Herein, we report the discovery of a novel potent, selective, CNS penetrant, and orally bioavailable mGlu PAM, VU0652957 (VU2957, Valiglurax). VU2957 possessed attractive and 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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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6421540 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.8b00426 | DOI Listing |
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