Описание
Управление по контролю за лекарственными средствами и пищевыми продуктами США (U.S. Food and Drug Administration — FDA) одобрило Лорбрена/Лорвиква (лорлатиниб) для использования у пациентов с ALK-позитивным метастатическим немелкоклеточным раком легкого. Основное действующее вещество — лорлатиниб.
Препарат Лорбрена/Лорвиква является ингибитором нового поколения киназы анапластической лимфомы (anaplastic lymphoma kinase — ALK). Он одобрен для использования у пациентов, ранее получавших терапию другими ALK-ингибиторами (одним и более), которая оказалась неэффективной (заболевание прогрессировало).
Решение FDA основано на данных нерандомизированного многоцентрового клинического исследования. Следует отметить, что среди больных с ALK-положительным немелкоклеточным раком легкого, которые ранее получали лечение одним или более ингибиторами ALK, общего ответа (overall response rate — ОRR) достигли 48 процентов.
Показания к применению препарата Лорбрена/Лорвиква:
Показан для лечения пациентов с:
- анапластической лимфомой киназы (ALK);
- немелкоклеточным метастатическим распространенным раком легкого, который прогрессировал при лечении алектинибом, кризотинибом, церитинибом (с метастазами).
Данные показания служат поводом к началу схемы лечения в случае проведения оценки клинического ответа во время предыдущего лечения. Решение о том, стоит ли ориентироваться на них или рассматривать другие способы лечения, должно приниматься в зависимости от клинической пользы (подтверждается определенными клиническими исследованиями).
Фармакодинамика
Вещество Лорлатиниб — обратимый мощный ингибитор тирозинкиназы Ⅲ поколения. Лорлатиниб нацелен на ALK и ROS1; он очень избирателен, преодолевает известные мутации резистентности к ALK и проникает через гематоэнцефалический барьер (ГЭБ). Обладает противоопухолевой активностью в отношении множества мутантных форм фермента ALK, включая некоторые мутации, обнаруженные в опухолях во время прогрессирования заболевания на кризотинибе и других ингибиторах ALK. Противоопухолевая активность вещества лорлатиниба дозозависима и коррелирует с ингибированием фосфорилирования ALK. Препарат также проявляет активность против TYK1, ACK, FER, FPS, TRKB, TRKA, TRKC, FAK и FAK2 .
Также он продемонстрировал эффективность у пациентов с распространенным ROS1-положительным немелкоклеточным раком легкого. Препарат Лорбрена/Лорвиква – ингибитор ALK и ROS1 третьего поколения, продемонстрировавший доклиническую активность в отношении в том числе резистентных форм рака легкого.
Препарат Лорбрена/Лорвиква — пероральный ингибитор ALK и ROS1, двух ферментов, которые играют роль в развитии рака.
Он также продемонстрировал клиническую активность у пациентов с прогрессирующим ROS1-позитивным НМРЛ. В том числе с метастазами в ЦНС и ранее лечившихся кризотинибом. Поскольку у пациентов с резистентностью к кризотинибу есть несколько вариантов терапии, может представлять собой важный целевой препарат следующего ряда.
Введение средства Лорлатиниб приводит к снижению активности злокачественного новообразования. Общая противоопухолевая активность главного компонента зависит от используемой дозы. Показатель средней биодоступности равен 81 процент при пероральном введении, связывание с белками плазмы происходит на уровне 66 процентов. Пища не оказывает клинически значимого влияния на процесс абсорбции вещества Лорлатиниб. Выводится препарат из организма практически в равных количествах через ЖКТ и мочевыделительную систему (приблизительно 48 процентов и 41 процент соответственно).
Фармакокинетика препарата Лорбрена/Лорвиква
Ингибитор ALK Лорлатиниб является небольшой молекулой ингибитора киназы из ALK и ROS1 , а также ряда других киназ . Он активен in vitro против многих мутировавших форм ALK.
Препарат принимают внутрь в виде таблеток. Он достигает максимальной концентрации в плазме крови через 1,2 часа после однократного приема или через 2 часа после приема пищи при регулярном приеме. Его абсолютная биодоступность составляет 80,8 процентов. Прием с жирной пищей увеличивает ее доступность на 5 процентов, что не считается клинически значимым. Находясь в кровотоке, 66 процентов вещества связывается с белками плазмы . Лорлатиниб способен преодолевать гематоэнцефалический барьер . Лорлатиниб инактивируется путем окисления , главным образом, через CYP3A4, и путем глюкуронизации , в основном, через UGT1A4 . Другие CYP и UGT играют второстепенную роль. Лорлатиниб и его метаболиты выводятся с периодом полувыведения 23,6 часа после однократного приема; 47,7 процентов в мочу (из которых менее 1 процента в неизмененном виде) и 40,9 процентов в фекалии (9,1 процентов в неизмененном виде).
Применение в период грудного вскармливания
Не проводилось специальных исследований по безопасности применения лорлатиниба в период грудного вскармливания.
Неизвестно, выделяется ли препарат в грудное человеческое молоко. Риск для грудного ребёнка не может быть исключён.
Противопоказан при кормлении грудью и в течение как минимум 7 дней после приёма последней дозировки лорлатиниба.
Применение при беременности
Не проводилось адекватных и строго контролируемых исследований по безопасности использования препарат при беременности у человека.
Проведённые на животных, исследования выявили доказательства того, что препарат может нанести вред развивающемуся плоду (например, аборты, гастрошизис, снижение веса плода, повёрнутые конечности, аномалии сосудов).
Женщины репродуктивного возраста и мужчины, ведущие половую жизнь, во время терапии и в течение как минимум 6 месяцев после приёма последней дозировки препарата Лорбрена/Лорвиква должны применять надёжные методы контрацепции. В случае наступления беременности, отсутствия менструации или при подозрении на возможную беременность пациентка должна сообщить об этом своему лечащему врачу. Если он используется в период беременности или беременность наступила во время терапии, пациентка должна быть предупреждена о потенциальной опасности для плода.
Применение у беременных женщин противопоказано. Женщины репродуктивного возраста должны применять эффективные методы контрацепции во время прохождения терапии и в течение как минимум 6 месяцев после приёма последней дозировки препарата.
Особенности применения препарата Лорбрена/Лорвиква:
Поскольку риска развития серьезной гепатотоксичности при одновременном использовании сильных индукторов CYP3A, от которых по клиническим показаниям в некоторых случаях нельзя отказываться, необходимо контролировать концентрацию печеночных ферментов AST, ALT и билирубин. Делать это необходимо через 48 часов после начала лечения препаратом Лорлатиниб и, по крайней мере, трижды в течение первой недели с момента старта курса. Если будет отмечаться персистирующая гепатотоксичность 2-ой степени или выше, стоит отказаться либо от Лорбрена, либо от индуктора CYP3A. Решение об этом принимает лечащий врач, отталкиваясь от относительной клинической важности того или иного препарата.
Чуть более чем у 50 процентов пациентов применение данного препарата выражается в виде широкого спектра воздействия на ЦНС. Сюда относятся изменения настроения (включая суицидальные мысли), судороги, галлюцинации и речи, психического состояния и сна. В целом по причине данных симптомов 1,5 процентов пациентов нуждаются в полной отмене Лорбрена, 9 процентов больных требуется временное прекращение терапии и 8 процентов — снижение дозировки.
Среди больных, получающих препарат Лорбрена /Лорвиква, часто развивается повышение уровня холестерина и триглицеридов в сыворотке крови. Из них 80 процентов приходилось назначать гиполипидемическую терапию (обычно такая необходимость возникала на 21-й день лечения препаратом). По этой причине крайне важную роль отводят мониторингу холестерина в сыворотке крови до начала терапии средством Лорбрена (Лорлатиниб), через 1 и 2 месяца после ее старта, и периодически после этого. При первом появлении гиперлипидемии лечение временно приостанавливают и возобновляют в той же дозировке. При повторном развитии данного нежелательного эффекта вновь назначают временную отмену препарата Лорбрена, затем опять возобновляют в той же или уменьшенной дозировке в зависимости от тяжести симптома. Цена за невнимательное отношение к данной особенности ведения терапии может оказаться слишком высокой для больного.
Фармацевтические характеристики препарата Лорбрена /Лорвиква
Препарат представляет собой порошок от белого до кремового цвета
Упаковка, срок годности, условия хранения препарата Лорбрена /Лорвиква
Необходимо поддерживать нормальный температурный режим — от 20 до 25°C. Также позаботьтесь о том, чтобы к лекарству не имели доступа дети. Срок годности — 2 года. Использовать препарат можно в течение срока, указанного производителем на упаковке.
Наша компания работает как на территории Казахстана, так и осуществляет доставку в страны ближнего зарубежья. Обращайтесь к нам за консультациями по контактным телефонам.
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