Gavestinel

Gavestinel (also known as GV150526) is a pharmaceutical drug that was developed by GlaxoSmithKline for the treatment of stroke. It is a selective antagonist for the glycine site of the N-methyl-D-aspartate receptor (NMDAR), which is a major subtype of glutamate receptor.

Mechanism of Action

Gavestinel works by selectively blocking the glycine site of the NMDAR. This site is crucial for the activation of the receptor. By blocking this site, Gavestinel prevents the excessive activation of the NMDAR, which is believed to be a major cause of neuronal death following a stroke.

Clinical Trials

Gavestinel has undergone several clinical trials to assess its efficacy and safety in the treatment of stroke. In early phase trials, it showed promise in reducing the severity of stroke symptoms. However, in larger phase III trials, it failed to show a significant benefit over placebo.

Side Effects

The most common side effects of Gavestinel include nausea, vomiting, and headache. In rare cases, it can cause serious side effects such as seizures and hallucinations.

Current Status

As of now, Gavestinel is not approved for use in any country. After the disappointing results of the phase III trials, GlaxoSmithKline decided to discontinue its development.

See Also

• Stroke
• Glutamate receptor
• Clinical trial