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培维索孟是使生长激素(GH)发生突变后再通过聚乙二醇化所产生的第一个生长激素受体(GHR)拮抗剂,也是目前唯一一个应用于临床治疗肢端肥大症的GHR拮抗剂。与传统治疗手段(手术、放疗、多巴胺激动剂及生长抑素类似物)不同,它直接作用于外周的GHR,阻止其形成功能性的二聚体,从而阻断GHR后续的信号转导,使肢端肥大症患者血胰岛素样生长因子Ⅰ(IGF-Ⅰ)水平恢复正常,有效地改善肢端肥大症患者的临床症状及代谢紊乱。培维索孟半衰期长,使用也相对较为安全。文章将从该药的作用机制、代谢、临床用途和副作用四个方面作一初步介绍。
Pegvisomant is the first growth hormone receptor (GHR) antagonist produced by the mutation of growth hormone (GH) and then pegylated, and is the only GHR used in clinical treatment of acromegaly Antagonists. Unlike traditional therapies (surgery, radiotherapy, dopamine agonists and somatostatin analogues), it acts directly on the peripheral GHRs, preventing them from forming functional dimers, thereby blocking the subsequent signal transduction of GHR, Acromegaly patients with blood insulin-like growth factor Ⅰ (IGF-Ⅰ) levels returned to normal, effectively improve the acromegaly patients with clinical symptoms and metabolic disorders. Pevisosone has a long half-life and is relatively safe to use. This article will make a preliminary introduction from four aspects of the drug’s mechanism of action, metabolism, clinical use and side effects.