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Drug intelligence / Profile preview
APG-1252 + ruxolitinib
- Development stage
- Discontinued
- 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
TNK2 (Activated Cdc42-associated kinase 1)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)BCL2L1 (B-cell lymphoma-extra large protein)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)JAK3 (Janus kinase 3)LCK (Proto-oncogene tyrosine-protein kinase Lck)RET (Rearranged during transfection receptor tyrosine kinase)NTRK2 (Tropomyosin-related kinase receptor type B)TYK2 (Tyrosine kinase 2)SRC (Proto-oncogene tyrosine-protein kinase Src)Bcl-w (B-cell lymphoma 2-like 2)
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