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Тайверб — Tykerb (Лапатиниб) по 250 мг/70 таб

Тайверб (Tykerb) лапатиниб 250мг/70таб Великобритания

Тайверб — Tykerb (Лапатиниб) по 250 мг/70 таб

Тайверб (Лапатиниб) является обратимым селективным ингибитором внутриклеточной тирозинкиназы, связывающийся с EGFR (рецептор эпидермального фактора роста, ErbB1), а также HER2 (рецептор эпидермального фактора роста человека, ЕrbВ2) рецепторами. Имеет отличия от других быстрообратимых ингибиторов тирозинкиназы более медленной диссоциацией с ErbB1 и ЕrbВ2 рецепторами (период диссоциации 50% лиганда из лиганд-рецепторного комплекса составляет приблизительно 300 мин).

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Описание

Тайверб (Лапатиниб) является обратимым селективным ингибитором внутриклеточной тирозинкиназы, связывающийся с EGFR (рецептор эпидермального фактора роста, ErbB1), а также HER2 (рецептор эпидермального фактора роста человека, ЕrbВ2) рецепторами. Имеет отличия от других быстрообратимых ингибиторов тирозинкиназы более медленной диссоциацией с ErbB1 и ЕrbВ2 рецепторами (период диссоциации 50% лиганда из лиганд-рецепторного комплекса составляет приблизительно 300 мин).

Описание Тайверб (Лапатиниб)

Компания Medical&Pharma предлагает современное лекарство Тайверб (Лапатиниб). Относится к группе противораковых препаратов, который содержит действующее вещество лапатиниба дитозилата моногидрат  (ингибитор протеинтирозин-киназы).

Тайверб применяют для лечения рака молочной железы с гиперэкспрессией HER2 (ЕгbВ2).

Состав

  • Активное вещество: лапатиниба дитозилата моногидрат.
  • одна таблетка, покрытая пленочной оболочкой, содержит 405 мг лапатиниба дитозилата моногидрат, что соответствует 250 мг лапатиниба.
  • Вспомогательные вещества: целлюлоза микрокристаллическая, натрия крахмалгликолят (тип А), магния стеарат, повидон КЗО;  оболочка:  Опадрай желтый YS-1-12524-A (гипромеллоза, титана диоксид (Е 171), железа оксид желтый (Е172), железа оксид красный (Е172), полисорбат 80, макрогол 400).

Показания к применению препарата Тайверб (Лапатиниб)

Тайверб показан для лечения Местно-распространенного или метастатического рака молочной железы с гиперэкспрессией HER2 (ЕгbВ2):

  • в комбинированной терапии с капецитабином после предшествующей терапии у пациенток с распространенным или метастатическим раком с прогрессированием, в соответствии со схемой лечения метастатических опухолей, включавшей антрациклины, таксаны и трастузумаб
  • в комбинированной терапии с трастузумабом у пациенток негативным гормоно-рецепторным статусом и с метастатическим раком, с прогрессированием после предшествующей терапии трастузумабом в сочетании с химиотерапией;
  • в комбинированной терапии с ингибитором ароматазы у женщин в постменопаузальном периоде с метастатическим раком и позитивным гормоно-рецепторным статусом, которым не показана химиотерапия.

Фармакодинамика

Механизм действия

Лапатиниб, 4-анилинохиназолин, — это обратимый селективный ингибитор внутриклеточной тирозинкиназы, который связывается с HER2 (human epidermal growth factor receptor; ЕгbВ2)  и EGFR (epidermal growth factor receptor; ЕгbВ1)  рецепторами. От других быстрообратимых ингибиторов тирозинкиназы отличается медленной диссоциацией рецепторами с ЕгbВ1 и с ЕгbВ2 (не менее 300 мин составляет период диссоциации 50% лиганда из лиганд-рецепторного комплекса). Показано, что, как in vitro, так и в ряде моделей исследования на животных, Лапатиниб ингибирует рост раковых клеток, вызванный ЕгbB.

Взаимодействие трастузумаба и лапатиниба может иметь взаимодополняющий способ воздействия, и может обеспечивать  неперекрещивающиеся способы преодоления резистентности. Ингибирующий эффект лапатиниба изучался на клеточных линиях, обработанных трастузумабом.В исследованиях  in vitro  Лапатиниб показал  повышенную активность  в отношении линий HER2  опухолевых клеток, выбранных для долгосрочного роста в средах, содержащих трастузумаб, и в данных линиях клеток проявил синергичное действие в сочетании с трастузумабом.

Фармакокинетика

Всасывание

Данные по абсолютной биодоступности препарата после приема внутрь являются неполными и вариабельными. Коэффициент вариабельности равен почти 70%, в соотношении площади под кривой «концентрация — время» (AUC). Лапатиниб определяется в системном кровотоке в среднем через 0,25 часа (диапазон 0-1,5 ч). Максимальная концентрация после приема лапатиниба в плазме крови (Сmах) достигается примерно через 4 часа.

При ежедневном приеме 1250 мг лапатиниба, Сmах в равновесном состоянии составляет в среднем 2,43 (76%) мкг/мл, a AUC — 36,2 (79%) мкг × час/мл.

При приеме одновременно с пищей системная экспозиция лапатиниба увеличивается. , Сmах возрастает приблизительно в 2,5 и 3 раза, AUC — примерно в 3 и 4 раза выше при приеме с пищей с низким (5% жиров) или высоким (50% жиров) содержанием жиров.  Также системная экспозиция лапатиниба зависит от времени назначения, по отношению к приему пищи. Средние величины AUC приблизительно в 2 и 3 раза выше при приеме за один час до завтрака, чем при приеме лапатиниба через час после еды.

Распределение

Лапатиниб обладает высокой степенью связывания (более чем 99%) с альбумином и альфа т кислым гликопротеином плазмы крови. Согласно исследованиям in vitro известно, что лапатиниб является субстратом для переносчиков BCRP (ABCG1 — белка резистентности рака молочной железы) и р-гликопротеина (АВСВ1). Также Лапатиниб ингибирует эти эффлюксные переносчики, а также переносчик ОАТР 1В1 печеночного захвата в клинически значимых концентрациях (IC50 = 2,3 мкг/мл), что было показано in vitro. Клиническое значение данных эффектов на фармакокинетику или фармакологическую активность других противораковых лекарственных средств или препаратов пока не изучено.

Метаболизм

Основные изоферменты интенсивного метаболизма — CYP3A4 и CYP3A5, в меньшей степени изоферментами CYP2C8 и CYP2C19  с образованием различных окисленных метаболитов, концентрация которых составляет не более 10% дозы лапатиниба в плазме или 14% концентрации, обнаруживаемой кале.

In vitro Лапатиниб в клинически значимых концентрациях ингибирует изоферменты CYP2C8 (0,3 мкг/мл) и CYP3A (Ki 0,6-2,3 мкг/мл).

Лапатиниб незначительно ингибирует микросомальные ферменты печени: CYP1A2, CYP2C19,CYP2C9 и CYP2D6 или ферменты UGT (было не менее 6,9 мкг/мл величины IC50 in vitro ).

Выведение

При приеме однократных доз, период полувыведения (Т1/2) увеличивается дозозависимо. Через 6-7 суток приема достигается равновесное состояние достигается, Т1/2 равновесного состояния составляет 24 часа. Лапатиниб в основном выводится с помощью кишечником — в среднем 27% (3-67%) в неизмененном виде, менее 2% принятой дозы выводится в неизмененном виде и в виде метаболитов почками.

Пациенты с нарушением функции почек

Отдельных исследований на фармакокинетику лапатиниба у пациентов с почечной недостаточностью или пациентов, находящихся на гемодиализе не проводилось. По имеющимся данным, можно предположить, что коррекции дозы у пациентов с почечной недостаточностью легкой или умеренной степени не требуется.

Пациенты с нарушением функции печени

Фармакокинетика лапатиниба изучалась при нарушениях функции печени: умеренных (n=8) и тяжелых (n=4) (согласно шкале Чайлд-Пью: от  7-9 баллов или более 9 баллов, соответственно), а также в качестве группы контроля на 8 здоровых добровольцах. После приема однократной дозы 100 мг внутрь, у пациентов с умеренными и тяжелыми нарушениями функции печени AUC лапатиниба  увеличивается на 56% и 85%. У пациентов с печеночной недостаточностью Лапатиниб следует применять с осторожностью.

Фармацевтические характеристики

Таблетки овальной формы,  желтого цвета,  покрытые пленочной оболочкой , двояковыпуклые. На одной стороне таблетки выгравирована надпись «GS XJG», другая сторона таблетки  гладкая.

Упаковка, срок годности, условия хранения

Таблетки выпускаются во флаконе из полиэтилена высокой плотности с устройством против вскрытия детьми.  Флакон закрывается  завинчивающейся крышкой и снабжен мембраной из алюминиевой фольги  и бумаги, полиэтилена  и полиэстера. Флакон  с инструкцией помещен в картонную пачку.  В одном флаконе  по 70 таблеток.

Препарат следует хранить  при температуре не выше 30°С, в недоступном для детей месте.

Срок годности — 2 года.

 

Заказать и купить Тайверб (Лапатиниб) в Алматы

Заказать и купить Тайверб (Лапатиниб) в Казахстане

Позвоните и узнайте цену Тайверб (Лапатиниб)

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

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