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Капрелса — Caprelsa (Вандетаниб)

Капрелса

Капрелса — Caprelsa (Вандетаниб)

Препарат Капрелса — это противоопухолевый препарат при терапии распространенного медуллярного рака щитовидной железы.

В 2005 году препарату Капрелса был присвоин статус орфанного. В настоящее время он зарегистрирован в 28 странах для лечения нерезектабельного метастатического медуллярного рака щитовидной железы.

Действующим веществом лекарственного средства Капрелса, является Вандетаниб. Он оказывает подавляющее воздействие на тирозин-специфичную протеинкиназу, что способствует замедлению роста плоских клеток внутренней поверхности сосудов.

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Описание

Препарат Капрелса — это противоопухолевый препарат при терапии распространенного медуллярного рака щитовидной железы.

В 2005 году препарату Капрелса был присвоин статус орфанного. В настоящее время он зарегистрирован в 28 странах для лечения нерезектабельного метастатического медуллярного рака щитовидной железы.

Действующим веществом лекарственного средства Капрелса, является Вандетаниб. Он оказывает подавляющее воздействие на тирозин-специфичную протеинкиназу, что способствует замедлению роста плоских клеток внутренней поверхности сосудов.

Вандетаниб, будучи ингибитором тирозинкиназы, останавливает рост опухоли и метастазы. В результате проведенных клинических испытаний в пробирке, было выявлено, что вещество вандетаниб способно подавлять клеточные перемещения и новообразования, вызванные фактором роста сосудистого эндотелия. Исследования, проведенные на бестимусных мышах, показали, что активный компонент препарата Капрелсы существенно снижает процесс возникновения кровеносных сосудов в тканях и органах, происходящий на фоне активности опухолевых клеток. Кроме того, этот активный компонент препарата Капрелса ингибирует белки патологических клеток, активизирующих рост эпителиальных клеток, а также деактивизирует протеинкиназы, перестроенные в процессе наполнения клеток эукариот нуклеиновой кислотой. Согласно проведенным клиническим испытаниям с участием более трехсот больных, имеющих рак щитовидной железы, было выявлено отсутствие прогрессирования заболевания после приема лекарственного средства Капрелса.

Состав Капрелса

Таблетки — 1 таб.:

  • активное вещество: вандетаниб 100,0 мг;
  • вспомогательные вещества: кальция гидрофосфата дигидрат, кросповидон, целлюлоза микрокристаллическая, повидон-К29-32, магния стеарат;
  • оболочка таблетки: гипромеллоза 2910, макрогол 300, титана диоксид.

Показания к применению Капрелса

Нерезектабельный местнораспространенный или метастатический медуллярный рак щитовидной железы.

Фармакодинамика

Вандетаниб, являясь селективным ингибитором тирозинкиназы, оказывает подавляющее воздействие на тирозин-специфичную протеинкиназу рецептора-2 фактора роста сосудистого эндотелия (VEGF), стимулированного фактором роста сосудистого эндотелия (VEGF) в эндотелиальных клетках. Вандетаниб подавляет миграцию, пролиферацию, выживаемость эндотелиальных клеток, а также ингибирует образование новых кровеносных сосудов, стимулированных VEGF на in vitro моделях ангиогенеза. In vivo вандетаниб снижал ангиогенез, индуцированный опухолевыми клетками, проницаемость сосудов oпухоли и плотность микрососудистой сети опухоли, ингибировал рост опухоли и метастазов у бестимусных мышей на моделях гетеротрансплантата рака легкого челoвека.

Кроме того, в эндотелиальных клетках и клетках oпухоли вандетаниб подавляет тирозинкиназу рецептора эпидермального фактора роста (EGF), стимулированного EGF. Вандетаниб ингибирует EGFR-зависимую прoлиферацию и выживаемость клеток in vitro.

In vitro исследования показали, что вандетаниб также подавляет активность других тирозинкиназ, включая реаранжированных во время трансфекции (RET) и тирозинкиназ рецептора-3 VEGF.

В ходе клинического исследования с участием 331 пациента с нерезектабельным местно-распространенным или метастатическим медуллярным раком щитовидной железы было показано статистически значимое улучшение выживаемости без прогрессирования. Также по сравнению с плацебо было показано преимущество в частоте ответа, контроле над заболеванием, биохимическом ответе и времени до ухудшения болевого синдрома у больных при приеме вандетаниба. Согласно проведенным клиническим испытаниям с участием пациентов, имеющих рак щитовидной было выявлено отсутствие прогрессирования заболевания после приема лекарственного средства Капрелса.

Не доказана зависимость эффективности терапии вандетанибом от статуса мутации RET.

Фармакокинетика

Фармакокинетика вандетаниба в дозировке 300 мг у пациентов с медуллярным раком щитовидной железы характеризуется клиренсом приблизительно 13,2 л/час, объемом распределения приблизительно 7450 литров и периодом полувыведения из плазмы приблизительно за 19 дней.

Всасывание Капрелса

При приеме внутрь происходит медленное всасывание вандетаниба. После приема максимальная концентрация в плазме обычно достигается в среднем через 6 часов (диапазон 4-10 часов. При многократном применении наблюдалась 8-кратная кумуляция вещества вандетаниба, с достижением равновесного состояния примерно через 2 месяца.

Распределение Капрелса

Вандетаниб связывается с альбумином и альфа-1-кислым гликопротеином сыворотки человека. При этом in vitro связывание с белками составляет примерно 90 процентов. В ex vivo образцах плазмы пациентов с колоректальным раком при равновесной экспозиции после приема препарата в дозировке 300 мг/сутки связывание препарата Капрелса с белками в среднем составляло 93,7 процентов (диапазон 92,2 процента -95,7 процента).

Метаболизм

После приема внутрь меченого 14С-вандетаниба неизмененный вандетаниб и метаболиты вандетаниб-N-оксид и N-десметил-вандетаниб были обнаружены в плазме, фекалиях и моче. Конъюгат глюкуроновой кислоты был незначительным метаболитом только в экскрете. N-десметил-вандетаниб, главным образом, образуется под действием изофермента CYP3A4, а вандетаниб-N-оксид — под действием флавинсодержащих монооксигеназ FMО1 и FMО3. N-десметил-вандетаниб и вандетаниб-N-оксид циркулируют в крови в концентрациях приблизительно 11 процентов и 1,4 процентов соответственно от концентрации вандетаниба.

Выведение

В течение 21 дня после однократного приема меченого 14С-вандетаниба примерно 69 процентов препарата выводилось: 44 процента с фекалиями и 25 процентов с мочой. Выведение препарата Капрелса происходило медленно, и, следует ожидать, что дальнейшее выведение после 21 дня основывается на периоде полувыведения из плазмы крови.

Вандетаниб не являлся субстратом ЮСТ2, экспрессированного в НЕК293 клетках. Вандетаниб подавляет поглощение селективного субстрата ОСТ2 маркера 14С- креатинина НЕК-ОСТ2 клетками, при этом среднее значение IC50 составляет приблизительно 2,1 мкг/мл. Это выше, чем плазменные концентрации вандетаниба (примерно 0,81 и 0,32 мкг/мл), достигаемые после многократного приема препарата в дозировках 300 мг и 100 мг, соответственно. Вандетаниб подавляет почечную экскрецию креатинина, в результате чего концентрация креатинина в плазме крови больных, принимающих вандетаниб, увеличивается.

 

Применение при беременности и детям

Беременность

С участием беременных женщин не проводились адекватные и хорошо-контролируемые исследования препарата Капрелса. Согласно данным доклинических исследований применение препарата Капрелса способно нанести вред плоду, поскольку высок риск развития патологий эмбриона/плода. В соответствии с фармакологическим действием препарат Капрелса оказывал значимое воздействие на все стадии репродуктивной функции у самок крыс.

Применение препарата в период беременности противопоказано.

Период грудного вскармливания

Данные о применении препарата Капрелса у женщин в период грудного вскармливания отсутствуют. Вандетаниб выделялся в молоко крыс, и обнаруживался в плазме крови детёнышей после введения препарата лактирующим крысам. Грудное вскармливание противопоказано в период лечения препаратом Капрелса.

Фармацевтические характеристики Капрелса

Таблетки, покрытые пленочной оболочкой, 100 мг. Круглые, двояковыпуклые таблетки, покрытые пленочной оболочкой белого цвета, с гравировкой Z100 на одной стороне.

Упаковка, срок годности, условия хранения Капрелса

По 10 таблеток в блистере, сформированном из непластифицированной поливинилхлоридной (ПВХ) пленки с поливинилиденхлоридом (ПВДХ), запечатанном алюминиевой фольгой высокой твердости, покрытой термолаком. По три блистера с инструкцией по применению в картонной пачке с контролем первого вскрытия.

Условия хранения препарата Капрелса: при температуре не выше 30 °C. Хранить в недоступном для детей месте.

Срок годности препарата Капрелса 3 года. Не применять по истечении срока годности, указанного на упаковке.

 

 

 

 

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