Understanding effect site pharmacology of uprifosbuvir, a hepatitis C virus nucleoside inhibitor: Case study of a multidisciplinary modeling approach in drug development

CPT Pharmacometrics Syst Pharmacol. 2021 Jul;10(7):658-670. doi: 10.1002/psp4.12644. Epub 2021 Jun 18.

Abstract

Uprifosbuvir is a uridine nucleoside monophosphate prodrug inhibitor of the hepatitis C virus NS5B RNA polymerase. To quantitatively elucidate key metabolic pathways, assess the link between unmeasurable effect site concentrations and viral load reduction, and evaluate the influence of intrinsic and extrinsic factors on pharmacokinetics and pharmacodynamics, a model-informed drug development (MIDD) framework was initiated at an early stage. Originally scoped as a modeling effort focused on minimal physiologically based pharmacokinetic and covariate analyses, this project turned into a collaborative effort focused on gaining a deeper understanding of the data from drug metabolism, biopharmaceutics, pharmacometrics, and clinical pharmacology perspectives. This article presents an example of the practical execution of a MIDD-based, cooperative multidisciplinary modeling approach, creating a model that grows along with the team's integrated knowledge. Insights gained from this process could be used in forming optimal collaborations between disciplines in drug development for other investigative compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / pharmacology*
  • Cooperative Behavior
  • Drug Development / methods
  • Hepacivirus / drug effects*
  • Hepacivirus / enzymology
  • Hepatitis C / drug therapy
  • Hepatitis C / microbiology
  • Humans
  • Models, Biological*
  • RNA-Dependent RNA Polymerase / antagonists & inhibitors
  • Uridine / analogs & derivatives*
  • Uridine / pharmacology
  • Viral Load / drug effects
  • Viral Nonstructural Proteins / antagonists & inhibitors

Substances

  • Antiviral Agents
  • Viral Nonstructural Proteins
  • NS-5 protein, hepatitis C virus
  • RNA-Dependent RNA Polymerase
  • uprifosbuvir
  • Uridine