Fidest – Agenzia giornalistica/press agency

Quotidiano di informazione – Anno 31 n°14

Poxel Announces Presentation of PXL065 Data at the 2019 NASH-TAG Conference

Posted by fidest press agency su martedì, 8 gennaio 2019

POXEL SA (Euronext: POXEL – FR0012432516), a biopharmaceutical company focused on the development of innovative treatments for metabolic disorders, including type 2 diabetes and non-alcoholic steatohepatitis (NASH), today announced that an oral presentation, including data for PXL065, the deuterium-stabilized R-stereoisomer of pioglitazone, was made at the 2019 NASH-TAG Conference. The presentation titled “PXL065, Pioglitazone (pio), and Thiazolidinediones (TZDs): Unravelling Pio’s superior efficacy for NASH and role of stereoisomers” was given on January 5, 2019 in Park City, Utah.The presentation highlighted key aspects related to the pharmacokinetic (PK) and pharmacodynamic (PD) role of stereoisomers within the class of compounds known as TZDs and the potential relevance for the treatment of NASH. Representative TZDs included rosiglitazone, pioglitazone and lobeglitazone, all of which are a mixture of interconverting R- and S- stereoisomers that have exhibited varying levels of efficacy for NASH in animal and/or human studies.Key findings presented included: 1) a comparison of the striking species-dependent stereoselectivity of the PK for pioglitazone with other TZDs, 2) a comparison of unexpected differences in peroxisome proliferator-activated receptor gamma (PPARγ) activity with the eight stereoisomers that make up pioglitazone and its two active metabolites and 3) stabilization of pioglitazone’s stereoisomers with deuterium to characterize and identify R-pioglitazone as the preferred stereoisomer for the treatment of NASH.Data presented demonstrated that each stereoisomer of pioglitazone and its active metabolites exhibits different PPARγ activity. The presentation also included data showing that PXL065 is a mitochondrial pyruvate carrier (MPC) inhibitor without PPARγ activity in a cofactor recruitment assay. In mouse models, PXL065 demonstrated the hepatic benefits observed with pioglitazone in NASH patients. In preclinical models, PXL065 exhibited little or no weight gain or fluid retention, side effects mainly associated with the PPARγ active, S-pioglitazone.Pioglitazone (Actos®*), a drug approved for the treatment of type 2 diabetes, has demonstrated therapeutic efficacy for NASH, even in patients with advanced fibrosis. However, its therapeutic use and potential have been limited due to the PPARγ-related side effects of weight gain, bone fractures and fluid retention. PXL065 offers a proprietary new approach for the treatment of NASH. PXL065 has the potential to preserve the pharmacological benefits of pioglitazone required for the treatment of NASH, such as a reduction of hepatic steatosis, inflammation, ballooning and fibrosis and could reduce PPARγ-related side effects that are thought to be associated with S-pioglitazone.

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