Drug intelligence / Profile preview

mesutoclax + orelabrutinib

Development stage
Phase 3
Lead developer
Innocare
Modality
Small Molecules
Administration
Oral
01

Overview

Mesutoclax + orelabrutinib is an all-oral, chemo-free combination regimen being developed by InnoCare for the treatment of various B-cell malignancies. The combination consists of mesutoclax (ICP-248), a novel, highly selective oral B-cell lymphoma 2 (BCL2) inhibitor, and orelabrutinib (ICP-022), an approved selective Bruton's tyrosine kinase (BTK) inhibitor. By targeting both BCL2 and BTK, the regimen simultaneously inhibits two complementary survival pathways in B-cell malignancies to restore apoptosis and block B-cell receptor signaling. The combination is currently in Phase III clinical development for first-line chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) and relapsed/refractory mantle cell lymphoma (MCL), and has received Breakthrough Therapy Designation in China for relapsed/refractory marginal zone lymphoma (MZL).

Other names
ICP-248 + ICP-022ICP-248 + orelabrutinibmesutoclax + ICP-022orelabrutinib + ICP-248orelabrutinib + mesutoclax
02

Targets

BCL-2 (BCL-2 family)BTK (Bruton tyrosine kinase)

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