Cleavable Linkers

Cleavable PEG Reagents play a crucial role in the success of antibody-drug conjugates. It determines the fate of the cytotoxic drug in the biological system. In order to make the ADC effective, it requires the Cleavable reagents to be stable enough in the blood circulation for a substantial amount of time to avoid side toxicity and to allow ADC to reach the target. It also requires the reagents to be labile so that they efficiently release corresponding payload in the tumor environment.

AxisPharm provides functionalized cleavable PEGs with disulfide bonds or photocleavable bonds. Different kinds of antibody-drug conjugates Reagents may be available by custom synthesis.

Cleavable linkers are a class of chemical compounds that connect different molecular entities, such as drugs and targeting molecules, in drug research and development. These linkers contain specific functional groups that enable their controlled and selective cleavage, releasing the desired components at the target site. This process allows for the delivery of drugs to specific cells or tissues, reducing off-target effects and increasing therapeutic efficacy.

Functional groups play a crucial role in the design and selection of cleavable linkers for drug development. Common functional groups used in cleavable linkers include disulfide bonds, esters, amides, and hydrazones. Each functional group has unique properties that can be exploited to control the release of drugs and increase their selectivity.

In drug development, the selection of an appropriate cleavable linker is essential for the success of the therapeutic agent. The choice of linker depends on factors such as the pharmacokinetics of the drug, the mechanism of action, and the target site. Additionally, the stability and cleavability of the linker need to be carefully considered to ensure that the drug is released at the desired location and rate.

Ref:

Ultimate Guide to Choosing the Right Cleavable Linker for ADCs 

Su Z, Xiao D, Xie F, Liu L, Wang Y, Fan S, Zhou X, Li S. Antibody-drug conjugates: Recent advances in linker chemistry. Acta Pharm Sin B. 2021 Dec;11(12):3889-3907. doi: 10.1016/j.apsb.2021.03.042. Epub 2021 Apr 6. PMID: 35024314; PMCID: PMC8727783.