Success of glaucoma filtration surgery is influenced by the wound healing response. Attention has been focused on pharmacological agents to control a process that leads to excessive scarring and eventual failure of glaucoma filtration surgery. Several agents, including 5-fluorouracil and mitomycin C, as well as other antiproliferative drugs will be discussed. Newer antifibrotic agents and novel drug delivery systems are under development in tissue culture and animal models in an effort to improve efficacy and safety. This article summarizes current treatment modalities and future prospects to prevent excessive wound healing and improve the success of glaucoma filtration surgery.