRBN (Cereblon)CD20 (B-lymphocyte antigen CD20)BTK (Bruton tyrosine kinase)

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