Osteoarthritis (OA) is an age-related degenerative disease, which is characterized by chronic joint pain, inflammation and the damage of joint cartilage. At present, steroidal drugs and nonsteroidal anti-inflammatory drugs (NSAIDS), selective cyclooxygenase-2 (COX-2) inhibitors, are the first-line drugs for the treatment of OA. However, these drugs could lead to some cardiovascular side effects. Therefore, it is urgent to develop novel agents for the treatment of OA. Matrix metalloproteinase-13 (MMP-13), an important member of matrix metalloproteinases (MMPs) family, plays a vital role by degrading type II collagen in articular cartilage and bone in OA. It is noted that MMP-13 is specially expressed in the OA patients, and not in normal adults. In addition, broadspectrum MMP inhibitors could result in some painful and joint-stiffening side effects, called musculoskeletal syndrome (MSS) in the clinical trials. Thus, developing selective MMP-13 inhibitors is a potential strategy for the therapy of OA. In this review, we summarize the recent progress of selective MMP-13 inhibitors including two subfamilies, namely zinc-binding and non-zinc-binding selective MMP-13 inhibitors.

骨关节炎（OA）是一种与年龄有关的变性疾病，其特征在于慢性关节痛，炎症和关节软骨损伤。目前，甾体药物和非甾体抗炎药（NSAIDS），选择性环氧合酶2（COX-2）抑制剂是治疗OA的一线药物。但是，这些药物可能导致某些心血管副作用。因此，迫切需要开发用于治疗OA的新型药物。基质金属蛋白酶-13（MMP-13）是基质金属蛋白酶（MMPs）家族的重要成员，它通过降解OA的关节软骨和骨骼中的II型胶原发挥重要作用。应当指出，MMP-13在OA患者中特别表达，而不在正常成年人中表达。此外，广谱MMP抑制剂可能导致某些疼痛和关节僵硬的副作用，在临床试验中称为肌肉骨骼综合症（MSS）。因此，开发选择性MMP-13抑制剂是治疗OA的潜在策略。在这篇综述中，我们总结了选择性MMP-13抑制剂的最新进展，包括两个亚家族，即锌结合和非锌结合选择性MMP-13抑制剂。