2024年2月1日 · In this study, a Fab-nondestructive ADC loaded with maytansine (DM1) (T-NPLG-DM135) was prepared with drug-to-antibody ratio (DAR) of up to 35 by utilizing the carboxyl groups on the side-chain of poly (L-glutamic acid) (PLG) as the payload binding sites.

2019年12月16日 · DM1 has a narrow therapeutic window for oncology, but its linkage to trastuzumab, with an average of 3.5 linker-payload molecules per antibody (drug–antibody ratio [DAR] of 3.5), selectively...

2018年2月20日 · In this study, the stability of Trastuzumab (recombinant humanized IgG1 mAb, targeting HER2 receptor) and its ADC with DM1 (anti-tubulin anticancer drug), Trastuzumab emtansine (T-DM1) were studied. SE-HPLC was used to monitor formation of aggregates and/or fragments of the monoclonal antibodies (mAb).

2021年8月23日 · t-dm1中平均每个抗体分子能够携带3.5个dm1效应分子，具有比较理想的药物抗体比（dar）。 尽管理论上较高的DAR值对应更强的药效，然而随着DAR增加，ADC的疏水性以及抗体分子天然结构受到的影响也会增加，最终导致药物分子的清除率增高，体内半衰期降低[7,8]。

TDM1即恩美曲妥珠单抗，商品名为赫塞莱，是乳腺癌中第一款ADC药物，于2019年在美国上市。 T-DM1由抗体部分（Trastuzumab，即曲妥珠单抗）、化疗药部分（DM1，即美坦新衍生物，一种微管蛋白抑制剂）及将二者连接起来的连接子（不可裂解的硫醚连接子）组成。 恩美曲妥珠单抗简要说明书： 药品中文名：注射用恩美曲妥珠单抗. 药品英文名：Trastuzumab Emtansine for Injection. 药品商品名：赫赛莱®/Kadcyla®. 研发代号：T-DM1. 研发公司：罗氏制药有. 规 …

2013年12月1日 · Here, we present results from preclinical studies characterizing the toxicity profile of T-DM1, including limited assessment of unconjugated DM1. T-DM1 binds primate ErbB2 and human HER2 but not the rodent homolog c-neu.

2014年6月26日 · Ado-trastuzumab emtansine (T-DM1) is an antibody–drug conjugate that combines the antitumor properties of the humanized anti-human epidermal growth factor receptor 2 (HER2) antibody, trastuzumab, with the maytansinoid, DM1, a potent microtubule-disrupting agent, joined by a stable linker.

2017年10月15日 · DS-8201a has a drug-to-antibody-ratio (DAR) of 8, which is higher than that of T-DM1 (3.5). Owing to these unique characteristics and unlike T-DM1, DS-8201a is effective against cancers with low-HER2 expression.

T-DM1 comprises trastuzumab linked to DM1 (0–8 DM1 molecules per antibody) using the heterobifunctional reagent succinimidyl-trans-4-[maleimidylmethyl] cyclohexane-1-carboxylate, a stable thioether linker that binds primarily to antibody lysine residues [7–9].

糖基化的t-dm1 在本研究中，我们选用曲妥珠单抗-恩他辛 (t-dm1)作为研究 对象，主要用于治疗her-2阳性转移性乳腺癌。t-dm1由曲妥珠单 抗通过赖氨酸残基共价结合具有细胞毒性的dm1药物分子，结构 如图1所示。当t-dm1被靶细胞内化后，细胞毒性药物分子将被释