LOXO-101 (ARRY-470, Larotrectinib) sulfate is potent, selective pan-TRK inhibitor with cellular IC50 of 2-20 nM against TRKA, TRKB, and TRKC kinases.
LOXO-101 (ARRY-470, Larotrectinib) demonstrates excellent selectivity against a panel of 226 non-TRK kinases with one exception (TNK2 IC50=576 nM).
LOXO-101 inhibits fusion oncoprotein and cellular proliferation in TRK-fusion-bearing human-derived cancer cell lines.
LOXO-101 markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone.
LOXO-101 inhibits tumor growth in vivo in TRK fusion-positive cancer models.
