Department of Synthetic Organic Chemistry, Graduate School of Biomedical and Health Sciences, Hiroshima University.
Chem Pharm Bull (Tokyo). 2024;72(2):136-142. doi: 10.1248/cpb.c23-00535.
In the aging global population, prostate cancer is a worldwide health problem because the incidence rate of this disease increases at advanced ages. Although early-stage prostate cancer can be treated by total prostatectomy, the surgery causes side effects, such as incontinence and dysuria, that lower QOL. Once the disease progresses to metastatic castration-resistant prostate cancer (mCRPC), there are no effective chemotherapeutic agents without systematic side effects. Therefore, targeted therapies for mCPRC are urgently needed. Traditional antibody-drug conjugate treatments for prostate cancer have been tested in clinical trials and several side effects have been observed. Meanwhile, small-molecule drug conjugates (SMDCs) have certain advantages over antibody drug conjugates in terms of non-immunogenicity, reproducibility, and permeability. In this review, prostate-specific membrane antigen-targeted SMDCs for treating prostate cancer are summarized.
在全球人口老龄化的背景下，前列腺癌是一个全球性的健康问题，因为这种疾病的发病率在高龄时会增加。虽然早期前列腺癌可以通过全前列腺切除术治疗，但手术会导致尿失禁和排尿困难等副作用，从而降低生活质量。一旦疾病进展为转移性去势抵抗性前列腺癌（mCRPC），就没有没有系统性副作用的有效化疗药物。因此，迫切需要针对 mCPRC 的靶向治疗方法。针对前列腺癌的传统抗体药物偶联物治疗已在临床试验中进行了测试，并观察到了几种副作用。同时，小分子药物偶联物（SMDC）在非免疫原性、重现性和通透性方面比抗体药物偶联物具有一定的优势。在这篇综述中，总结了用于治疗前列腺癌的前列腺特异性膜抗原靶向 SMDC。
