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Сутент — Sutent (Сунитиниб) 12,5 мг; 25 мг; 50 мг.

Сутент - Sutent (Сунитиниб) 12,5 мг; 25 мг; 50 мг.

Сутент — Sutent (Сунитиниб) 12,5 мг; 25 мг; 50 мг.

Компания Medical&Pharma предлагает современное противоопухолевое средство Сутент (Sutent). Он, главным образом, применим при лечении рака желудка — гастроинтестинальной стромальной опухоли (когда терапия с иматинибом не дает положительного результата, или противопоказана). Средство также используют при терапии прогрессивного роста образований в поджелудочной железе. Активное действующее противоопухолевое вещество Сутента — Сунитиниба малат — это ингибитор рецепторов тирозинкиназ, ферментов, участвующих в процессах роста опухолей, образовании  метатстаз и патологического ангиогенеза. Сутент применим также в качестве средства, применяемого при терапии почечно-клеточного канцерогенеза. Сунитиниб был зарегистрирован и одобрен к применению в 2006 году. В России препарат зарегистрирован с 2007 года.

Артикул: 12-1 Категория:

Описание

Компания Medical&Pharma предлагает современное противоопухолевое средство Сутент (Sutent). Он, главным образом, применим при лечении рака желудка — гастроинтестинальной стромальной опухоли (когда терапия с иматинибом не дает положительного результата, или противопоказана). Средство также используют при терапии прогрессивного роста образований в поджелудочной железе. Активное действующее противоопухолевое вещество Сутента — Сунитиниба малат — это ингибитор рецепторов тирозинкиназ, ферментов, участвующих в процессах роста опухолей, образовании  метатстаз и патологического ангиогенеза. Сутент применим также в качестве средства, применяемого при терапии почечно-клеточного канцерогенеза. Сунитиниб был зарегистрирован и одобрен к применению в 2006 году. В России препарат зарегистрирован с 2007 года.

Процесс роста опухолевых клеток во многом зависит от активности рецепторов, взаимодействующих с различными стимулирующими ростовыми причинами, относящимися к группе тирозинкиназ. Механизм действия вещества характеризуется его способностью связываться с этими рецепторами, препятствуя тем самым рецепторам возможности связываться со стимулирующими опухолевый рост веществами.

Показания препарата

  • гастроинтестинальные стромальные опухоли после неэффективной терапии иматинибом мезилат;
  • почечно-клеточной рак
  • нерезектабельные или метастатические высокодифференцированные нейроэндокринные опухоли поджелудочной железы у взрослых с прогрессированием заболевания.

Состав

Одна капсула 12,5 мг содержит

  • активное вещество — сунитиниба малат 16,7 мг (соответствует сунитинибу 12.5мг),
  • вспомогательные вещества: маннитол, натрия кроскармеллоза, магния стеарат, повидон К-25.
  • состав оболочки капсулы (корпус и крышка): желатин, железа (III) оксид красный, титана диоксид..

Одна капсула 25 мг содержит

  • активное вещество — сунитиниба малат 33.4 мг (соответствует сунитинибу 25мг),
  • вспомогательные вещества: маннитол, натрия кроскармеллоза, магния стеарат, повидон К-25.
  • состав оболочки капсулы:
  • корпус: корпус: желатин, железа (III) оксид красный, титана диоксид.
  • крышка: корпус: желатин, железа (III) оксид красный, титана диоксид, железа (II, III) оксид черный, железа (III) оксид желтый.

Одна капсула 50 мг содержит

  • активное вещество — сунитиниба малат 66,8 мг (соответствует сунитинибу 50мг),
  • вспомогательные вещества: маннитол, натрия кроскармеллоза, магния стеарат, повидон К-25.
  • состав оболочки капсулы (корпус и крышка): корпус: желатин, железа (III) оксид красный, титана диоксид, железа (II, III) оксид черный, железа (III) оксид желтый.
  • белые чернила: шеллак, этанол безводный, 2-пропанол, бутанол,титана диоксид, пропиленгликоль, натрия гидроксид, повидон.

Фармакодинамика

Сунитиниба малат – это небольшую молекулу, подавляющая рецепторы различных тирозинкиназ, участвующих в процессах патологического ангиогенеза, роста опухолей и образования метастаз. Сунитиниб проявляет ингибирующую способность в отношении многих киназ; является мощным ингибитором рецепторов тромбоцитарного фактора роста, рецепторов фактора роста сосудистого эндотелия, рецептора фактора стволовых клеток, рецептора Fms -подобной тирозинкиназы-3, рецептора нейротрофического глиального фактора, рецептора колониестимулируюшего фактора. Активность основного метаболита была сходной с таковой сунитиниба.

В биохимических и клеточных исследованиях было показано ингибирование тирозинкиназной активности рецепторов тирозинкиназы сунитинибом. В тестах по пролиферации было продемонстрировано функциональное подавление процессов пролиферации. По сведениям биохимических и клеточных опытов активность главного метаболита была аналогична сунитинубу.

Сунитиниб ингибировал фосфорилирование многих РТК в ксенотрансплантатах опухолей. На опытных моделях различных опухолей также он демонстрировал ингибирование роста опухоли или ее регрессию и/или подавление метастаз.

Фармакокинетика

Всасывание

Сунитиниб применяется перорально в форме малата, в желатиновых капсулах, независимо от приёма пищи. После приёма препарата максимальная концентрация сунитиниба в плазме крови достигается примерно через 6—12 часов после приёма; приём пищи на биодоступность сунитиниба не влияет. / При приеме внутрь сунитиниб хорошо всасывается из ЖКТ. Время достижения Cmax составляет 6-12 ч. Прием пищи не влияет на биодоступность сунитиниба.

Распределение

Равновесные концентрации сунитиниба и его основного метаболита в плазме крови достигаются через 10—14 дней после начала приёма препарата. Связь сунитиниба и его метаболита с белками плазмы — 95 и 90 % соответственно.

Средний объем распределения составляет 2230 л, демонстрируя распределение в тканях. Кажущийся объем распределения сунитиниба был значительным — 2230 л, что указывает на его распределение в тканях. В дозовом диапазоне 25–100 мг площадь под кривой (AUC) времени и концентрации в плазме крови и Cmax увеличивались пропорционально дозе.

Метаболизм

Метаболизм сунитиниба происходит в основном в печени — за счёт окисления, опосредуемого изоферментом CYP3A4, в результате чего происходит образование основного активного метаболита (который дальше метаболизируется тем же изоферментом CYP3A4). Активность основного метаболита сходна с активностью самого сунитиниба. Доля циркулирующего в плазме активного метаболита составляет 23—37 % от величины площади под кривой «концентрация-время».

По данным клинических экспериментов in vitro показывают, что сунитиниб не ингибирует и не индуцирует основные ферменты CYP, включая CYP3A4. Биотрансформация сунитиниба осуществляется в основном изоферментом CYP3A4 в результате чего образуется основной активный метаболит. Доля активного метаболита составляет 23-37% от величины AUC. К 14 дню суммарная концентрация сунитиниба и его основного активного метаболита в плазме составляет 62.9-101 нг/мл. При многократном ежедневном применении или повторных циклах с различным режимом дозирования никаких значительных изменений фармакокинетики сунитиниба и его основного активного метаболита не обнаружено.

Выведение

Сунитиниб выводится в основном с калом — 61%. Почками в виде неизмененного вещества и его метаболитов выводится примерно 16% дозы. Общий клиренс при приеме внутрь достигал 34-62 л/ч. Период полураспада сунитиниба и его основного активного метаболита составляет 40-60 ч и 80-110 ч соответственно. При повторном ежедневном применении происходит 3-4-кратное кумуляция сунитиниба и 7-10-кратное кумуляция его основного метаболита.

Фармакокинетика в особых клинических случаях

Печёночная недостаточность

Сунитиниб и его основной активный метаболит подвергаются метаболизму, главным образом, в печени. Системная экспозиция после однократного приема сунитиниба была одинакова у пациентов с легкой и умеренно выраженной степенью печеночной недостаточности по сравнению со здоровыми пациентами. Применение сунитиниба у пациентов с тяжелой степенью печеночной недостаточности не изучалось.

Почечная недостаточность

По данным популяционного фармакокинетического анализа было показано, что у пациентов с зафиксированным клиренсом креатинина в пределах 42– 347 мл/мин фармакокинетика сунитиниба не изменялась. Системная экспозиция после однократного приема препарата Сутента была одинакова у пациентов с тяжёлой степенью почечной недостаточности (CLcr<30 мл/мин) по сравнению с пациентами с нормальным функционированием почек (CLcr >80 мл/мин). Несмотря на то, что сунитиниб и его первичный активный метаболит не выводятся посредством гемодиализа у пациентов с терминальной стадией почечной недостаточности, общие системные экспозиции были ниже на 47% для сунитиниба и 31% для его первичного метаболита по сравнению с пациентами с нормальным функционированием почек.

Популяционная фармакокинетика

Фармакокинетический популяционный анализ демографических данных показывает, что нет клинически значимой зависимости от возраста, массы тела, клиренса креатинина, расы, пола пациента не имеют клинически важного значения на фармакокинетику препарата и его активного метаболита.

Пол

Имеющиеся данные свидетельствуют, что определенный клиренс сунитиниба для женщин может быть на 30% ниже, чем для мужчин; это отличие не требует корректировки начальной дозы.

Фармацевтические характеристики

Твердые желатиновые капсулы с дозировкой:

  • Капсула 12,5 мг. (имеет корпус красно-коричневого цвета, с гравировками «Pfizer», «STN 12,5 mg»).
  • Капсула 25 мг. (имеет корпус коричневато-оранжевого цвета, с красно-коричневым основанием, с гравировками на корпусе «Pfizer», «STN 25 mg»).
  • Капсула 50 мг. (имеет корпус светлого коричневато-оранжевого цвета,  с гравировками на корпусе «Pfizer», «STN 50 mg»).

Содержимое капсул: гранулы от желтого до оранжевого цвета.

Упаковка, срок годности, условия хранения

Капсулы по 12,5 мг, 25 мг или 50 мг. По 30 капсул упакованы в в полиэтиленовый флакон с полипропиленовой крышкой. По одному флакону вместе с инструкцией вложены в пачку из картона.

Хранить при температуре не выше 25°С. Хранить в недоступном для детей месте.

Срок хранения 3 года.

 

 

 

 

Наша компания работает как на территории Казахстана, так и осуществляет доставку в страны ближнего зарубежья. Обращайтесь к нам за консультациями по контактным телефонам.

Заказать и купить Сутент (Сунитиниб) в Алматы

Заказать и купить Сутент (Сунитиниб) в Казахстане

Позвоните и узнайте цену Сутент (Сунитиниб)

Работаем и отправляем Сутент (Сунитиниб) по странам СНГ: Россия, Украина, Кыргызстан (Бишкек), Белоруссия, Узбекистан (Ташкент),
а также можем отправить Сутент (Сунитиниб) по регионам Казахстана: Нур-Султан (Астана), Шымкент, Талдыкорган, Актау и другие.

Детали

Производитель

Pfizer

Страна производитель

США

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