Medicinal Chemistry


Medicinal chemistry is a fundamental discipline that lies at the foundation of the core mission of the EIDD. The mission of the Institute is to develop new therapies to address unmet infectious diseases and public health threats, and to provide a continuous flow of new and increasingly optimized therapeutic agents as required to maintain our development pipeline.

Our medicinal chemistry team consists of a panel of experts in the field of virology from both industry and academia. We utilize a mechanism-based approach to the discovery of novel antiviral agents that is focused on competitive alternative substrate inhibitors or allosteric inhibitors of the viral RNA directed RNA polymerase (RdRp) as well as inhibitors of viral proteases. Our facilities capable of carry out hit to lead identification as well as lead optimization focusing on key pharmacologic parameters including potency, mechanism of action, drug metabolism, pharmacokinetics, and toxicity. Our successes include the discovery and preclinical development of an orally available and broadly acting ribonucleoside EIDD-2801 (Molnupiravir), which was approved by the FDA for Emergency Use Authorization (EUA) against COVID-19 in December 2021. We also identified EIDD-2173, a nucleoside prodrug that is an effective hepatitis B (HBV) inhibitor. This compound was licensed to Antios Therapeutics, a start-up biotechnology company and it is currently in Phase 2 clinical trials. In addition, we identified EIDD-2023 as an orally available nucleoside antiviral active against hepatitis C virus (HCV), rhinovirus and picornavirus, which was licensed to Abbvie for further development as a treatment for chronic HCV infections. EIDD-2749 is our recent lead compound that was discovered through an internal SAR study, a broadly active ribonucleoside that is therapeutically effective in animal models of arenavirus, Ebola, influenza and SARS-Cov-2.

Apart from nucleosides-based drug, our expertise also extends to the development of non-nucleoside small molecules against a broad spectrum of viral targets. One of the best examples is the development of ERDRP-519, a highly efficacious, safe, and orally bioavailable preclinical candidate active against Measles and other paramyxoviruses. Identified by HTS, it was further developed by rigorously SAR and PK studies using our in-house facilities. Under AViDD program, we are currently engaged in the development several non-nucleoside small molecules as a polymerase or protease inhibitors against viruses with a pandemic potential.