12:00 AM
Apr 22, 2013
 |  BioCentury  |  Emerging Company Profile

SiteOne's saxy synthesis

SiteOne synthesizing sodium channel inhibitors for non-narcotic pain relief

SiteOne Therapeutics Inc. is developing synthetic sodium channel blockers for pain that have a different chemical scaffold and better characterized binding site than competing molecules. The result, according to the company, should be advantages in potency, selectivity and solubility.

SiteOne's sodium channel platform is based on marine guanidinium toxins, which include tetrodotoxins, saxitoxins and gonyautoxins. These small molecules are used as pharmacological tools and have potent activity against voltage-gated sodium channels. The problem is that the difference between a therapeutic and a toxic dose of guanidinium toxins is small.

In 2006, Stanford University researchers James Fleming and Justin Du Bois published in the Journal of the American Chemical Societythe first asymmetric total synthesis of the isomer of saxitoxin responsible for the molecule's potent sodium channel inhibition.

Two years later, Du Bois and John Mulcahy published in JACS the first gonyautoxin synthesis. Du Bois and Mulcahy are SiteOne co-founders; Du Bois is a board member, and Mulcahy is director of R&D.

SiteOne was founded to use these syntheses as the starting point...

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