selitrectinib

Selitrectinib is an orally bioavailable, selective small molecule inhibitor of tropomyosin receptor kinases (TRK), specifically targeting the neurotrophic tyrosine receptor kinase (NTRK) family members NTRK1, NTRK2, and NTRK3. It is designed to inhibit both wild-type and mutant TRKs, including those with acquired resistance mutations that develop after treatment with first-generation TRK inhibitors such as larotrectinib. By binding to these kinases, selitrectinib blocks neurotrophin-mediated TRK activation and signaling pathways involved in tumor cell growth and survival. This leads to apoptosis and inhibition of proliferation in tumors harboring NTRK gene fusions or activating mutations. Selitrectinib was developed for the treatment of solid tumors with NTRK gene fusions that have progressed on prior TRK inhibitor therapy[1][6][7]. The drug was originally developed by Array BioPharma and later by Bayer.

Other names

selitrectinib