专利名称: Linker-drug and antibody-drug conjugate (ADC) employing the same
专利号: EP3335734A1
公开日期: 2018年6月20日
发明者: Maggie Lu 等

摘要 / Abstract

Antibody-drug conjugates (ADCs) represent an innovative approach in targeted cancer therapy.
抗体-药物偶联物（ADC）是一种用于癌症治疗的创新靶向技术。

This patent (EP3335734A1) describes novel linker-drug compounds that enhance the stability and efficacy of ADCs.
本专利（EP3335734A1）描述了一种新型连接子-药物化合物，旨在提高ADC的稳定性和疗效。

连接子-药物的特点与应用 / Features and Applications of Linker-Drug Compounds

1. Stable in Circulation / 血液中稳定
   • o Designed to prevent premature drug release in the bloodstream.
   • o 设计目的是防止药物在血液中过早释放。
2. Efficient Drug Release / 高效药物释放
   • o Responsive to tumor-specific conditions, such as pH changes or enzymatic activity.
   • o 可响应肿瘤特定环境（如pH值变化或酶活性）。
3. Versatile Antibody Conjugation / 多样化抗体结合
   • o Can be conjugated to various antibodies for personalized therapy.
   • o 可与多种抗体结合，用于个性化治疗。

作用机制与前景 / Mechanism and Future Prospects

The ADC binds to cancer-specific antigens and delivers the cytotoxic drug directly to tumor cells.
ADC通过靶向肿瘤特异性抗原，将细胞毒药物直接递送到肿瘤细胞。

Future research will focus on optimizing linker-drug properties to address various cancer types.
未来研究将重点优化连接子-药物的特性，以应对不同癌症类型。

总结 / Conclusion

The patent EP3335734A1 provides a promising framework for the development of next-generation ADCs.
专利EP3335734A1为下一代ADC的开发提供了一个有前景的框架。

By leveraging these innovative linker-drug compounds, precision medicine can achieve higher efficacy and safety in cancer treatment.
通过利用这些创新的连接子-药物化合物，精准医学可以在癌症治疗中实现更高的疗效和安全性。

Compounds and CAS Numbers / 化合物及其CAS号

Below are related compounds categorized by their functions in ADC development:

以下是按照ADC开发功能分类的相关化合物：

1. Linker-Related Compounds / 连接子相关化合物

- Boc-NH-PEG4-CH2COOH (A cleavable linker used in ADCs.)
  CAS: 876345-13-0

- Fmoc-NH-PEG4-CH2COOH (A PEG-based linker widely used in ADC development.)
  CAS: 437655-95-3

2. Cytotoxic Payloads / 细胞毒药物

- MMAE (Monomethyl auristatin E) (A microtubule inhibitor used in many ADCs.)
  CAS: 474645-27-7

- MMAF (Monomethyl auristatin F) (A hydrophilic variant of MMAE.)
  CAS: 745017-94-1

- Doxorubicin (An anti-tumor antibiotic used in ADCs.)
  CAS: 23214-92-8

3. Antibody Modification Reagents / 抗体修饰试剂

- Sulfo-SMCC (A crosslinker for thiol groups on antibodies.)
  CAS: 92921-24-9

Conclusion / 总结

The compounds listed above are integral to the development of antibody-drug conjugates and align with the innovations described in the patent EP3335734A1.
以上列出的化合物是抗体-药物偶联物开发的重要组成部分，与专利EP3335734A1中描述的创新相一致。