Raxatrigine

Raxatrigine (also known as CNV1014802 and GSK1014802) is a drug that was under development by Convergence Pharmaceuticals and GlaxoSmithKline for the treatment of neuropathic pain and lumbosacral radiculopathy, also known as sciatica. It acts as a state-dependent blocker of sodium channels, particularly Nav1.7, which is involved in the transmission of pain signals in the nervous system.

Development and Clinical Trials

Raxatrigine was developed by Convergence Pharmaceuticals, which was later acquired by Biogen. The drug was in Phase II clinical trials for the treatment of trigeminal neuralgia and lumbosacral radiculopathy. However, the development was discontinued in 2016.

Mechanism of Action

Raxatrigine works by blocking sodium channels, particularly Nav1.7, in a state-dependent manner. This means that it preferentially blocks channels that are in the open or inactivated state, rather than those that are in the resting state. This property makes it particularly effective at reducing the activity of neurons that are firing at high frequencies, such as those involved in the transmission of pain signals.

Potential Uses

While the development of raxatrigine was discontinued, its mechanism of action suggests that it could potentially be useful in the treatment of other conditions characterized by overactive neurons, such as epilepsy or certain types of psychiatric disorders. However, further research would be needed to explore these possibilities.

See Also

• Neuropathic pain
• Lumbosacral radiculopathy
• Sodium channel blocker
• Nav1.7
• Convergence Pharmaceuticals
• GlaxoSmithKline

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