molecules of the month


zwitterionic oral selective Nav1.7 inh. for pain

predicted QD dosing, completed Ph. I, discont.

PK optimization of prior scaffold

J. Med. Chem., Mar. 8, 2021

Genentech, South San Francisco, CA / Xenon

Structure of GDC-0310
1 min read

The Genentech Nav1.7 inhibitor (GDC-0310) is a oral Ph. I clinical candidate for pain. Nav1.7 has been a hot target for pain, and we previously highlighted a Nav1.7 inhibitor as one of 2020’s Small Molecules of the Year. It is interesting among Nav1.7 inhibitors due to the presence of a very polar amine group where highly lipophilic elements were formerly incorporated, and is also an interesting example of an orally available zwitterion with a membrane-bound target. This acyl-sulfonamide derivative demonstrates >300-fold selectivity over Nav1.1, Nav1.5, and Nav1.6. Preclinical studies of GDC-0310 were conducted based on measuring its ability to block a response to aconitine (a plant alkaloid that causes abnormal opening of sodium channels). Unfortunately development of this molecule has…

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