Safety, Tolerability, and Pharmacokinetics of a Long-Acting Broadly Neutralizing Human Immunodeficiency Virus Type 1 (HIV-1) Monoclonal Antibody VRC01LS in HIV-1-Exposed Newborn Infants

J Infect Dis. 2021 Dec 1;224(11):1916-1924. doi: 10.1093/infdis/jiab229.

Abstract

Background: Perinatal human immunodeficiency virus type 1 (HIV-1) continues to occur due to barriers to effective antiretroviral prevention that might be mitigated by long-acting broadly neutralizing monoclonal antibodies (bNAbs).

Methods: An extended half-life bNAb, VRC01LS, was administered subcutaneously at 80 mg/dose after birth to HIV-1-exposed, nonbreastfed (cohort 1, n = 10) and breastfed (cohort 2, n = 11) infants. Cohort 2 received a second dose (100 mg) at 12 weeks. All received antiretroviral prophylaxis. VRC01LS levels were compared to VRC01 levels determined in a prior cohort.

Results: Local reactions (all grade ≤2) occurred in 67% and 20% after dose 1 and dose 2, respectively. The weight-banded dose (mean 28.8 mg/kg) of VRC01LS administered subcutaneously achieved a mean (standard deviation) plasma level of 222.3 (71.6) µg/mL by 24 hours and 44.0 (11.6) µg/mL at week 12, prior to dose 2. The preestablished target of ≥50 µg/mL was attained in 95% and 32% at weeks 8 and 12, respectively. The terminal half-life was 37-41 days. VRC01LS level after 1 dose was significantly greater (P <.002) than after a VRC01 dose (20 mg/kg). No infants acquired HIV-1.

Conclusions: VRC01LS was well tolerated with pharmacokinetics that support further studies of more potent long-acting bNAbs as adjunct treatment with antiretrovirals to prevent infant HIV-1 transmission.

Keywords: HIV-1; HIV-1 prevention; VRC01; VRC01LS; bNAb; broadly neutralizing antibodies; monoclonal antibodies; neonates; passive immunization; perinatal HIV-1 transmission; pharmacokinetics.

Publication types

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

MeSH terms

  • Anti-Retroviral Agents / administration & dosage*
  • Anti-Retroviral Agents / therapeutic use
  • Antibodies, Monoclonal / administration & dosage
  • Antibodies, Monoclonal / adverse effects
  • Antibodies, Monoclonal / pharmacokinetics*
  • Broadly Neutralizing Antibodies / administration & dosage
  • Broadly Neutralizing Antibodies / pharmacology*
  • Dose-Response Relationship, Drug
  • Female
  • HIV Antibodies* / administration & dosage
  • HIV Antibodies* / adverse effects
  • HIV Infections / blood
  • HIV Infections / drug therapy
  • HIV Infections / prevention & control*
  • HIV-1 / drug effects*
  • HIV-1 / immunology
  • HIV-1 / pathogenicity
  • Half-Life
  • Humans
  • Infant, Newborn
  • Infectious Disease Transmission, Vertical / prevention & control*
  • Male

Substances

  • Anti-Retroviral Agents
  • Antibodies, Monoclonal
  • Broadly Neutralizing Antibodies
  • HIV Antibodies
  • VRC01 monoclonal antibody