Library of optimized drug linker couples

The ADC platform can pe paired with enzyme-cleavable moieties (Val-Cit, Val-Ala, glucoronide triggers…) or can be used in non-cleavable linker designs (when the final proteolytic degradation of the ADC is predominantly held responsible for the release of the toxic payload).

Most of the highly-potent cytotoxic drugs used in the ADC field are DNA damaging agents (such as pyrrolobenzodiazepine or « PBDs ») or microtubules inhibitors (such as maytansinoids or auristatins). To anticipate resistance to these current payloads in the clinic, we are also working with new compounds displaying innovative mechanisms of action. For instance, DNA or RNA topoisomerase inhibitors (PNU-159682, α-amanitin), spliceosome inhibitors (thailanstatins) or kinesin splindle protein (KSP) inhibitors.

Mablink has developed a drug linker librairy with tested drug-linker associations and can provide you with the right linker for virtually any cytotoxic compound.

We have built up a library of optimized drug-linker couples, validating the best linker for each cytotoxic drug. The cytotoxic drugs we use have new mechanisms of action and confers to our PSARlink ADCs an improved therapeutic index for better clinical transfer.

To date, Mablink offers four drug linker couples, but can also work with the cytotoxic of your choice and set up the best coupling conditions.

Cytotoxic Payload Mechanism of action Linker nature
MMAE / MMAF Microtubule inhibitor Cleavable & Non-cleavable
Exatecan Topoisomerase I inhibitor Cleavable
SN38 Topoisomerase I inhibitor Cleavable
PNU-159682 Topoisomerase II inhibitor &
DNA damaging agent