loxo 101

Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase, demonstrating high selectivity exclusively for the TRK family of receptors (IC50s = 2-20 nM).

TRK-IN-12 (Compound 9e), a macrocyclic derivative, is a potent TRK inhibitor, with efficacy against TRK G595R (IC 50 = 13.1 nM). It demonstrates significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC 50 = 0.080 μM) and exhibits superior inhibitory performance (IC 50 = 0.646 μM) compared to the control agent LOXO-101 in the Ba/F3-LMNA-NTRK1-G595R cell line [1].