Acute dose tolerance and pharmacokinetic study of BWA78U and placebo in normal male volunteers

Despite the variety of antiepileptic medications currently marketed in the United States, approximately one-fifth of patients fail to experience adequate seizure control1 and others do so only at the expense of toxic side effects. Thus a need for new antiepileptic drugs with greater efficacy and less toxicity remains. BWA78U is a structurally unique antiepileptic compound developed in the Wellcome Research Laboratories. It is a purine structurally related to the methylxanthines and designated by the chemical name 9- [2-fluorobenzyl]-6-methylamino-9H-purine mono-hydrochloride. Pharmacological studies in animals have shown BWA78U to protects rats against maximal electroshock and 3-mercaptoproprionic acid-induced seizures and audiogenic seizures. When compared with known antiepileptic agents, this pattern of protection against experimentally-induced seizures would predict effectiveness in focal partial seizures, generalized seizure with focal origin and bilateral generalized seizures.