Rapastinel

Products

Rapastinel is in clinical development at Allergan and is not yet commercially available. It was originally developed by Naurex Inc, a pharmaceutical company based in Evanston, Ill. Naurex was acquired by Allergan in 2015 for more than half a billion US$. Other companies are also working on glyxins.

Structure and properties

Rapastinel (C18H31N5O6, Mr = 413.5 g/mol) is an amidated tetrapeptide designed starting from an antibody. It has the structure threonine-proline-proline-threonine-amide (Thr-Pro-Pro-Thr-CONH2).

Effects

Rapastinel has antidepressant properties. It additionally improves cognitive abilities such as learning ability and memory. Unlike traditional antidepressants, the onset of action is very rapid, within hours, and lasts for more than a week. The onset of action of currently available antidepressants is in the range of weeks. The effects of rapastinel are due to partial agonism at the glycine-binding site of NMDA receptors in the central nervous system.

Indications

For the treatment of depression.

Dosage

Because the active ingredient is a peptide, the drug is administered intravenously. The follow-up active ingredient, NRX-1074, is available orally.

Abuse

Rapastinel can potentially be misused as a smart drug and lifestyle medication due to its pharmacologic properties.