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XL647 + XL147
- Development stage
- Preclinical
- Lead developer
- Exelixis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
XL647 + XL147 is an investigational oral combination of two small‑molecule targeted anticancer agents: XL647, a multitargeted receptor tyrosine kinase inhibitor of EGFR, VEGFR2, HER2, and EphB4, and XL147 (also known as SAR245408), a selective class I PI3K inhibitor (p110α/β/γ/δ). The combination was explored in early-phase oncology trials to assess safety, tolerability, and pharmacodynamics in adults with solid tumors, aiming to concurrently block receptor tyrosine kinase signaling and downstream PI3K pathway activation implicated in tumor growth and resistance mechanisms.[1][2][5][7]
- Other names
- tesevatinib + pilaralisib
02
Targets
DNA-PK (DNA-dependent protein kinase)EGFR (Epidermal growth factor receptor)EPHB4 (Ephrin type-B receptor 4)ERBB2 (Erb-b2 receptor tyrosine kinase 2)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)PIK3C3 (PI3K class III)PIK3CA (Phosphoinositide 3-kinase alpha)
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