AQSh FDA Caplyta (lumateperon) ni tasdiqlaydi: bipolyar tip I yoki II tip buzilish bilan bog'liq depressiya epizodlarini davolash!

Intra-Cellular Therapies (ICT) - markaziy asab tizimi (CNS) kasalliklarini davolash uchun innovatsion terapiyani ishlab chiqishga qaratilgan biofarmatsevtika kompaniyasi. Yaqinda kompaniya AQSh oziq-ovqat va farmatsevtika idorasi (FDA) Caplyta (lumateperon) ni yangi ko'rsatkich uchun ma'qullaganini e'lon qildi: monoterapiya sifatida va katta yoshli bemorlarni davolash uchun lityum yoki valproat bilan yordamchi terapiya sifatida Bipolyar bilan bog'liq depressiya epizodlarini davolash I yoki II turdagi buzilish (bipolyar depressiya).

It is worth mentioning that Caplyta is the only drug approved by the US FDA as a monotherapy and as a lithium or valproate adjuvant therapy for the treatment of adult bipolar type I or type II disorder-related depressive episodes. Clinical data shows that Caplyta has consistently good performance in terms of body weight, cardiometabolic parameters, and extrapyramidal symptoms (dyskinesias).

Caplyta shizofreniya bilan og'rigan katta yoshli bemorlarni davolash uchun 2019 yil dekabr oyida AQSh FDA tomonidan tasdiqlangan. Dori-darmonlarga kelsak, Kaplytaning tavsiya etilgan dozasi 42 mg ni tashkil qiladi, kuniga bir marta ovqat bilan qabul qilinadi, dozani titrlash talab qilinmaydi. Shuni ta'kidlash kerakki, Caplyta' ning dori yorlig'ida qora quti ogohlantirishi bor: demans bilan bog'liq psixoz bilan og'rigan bemorlar o'lim xavfini oshirish uchun antipsikotik dorilarni qo'llashadi; Caplyta demans bilan bog'liq psixoz bilan og'rigan bemorlarni davolash uchun ruxsat etilmaydi.

The approval of the new indication is based on the positive results of two phase 3 placebo-controlled bipolar depression studies. These studies evaluated the effects of Caplyta as a monotherapy (Study 404), as a lithium or valproate adjuvant therapy (Study 402) on depressive episodes in adults with bipolar I or bipolar II disorder. In these studies, the efficacy of Caplyta 42mg was determined by demonstrating a statistically significant improvement in the Montgomery-Asperger Depression Rating Scale (MADRS) total score compared to baseline at the 6th week of treatment. Caplyta 42mg also showed a statistically significant improvement in key secondary endpoints related to the overall clinical impression of bipolar disorder in each study.

In addition, Caplyta showed good tolerability and safety, consistent with the results of previous clinical studies on schizophrenia. The most common adverse reactions (incidence ≥5% and at least twice that of placebo) are drowsiness/sedation, dizziness, nausea, and dry mouth. The Caplyta group and the placebo group had similar changes in body weight, fasting blood glucose, total cholesterol, triglycerides, and low-density lipoprotein cholesterol to the baseline.

Lumateperonning molekulyar tuzilishi

Bipolyar I va Bipolyar II buzilishlar jiddiy, juda keng tarqalgan ruhiy surunkali kasalliklar bo'lib, Qo'shma Shtatlardagi taxminan 11 million kattalarga ta'sir qiladi. Ular bipolyar buzuqlik deb ataladigan takrorlanuvchi maniya yoki gipomaniya bilan tavsiflanadi. Depressiv asosiy depressiv epizod. Bipolyar I va Bipolyar II har biri bipolyar buzuqlik bilan kasallangan bemorlarning umumiy sonining yarmini tashkil qiladi. Bipolyar depressiya bipolyar buzilishning eng keng tarqalgan klinik ko'rinishidir. Ushbu depressiv epizodlar manik/gipomanik epizodlarga qaraganda uzoq davom etadi, tez-tez takrorlanadi va prognozi yomonroqdir. Bipolyar depressiya hali ham jiddiy tibbiy ehtiyoj bo'lib qolmoqda va FDA tomonidan tasdiqlangan bir nechta davolash usullari mavjud. Ushbu terapiya odatda tolerantlik muammolari bilan bog'liq.

Caplyta ning faol farmatsevtik moddasi lumateperon bo'lib, u og'ir ruhiy kasalliklarda ishtirok etadigan uchta neyrotransmitter bo'lgan serotonin, dopamin va glutamatni tanlab va bir vaqtning o'zida modulyatsiya qila oladigan birinchi sinf kichik molekulali preparatdir. Sifatli yo'l. Farmakodinamik tadqiqotlar shuni ko'rsatdiki, lumateperon kuchli antagonist sifatida serotonin 5-HT2A retseptorlari bilan yuqori bog'lanishga ega, antagonist sifatida postsinaptik D2 retseptorlari bilan o'rtacha bog'lanishga ega va serotonin tashuvchisi (SERT) qaytarib olish inhibitörleri sifatida D1 retseptorlari uchun o'rtacha yaqinlik (bu AMPA va NMDA retseptorlarining bilvosita faollashishiga yordam berishi mumkin). Ushbu retseptorlar shizofreniya, bipolyar buzuqlik, depressiya va boshqa neyropsikiyatrik kasalliklarda muhim rol o'ynaydi. In vitro tadqiqotlar shuni ko'rsatdiki, D2 retseptorlari bilan solishtirganda, lumateperon 5-HT2A retseptorlari uchun taxminan 60 baravar yuqori yaqinlikka ega.

Amerika Qo'shma Shtatlarida FDA 2017 yilning noyabr oyida shizofreniyani davolash uchun lumateperon tezkor maqomini berdi. Shizofreniyadan tashqari, AKT kompaniyalari bipolyar depressiya, depressiya va boshqa neyropsikiyatrik va nevrologik kasalliklarni davolash uchun lumateperonni ham ishlab chiqmoqda.

The industry is very optimistic about Caplyta's prospects. EvaluatePharma, a pharmaceutical market research organization, predicts that Caplyta's sales in 2026 will reach 2 billion US dollars, half of which will come from schizophrenia, and the other half will come from bipolar depression.