CASE STUDY: Discovering Selective VEGFR3 (FLT4) Inhibitor for Solid Tumors

Case study

Program co-owned - target ID by analysis of tumor samples from cancer patients done by our partner Oncobox.

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Target	VEGFR3(FLT4)
Chemical space	Enamine REAL 3B
Models we used	B1
Hit rate (<10 μM)	3.6%
Selectivity	45x VEGFR1, 58x VEGFR2
Best hit IC50	1.7 μM

Challenge

Existing VEGFR-targeting cancer drugs are pan-inhibitors Unmet need for a highly selective VEGFR3 inhibitor, which would be a safer (less metastasis, cardiotoxicity) and more efficacious drug for thyroid, kidney, pancreatic, and ovarian cancers (~$10B combined market)

Solution & Impact

BIOPTIC B1 model identified a chemically novel 1.7 uM FLT4 inhibitor which is highly selective against 2 closest targets VEGFR1 (45x) & VEGFR2 (58x).

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