Intepirdine

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Intepirdine

Chemical structure of Intepirdine

Intepirdine is a pharmaceutical compound that was investigated for its potential use in the treatment of Alzheimer's disease and other forms of dementia. It is a selective antagonist of the 5-HT6 receptor, a subtype of the serotonin receptor that is primarily expressed in the central nervous system.

Mechanism of Action

Intepirdine functions by blocking the 5-HT6 receptor, which is believed to play a role in the regulation of neurotransmitter release, including acetylcholine, dopamine, and glutamate. By inhibiting this receptor, intepirdine was hypothesized to enhance cognitive function and improve memory in patients with Alzheimer's disease.

Clinical Development

Intepirdine was initially developed by GlaxoSmithKline and later acquired by Axovant Sciences. It underwent several clinical trials to assess its efficacy and safety in patients with Alzheimer's disease. Despite initial promise, the results of the pivotal phase III trial, known as the MINDSET study, did not demonstrate significant improvement in cognitive function compared to placebo.

Discontinuation

Following the disappointing results from the MINDSET study, Axovant Sciences announced the discontinuation of further development of intepirdine for Alzheimer's disease. The decision was based on the lack of efficacy observed in the clinical trials, which did not support the continuation of its development for this indication.

Potential Applications

Although intepirdine was not successful in treating Alzheimer's disease, research into 5-HT6 receptor antagonists continues, as they may hold potential for other neurological disorders. The exploration of alternative therapeutic targets and combinations with other treatments remains an area of active investigation.

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Contributors: Prab R. Tumpati, MD