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Re: DewDiligence post# 2462

Monday, 04/17/2023 12:19:24 PM

Monday, April 17, 2023 12:19:24 PM

Post# of 3013

More preclinical data on EDP-235, EDP-323 @ECCMID:



Thanks Dew for the heads up. The preclinical data certainly shows EDP-235 has the properties to make it the best in class anti-Covid drug.

To determine the in vivo drug distribution into target tissues, including potential COVID-19 reservoirs: lung, heart, salivary glands, kidney, adipose tissue and lung alveolar macrophages, rats were dosed orally with 25 mg/kg of EDP-235 or nirmatrelvir and plasma and tissue drug levels were analyzed by liquid chromatography-tandem mass spectrometry. The ratios of intracellular to extracellular concentrations of EDP-235 in salivary gland epithelial cells, adipocytes, and macrophages were 11.3, 33.6 and 30.5, respectively, compared to ratios ranged from 0.6 to 1.2 for nirmatrelvir in these human cells. Consistent with the in vitro observations, EDP-235 showed excellent target tissue exposure with tissue-to-plasma ratios of 6.5 in salivary glands, 23.0 in adipose tissues, and 28.4 in lung alveolar macrophages, whereas nirmatrelvir had corresponding values of 0.8, 0.6, and 0.5. These preclinical data demonstrate that EDP-235 achieved preferential target tissue distribution and cell penetration, enabling EDP-235 to target viral reservoirs and minimize viral persistence, which are important factors potentially related to some cases of long COVID-19.



We just need the phase 2 data to show a good safety profile and ENTA and its EDP-235 drug will have a really good chance for success, although that will take more time. I believe the phase 2 data is due by the end of May. A partnership announcement sooner rather than later would go a long way to making me feel more confident.
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