Nav1.7 Inhibitors for Pain


Selective Inhibitors of NaV1.7 for the Treatment of Pain

In December 2011, we entered into a collaborative research and license agreement with Genentech and its affiliate, F. Hoffman-La Roche Ltd, or Roche, to discover and develop selective oral inhibitors of NaV1.7 for the treatment of pain. Based on our discovery of NaV1.7 deficiency underlying the rare human disease called congenital indifference to pain, or CIP, where individuals with CIP are unable to feel pain, we believe that NaV1.7 is a highly-validated target for the treatment of pain.

Chronic pain conditions, such as severe cancer pain and neuropathic pain, are generally recognized as unmet medical needs providing potential commercial opportunities for a new oral pain drug. Currently available pain drugs often have either a lack of meaningful pain relief or dose limiting side effects for many patients. An orally administered selective NaV1.7 inhibitor could present a novel mechanism for the treatment of moderate to severe pain as a single agent or in combination with existing analgesics that work through different mechanisms. We believe that the selective inhibition of NaV1.7 may lower the potential for dose-limiting central nervous system side-effects and allow for an improved side-effect profile for oral administration of such an inhibitor, which could potentially allow for the treatment of pain that has a central or deep tissue component, including cancer pain and neuropathic pain.

 

Ongoing Collaboration


We have an ongoing collaboration with Genentech focused on developing novel inhibitors of NaV1.7 for the treatment of pain. Genentech completed a Phase 1 clinical trial with GDC-0310, which is an oral, selective NaV1.7 small-molecule inhibitor developed for the potential treatment of pain. After completing an analysis of additional pre-clinical studies with GDC-0310 and reviewing the totality of data available, Genentech has decided to discontinue further clinical development of GDC-0310 and elected to focus its future Nav1.7 development efforts on back-up molecules.

 




Shutting Down Pain” Video

In this video, learn more more about how Genentech scientists teamed up with the Xenon team to develop a new tool that could be a game changer in the way we treat all forms of pain.