Rapid viral expansion and short drug half-life explain the incomplete effectiveness of current herpes simplex virus 2-directed antiviral agents

Antimicrob Agents Chemother. 2013 Dec;57(12):5820-9. doi: 10.1128/AAC.01114-13. Epub 2013 Sep 9.

Abstract

The nucleoside analogues acyclovir (ACV) and famciclovir (FCV) reduce the frequency and severity of herpes simplex virus 2 (HSV-2) genital shedding, yet despite their high potency in vitro and a lack of induced drug resistance, frequent episodes of breakthrough mucosal shedding occur. We tested a published stochastic, spatial mathematical model of HSV-2 replication and spread, in concert with pharmacokinetic and pharmacodynamic equations, against virologic data from clinical trials of twice-daily acyclovir and famciclovir suppression. The model reproduced the key features of clinical trial data, including genital shedding episode rate, expansion and decay dynamics, and heterogeneous peak viral production and duration. In simulations, these agents shortened episode duration by limiting the extent of viral production by 1 to 2 log units and limiting the formation of secondary ulcers by ∼50%. However, drug concentrations were noninhibitory during 42% of the dosing cycle. Even if drug concentrations were high at episode initiation, prolonged episodes often ensued due to drug decay over ensuing hours and subsequent rebound of rapidly replicating HSV-2. The local CD8(+) T-cell density was more predictive of episode viral production (R(2) = 0.42) and duration (R(2) = 0.21) than the drug concentration at episode onset (R(2) = 0.14 and 0.05, respectively), though the model projected that an agent with an equivalent potency but a two times longer half-life would decrease shedding by 80% compared to that of standard twice-daily regimens. Therefore, long half-life is a key characteristic of any agent that might fully suppress HSV-2 reactivations.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • 2-Aminopurine / analogs & derivatives*
  • 2-Aminopurine / pharmacokinetics
  • 2-Aminopurine / pharmacology
  • Acyclovir / pharmacokinetics*
  • Acyclovir / pharmacology
  • Antiviral Agents / pharmacokinetics*
  • Antiviral Agents / pharmacology
  • Biological Availability
  • CD8-Positive T-Lymphocytes / virology
  • Clinical Trials as Topic
  • Computer Simulation
  • Drug Administration Schedule
  • Famciclovir
  • Half-Life
  • Herpes Genitalis / drug therapy
  • Herpes Genitalis / virology
  • Herpesvirus 2, Human / drug effects
  • Herpesvirus 2, Human / physiology*
  • Humans
  • Lymphocyte Count
  • Models, Statistical*
  • Viral Load / drug effects
  • Virus Replication / drug effects
  • Virus Shedding / drug effects

Substances

  • Antiviral Agents
  • 2-Aminopurine
  • Famciclovir
  • Acyclovir