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Ервой — Yervoy (Ипилимумаб)

Ервой Ипилимумаб

Ервой — Yervoy (Ипилимумаб)

Препарат Ервой предназначен для иммуннотерапии меланомы с метастазами и действует достаточно уникально. Он не воздействует на сами  злокачественные клетки, а лишь восстанавливает нормальный иммунный ответ организма.

Слегка опалесцирующая или прозрачная жидкость от светло-желтого цвета до бесцветного с действующим веществом: Ипилимумаб. Относится к фармакотерапевтической группе противоопухолевые средства (антитела моноклональные) и выпускается в виде концентрата для приготовления раствора инфузий, 5 мг/мл.

Категория:

Описание

Препарат Ервой предназначен для иммуннотерапии меланомы с метастазами и действует достаточно уникально. Он не воздействует на сами  злокачественные клетки, а лишь восстанавливает нормальный иммунный ответ организма.

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Состав:

Один флакон с концентратом для приготовления раствора для инфузий содержит:

  • активное вещество: ипилимумаб 53.5 мг,
  • также: трометамола гидрохлорид 33.7 мг; маннитол 107.0 мг; натрия хлорид 62.6 мг; полисорбат 80 1.18 мг; пентетовая кислота 0.42 мг; натрия гидроксид и хлористоводородная кислота для pH 7.0; вода для инъекций до 10.7 мл.

Фармакодинамика:

Вещество Ипилимумаб — рекомбинантное человеческое моноклональное антитело, связывающееся с CTLA-4 (цитотоксическим Т-лимфоцит-ассоциированным антигеном 4). Вещество является иммуноглобулином G1 каппа (IgGlк) и производится методом генной инженерии при выделении культуры клеток млекопитающих. Молекулярная масса составляет около 148 кДа.

Антиген CTLA-4 является ключевым регулятором активации для Т-лимфоцитов. Вещество Ипилимумаб является ингибитором CTLA-4, который блокирует тормозные сигналы каскада CTLA-4, тем самым увеличивая количество противоопухолевых Т-хэлперов, которые в этот момент вызывают рост количества прямых Т-киллеров. Доказано, что блокада CTLA-4 также уменьшает регуляторную функцию Т-клеток, что в свою очередь может приводить к усилению иммунного противоопухолевого ответа организма.

Также Ипилимумаб может селективно уменьшать количество Т-регуляторных клеток в области раковой опухоли, приводя к росту отношения противоопухолевых Т-хэлперов к Т-регуляторам, что и приводит к гибели злокачественных клеток.

Фармакокинетика:

Фармакокинетику вещества ипилимумаба изучали у пациентов с прогрессирующей меланомой, получающих каждые 3 недели ипилимумаб в дозах от 0,3 до 10 мг/кг (совокупно четыре дозы). Выявлено, что в изученном диапазоне доз Смакс, и Смин (максимальная и минимальная концентрации  соответственно), а также площадь под кривой «концентрация/время» (AUC) пропорциональны введенной дозе пациенту.

При следующем введении каждые три недели клиренс не зависел от времени; мин. системная кумуляция наблюдалась при индексе кумуляции от 1,5 и менее. При этом равновесная концентрация вещества в плазме достигалась при получении 3-ей дозы пациентом.

По данным популяционного фармакокинетического анализа вещества достигались следующие средние показатели: средний конечный период полувыведения составил 15,4 суток ; средний системный клиренс — 16,8 мл/ч и средний объем распределения при равновесной концентрации — 7,47 литров.

А при введении в дозе 3 мг/кг средняя минимальная равновесная концентрация вещества в плазме составляла 19,4 мкг/мл. При этом площадь под кривой «концентрация/время» (AUC) у детей от 12 лет и старше сопоставима с показателями у взрослых пациентов, получавших такую же дозу препарата.

Также отметим, что клиренс ипилимумаба возрастал при увеличении массы тела, а также при повышении активности лактатдегидрогеназы. Но однако коррекции дозы в этих случаях не нужна.

Клиренс не зависит от возраста или пола пациента, функции почек, функции печени, статуса физ. активности пациента и статуса HLA-A2*0201, а также от предшествующей противоопухолевой терапии у пациента.

Выявленное среднее геометрическое значение клиренса у детей от 12 лет и старше составило 8,72 мл/час.

Препарат Ервой в дозе 3 мг/кг совместно с ниволумабом в дозе 1 мг/кг, ниволумаб не оказывал влияния на клиренс вещества ипилимумаба. Также при применении в комбинации, в присутствии антител к веществу ипилимумаб, клиренс ипилимумаба не изменялся совсем.

Показания:

  • Препарат Ервой в виде монотерапии показан при неоперабельной или метастатической меланоме у взрослых пациентов и детей от 12 лет и старше.
  • Препарат Ервой в комбинации с ниволумабом показан при неоперабельной или метастатической меланоме для взрослых пациентов.

Упаковка:

По 10,7 мл во флаконе прозрачного бесцветного стекла типа I, закупоренный бутилрезиновой пробкой, а также алюминиевым колпачком с защитной пластиковой крышкой. Размещают в картонной пачке по одному флакону вместе с инструкцией по применению.

Условия хранения и срок годности:

Препарат хранить при температуре от 2 до 8 °С, в защищенном от света и недоступном для детей месте!

Препарат нельзя замораживать!

Срок хранения: 3 года. Препарат нельзя применять по истечении срока годности.

 

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Работаем и отправляем Ервой (Ипилимумаб) по странам СНГ: Россия, Украина, Кыргызстан (Бишкек), Белоруссия, Узбекистан (Ташкент),
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