Drug intelligence / Profile preview

tirabrutinib + rituximab + methotrexate + procarbazine + vincristine

Development stage
Phase 2
Lead developer
Ono Pharmaceutical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of tirabrutinib, rituximab, methotrexate, procarbazine, and vincristine, most commonly under investigation for the treatment of primary central nervous system lymphoma (PCNSL). **Tirabrutinib** is a Bruton's tyrosine kinase (BTK) inhibitor that blocks B-cell receptor signaling, inhibiting malignant B-cell proliferation. **Rituximab** is a monoclonal antibody targeting CD20 on B-lymphocytes, inducing antibody-dependent and complement-mediated cytotoxicity. **Methotrexate** is an antimetabolite that inhibits dihydrofolate reductase, preventing DNA synthesis. **Procarbazine** is an an alkylating agent disrupting DNA, while **vincristine** inhibits microtubule formation, arresting cell division. This multi-agent regimen is used as induction chemotherapy for PCNSL and potentially other CNS lymphomas, aiming to combine the benefits of targeted, immunotherapeutic, and cytotoxic mechanisms for improved response rates and disease control[1][2][4][6][8].

Brand names
rituximab (Rituxan)
Other names
R-MPV plus tirabrutinibtirabrutinib + R-MPV
02

Targets

BTK (Bruton tyrosine kinase)CD20 (B-lymphocyte antigen CD20)DNADHFR (Dihydrofolate reductase)TUBB (Tubulin (alpha and beta subunits))

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