Drug intelligence / Profile preview

dinaciclib + rituximab

Development stage
Phase 1
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

Dinaciclib + rituximab is a combination of two drugs: **dinaciclib**, a selective small molecule inhibitor of cyclin-dependent kinases (CDK1, CDK2, CDK5, and CDK9), and **rituximab**, a monoclonal antibody that targets CD20 on B-lymphocytes. This regimen has been studied in patients with relapsed or refractory chronic lymphocytic leukemia (CLL). Dinaciclib’s mechanism involves inhibiting cell cycle progression, blocking transcription, and promoting apoptosis via downregulation of anti-apoptotic proteins such as BCL-XL and BCL2. Rituximab targets and depletes CD20-positive B cells through immune-mediated mechanisms including complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity. Clinical studies indicate this combination is well tolerated and demonstrates encouraging activity in CLL patients, including those with high-risk features[1][5][9].

02

Targets

BRDT (Bromodomain testis-specific protein)C1Q (Complement C1q)CD20 (B-lymphocyte antigen CD20)CDK1 (Cyclin-dependent kinase 1)CDK2 (Cyclin-dependent kinase 2)CDK5 (Cyclin-dependent kinase 5)CDK9 (Cyclin-dependent kinase 9)FCGRT (Neonatal crystallizable fragment receptor)FcγR (Low affinity immunoglobulin gamma Fc region receptor II-c)

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