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ASP-08001 is a small molecule, ATP-competitive dual inhibitor of the receptor tyrosine kinases c-Met (hepatocyte growth factor receptor, HGFR) and VEGFR-2 (vascular endothelial growth factor receptor 2, KDR). Developed by Ascepion Pharmaceuticals, the compound simultaneously targets tumor growth, invasion, and angiogenesis. In preclinical studies, ASP-08001 demonstrated potent inhibition of c-Met and VEGFR-2 phosphorylation, leading to significant antitumor efficacy and tumor regression in mouse xenograft models of non-small cell lung cancer (NSCLC), breast, gastric, and prostate cancers. It has shown a favorable pharmacokinetic profile and a promising safety margin in animal models.
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