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utatrectinib
- Development stage
- Phase 1
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Utatrectinib (AZD7451) is a potent, selective, orally active small molecule inhibitor of the tropomyosin receptor kinase (TRK) family. It acts as a pan-TRK inhibitor targeting neurotrophic tyrosine kinase receptors (NTRK), including TRKA, TRKB, and TRKC. By inhibiting these kinases, utatrectinib blocks downstream signaling pathways involved in tumor cell growth and invasion. The drug was developed primarily for its antineoplastic activity in cancers driven by NTRK fusions or mutations. Preclinical studies have shown that it potently inhibits phosphorylation of TRKA and suppresses proliferation in certain cancer cell lines. Utatrectinib has been investigated mainly for recurrent gliomas and glioblastoma multiforme[2][3][4][5][6][7].
- Other names
- utatrectinib
02
Targets
ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)NTRK1 (Tropomyosin-related receptor kinase A)NTRK2 (Tropomyosin-related kinase receptor type B)NTRK3 (Tropomyosin receptor kinase C)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)
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