J. Hesselink
2017
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Abstract
Raxatrigine (5R)-5-{4-[(2-fluorobenzyl)oxy]phenyl}-L-prolinamide; chemical formula: C18H19FN2O2) is a sodium channel blocker first synthesized by GlaxoSmithKline, explored and developed under de code name GSK1014802 as a central NaV1.3 blocker up to and including phase I in the period 2005-2009. Related to its central mechanism of action, the target indication selected at that time was bipolar disorder, pain and perhaps epilepsy. Subsequently the Glaxo group revamped its R&D focus and stopped working in the field of pain around 2010. The Glaxo research group working on sodium channels left the company and created a spin-out: Covergence Pharmaceuticals, taking with them the rights on the compound, renamed CNV1014802. The characterization of the compound changed into a sodium channel inhibitor reported to have high selectivity for the peripheral Nav1.7 subtype channel, and phase II development started in neuropathic pain, in lumbosacral radiculopathy and trigeminal neuralgia. In 2015 Convergence was taken over by Biogen and the compound was recoded BIB074. Recent published data do not characterize the compound as a selective Nav1.7 inhibitor, but rather as an unspecific sodium channel blocker. We will analyze scientific and press communications referring to this compound in the period 2005-2016 and discuss the moving target for the compound. Correspondence to: Jan M. Keppel Hesselink, professor of molecular pharmacology, consultant drug development, Institute Neuropathic Pain, the Netherlands, E-mail: jan@neuropathie.nu