Val-Cit-PAB-MMAE is a drug-linker conjugate for antibody-drug conjugates (ADCs) consisting of a cleavable peptide linker Val-Cit-PAB and a highly potent microtubule inhibitor MMAE (methylaurestatin E)[1, 2]. MMAE is a synthetic antitumor drug that can be bound to a monoclonal antibody (MAB) to direct it to cancer cells[3]. As a core component of ADCs, Val-Cit-PAB-MMAE is widely used in the development of targeted anticancer drugs. Through antibody-mediated precise delivery, this linker system can achieve efficient and controllable drug release, improve therapeutic efficacy, and reduce systemic toxicity[4].
References:
[1] Watanabe T, Arashida N, Fujii T, et al. Exo-cleavable linkers: enhanced stability and therapeutic efficacy in antibody–drug conjugates[J]. Journal of medicinal chemistry, 2024, 67(20): 18124-18138.
[2] Fang P, You M, Cao Y, et al. Development and validation of bioanalytical assays for the quantification of 9MW2821, a nectin-4-targeting antibody–drug conjugate[J]. Journal of Pharmaceutical and Biomedical Analysis, 2024, 248: 116318.
[3] Yao X, Jiang J, Wang X, et al. A novel humanized anti-HER2 antibody conjugated with MMAE exerts potent anti-tumor activity[J]. Breast cancer research and treatment, 2015, 153(1): 123-133.
[4] Yap M L, McFadyen J D, Wang X, et al. Activated platelets in the tumor microenvironment for targeting of antibody-drug conjugates to tumors and metastases[J]. Theranostics, 2019, 9(4): 1154.
Val-Cit-PAB-MMAE是一种用于抗体药物偶联物（ADC）的药物-连接子偶联物，由可裂解的肽连接子Val-Cit-PAB和高效的微管蛋白抑制剂MMAE（一甲基澳瑞他汀E）组成[1, 2]。MMAE是一种合成抗肿瘤药物，它可以结合到单克隆抗体（MAB）上，使其导向癌细胞[3]。作为ADC的核心组成部分，Val-Cit-PAB-MMAE广泛应用于靶向抗癌药物的开发，通过抗体介导的精准递送，该连接子系统能够实现高效、可控的药物释放，提升治疗效果并降低系统性毒性[4]。