Drug intelligence / Profile preview

dapolsertib + glofitamab

Development stage
Unknown
Lead developer
Menarini
Modality
Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

dapolsertib + glofitamab is a combination investigational therapy currently in clinical development for **relapsed/refractory aggressive B-cell non-Hodgkin lymphoma**. - **dapolsertib** (MEN1703, SEL24) is an orally bioavailable, small-molecule **dual inhibitor of PIM and FLT3 kinases**, implicated in malignant transformation and lymphomagenesis[5]. - **glofitamab** is a bispecific monoclonal antibody that binds **bivalently to CD20** on B cells and **monovalently to CD3** on T cells, bridging them to form an immunological synapse, resulting in T-cell activation, cytokine release, and lysis of CD20-expressing malignant B cells[2][4][8][10]. The combination is being evaluated primarily for B-cell non-Hodgkin lymphoma in phase II clinical trials[1][5], aiming to leverage dapolsertib's kinase inhibition together with the T-cell-mediated cytotoxicity promoted by glofitamab.

Other names
dapolsertib hydrochlorideglofitamab
02

Targets

PIM3 (Proviral integration site for Moloney murine leukemia virus kinase 3)CD20 (B-lymphocyte antigen CD20)CD3 (T-cell surface glycoprotein CD3)PIM2 (Proto-oncogene serine/threonine-protein kinase Pim2)PIM1 (Proviral integration site for moloney murine leukemia virus kinase 1)FLT3 (Fms related receptor tyrosine kinase 3)

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