Complement factor D-IN-1 is an effective and selective small-molecule reversible factor d inhibitor (IC50s: 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively).

FD:0.006 μM, MAC:0.05 μM

Complement factor D-IN-1 displays similar potency against human and monkey FD (IC50s: 0.005 μM in FD thioesterolytic assays and 0.011 μM in 50% serum MAC deposition assays for both human and monkey) [1].

Complement factor D-IN-1 shows an excellent oral PK profile in Sprague–Dawley rats and, following an oral dose (10 mg/kg) in Brown Norway rats, demonstrates a good distribution and sustained exposure in ocular tissues including the neural retina. Mean exposure levels in plasma, the PEC, and the retina at 6 h after dosing are 0.36, 0.43, and 0.09 μM, respectively [1].