Rapastinel — EU research guide.

What is Rapastinel?

Rapastinel (Thr-Pro-Pro-Thr-NH2, also known as GLYX-13 and BV-102) is a synthetic tetrapeptide amide developed by Naurex and later Allergan for major depressive disorder. It was given by intravenous injection in clinical trials. Early publications described it as a partial agonist at the glycine site of the NMDA receptor, while later sources describe binding to a distinct site on the receptor complex and enhancing NMDA receptor activity independently of glycine, so its exact mechanism is described differently in different sources.

What does the research show?

A phase 2 proof-of-concept trial in major depression not responding to a previous antidepressant was published (Preskorn et al., J Psychiatr Pract 2015); its abstract was not read here, but company reports described rapid, lasting antidepressant effects with good tolerability and no ketamine-like psychotomimetic signal. A 2014 company press release on a phase 2b study reported effects lasting about a week after a single intravenous dose (not peer-reviewed). The phase 3 programme then failed: on 6 March 2019 Allergan announced that three acute adjunctive phase 3 studies (RAP-MD-01, n=457; RAP-MD-02, n=638; RAP-MD-03, n=415) did not meet their primary endpoint, and that an interim look at the relapse-prevention study suggested its primary endpoint would not be met. The study drug was a once-weekly intravenous bolus given on top of an oral antidepressant, and Allergan said it was well tolerated. A 2020 review states that GLYX-13 failed to meet primary or secondary endpoints in large phase 3 trials. The human evidence for benefit is therefore negative in the largest trials.

EU legal status

Rapastinel is not authorised as a medicine in the EU or anywhere else. It is an unapproved investigational substance whose development was discontinued after the 2019 phase 3 failure (Allergan press release of 6 March 2019; discontinued status per secondary sources, a drug-database summary and Wikipedia, as the formal discontinuation announcement was not found). No EMA or national marketing authorisation was found, although not every member-state register was searched. It is not named on the 2026 WADA Prohibited List, but it would fall under S0 (non-approved substances), prohibited at all times; this is an inference from the category definition, not a named listing.