卫材抗癫痫新药呲仑帕奈在中国获批新适应症！

China's National Medical Products Administration (NMPA) announced in August 2021 that the new indication marketing application for the anti-epileptic drug (perampanel, trade name: Vectai) developed by Eisai has been approved. According to an earlier press release issued by Eisai, it is speculated that the new indication for parampanel to be approved this time may be: monotherapy for pediatric partial seizures in patients aged 4 years and above.

About epilepsy

In 2005, the International League Against Epilepsy (ILAE) defined epilepsy as a brain disorder characterized by persistent susceptibility to epileptic seizures and corresponding neurobiological, cognitive, psychological and sociological consequences. The prevalence rate of epilepsy in my country is 4%c~7%, and the prevalence rate of active epilepsy is about 4.6%, of which 60% originate in childhood. At present, clinical studies have shown that it is still the first choice for newly diagnosed epilepsy patients to receive standardized and reasonable anti-epileptic drug treatment. Although about 30% of epilepsy patients are poorly cured by anti-epileptic drugs (antiepileptic drugs, AEDs), about 70% of patients still have good control of epileptic seizures through AEDs. New anti-epileptic drugs with new mechanisms of action approved in recent years are usually considered third-generation anti-epileptic drugs, such as pregabalin, lacosamide, eslicarbazepine, perampanel, etc.

Paraampanel is currently the only highly selective, non-competitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist. AMPA受体是一类位于突触后神经$的离子型谷氨酸受体。谷氨酸是大脑中主要的兴奋性神经递质，谷氨酸能系统与多种神经系统疾病的发病机制相关。 Before and during seizures in epileptic patients, the extracellular glutamate concentration in the hippocampus continues to increase. The postsynaptic effects of glutamate are mainly mediated by three ion receptors, namely AMPA receptors, N-methyl-D-aspartate (NMDA) receptors and kainate (KA) receptors. Systemic or intracerebrovascular administration of AMPA induces strong seizure activity in animal models of epilepsy, while galampanel, as an AMPA receptor antagonist, has anti-epileptic activity in various preclinical animal models of epilepsy, showing its good prospects as an oral anti-epileptic drug.

The multi-center open-label pilot study 232 trial (NCTO1527006) with expansion phase included 42 epilepsy patients aged 2 to 12 years old, evaluated the pharmacokinetic characteristics of garampanel in children, and preliminarily confirmed the safety and effectiveness of garampanel oral suspension. Dosing at the same weight-to-dose ratio (0.18 mg·kg-1·d-1), combined analysis of pediatric data from Trial 232 with adolescent data from Phase II studies (Trial 235) and Phase III studies (Trial 304, Trial 305, Trial 306) of garampanel using a nonlinear mixed-effects model showed that the drug has similar pharmacokinetic profiles in children, adolescents, and adults.

Randomized, double-blind, placebo-controlled phase II clinical study 235 trial (NCT01161524) included a total of 133 adolescent patients (12 years old ≤ age <18 years old) with focal seizures. Garampanel was increased in increments of 2 mg·d per week to 8~12 mg·d-1 for 19 weeks. The changes in neuropsychological outcomes of the patients from baseline to the end of the maintenance period were evaluated.

The results showed that compared with placebo, adjuvant treatment with parampanel had no significant impact on the overall cognitive drug research (CDR) system score of patients. The least square mean difference between the two groups was -2.2 (95% Cl: -5.2~0.8, P>0.05), indicating that adjuvant treatment with parampanel had no impact on the overall cognition of adolescents with focal epilepsy. The trial's Phase II open-label extension study confirmed the efficacy and safety of long-term adjuvant treatment with garampanel in adolescent patients with focal-onset epilepsy.

Note: The above information comes from the Internet and is compiled and edited by Medical Companion Travel (please correct me if there are any errors or omissions). It is only to provide information on the latest drugs on the market in the world and help Chinese patients understand the latest international new drug trends. It is only for internal discussion among medical staff and does not serve as any basis for medication. For specific medication guidelines, please consult the attending physician.

Recommended hot articles: