Drug intelligence / Profile preview

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)NTRK3 (Tropomyosin receptor kinase C)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)NTRK1 (Tropomyosin-related receptor kinase A)NTRK2 (Tropomyosin-related kinase receptor type B)

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