"LinXis’ linker-payload manufacturing technology published in Green Chemistry"

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Products - Oncology

Breast cancer hits millions of women worldwide every year.

In many of these cases, the cancer cells express a particular trait called HER2. This molecule plays a role in the growth of the cancer. More importantly however, the HER2 molecule represents an excellent target for antibody-drug-conjugates.

Not surprisingly, the breast cancer field has seen one HER2-targeting ADC approved, while many others are in clinical development. Although these ADCs are diverse in design, most have one thing in common: After injection, they tend to lose the drugs they are intended to deliver before ever reaching the cancer cells. This decreases their efficacy because they will deliver less drugs to the cancer cells. What is worse, the released drugs can dissipate freely into healthy organs, causing severe side effects.

The Lx® Linker represents an excellent opportunity to bypass this common failure mode, as it enables the generation of ADCs with unprecedented stability. For breast cancer, we have developed LxC-001, by conjugating he super-potent drug Auristatin F to the HER2-targeting trastuzumab antibody, using Lx® Linker technology. In several laboratory studies, we showed that LxC-001 attacked tumors decidedly more effective than benchmark ADCs whilst being well tolerated at the same time, for a large part because it did not lose any drugs along the way.

LxC-001 comprises the Her2-targeting antibody trastuzumab and the super-potent drug Auristatin F, which are coupled by means of the Lx® Linker. The trastuzumab carrier moiety ensures selective delivery to Her2-expressing cancer cells, where Auristatin F is released to exert its cytotoxic effect.