4.2 Article

A commentary on the use of pharmacoenhancers in the pharmaceutical industry and the implication for DMPK drug discovery strategies

Journal

XENOBIOTICA
Volume 52, Issue 8, Pages 786-796

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/00498254.2022.2130838

Keywords

Pharmacoenhancer; ADMET; CYP inhibition; P-glycoprotein inhibition; pharmacokinetics

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Paxlovid, a drug combining nirmatrelvir and ritonavir, has been approved for emergency use by the FDA for treating COVID-19. Co-administration with pharmacoenhancers can enhance the pharmacokinetics and provide various benefits such as ensuring therapeutic exposure and reducing toxic metabolite formation. Technology advancements and improved integration between interdisciplinary teams can enhance drug discovery outcomes.
1. Paxlovid, a drug combining nirmatrelvir and ritonavir, was designed for the treatment of COVID-19 and its rapid development has led to emergency use approval by the FDA to reduce the impact of COVID-19 infection on patients. 2. In order to overcome potentially suboptimal therapeutic exposures, nirmatrelvir is dosed in combination with ritonavir to boost the pharmacokinetics of the active product. 3. Here we consider examples of drugs co-administered with pharmacoenhancers. 4. Pharmacoenhancers have been adopted for multiple purposes such as ensuring therapeutic exposure of the active product, reducing formation of toxic metabolites, changing the route of administration, and increasing the cost-effectiveness of a therapy. 5. We weigh the benefits and risks of this approach, examining the impact of technology developments on drug design and how enhanced integration between cross-discipline teams can improve the outcome of drug discovery.

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