remacemide, and exhibits modest binding to NMDAR and modest effects on convulsions and mortality in test mice and rats. FPL 14331 and FPL 14465 FPL 14331 and FPL 14465 are the p-hydroxy-desglycinates of remacemide, and they exhibit some efficacy against maximal electroconvulsive shock after i.p. and i.v. dosing. FPL 15455 FPL 15455 is an oxoacetate matabolite of remacemide, but has no demonstrated biological activity. FPL 14991 and FPL 14981 FPL 14991 and FPL 14981 are both β-Miydroxy-desglycinates of remacemide, and they display modest efficacy against maximal electroconvulsive shock in mice. However FPL 14981 and not FPL 14991 prevents NMDLA-induced convulsions and mortality in mice. FPL 13592 and FPL 15112 The hydroxy-methyl derivative of remacemide (FPL 13592) and its desglycinate (FPL 15112) prevents electric shock-induced convulsions only after i.v. administration; only the desglycine derivative binds to NMDAR. FPL 14467 FPL 14467 (p-dihydroxy-desglycine) is inactive in vivo and weak in binding NMDAR. Pharmacodynamics The values for 50% displacement of [3H]MK801 were 68 μM for remacemide and 0.48 μM for FPL 12495AA. History Current status Remacemide is an experimental drug most recently being developed by the British multinational pharmaceutical company AstraZeneca. However, there has been little news of its progress since 2000. A few sources indicate that its development has been discontinued. Changing hands Remacemide was one of the last drugs under development by the now-defunct English pharmaceutical company Fisons. In 1995, it was acquired along with most of Fisons' research and development operations by the Swedish pharmaceutical company Astra, which in 1999 merged with the British company Zeneca to form AstraZeneca. In 2000, AstraZeneca considered possibly licensing out remacemide to some other pharmaceutical company, but there has been little news about remacemide since then. Remacemide's development may have been discontinued in July 2001. Discovery and development under Fisons In 1990, researchers at Fisons found that remacemide acted as an anticonvulsant in mice and rats . Because of remacemide's potential as a neuroprotective agent through preventing glutamate toxicity, it was soon also under investigation as a treatment for Huntington's disease and Parkinson's disease. Astra By 1995, when Astra acquired remacemide, it was already in Phase IIb clinical development as an anti-epileptic drug and Phase I clinical development as a treatment for Huntington's . AstraZeneca By 1998, when Astra announced its merger with Zeneca, remacemide had progressed to Phase III trials for epilepsy and Phase II trials for Parkinson's disease, and Astra was also investigating its potential for treating neuropathic pain In 1999, after the merger, AstraZeneca reported that they were investigating remacemide for its neuroprotective effects, and that they planned regulatory submissions for Huntington's disease in 2001 and for Parkinson's disease and epilepsy in 2003. Remacemide, under the trade name Ecovia, was designated an orphan drug for the treatment of Huntington's disease by the FDA in March 2000. Remacemide was last mentioned in AstraZeneca's reports on its R&D pipeline in 2000, when it was in Phase III clinical trials for remacemide in the treatment of Huntington's disease and Phase II for treatment of Parkinson's disease. At that time, the submission of the New Drug Application (NDA) to the FDA and the Marketing Authorization Application to the CHMP was projected for Huntington's in 2001 and for Parkinson's after 2003, but there has been no news of such submission. In this report, it was also noted that remacemide was "under strategic review and a potential candidate for licensing activity" (see this external article about drug licensing.) Current news There are no clinical trials of remacemide in progress, according to the Huntington Study Group, and the Parkinson Study Group. Availability Remacemide is an experimental drug not