Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent. Because of its toxicity, it cannot be used as a drug itself; instead, it is linked to a monoclonal antibody (MAB) which directs it to the cancer cells.

Background: Monomethyl auristatin E (MMAE) has been used as a payload for several Food and Drug Administration (FDA) approved antibody-drug conjugates (ADCs). It is known that MMAE is released from the ADC following binding, internalisation and proteolytic degradation in …

2022年7月5日 · Tumor-directed antibodies and peptides conjugated to radiosensitizing monomethyl auristatin E (MMAE) specifically produce CD8 T cell dependent durable tumor control of irradiated tumors and...

2024年9月25日 · In this study, we prepared humanized anti-TF Ab (clone.1084) conjugated with monomethyl auristatin E (MMAE) or deruxtecan (DXd), and evaluated the efficacy in several cell line- and patient-derived xenograft models of pancreatic cancer.

Monomethyl auristatin F (MMAF), which also inhibits cellular division via inhibition of tubulin polymerization, has attenuated activity compared to MMAE due to the presence of a charged C-terminal phenylalanine. Taking a typical auristatin-based ADCs – brentuximab vedotinas as an example, MOA of MMAE is showed as the figure 3.

2023年11月9日 · 抗体药物偶联物 （antibody-drug conjugate，ADC）是一类用于治疗癌症的新兴靶向疗法，旨在将小分子化疗直接递送并杀伤肿瘤细胞，同时保留健康细胞。 自2000年MYLOTARG成功获批以来，抗体药物偶联物（ADC）已成为癌症靶向治疗的关键类别，它主要包含三部分： 单克隆抗体 、 连接子 和 毒素。 单克隆抗体是决定ADC疗效的关键；连接子决定着ADC药物系统毒性及临床疗效；毒素是决定ADC药物杀伤力大小的关键因素。 尽管目前公布 …

Auristatins are important payloads used in antibody drug conjugates (ADCs), and the most well-known compound family member, monomethyl auristatin (MMAE), is used in two Food and Drug Administration (FDA)-approved ADCs, Adcetris ® and Polivy ®. Multiple other auristatin-based ADCs are currently being evaluated in human clinical trials and ...

2021年6月15日 · Monomethyl auristatin E (MMAE) is a potent anti-cancer microtubule-targeting agent (MTA) used as a payload in three approved MMAE-containing antibody drug conjugates (ADCs) and multiple ADCs in clinical development to treat different types of cancers.

Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.

2022年11月3日 · Monomethyl auristatin E (MMAE) and monomethyl auristatin F (MMAF) are identified as the best analogs of dolastatin 10, which bind to microtubules and prevent cell proliferation by inhibiting mitosis. Their molecules are highly stable and show no signs of degradation in plasma, liver lysosomal extracts or proteases such as cathepsin B.