Concepedia

Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis

F. Brebion, Romain Gosmini, Pierre Deprez, Marie Varin, Christophe Peixoto, Luke J. Alvey, Hélène Jary, Natacha Bienvenu, Nicolas Triballeau, Roland Blanqué,

Journal of Medicinal Chemistry · 2021 · 56 citations · 23 references

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Abstract

< 1.5 μM). The cocrystal structure of GLPG1972/S201086 with human recombinant ADAMTS-5 is discussed. GLPG1972/S201086 has been investigated in a phase 2 clinical study in patients with knee OA (NCT03595618).

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