- Guide to PHARMACOLOGY
Synonyms: AB-106 | AB106 | DS-6051b | DS6051b
Compound class: Synthetic organic
Comment: Taletrectinib (DS-6051b) is a next-generation selective ROS1/NTRK inhibitor . It was designed to treat ROS1- or NTRK-rearranged cancers. DS-6051b is able to inhibit the ROS1G2032R mutation that confers resistance to crizotinib, lorlatinib and entrectinib. The compound originates from Daiichi Sankyo and has been licensed to AnHeart.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Fujiwara Y, Takeda M, Yamamoto N, Nakagawa K, Nosaki K, Toyozawa R, Abe C, Shiga R, Nakamaru K, Seto T. (2018)
Safety and pharmacokinetics of DS-6051b in Japanese patients with non-small cell lung cancer harboring ROS1 fusions: a phase I study.
Oncotarget, 9 (34): 23729-23737. [PMID:29805770]
2. Katayama R, Gong B, Togashi N, Miyamoto M, Kiga M, Iwasaki S, Kamai Y, Tominaga Y, Takeda Y, Kagoshima Y et al.. (2019)
The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models.
Nat Commun, 10 (1): 3604. [PMID:31399568]