The United States Food and Drug Administration (FDA) has approved a plethora of peptide-based drugs as effective drugs in cancer therapy. Peptides possess high specificity, permeability, target engagement, and a tolerable safety profile. They exhibit selective binding with cell surface receptors and proteins, functioning as agonists or antagonists. They also serve as imaging agents for diagnostic applications or can serve a dual-purpose as both diagnostic and therapeutic (theragnostic) agents. Therefore, they have been exploited in various forms, including linkers, peptide conjugates, and payloads. In this review, the FDA-approved prostate-specific membrane antigen (PSMA) peptide antagonists, peptide receptor radionuclide therapy (PRRT), somatostatin analogs, antibody–drug conjugates (ADCs), gonadotropin-releasing hormone (GnRH) analogs, and other peptide-based anticancer drugs are analyzed in terms of their chemical structures and properties, therapeutic targets and mechanisms of action, development journey, administration routes, and side effects.
美国食品药品监督管理局（FDA）已批准大量肽类药物作为癌症治疗的有效药物。肽类物质具有高特异性、高渗透性、靶向结合能力强及可耐受的安全性特征。它们能够选择性结合细胞表面受体和蛋白质，发挥激动剂或拮抗剂功能；同时可作为诊断应用的显像剂，或兼具诊断与治疗双重功能（诊疗一体化）。因此，肽类物质已以多种形式应用于临床，包括连接子、肽缀合物及有效载荷等。本综述从化学结构与特性、治疗靶点与作用机制、研发历程、给药途径及副作用等方面，系统分析了FDA批准的前列腺特异性膜抗原（PSMA）肽拮抗剂、肽受体放射性核素治疗（PRRT）、生长抑素类似物、抗体偶联药物（ADCs）、促性腺激素释放激素（GnRH）类似物及其他肽类抗癌药物。
Peptide Therapeutics: Unveiling the Potential against Cancer—A Journey through 1989
肿瘤(癌症)患者之家