Apolipoprotein A-I Mimetic Peptide L-4F Removes Bruch's Membrane Lipids in Aged Nonhuman Primates

Invest Ophthalmol Vis Sci. 2019 Feb 1;60(2):461-472. doi: 10.1167/iovs.18-25786.

Abstract

Purpose: Multiple evidence lines support Bruch's membrane lipid deposition as a major precursor of soft drusen and age-related macular degeneration as including a potentially treatable atherosclerosis-like progression in the subretinal pigment epithelium (RPE)-basal lamina space. We evaluated the effect of anti-inflammatory, antiatherogenic peptide L-4F on Bruch's membrane of aged nonhuman primates in a dose-escalating study.

Methods: Macaca fascicularis ≥20 years of age evaluated by color fundus photography and optical coherence tomography received monocular intravitreal injections of L-4F (n = 7) or a placebo-scrambled peptide (n = 2) in 6 doses of 25 to 175 μg over 6 months. Eyes were processed for detection and masked semiquantitative assessment of macular Bruch's membrane neutral lipid (oil red O staining), esterified cholesterol (filipin histochemistry), membrane attack complex (immunofluorescence), and paramacular thickness (transmission electron microscopy).

Results: Bruch's membrane neutral lipid, esterified cholesterol, and membrane attack complex were cleared and ultrastructure was improved in L-4F-injected eyes, compared to placebo-injected eyes. Fellow eyes were also affected to the same degree as the injected eyes. Punctate yellow fundus lesions without corresponding RPE elevations on optical coherence tomography correlated to RPE lipoidal degeneration (engorgement with lipid droplets), which was unchanged by this treatment.

Conclusions: Clinical-stage apolipoprotein A-I mimetic peptide L-4F, delivered intravitreally in repeated doses, produced a substantial pharmacologic reduction of Bruch's membrane lipid and restoration of ultrastructure in a nonhuman primate model that exhibits an important precursor of soft drusen, if not soft drusen themselves.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aging / physiology*
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Azo Compounds / metabolism
  • Bruch Membrane / drug effects*
  • Bruch Membrane / metabolism
  • Bruch Membrane / ultrastructure
  • Complement Membrane Attack Complex / metabolism
  • Dose-Response Relationship, Drug
  • Filipin / metabolism
  • Fundus Oculi
  • Histocytochemistry / methods
  • Intravitreal Injections
  • Macaca fascicularis
  • Membrane Lipids / metabolism*
  • Microscopy, Electron, Transmission
  • Multimodal Imaging
  • Peptides / administration & dosage
  • Peptides / pharmacology*
  • Photography
  • Tomography, Optical Coherence

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Azo Compounds
  • Complement Membrane Attack Complex
  • Membrane Lipids
  • Peptides
  • apolipoprotein A-I mimetic peptide 4F
  • Filipin
  • oil red O