Sunday, November 22, 2015

Drugs in Clinical Pipeline: LIK066

LIK066 [(2S,3R,4R,5S,6R)-2-(3-((2,3- dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-4-ethylphenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, (S)-Pyrrolidine-2-carboxylic acid (2:1)] is an orally available, potent dual inhibitor of sodium-glucose transporter-1 (SGLT1) and sodium-glucose transporter-2 (SGLT2), with an in vivo inhibitory concentration (IC50) of 22.0 nM against human SGLT1 and 0.5 nM against human SGLT2 [1, 2].

1. Opinion of the Paediatric Committee on the agreement of a Paediatric Investigation Plan and a deferral and a waiver. 2014EMEA-001527-PIP01-13 (here) [ Novartis revealed the IUPAC name here].
2. Bebernitz, G. R. Glycoside derivatives and their uses for the treatment of diabetes. WO2012140597A1 (synthesis and activity)