New drug express! The gospel of 50 million epilepsy patients

Cenobamate (trade name: XCOPRI?), developed by SK Life Science (a subsidiary of SK Biopharmaceuticals), is used to treat partial-onset seizures (POS) and approved by the FDA on 21 November 2019 Figure 1 Cenobamate (trade name: xcopri ®) Xcopri ® is an innovative treatment for epilepsy However, the exact mechanism of its therapeutic effect is not clear at present It may work through two mechanisms: positive regulation of GABAA receptor activity to enhance inhibitory signal; inhibition of persistent sodium ion flow to inhibit excitatory signal Xcopri ® is expected to be available in the second quarter of 2020, pending a timetable review by the US Drug Control Agency (DEA) In early 2019, arvelle therapeutics GmbH entered into an exclusive license agreement with SK biopharmaceuticals to acquire the right to develop and commercialize xcopri ® in Europe Epilepsy is a common nervous system disease characterized by epilepsy According to the World Health Organization (who) report, the global active epilepsy patients account for about 8.2% of the world's total population, with a total of more than 50 million people, adding 2 million epilepsy patients every year Epileptics are often at risk for accidents and other health complications, including falls, drowning, depression and sudden death from epilepsy (SUDEP) Although there are many antiepileptic therapies, even after the use of two antiepileptic drugs (AEDs), about 40% of adults with partial seizures are still unable to fully control the seizures At present, the first-line drugs for the treatment of partial seizure epilepsy (POS) include buvasitan, pirampanide, escalicarbine acetate, lakosamide, everolimus, levetiracetam, tiagabin hydrochloride, lamotrigine and okasside Among them, the approved new antiepileptic drugs, buvasitan and pirampanide, have become the leading role in the global antiepileptic drug market, driving the market to climb step by step Buvasitan is another drug with the same target launched by UCB after its encounter with patent cliff of levetiracetam Compared with levetiracetam, the best-selling antiepileptic drug in the world, the binding ability of buvasitan to SV2A (synaptic vesicular protein 2a in presynaptic nerve endings) was increased 10 times After going public in 2016, the sales volume continued to grow, reaching US $175 million in 2018 It is expected to become another antiepileptic drug after levetiracetam On October 15, the new antiepileptic drug of Weicai company was approved by nmpa of China Pirampanide is the first FDA approved non competitive α - amino 3-hydroxy-5-methyl-4-isoxazolpropionic acid glutamate receptor (AMPA) antagonist for epilepsy Up to now, it has been approved for partial epilepsy treatment in as many as 60 countries Figure 2 Global sales performance of buvasitan and piranpanet in recent years Collate self medication database and company financial report There are 12 new drugs (including drugs on the market and under development) for the treatment of partial seizure epilepsy (POS) in the world In addition to the approved marketing of buvasitan, piranpanet, escalicarbine acetate, lakosamide, Everest, levetiracetam, tiagabin hydrochloride, lamotrigine and okassi, there is also a vlb-01 (Marco Polo) in clinical phase III Valexfarm, a subsidiary of pharmaceuticals, has no latest research progress at present Two types of huperizine-a (Research and development of Biscayne pharmaceuticals) and cannabidivarin (joint research and development of Otsuka pharmaceutical) are in clinical phase II Figure 3 Global pipeline for the development of new drugs for the treatment of partial epilepsy (POS) (only the drugs under research and development are counted, as of November 2019) At present, there are 7 kinds of antiepileptic drugs in China, including dp-vpa (clinical phase II, Jiangsu Enhua), chlorobutylamine (clinical phase II, Desa pharmaceutical), Payne Gabin (clinical phase II, Shanghai Institute of pharmaceutical research, Chinese Academy of Sciences), isopropylbisphenol (clinical phase I, Xi'an Libang pharmaceutical), benzoxazine (clinical phase I, Jilin yinglianshangde), tpn102 (clinical phase I, Chinese Science) Shanghai Pharmaceutical Research Institute, Suzhou wangshanwangshui, Shanghai specialty, wx0005 (clinical phase I, Harbin Pharmaceutical Group) Figure 6 Research and development pipeline of new antiepileptic drugs in China (only drugs under development will be counted as of November 2019) Transaction & Investment and financing information of domestic anti epileptic drug research enterprises (as of November 2019): 1 Jiangsu Enhua pharmaceutical and Israel d-pharm signed the license and joint development agreement on dp-vpa compound Dp-vpa is exclusively obtained to carry out clinical research, registration, production and sales in China for the treatment of epilepsy patients D-pharm received advances and development milestone payments totalling $2.4 million 2 Chlorobutylamine was first discovered and synthesized by Peking University After that, Disha pharmaceutical obtained a license from Peking University for research and development, and carried out clinical research in China At present, it is in the second phase of clinical research for the treatment of epilepsy Xcopri ® is independently developed by SK life science and is an innovative treatment for epilepsy As one of the best-selling treatment categories in the global prescription drug market, the successful listing of xcopri ® has undoubtedly injected fresh blood into this treatment field.