A Concise Synthetic Approach to Highly Reactive Click-to-Release Trans-Cyclooctene Linkers

Liu, Bing; Hoeve, Wolter ten; Versteegen, Ron M.; Rossin, Raffaella; Kleijn, Laurens H. J.; Robillard, Marc S.

doi:10.26434/chemrxiv-2022-xrq3p-v2

Cited by 1 publication

(1 citation statement)

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“…Besides, to address the low DAR of conventional coupling techniques, Dantari's T‐HDC technology “packages” the payload by using polymer molecules and then couples the polymer‐packaged payload to the antibody. This load‐release system can carry more payloads, and one antibody can carry more than 60 payload molecules [78]. Dolaflexin, a multiwarhead ADC platform of Mersana, also uses polymers to develop high DAR ADC drugs.…”

Section: Future Developments On Adcsmentioning

confidence: 99%

Development of antibody‐drug conjugates in cancer: Overview and prospects

Ruan,

Wu,

Meng

et al. 2023

Cancer Communications

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In recent years, remarkable breakthroughs have been reported on antibody‐drug conjugates (ADCs), with 15 ADCs successfully entering the market over the past decade. This substantial development has positioned ADCs as one of the fastest‐growing domains in the realm of anticancer drugs, demonstrating their efficacy in treating a wide array of malignancies. Nonetheless, there is still an unmet clinical need for wider application, better efficacy, and fewer side effects of ADCs. An ADC generally comprises an antibody, a linker and a payload, and the combination has profound effects on drug structure, pharmacokinetic profile and efficacy. Hence, optimization of the key components provides an opportunity to develop ADCs with higher potency and fewer side effects. In this review, we comprehensively reviewed the current development and the prospects of ADC, provided an analysis of marketed ADCs and the ongoing pipelines globally as well as in China, highlighted several ADC platforms and technologies specific to different pharmaceutical enterprises and biotech companies, and also discussed the new related technologies, possibility of next‐generation ADCs and the directions of clinical research.

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Section: Future Developments On Adcsmentioning

confidence: 99%