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PROLOR's RevPEG technology is complimentary to the CTP technology and allows the development of long-acting small peptides and small chemical molecules for which CTP is not suitable.
Conventional PEGylation technology is based on the conjugation of the peptide or small molecule to a PEG chain -- resulting in extended circulation time in the body. However, the PEG chain is very large in comparison to the drug molecule, and in some case creates great interference in the ability of the drug molecule to provide proper biological activity.
In contrast, the RevPEG technology is based on the conjugation of the peptide or small molecule to a PEG chain via a hydrolizable linker. The PEG chain and the linker slowly detach from the drug molecule leaving the authentic drug molecule intact - resulting in extended circulation time in the body and proper biological activity.
The mechanism of action of many peptide and small molecule drugs requires their internalization into cells and/or crossing the blood brain barrier. In many PEGylated drugs the PEG chain interferes with this requirement due to the size and structure of the PEG chain. The controlled detachment from the PEG chain is therefore especially important for drugs that need to cross the blood brain barrier or penetrate through cellular membranes.