BioCentury
ARTICLE | Distillery Therapeutics

Therapeutics: Carbonic anhydrase I (CAI); CAII; CAIX; CAXII

May 14, 2015 7:00 AM UTC

In vitro and rabbit studies suggest carbonic anhydrase-inhibiting dendrimers could help treat glaucoma. Chemical synthesis and in vitro testing of poly(amidoamine) (PAMAM)-based dendrimers linked to multiple carbonic anhydrase-inhibiting benzenesulfonamide functional groups identified four lead compounds that inhibited the activity of CAI, CAII, CAIX and CAXII with potency comparable to or greater than dorzolamide. In a rabbit model of glaucoma, intraconjunctival application of a lead compound decreased intraocular pressure (IOP) - a measure of disease severity - with an increased duration of action compared with dorzolamide. Next steps could include testing the safety of the dendrimers in models of glaucoma...