Aptiom, First medicine developed in Portugal, approved by the FDA for sale in the U.S.

November 11,2013 | By Márcio Barra

The first drug developed in Portugal, Eslicarbazepine acetate, from pharmaceutical BIAL, received on Friday approval from the U.S. Food and Drug Administration (FDA) for marketing in the United States.

Branded as Aptiom, the drug was approved as an add-on medication to reduce the frequency of partial seizures associated with epilepsy. The FDA based its approval primarily on three clinical trials, where Aptiom was shown to reduce the frequency of seizures in testing the drug against a placebo, while the ratings of depression and patients’ self-reported quality of life phases showed improvements over pre-treatment baseline during the extension. Participating subjects continued to use their previous anti-epileptic medications throughout the trials.

Pooled results from the three 12-week, double-blind trials showed that 21.5% of the 279 patients assigned to placebo showed reductions of at least 50% in seizure frequency compared with 36.5% of 262 patients receiving 800 mg/day of Eslicarbazepine and 43.5% of 253 patients receiving 1,200 mg/day (both P<0.001 versus placebo).

The drug, a once-daily voltage-gated sodium channel blocker, is a prodrug for eslicarbazepine, which is the active metabolite of an existing seizure medication, oxcarbazepine (Trileptal).While both compounds are dibenzazepine derivatives, eslicarbazepine is structurally distinct from carbamazepine. This molecular distinction results in differences in metabolism, and pharmacokinetic studies have suggested that eslicarbazepine acetate is metabolized more slowly, reducing peak levels of the metabolite in circulation, and is thought to improve its tolerability for some patients. Moreover, contrarily to carbamazepine, eslicarbazepine is not susceptible to metabolic auto-induction.

The drug, approved under the brand name Zebinix in Europe since 2009 and sold since 2010, will be marketed in the U.S. by licensee Sunovion. An initial application for FDA approval was rejected in 2010 with the agency requesting more data from Sunovion. The drug is approved for the treatment of adults with partial-onset seizures (epileptic fits) with or without secondary generalisation.

Aptiom is the first drug developed entirely in Portugal. It took more than 15 years since the pre-clinical research to reach pharmacies, with a total investment of 300 million euros.

“After Europe, it is with great pleasure that we now see our fifteen years of research recognized by the U.S. regulatory authorities, whose quality standards, like the EMA, are extraordinarily high,” said António Portela, CEO of the BIAL group, in a statement to Diário Económico. “We are especially proud because it is also the first time that the Portuguese pharmaceutical industry has an innovative drug approved in the U.S.,” he added.

“To be finally able to cross the Atlantic and commercialize our product in the United States is of a huge relevance, as we are entering a country that represents about 50% of the world market of drugs for epilepsy.” He concluded.


Diário Económico

Hainzl D, Parada A, Soares-da-Silva P. Metabolism of two new antiepileptic drugs and their principal metabolites S(+)- and R(−)-10,11-dihydro-10-hydroxy carbamazepine. Epilepsy Res. 2001;44(2–3):197–206. doi: 10.1016/S0920-1211(01)00231-5.

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