In some cases, modulation of wound healing, in association with glaucoma filtration surgery, results in lower postoperative intraocular pressures than would occur without such therapy. Treatments affecting wound healing increase the likelihood of achieving long-term filtration, especially in eyes with a poor surgical prognosis. After summarizing the wound-healing process following filtration procedures, we review the mechanism of action, the effectiveness, and the complications associated with some of the most commonly used wound healing inhibitors and then discuss new alternatives currently under investigation. Although much progress has been made, the challenge remains to develop new drugs or combinations of drugs that are less toxic and can yield more predictable results.