α5β1-Integrin inhibitor (CLT-28643) effective in rabbit trabeculectomy model

Acta Ophthalmol. 2017 Feb;95(1):e1-e9. doi: 10.1111/aos.13215. Epub 2016 Aug 31.

Abstract

Purpose: Glaucoma filtration surgery (GFS) fails due to fibrosis. The α5β1-integrin plays a pivotal role in fibrosis, angiogenesis and inflammation. This is the first experiment evaluating the prevention of fibrosis after GFS by a specific small molecule α5β1-integrin inhibitor (CLT-28643).

Methods: Twenty-four rabbits received trabeculectomy on their right eyes. The rabbits were randomized into three groups of eight eyes each. CLT-28643 was given as a single subconjunctival injection intraoperatively to two of the right eye groups followed by postoperative vehicle eye drops (CLT+ group) or CLT-28643 eye drops 4 times daily (CLT++ group). A third group received mitomycin-C (MMC) intraoperatively (sponge application, 0.04%, 2 min) followed by vehicle eye drops postoperatively. The control-surgery group consisted of 12 left eyes having trabeculectomy with no adjunctive therapy. The remaining 12 left eyes formed the untreated group. Clinical assessment included intraocular pressure (IOP) measurement, slit-lamp examination (including bleb survival and morphology) and bleb photography. The rabbits were killed after four weeks for histology.

Results: Both CLT-28643-treated groups showed significantly prolonged bleb survival, and better bleb score compared to the control-surgery group. At end of the study, most functioning blebs were found in the MMC group (MMC group 75%; CLT+ group 12.5%, CLT++ group 25%; CLT+ group 12.5%, control-surgery group 0%). CLT-28643 was non-toxic and well tolerated.

Conclusions: This rabbit GFS study indicates that inhibition of α5β1-integrin by the novel α5β1-integrin antagonist CLT-28643 significantly improved the outcome. The effect of a single intro-operative application of CLT-28643 seems to be inferior to 0.04% MMC.

Keywords: CLT-28643; bleb; glaucoma surgery; intraocular pressure; mitomycin; trabeculectomy; α5β1-integrin.

MeSH terms

  • Administration, Topical
  • Alkylating Agents / administration & dosage
  • Aminoquinolines / pharmacology*
  • Animals
  • Collagen / metabolism
  • Conjunctiva / metabolism
  • Conjunctiva / pathology*
  • Disease Models, Animal*
  • Fibrosis / prevention & control
  • Glaucoma / surgery
  • Injections, Intraocular
  • Integrin alpha5beta1 / antagonists & inhibitors*
  • Intraocular Pressure / drug effects
  • Male
  • Mitomycin / administration & dosage
  • Ophthalmic Solutions
  • Rabbits
  • Surgical Stomas*
  • Trabeculectomy*
  • Wound Healing / drug effects*

Substances

  • Alkylating Agents
  • Aminoquinolines
  • CLT-28643
  • Integrin alpha5beta1
  • Ophthalmic Solutions
  • Mitomycin
  • Collagen