Potent (IC50’s < 11 nM) inhibitor of tropomyosin receptor kinases A, B, and C (TrkA, B, and C). It is >100 fold selective against a panel of 229 kinases. Markedly attenuats bone cancer pain, and significantly blocks formation of neuroma-like structures and the sprouting of sensory nerve fibers....
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Potent (IC50’s < 11 nM) inhibitor of tropomyosin receptor kinases A, B, and C (TrkA, B, and C). It is >100 fold selective against a panel of 229 kinases. Markedly attenuats bone cancer pain, and significantly blocks formation of neuroma-like structures and the sprouting of sensory nerve fibers. Larotrectinib caused substantial tumor regression in various cancers displaying TRK gene fusions and is the first tissue agnostic cancer drug approved by the FDA
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