Drug intelligence / Profile preview

APG-1252 + ruxolitinib

Development stage
Unknown
Lead developer
Ascentage Pharma
Modality
Small Molecules
Administration
Oral (for Ruxolitinib), Intravenous (for APG-1252)
01

Overview

**APG-1252 + ruxolitinib** is an investigational combination therapy comprising APG-1252 (pelcitoclax), a dual inhibitor of anti-apoptotic BCL-2 family proteins (notably BCL-2 and BCL-xL), and ruxolitinib, an inhibitor of Janus kinase 1 and 2 (JAK1 and JAK2). APG-1252 induces apoptosis in cancer cells by blocking survival pathways, whereas ruxolitinib inhibits JAK-mediated cytokine signaling involved in myeloproliferative neoplasms. The combination is under study particularly for myelofibrosis and other hematologic malignancies where resistance to JAK inhibition occurs, with the proposed rationale that APG-1252 may overcome resistance mechanisms via enhanced apoptosis[6][7][9].

Brand names
pelcitoclax (for APG-1252)Jakafi (for ruxolitinib)
Other names
APG-1252 + ruxolitinibpelcitoclax + ruxolitinib
02

Targets

TYK2 (Tyrosine kinase 2)JAK2 (Janus kinase 2)TNK2 (Activated Cdc42-associated kinase 1)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)BCL2L1 (B-cell lymphoma-extra large protein)LCK (Proto-oncogene tyrosine-protein kinase Lck)JAK1 (Janus kinase 1)SRC (Proto-oncogene tyrosine-protein kinase Src)JAK3 (Janus kinase 3)RET (Rearranged during transfection receptor tyrosine kinase)NTRK2 (Tropomyosin-related kinase receptor type B)

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