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ibrutinib + lenalidomide + DA-EPOCH-R

Development stage
Preclinical
Lead developer
Pharmacyclics
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a **combination regimen** comprised of three main components: **ibrutinib**, **lenalidomide**, and **DA-EPOCH-R**. - **Ibrutinib** is a small molecule inhibitor that binds covalently to Bruton's tyrosine kinase, a critical enzyme in B-cell receptor signaling, resulting in inhibition of malignant B-cell proliferation and survival. - **Lenalidomide** is an immunomodulatory agent that has direct anti-tumor effects, inhibits angiogenesis, and modulates the immune system to enhance immune-mediated tumor destruction. - **DA-EPOCH-R** (dose-adjusted etoposide, prednisone, vincristine, cyclophosphamide, doxorubicin, rituximab) is an intensive chemotherapy regimen designed for aggressive B-cell lymphomas, including MYC-rearranged lymphomas and "double-hit" or "triple-hit" lymphomas. DA-EPOCH-R combines a monoclonal antibody (rituximab) and multiple cytotoxic agents with different mechanisms: anthracycline (doxorubicin), alkylating agent (cyclophosphamide), topoisomerase inhibitor (etoposide), vinca alkaloid (vincristine), and corticosteroid (prednisone)[1][2][3][4][5]. This regimen is used primarily in high-risk or refractory lymphoma, with the intention of maximizing anti-tumor activity by targeting complementary oncogenic pathways.

Other names
DA-EPOCH-R-Pharmacyclics LLC.-diffuse large B-cell lymphomaIbrutinib and Lenalidomide with DA-EPOCH-RDA-EPOCH-R plus ibrutinib and lenalidomide
02

Targets

CD20 (B-lymphocyte antigen CD20)CRBN (Cereblon)BLK (B lymphoid tyrosine kinase)BTK (Bruton tyrosine kinase)IKZF3 (Zinc finger protein Aiolos)IKZF1 (Ikaros family zinc finger protein 1)ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)ITK (Interleukin 2-inducible T-cell kinase)

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