ArticleDrug metabolism and disposition: the biological fate of chemicals2025
Mechanistic insights into human carboxylesterase 2 (CES2) inhibition by the CES1 prodrug substrate remdesivir.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
COVID-19 remains a significant health threat, particularly to people over the age of 65 with existing comorbidities like diabetes, hypertension, cancer, and viral infections. Despite expedited drug approvals, drug-drug interaction profiles for COVID-19 antiviral drugs have not yet been completely defined. The antiviral drugs remdesivir and molnupiravir are ester prodrugs with carboxylesterases (CES) playing a critical role in their bioactivation. In this study, we investigated the effect of COVID-19 antiviral drugs on CES hydrolysis activity. Of the 3 drugs tested, remdesivir inhibited 50% of CES2 activity in a nanomolar concentration range. Furthermore, time-dependent inhibition of CES2 activity by remdesivir was identified with an IC
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