Ismuha Ratu Ralna, Ritawidya Rien, Daruwati Isti, Muchtaridi Muchtaridi
Department of Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang 45363, Indonesia.
Department of Pharmacy, Dharmais Cancer Hospital-National Cancer Center, Jakarta 11420, Indonesia.
Molecules. 2024 Dec 23;29(24):6062. doi: 10.3390/molecules29246062.
Prostate cancer ranks as the fourth most common cancer among men, with approximately 1.47 million new cases reported annually. The emergence of prostate-specific membrane antigen (PSMA) as a critical biomarker has revolutionized the diagnosis and treatment of prostate cancer. Recent advancements in low-molecular-weight PSMA inhibitors, with their diverse chemical structures and binding properties, have opened new avenues for research and therapeutic applications in prostate cancer management. These novel agents exhibit enhanced tumor targeting and specificity due to their small size, facilitating rapid uptake and localization at the target site while minimizing the retention in non-target tissues. The primary aim of this study is to evaluate the potential of low-molecular-weight PSMA inhibitors labeled with radioisotopes as theranostic agents for prostate cancer. This includes assessing their efficacy in targeted imaging and therapy and understanding their pharmacokinetic properties and mechanisms of action. This study is a literature review focusing on in vitro and clinical research data. The in vitro studies utilize PSMA-targeted radioligands labeled with radioisotopes to assess their binding affinity, specificity, and internalization in prostate cancer cell lines. Additionally, the clinical studies evaluate the safety, effectiveness, and biodistribution of radiolabeled PSMA ligands in patients with advanced prostate cancer. The findings indicate promising outcomes regarding the safety and efficacy of PSMA-targeted radiopharmaceuticals in clinical settings. The specific accumulation of these agents in prostate tumor lesions suggests their potential for various applications, including imaging and therapy. This research underscores the promise of radiopharmaceuticals targeting PSMA in advancing the diagnosis and treatment of prostate cancer. These agents improve diagnostic accuracy and patients' outcomes by enhancing imaging capabilities and enabling personalized treatment strategies.
前列腺癌是男性中第四大常见癌症，每年报告的新病例约为147万例。前列腺特异性膜抗原（PSMA）作为一种关键生物标志物的出现，彻底改变了前列腺癌的诊断和治疗。低分子量PSMA抑制剂的最新进展，因其多样的化学结构和结合特性，为前列腺癌管理的研究和治疗应用开辟了新途径。这些新型药物由于体积小，具有增强的肿瘤靶向性和特异性，便于在靶部位快速摄取和定位，同时最大限度地减少在非靶组织中的滞留。本研究的主要目的是评估放射性同位素标记的低分子量PSMA抑制剂作为前列腺癌诊疗药物的潜力。这包括评估它们在靶向成像和治疗中的疗效，以及了解它们的药代动力学特性和作用机制。本研究是一篇聚焦于体外和临床研究数据的文献综述。体外研究利用放射性同位素标记的PSMA靶向放射性配体，评估它们在前列腺癌细胞系中的结合亲和力、特异性和内化情况。此外，临床研究评估放射性标记的PSMA配体在晚期前列腺癌患者中的安全性、有效性和生物分布。研究结果表明，PSMA靶向放射性药物在临床环境中的安全性和疗效前景良好。这些药物在前列腺肿瘤病变中的特异性积聚表明它们在包括成像和治疗在内的各种应用中的潜力。这项研究强调了靶向PSMA的放射性药物在推进前列腺癌诊断和治疗方面的前景。这些药物通过增强成像能力和实现个性化治疗策略，提高了诊断准确性和患者的治疗效果。
