molecules of the month


oral CFTR ABC transporter potentiator

Ph. II for cystic fibrosis (5-80 mg QD), discont.

similarity screen of 589 cmpds + scaffold hop

J. Med. Chem., Jan. 5, 2021

Galapagos NV, Mechelen, BE

Structure of the Galapagos CFTR potentiator - GLPG2451
1 min read

The Galapagos CFTR potentiator, GLPG2451, is an oral, once-daily clinical candidate for cystic fibrosis (5-80 mg QD). It was advanced into a high-profile Ph. II triple-combo study with the CFTR correctors GLPG2737 and GLPG2222 in partnership with AbbVie, and was seen as a potential competitor to Vertex’s CF franchise, but unfortunately weak efficacy data appears to have ended development. The GLPG team was able to get away from their original thiophene core by conducting an interesting scaffold hop in which a hydrogen bond donor and acceptor were swapped across a ring, resulting in their much nicer looking final scaffold.

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