Incorporation of Hydrophilic Macrocycles Into Drug-Linker Reagents Produces Antibody-Drug Conjugates With Enhanced in vivo Performance

Antibody-drug conjugates (ADCs) have begun to fulfill their promise as targeted cancer therapeutics with ten clinical approvals to date. Recently the role that linker-payload reagent design has on the properties of ADCs has been highlighted as an important consideration for developers. In this paper from Abzena, the effect of incorporating hydrophilic macrocycles like cyclodextrin into reagent structures on the in vitro and in vivo behavior of ADCs.

Nick EvansRuslan GrygorashNicolas CamperMark FrigerioMatthew Bird et al

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Prostate-specific membrane antigen (PSMA) ligands comprising an amylase cleavable linker

Using sugars in a prodrug concept is a fascinating idea as these compounds can bring so much to the table like improve stability, PK, or help in targeting. In this patent from Heidelberg University oligosaccharide conjugated prostate-specific membrane antigens are described where the bonds are cleaved by amylase in the body.

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