Larotrectinib is a potent (IC50s < 11 nM) inhibitor of tropomyosin receptor kinases A, B, and C (TrkA, B, and C).1 It is >100 fold selective against a panel of 229 kinases. Larotrectinib markedly attenuated bone cancer pain and significantly blocked the formation of neuroma-like structures and the sprouting of sensory nerve fibers. Larotrectinib caused substantial tumor regression in various cancers displaying TRK gene fusions.2-4 Larotrectinib is the first tissue agnostic drug approved by the FDA.
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