Abstract |
Herein, we report the discovery of a novel potent, selective, CNS penetrant, and orally bioavailable mGlu4 PAM, VU0652957 ( VU2957, Valiglurax). VU2957 possessed attractive in vitro and in vivo pharmacological and DMPK properties across species. To advance toward the clinic, a spray-dried dispersion (SDD) formulation of VU2957 was developed to support IND-enabling toxicology studies. Based on its overall profile, VU2957 was evaluated as a preclinical development candidate for the treatment of Parkinson's disease.
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Authors | Joseph D Panarese, Darren W Engers, Yong-Jin Wu, Joanne J Bronson, John E Macor, Aspen Chun, Alice L Rodriguez, Andrew S Felts, Julie L Engers, Matthew T Loch, Kyle A Emmitte, Arlindo L Castelhano, Michael J Kates, Michael A Nader, Carrie K Jones, Anna L Blobaum, P Jeffrey Conn, Colleen M Niswender, Corey R Hopkins, Craig W Lindsley |
Journal | ACS medicinal chemistry letters
(ACS Med Chem Lett)
Vol. 10
Issue 3
Pg. 255-260
(Mar 14 2019)
ISSN: 1948-5875 [Print] United States |
PMID | 30891122
(Publication Type: Journal Article)
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