Drug intelligence / Profile preview

amcasertib + sunitinib

Development stage
Phase 1
Lead developer
Sumitomo Pharma America
Modality
Small Molecules
Administration
Oral
01

Overview

**Amcasertib + sunitinib** is an investigational combination therapy composed of two small molecule inhibitors: amcasertib (BBI-503), a first-in-class orally available stemness kinase inhibitor targeting key cancer stem cell pathways including NANOG via inhibition of serine-threonine kinases, and sunitinib, a multi-targeted receptor tyrosine kinase inhibitor approved for various cancers, primarily by inhibiting angiogenesis and cell proliferation. Amcasertib is primarily developed for overcoming cancer stemness, drug resistance, and recurrence by suppressing stemness-related signaling, while sunitinib exerts antiangiogenic and antiproliferative effects through inhibition of multiple receptor tyrosine kinases (e.g., VEGFR, PDGFR, KIT). The combination is being explored due to potential synergistic activity in treating cancers driven by cancer stem cells and in resistant or refractory solid tumors[1][2][4].

Other names
amcasertib plus sunitinib
02

Targets

FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)NQO1PDGFRB (Platelet-derived growth factor receptor beta)STAT3 (Signal Transducer and Activator of Transcription 3)VEGFR2 (Vascular endothelial growth factor receptor 2)NANOG (Nanog Homeobox)

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