Safety and Pharmacokinetics of Lopinavir/Ritonavir Oral Solution in Preterm and Term Infants Starting Before 3 Months of Age

Pediatr Infect Dis J. 2024 Apr 1;43(4):355-360. doi: 10.1097/INF.0000000000004243. Epub 2024 Jan 4.

Abstract

Background: Study of liquid lopinavir/ritonavir (LPV/r) in young infants has been limited by concerns for its safety in neonates.

Methods: International Maternal Pediatric Adolescent AIDS Clinical Trials Network P1106 was a phase IV, prospective, trial evaluating the safety and pharmacokinetics of antiretroviral medications administered according to local guidelines to South African preterm and term infants <3 months of age. Safety evaluation through 24-week follow-up included clinical, cardiac and laboratory assessments. Pharmacokinetic data from P1106 were combined with data from International Maternal Pediatric Adolescent AIDS Clinical Trials Network studies P1030 and P1083 in a population pharmacokinetics model used to simulate LPV exposures with a weight-band dosing regimen in infants through age 6 months.

Results: Safety and pharmacokinetics results were similar in 13/28 (46%) infants initiating LPV/r <42 weeks postmenstrual age (PMA) and in those starting ≥42 weeks PMA. LPV/r was started at a median (range) age of 47 (13-121) days. No grade 3 or higher adverse events were considered treatment related. Modeling and simulation predicted that for infants with gestational age ≥27 weeks who receive the weight-band dosing regimen, 82.6% will achieve LPV trough concentration above the target trough concentration of 1.0 µg/mL and 56.6% would exceed the observed adult lower limit of LPV exposure of 55.9 µg·h/mL through age 6 months.

Conclusions: LPV/r oral solution was safely initiated in a relatively small sample size of infants ≥34 weeks PMA and >2 weeks of life. No serious drug-related safety signal was observed; however, adrenal function assessments were not performed. Weight-band dosing regimen in infants with gestational age ≥27 weeks is predicted to result in LPV exposures equivalent to those observed in other pediatric studies.

Trial registration: ClinicalTrials.gov NCT02383849.

Publication types

  • Clinical Trial, Phase IV

MeSH terms

  • Acquired Immunodeficiency Syndrome / drug therapy
  • Administration, Oral
  • HIV Protease Inhibitors* / adverse effects
  • HIV Protease Inhibitors* / pharmacokinetics
  • Humans
  • Infant
  • Infant, Newborn
  • Lopinavir* / adverse effects
  • Lopinavir* / pharmacokinetics
  • Prospective Studies
  • Ritonavir* / adverse effects
  • Ritonavir* / pharmacokinetics

Substances

  • HIV Protease Inhibitors
  • Lopinavir
  • Ritonavir

Associated data

  • ClinicalTrials.gov/NCT02383849