VPR_423



NAME OF DRUG : VPR_423

ALSO KNOWN AS : VPR_423

LABORATORY : VisionaryPharmaceuticals

STATUS AND ADVANCEMENT

Type of drug : RORgammaT

Clinical trials advancement : Preclinic

Estimated time to market : 136 months.

LABORATORY ABSTRACT ON THE DRUG

VPR-423 is an IND candidate that derives from molecules discovered by Visionary Pharmaceuticals and feasibility studies performed by Dr. Tatiana Kisseleva and Dr. David Brenner at UCSD. We show that blocking of IL-17 signaling (via genetic ablation in IL-17RA-/- mice) attenuated development of liver fibrosis in preclinical mouse models of NASH. Expression of IL-17 cytokines is strictly controlled by retinoid-related orphan receptor g (RORγ, a nuclear receptor (NR) protein). We hypothesized that small molecules targeting RORγ block IL-17 cytokine expression and are effective in preclinical models of NASH. To this end, we show that an RORγ inverse agonist blocks liver fibrosis in both the bile duct ligation (BDL)- and CCl4-induced mouse models. We believe that we are the first to propose RORγ inverse agonist for treating NASH. Existing RORγ inverse agonists have poor chemical properties that have blocked their development. Visionary’s molecules are small molecular weight with favorable drug properties including low cost of goods and excellent bioavailability.

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