PF 00337210

PF-00337210 is a potent and selective inhibitor of VEGFRs, designed for treating age-related macular degeneration via intravitreal injection. The formulation strategy focused on developing an ophthalmic solution that would precipitate upon injection into the vitreous, ensuring sustained drug delivery. Challenges included maintaining low dosing volumes, selecting safe excipients for intravitreal use, and addressing the drug's unique physicochemical properties. The final formulation, an isotonic solution in a citrate-buffered vehicle with NaCl, demonstrated stability, potency, and recovery through intravitreal dosing syringes. It formed a depot upon injection into vitreous humor, representing a novel nonpolymeric in situ-forming depot formulation for intravitreal drug delivery.

• Data Sheet (270 KB)