Fibrogenesis, as occurs in wound healing and fibrotic diseases, involves oxidative stress and inflammation followed by fibrosis. Pirfenidone is an orally active small molecule drug with antioxidant, anti-inflammatory, and anti-fibrotic effects. It has numerous cellular and in vivo effects, including the reduction of inflammatory cytokine production, suppression of TGF-β expression and TGF-mediated collagen I expression, and diminution of markers of oxidative stress. Pirfenidone has demonstrated effectiveness in both animal and human idiopathic pulmonary fibrosis. Moreover, it has use in other conditions with a significant fibrotic component, including tissue scarring, liver fibrosis, and diabetic nephropathy.