Описание
Кстанди (Энзалутамид) — продолговатая мягкая желатиновая капсула белого цвета с надписью черного цвета. Содержимое капсулы — маслянистая жидкость светло-жёлтого цвета с веществом энзалутамид. Относится к противоопухолевым средствам (антиандроген АТХ).
Состав препарата Кстанди
- действующее активное вещество: энзалутамид (MDV3100) 40,0 мг;
- вспомогательные вещества: каприлокапроил макроголглицериды 905,81 мг, бутилгидрокситолуол 0,095 мг, бутилгидроксианизол 0,095 мг; гелевая масса 444,3 мг..
Фармакокинетика
Вещество энзалутамид плохо растворяется в воде. В этом препарате растворимость энзалутамида улучшена за счет использования эмульгатора/сурфактанта и каприлокапроил макроголглицеридов. Предварительные исследования показали, что абсорбция энзалутамида улучшалась в момент растворении в каприлокапроил макроголглицеридах.
Воздействие был0 изучено у пациентов с раком предстательной железы и у здоровых людей. Средний период полувыведения (Т1/2) вещества у больных после одного перорального приема составляет около шести суток (от 2,8 до 10,2 дней), а примерно через месяц достигается равновесная концентрация. Ежедневное пероральное введение препарата аккумулируется примерно в 8,3 раза быстрее чем разовая доза. При этом суточные колебания концентрации в плазме незначительны, соотношение от минимума до пика — 1,25. Выведение, в основном, происходит путем печеночного метаболизма с образованием активного метаболита, являющийся столь же активным, как и само вещество. При этом метаболит циркулирует в плазме примерно в тех же концентрациях, что и вещество энзалутамид.
Фармакодинамика
Раковые клетки предстательной железы напрямую зависят от наличия андрогенов и реагируют на уменьшение активности андрогенных рецепторов. Не смотря на малые или даже не выявляемые уровни андрогенов в плазме, активность андрогенных рецепторов в клетках опухоли продолжает способствовать росту опухолевых клеток. Стимуляция роста опухоли при помощи андрогенных рецепторов требует связывания с ДНК при их транслокации в ядро клетки. Вещество энзалутамид является мощным ингибитором андрогенных рецепторов, блокирующий несколько этапов их сигнального пути. Оно также конкурентно ингибирует связывание андрогенов с андрогенными рецепторами, а также ингибирует связывание активированных рецепторов андрогенов с ДНК даже в условиях сильной экспрессии андрогенных рецепторов в клетках опухоли, резистентных к антиандрогенам, угнетает ядерную транслокацию активированных рецепторо. Лечение данным веществом снижает рост клеток опухоли предстательной железы in vitro и может индуцировать гибель клеток и уменьшение опухоли. При первоначальных исследованиях у энзалутамида активность агониста андрогенных рецепторов отсутствовала .
Показания применения препарата Кстанди
Кстанди показан для лечения кастрационно-резистентного рака предстательной железы;
Кстанди показан для лечения гормоночувствительного рака предстательной железы с метастазами.
Форма выпуска/дозировка
Выпускается в капсулах по 40 мг. Упаковывается по 28 капсул в блистере из ПХТФЭ/ПВХ/фольги. По одному блистеру в картонный футляр. По четыре картонных футляра, содержащем 112 капсул, также с инструкцией в картонной пачке.
Условия хранения, срок годности
Хранить в недоступном для детей месте при температуре не выше 25°С на протяжении 3 лет со дня изготовления.
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