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EDP-514 in healthy subjects and nucleos(t)ide reverse transcriptase inhibitor-suppressed patients with chronic

Jordan J Feld1, Eric Lawitz2, Tuan Nguyen3

  • 1Toronto Centre for Liver Disease, University Health Network, Toronto, ON, Canada.

Antiviral Therapy
|November 16, 2022
PubMed

Insights

EDP-514, a hepatitis B virus (HBV) core inhibitor, demonstrated good tolerability and a pharmacokinetic profile suitable for daily dosing in healthy subjects and CHB patients. The drug effectively reduced HBV RNA levels in patients with chronic hepatitis B (CHB) who were already on nucleos(t)ide treatment.

Area of Science:

  • Hepatology
  • Virology
  • Pharmacology

Background:

  • Chronic hepatitis B (CHB) is a significant global health concern, contributing to substantial morbidity and mortality.
  • Hepatitis B virus (HBV) infection poses a major challenge in liver disease management.
  • EDP-514 is a novel HBV core inhibitor investigated for its therapeutic potential.

Purpose of the Study:

  • To evaluate the safety and tolerability of EDP-514 in healthy individuals.
  • To assess the pharmacokinetic profile of EDP-514 across various doses and conditions.
  • To determine the antiviral activity of EDP-514 in patients with chronic hepatitis B.

Main Methods:

  • A first-in-human Phase 1 study involving ascending single and multiple doses of EDP-514 in healthy subjects.
  • A Phase 2 study assessing EDP-514 in nucleos(t)ide-suppressed CHB patients over 28 days.
  • Pharmacokinetic analysis and measurement of HBV RNA levels were conducted.

Main Results:

  • EDP-514 was well-tolerated in both healthy subjects and CHB patients, with predominantly mild adverse events.
  • EDP-514 exhibited dose-proportional pharmacokinetics up to 600 mg (single dose) and 400 mg (multiple doses) in healthy subjects.
  • In CHB patients, EDP-514 showed linear exposure, some accumulation, and significant reductions in HBV RNA levels across tested doses.

Conclusions:

  • EDP-514 is safe and well-tolerated, supporting its further development for CHB treatment.
  • The pharmacokinetic profile of EDP-514 supports a once-daily dosing regimen.
  • EDP-514 demonstrated antiviral activity by reducing HBV RNA in NUC-suppressed CHB patients.
Abstract

Keywords:
Chronic hepatitis Bcapsid assembly modulatorcore inhibitorcore protein allosteric modulatorhepatitis B viruspharmacodynamicspharmacokineticssafety

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