Entasis Therapeutics Announces Initial ETX0282 Phase 1 Results

Entasis Therapeutics Holdings (NASDAQ:ETTX) has announced initial preliminary results from its first-in-human Phase 1 clinical trial of its oral beta-lactamase inhibitor ETX0282.

As quoted in the press release:

The Phase 1 trial is evaluating the safety, tolerability and pharmacokinetics of ETX0282 either alone or in combination with cefpodoxime proxetil, ETX0282CPDP, in healthy volunteers. The Company is developing ETX0282CPDP as an oral therapy for infections caused by multidrug-resistant (MDR) Gram-negative pathogens, including ESBL-producing and carbapenem-resistant Enterobacteriaceae.

This Phase 1 clinical trial (NCT03491748) is a randomized, double-blind, placebo-controlled study of ETX0282 in healthy subjects and consists of several parts including: single-ascending dose, multiple-ascending dose, effect of food on absorption, and assessment of drug-drug interaction between ETX0282 and cefpodoxime proxetil. The trial has currently enrolled 79 healthy subjects with 61 subjects having received at least one oral dose of ETX0282 between 100mg – 800mg. In the Phase 1 trial, ETX0282 in a “powder in capsule” formulation was rapidly absorbed, and plasma concentrations of the beta-lactamase inhibitor were in the projected therapeutic range. There was no drug-drug interaction between ETX0282 and cefpodoxime proxetil. When administered with a high fat meal, ETX0282 demonstrated similar overall exposures as compared to fasting subjects, but with a modified pharmacokinetic profile including decreased peak concentrations. ETX0282 was generally well tolerated either alone or in combination with cefpodoxime proxetil, with no serious adverse events reported. While eight subjects reported mild-to-moderate, transient emesis (vomiting), none of the volunteers who received ETX0282 with a high fat meal reported emesis. Additional studies are planned to further investigate the potential correlation between absorption profile and emesis and to formulate ETX0282 for further clinical development.

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