Lacosamide (LCM), (SPM 927, (R)-2-acetamido-N-benzyl-3-methoxypropionamide, 
previously referred to as harkoseride or ADD 234037) is a member of a series of 
functionalized amino acids that were specifically synthesized as anticonvulsive 
drug candidates. LCM has demonstrated antiepileptic effectiveness in different 
rodent seizure models and antinociceptive potential in experimental animal 
models that reflect distinct types and symptoms of neuropathic as well as 
chronic inflammatory pain. Recent results suggest that LCM has a dual mode of 
action underlying its anticonvulsant and analgesic activity. It was found that 
LCM selectively enhances slow inactivation of voltage-gated sodium channels 
without affecting fast inactivation. Furthermore, employing proteomic 
affinity-labeling techniques, collapsin-response mediator protein 2 (CRMP-2 
alias DRP-2) was identified as a binding partner. Follow-up experiments 
confirmed a functional interaction of LCM with CRMP-2 in vitro. LCM did not 
inhibit or induce a wide variety of cytochrome P450 enzymes at therapeutic 
concentrations. In safety pharmacology and toxicology studies conducted in mice, 
rats, rabbits, and dogs, LCM was well tolerated. Either none or only minor side 
effects were observed in safety studies involving the central nervous, 
respiratory, gastrointestinal, and renal systems and there is no indication of 
abuse liability. Repeated dose toxicity studies demonstrated that after either 
intravenous or oral administration of LCM the adverse events were reversible and 
consisted mostly of exaggerated pharmacodynamic effects on the CNS. No genotoxic 
or carcinogenic effects were observed in vivo, and LCM showed a favorable 
profile in reproductive and developmental animal studies. Currently, LCM is in a 
late stage of clinical development as an adjunctive treatment for patients with 
uncontrolled partial-onset seizures, and it is being assessed as monotherapy in 
patients with painful diabetic neuropathy. Further trials to identify LCM's 
potential in pain and for other indications have been initiated.