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 | 
Jan 17, 2018
 |  BioCentury  |  Emerging Company Profile

Computing brain entry

How 1st Biotherapeutics is applying computational tools to CNS drug discovery

1st Biotherapeutics Inc. aims to develop a pipeline of first- or best-in-class molecules for CNS diseases by using computational tools to achieve better blood-brain barrier penetration and PK properties than marketed drugs against the same targets. Lead candidate 1ST-102 is a preclinical ABL proto-oncogene 1 non-receptor tyrosine kinase (c-ABL; ABL; ABL1) inhibitor in development for Parkinson’s disease.

CEO Jamie Jae Eun Kim told BioCentury she launched 1st Biotherapeutics in 2016 after assembling a suite of computational tools capable of optimizing the properties of small molecules, in particular compound families that have been difficult to get into the CNS.

“Kinase inhibitors usually do not penetrate well, but we can find scaffolds with good potency, as well as good pharmacological properties as a central nervous system drug,” she said.

Use of in silico discovery tools also lets the company move fast, she said, noting it took only 10 months to generate a set of preclinical candidates against c-ABL, whereas...

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