Anti-infectives Developed as Racemic Drugs in the 21st Century: Norm or Exception?

Diego González Cabrera; Dennis A Smith; Gregory S Basarab; James Duffy; Thomas Spangenberg; Kelly Chibale

doi:10.1021/acsmedchemlett.3c00214

Anti-infectives Developed as Racemic Drugs in the 21st Century: Norm or Exception?

ACS Med Chem Lett. 2023 Jun 12;14(7):875-878. doi: 10.1021/acsmedchemlett.3c00214. eCollection 2023 Jul 13.

Authors

Diego González Cabrera¹, Dennis A Smith², Gregory S Basarab¹, James Duffy³, Thomas Spangenberg⁴, Kelly Chibale^{1

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Affiliations

¹ Drug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch 7701, South Africa.
² Independent, 4 The Maltings, Walmer, Kent CT147AR, United Kingdom.
³ Medicines for Malaria Venture, Geneva 1215, Switzerland.
⁴ Global Health Institute of Merck, Ares Trading S.A., Route de Crassier 1, 1262 Eysins, Switzerland.
⁵ South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry, and Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.

Abstract

This viewpoint outlines the case for developing new chemical entities (NCEs) as racemates in infectious diseases and where both enantiomers and racemate retain similar on- and off-target activities as well as similar PK profiles. There are not major regulatory impediments for the development of a racemic drug, and minimizing the manufacturing costs becomes a particularly important objective when bringing an anti-infective therapeutic to the marketplace in the endemic settings of infectious diseases.