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Genentech advances second Nav1.7 inhibitor for pain into clinical development

Xenon Pharmaceuticals' partner Genentech, a member of the Roche Group, has advanced a second Nav1.7 inhibitor into clinical development.

GDC-0310 is a selective, oral Nav1.7 small-molecule inhibitor, identified as part of the companies’ pain collaboration focused on the Nav1.7 target. Genentech has initiated a Phase 1 clinical trial in healthy volunteers for GDC-0310. Genentech is also developing GDC-0276, a selective, oral Nav1.7 small-molecule inhibitor for pain which is currently in a Phase 1 clinical trial.

Xenon president and CEO Simon Pimstone said: "We are delighted with the advancement of a second Nav1.7 inhibitor into clinical development, underscoring the potential of this novel class of compounds as a new way to treat pain, and the productivity of our broad Nav1.7-focused discovery and development collaboration with Genentech.

"We believe that Nav1.7 is a validated pain target and that both GDC-0276 and GDC-0310 are promising candidates."

Since 2011, Xenon and Genentech have been collaborating to discover and develop selective oral inhibitors of Nav1.7 for the treatment of pain.

Using its Extreme Genetics1 discovery platform, Xenon identified Nav1.7 as a drug target for pain after discovering that the Nav1.7 protein is deficient in the rare genetic disorder congenital indifference to pain, in which people are unable to feel pain. Nav1.7 appears to be involved in pain signaling and based on the human validation was selected as a key target for the development of novel analgesics.