Vepugratinib
In human trialsMeasured in people, not heightBy mouthSmall moleculeAlso LOXO-435, LY3866288
A cancer drug in late-stage trials that blocks the cartilage-brake receptor and mostly leaves its relatives alone.
FGFR3-selective kinase inhibitor. On the supplier's IC50 figures it is far more potent against FGFR3 S249C and the S249C/V555M double mutant than against FGFR2 or FGFR1, and it retains activity against FGFR3 gatekeeper mutations, V555M being the relevant resistance substitution. Oncology only, in the FORAGER-2 phase 3.
Risks. Diarrhoea, tiredness and liver blood tests going up are the common problems.
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