US FDA pom zoo Caplyta (lumateperone): kev kho mob ntawm bipolar hom I lossis hom II mob ntsig txog kev nyuaj siab!

Intra-Cellular Therapies (ICT) is a biopharmaceutical company focused on developing innovative therapies to treat central nervous system (CNS) diseases. Recently, the company announced that the US Food and Drug Administration (FDA) has approved Caplyta (lumateperone) for a new indication: as a monotherapy and as an adjuvant therapy with lithium or valproate for the treatment of adult patients Treat depressive episodes associated with bipolar type I or type II disorder (bipolar depression).

Nws yog tsim nyog hais tias Caplyta yog tib cov tshuaj pom zoo los ntawm US FDA raws li kev kho mob monotherapy thiab raws li lithium lossis valproate adjuvant therapy rau kev kho mob ntawm cov neeg laus bipolar type I lossis type II disorder-related depressive episodes. Cov ntaub ntawv kho mob qhia tau tias Caplyta muaj qhov ua tau zoo tsis tu ncua ntawm lub cev qhov hnyav, cov kab mob cardiometabolic, thiab cov tsos mob extrapyramidal (dyskinesia).

Caplyta tau pom zoo los ntawm US FDA thaum Lub Kaum Ob Hlis 2019 rau kev kho mob ntawm cov neeg laus uas muaj tus mob schizophrenia. Hais txog cov tshuaj, qhov pom zoo koob tshuaj Caplyta yog 42 mg, ib hnub ib zaug, noj nrog zaub mov, tsis tas yuav tsum muaj koob tshuaj titration. Nws yuav tsum raug sau tseg tias Caplyta' daim ntawv qhia tshuaj muaj lub thawv dub ceeb toom tias: cov neeg mob uas muaj kev puas siab puas ntsws dementia siv cov tshuaj tiv thaiv kab mob ua rau muaj kev pheej hmoo tuag; Caplyta tsis pom zoo rau kev kho mob ntawm cov neeg mob uas muaj kev puas siab puas ntsws ntsig txog kev puas hlwb.

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.

Molecular qauv ntawm lumateperone

Kev puas siab puas ntsws Bipolar I thiab Bipolar II yog qhov mob hnyav, muaj cov kab mob puas siab puas ntsws uas cuam tshuam txog kwv yees li 11 lab tus neeg laus hauv Tebchaws Meskas. Lawv yog tus cwj pwm los ntawm kev rov qab mania lossis hypomania, uas yog hu ua kev puas siab puas ntsws bipolar. Kev nyuaj siab loj heev kev nyuaj siab. Bipolar I thiab Bipolar II txhua tus account rau ib nrab ntawm tag nrho cov neeg mob uas muaj kev puas siab puas ntsws bipolar. Kev puas siab puas ntsws bipolar yog qhov tshwm sim feem ntau tshwm sim ntawm kev puas siab puas ntsws bipolar. Cov kab mob kev nyuaj siab no yuav kav ntev dua, rov qab ntau dua, thiab muaj qhov tshwm sim tsis zoo dua li manic/hypomanic ntu. Kev puas siab puas ntsws bipolar tseem yog ib qho kev xav tau kev kho mob tsis txaus, thiab tsuas yog ob peb txoj kev kho mob tau pom zoo los ntawm FDA. Cov kev kho no feem ntau muaj feem xyuam rau cov teeb meem tolerability.

Cov tshuaj nquag ntawm Caplyta yog lumateperone, uas yog thawj-hauv-chav kawm me me tshuaj molecule uas tuaj yeem xaiv thiab ib txhij hloov kho serotonin, dopamine thiab glutamate, peb lub neurotransmitters koom nrog kev mob hlwb hnyav. Txoj kev zoo. Cov kev tshawb fawb Pharmacodynamic tau pom tias lumateperone, raws li ib tug muaj zog antagonist, muaj siab affinity affinity ntawm serotonin 5-HT2A receptors, raws li ib tug antagonist, muaj nruab nrab binding affinity ntawm postsynaptic D2 receptors, thiab raws li ib yam ntawm cov Serotonin transporter (SERT) muaj ib tug reuptake inhibitors. Kev sib haum xeeb nruab nrab rau D1 receptors (qhov no yuav ua rau muaj kev cuam tshuam ncaj qha ntawm AMPA thiab NMDA receptors). Cov receptors no tau xav tias ua lub luag haujlwm tseem ceeb hauv schizophrenia, kev puas siab puas ntsws bipolar, kev nyuaj siab, thiab lwm yam kab mob neuropsychiatric. Cov kev tshawb fawb hauv vitro tau pom tias piv nrog D2 receptors, lumateperone muaj kev sib raug zoo rau 5-HT2A receptors txog 60 npaug ntau dua.

Hauv Tebchaws Meskas, FDA tau tso cai lumateperone nrawm nrawm rau kev kho tus mob schizophrenia thaum lub Kaum Ib Hlis 2017. Ntxiv nrog rau tus mob schizophrenia, cov tuam txhab ICT tseem tab tom tsim cov lumateperone los kho kev puas siab puas ntsws bipolar, kev nyuaj siab, thiab lwm yam kab mob neuropsychiatric thiab neurological.

Kev lag luam zoo siab heev txog Caplyta' qhov kev cia siab. EvaluatePharma, lub koom haum tshawb fawb txog kev lag luam tshuaj, kwv yees tias Caplyta' qhov muag hauv 2026 yuav ncav cuag 2 billion US dollars, ib nrab ntawm cov uas yuav los ntawm tus mob schizophrenia, thiab ib nrab yuav los ntawm kev puas siab puas ntsws bipolar.