molecules of the month


potent oral autotaxin phosphodiesterase inh.

orally efficacious in xenograft

from HTS and ligand-based design

ACS Med. Chem. Lett., May 19, 2020

Ono Pharmaceutical, Osaka, JP

Structure of autotaxin inhibitor ONO-8430506
1 min read

ONO-8430506 is a potent autotaxin phosphodiesterase inhibitor with significant oral exposure and low clearance in higher species. Autotaxin contributes to lysophosphatidic acid (LPA) production has been explored as a target in various diseases involving LPA signalling including IPF (GLPG1690, Ph. III), hyperplasia, and cancer (this paper). ONO-8430506 was first disclosed several years ago but the details around its discovery are disclosed here, including the clever strategy to “hybridize” an HTS hit with an endogenous ligand.

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