Accumulating research substantiates the statement that inflammation plays an important role in the development of stroke. Both proinflammatory and anti-inflammatory mediators are involved in the pathogenesis of stroke, an imbalance of which leads to inflammation. Anti-inflammation is a kind of hopeful strategy for the prevention and treatment of stroke. Substantial studies have demonstrated that minocycline, a second-generation semisynthetic antibiotic belonging to the tetracycline family, can inhibit neuroinflammation, inflammatory mediators and microglia activation, and improve neurological outcome. Experimental and clinical data have found the preclinical and clinical potential of minocycline in the treatment of stroke due to its anti-inflammation properties and anti-inflammation-induced pathogeneses, including antioxidative stress, antiapoptosis, inhibiting leukocyte migration and microglial activation, and decreasing matrix metalloproteinases activity. Hence, it suggests a great future for minocycline in the therapeutics of stroke that diminish the inflammatory progress of stroke.