Wang Lumin, Qiu Qining, Yang Dawei, Cao Chang, Lu Yanqin, Zeng Yulan, Jiang Weiwen, Shen Yun, Ye Yanrong
Zhongshan Hospital (Xiamen), Fudan University, Xiamen, Fujian Province, China.
Zhongshan Hospital, Fudan University, Shanghai, China.
Front Pharmacol. 2024 Mar 22;15:1173240. doi: 10.3389/fphar.2024.1173240. eCollection 2024.
Rapamycin, an established mTOR inhibitor in clinical practice, is widely recognized for its therapeutic efficacy. Ridaforolimus, a non-prodrug rapalog, offers improved aqueous solubility, stability, and affinity compared to rapamycin. In recent years, there has been a surge in clinical trials involving ridaforolimus. We searched PubMed for ridaforolimus over the past decade and selected clinical trials of ridaforolimus to make a summary of the research progress of ridaforolimus in clinical trials. The majority of these trials explored the application of ridaforolimus in treating various tumors, including endometrial cancer, ovarian cancer, prostate cancer, breast cancer, renal cell carcinoma, and other solid tumors. These trials employed diverse drug combinations, incorporating agents such as ponatinib, bicalutamide, dalotuzumab, MK-2206, MK-0752, and taxanes. The outcomes of these trials unveiled the diverse potential applications of ridaforolimus in disease treatment. Our review encompassed analyses of signaling pathways, ridaforolimus as a single therapeutic agent, its compatibility in combination with other drugs, and an assessment of adverse events (AEs). We conclude by recommending further research to advance our understanding of ridaforolimus's clinical applications.
雷帕霉素是临床实践中一种成熟的mTOR抑制剂,其治疗效果广为人知。地磷莫司,一种非前药雷帕霉素类似物,与雷帕霉素相比,具有更好的水溶性、稳定性和亲和力。近年来,涉及地磷莫司的临床试验激增。我们在过去十年里在PubMed上搜索了地磷莫司,并选择了地磷莫司的临床试验来总结其在临床试验中的研究进展。这些试验大多探索了地磷莫司在治疗各种肿瘤中的应用,包括子宫内膜癌、卵巢癌、前列腺癌、乳腺癌、肾细胞癌和其他实体瘤。这些试验采用了多种药物组合,纳入了波纳替尼、比卡鲁胺、达洛珠单抗、MK-2206、MK-0752和紫杉烷类等药物。这些试验的结果揭示了地磷莫司在疾病治疗中的多种潜在应用。我们的综述包括对信号通路的分析、地磷莫司作为单一治疗药物、其与其他药物联合使用的相容性以及对不良事件(AE)的评估。我们最后建议进一步开展研究,以增进我们对 地磷莫司临床应用的了解。