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Атрианс — Atriance (Неларабин) 5мг/10 таб.

Атрианс

Атрианс — Atriance (Неларабин) 5мг/10 таб.

Компания Medical&Pharma предлагает современное лекарство Атрианс (Неларабин).  Атрианс относят к противоопухолевым препаратам. Препарат характерен тем, что он конкурентно встраивается в ДНК цепь, что вызывает подавление синтеза ДНК и, следовательно, клеточную гибель. Прием препарата Атрианс позволяет достигнуть полной ремиссии при остром Т-клеточном лимфобластным лейкозом или Т-лимфомой.

Категория:

Описание

Компания Medical&Pharma предлагает современное лекарство Атрианс (Неларабин).  Атрианс относят к противоопухолевым препаратам. Препарат характерен тем, что он конкурентно встраивается в ДНК цепь, что вызывает подавление синтеза ДНК и, следовательно, клеточную гибель. Прием препарата Атрианс позволяет достигнуть полной ремиссии при остром Т-клеточном лимфобластным лейкозом или Т-лимфомой.

Состав

препарата Атрианс

  • Один мл содержит активное вещество: неларабин (5 мг)
  • Вспомогательные вещества: натрия хлорид, раствор хлористоводородной кислоты или раствор натрия гидроксида — для доведения значения pH до уровня 5.5-6.5 (среднее значение pH 6.0), вода для инъекций.

Фармакодинамика.

Противоопухолевый препарат, антиметаболит. Неларабин является пролекарством 9-β-D-арабинофуранозилгуанина (ара-Г), аналога дезоксигуанозина. Под воздействием аденозиндезаминазы неларабин быстро преобразуется в арабинофуранозилгуанин, и затем, в следствие процесса фосфорилирования образуется его 5-монофосфат и затем — ара-гуанозинтрифосфат. В следствие накопления ара-гуанозинтрифосфата в бластных клетках при лейкозе, он конкурентно встраивается в ДНК цепь, что вызывает подавление синтеза ДНК и, следовательно, клеточную гибель. Было показано in vitro, что к цитотоксическим эффектам неларабина более чувствительны T-клетки по сравнению с В-клетками.

Клиническая эффективность и безопасность

Хорошую клиническую эффективность в двух независимых клинических исследованиях — CALGB 19801 и COG Р9673 показал неларабин у пациентов в рекомендованной взрослой и детской дозе. У взрослых с Т-лимфомой или острым Т-клеточным лимфобластным лейкозом после двух и более курсов индукции монотерапия препаратом привела к полной ремиссии в 18% случаев (ДИ 95%: 6-37%) при продолжительности полной ремиссии от 15 до 195+ недель; выживаемость через 1 год составила 29%, что подтверждает клиническую эффективность препарата в этой группе пациентов, которым ранее проводилось интенсивное лечение. У пациентов не старше 21 года и у детей с рефрактерным или рецидивирующим острым Т-клеточным лимфобластным лейкозом или Т-лимфомой после двух и более курсов индукции (группа 02) были получены близкие показатели: монотерапия неларабином вызывала полную ремиссию в 13% случаев (ДИ 95%: 4-27%) при продолжительности полной ремиссии от 4.7 до 36.4 недель; выживаемость через 1 год составила 14%.

У части пациентов после нескольких неэффективных курсов лечения, в период полной ремиссии достигнутой на фоне монотерапии неларабином, была произведена пересадка стволовых клеток крови. На момент трансплантации продолжительность полной ремиссии составляла 1.6-9.3 недели у детей и 6.3-195.4+ недель у взрослых. В клинических исследованиях PGAA2001 данные о восстановлении гематологических показателей были показаны у 21 из 27 пациентов, у которых после терапии неларабином производилась трансплантация гемопоэтических стволовых клеток. Из них у 20 пациентов (95%) было подтверждено восстановление уровня нейтрофилов. В клинических исследованиях PGAA2002 данные о восстановлении гематологических показателей получены у 6 из 7 пациентов, которым после терапии неларабином производилась пересадка гемопоэтических стволовых клеток. У 3 из них (50%) отмечено восстановление уровня нейтрофилов.

У рефрактерных больных, после неэффективного курса лечения, монотерапия неларабином показала впечатляющую частоту полной ремиссии — 18% у взрослых и детей после двух и более предшествовавших курсов индукции и 44% у детей после одного предшествовавшего курса индукции.

Фармакокинетика

Всасывание

Максимальная концентрация арабинофуранозилгуанина в плазме крови достигается по завершении внутривенной системы неларабина и в среднем выше, чем максимальная концентрация неларабина, что предполагает быструю и интенсивную преобразование из пролекарства в лекарство. После двухчасовой в/в системы препарата в дозе 1500 мг/м2 взрослым пациентам средние значения концентрации неларабина и арабинофуранозилгуанина 13.9 мкмоль и 115 мкмоль.

После в/в системы препарата в дозе 1500 мг/м2 взрослым пациентам значения AUC неларабина и арабинофуранозилгуанина в среднем составляли 13.5 мкмоль/ч и 571 мкмоль/ч, соответственно. Внутриклеточная максимальная концентрация для ара-гуанозинтрифосфата в первые сутки курсового лечения достигается через 3-25 часа. Средние внутриклеточные значения концентрации, AUC ара-гуанозинтрифосфата для указанной дозы составляли 95.6 мкмоль и 2214 мкмоль/ч.

Распределение

Неларабин и арабинофуранозилгуанина характеризуются большим Vd. в равновесном состоянии Vd у детей и взрослых пациентов составлял, соответственно, 89.4 л/м2 и 115 л/м2. Vd арабинофуранозилгуанина составляет 44.8 л/м2 и 32.1 л/м2 у взрослых и детей.

Связывание неларабина и арабинофуранозилгуанина с белками плазмы крови несущественно и составляет менее 25%, для обоих компонентов и оно не зависит от концентрации в диапазоне до 600 мкмоль. Не установлено эффекта накопления ни арабинофуранозилгуанина, ни неларабина.

В лимфобластах в ходе продолжительного периода после в/в системы неларабина определялись внутриклеточные концентрации ара-гуанозинтрифосфата. Установлено накопление ара-гуанозинтрифосфата внутри клеток при повторных инфузиях неларабина по схеме «1, 3, 5» с увеличением значений концентраций и AUC(0-t) на третий день лечения на 50% и 30% соответственно, по сравнению с аналогичными показателями для первого дня курса.

Метаболизм

Основным способом биотрансформации неларабина является О-деметилирование аденозиндезаминазой с образованием ара-Г, в дальнейшем метаболизирующегося до гуанина. Кроме этого, неларабин частично гидролизуется до метилгуанина, который затем подвергается О-деметилированию с образованием гуанина. На следующем этапе биотрансформации осуществляется N-дезаминирование гуанина с получением ксантина и в последующем, его окисления до мочевой кислоты.

Выведение

Неларабин и арабинофуранозилгуанин быстро выводятся из плазмы крови, после в/в системы в дозе 1500 мг/м2 показано, что период полувыведения составляет, соответственно, 30 мин и 3 часа.

При введении неларабина в дозах от 104 до 2900 мг/м2 средний клиренс у взрослых и детей составлял соответственно 138 л/ч/м2 и 125 л/ч/м2 в первый день. Клиренс арабинофуранозилгуанина сравним в обеих возрастных группах и составляет 9.5 л/ч/м2 у взрослых и 10.8 л/ч/м2 у детей в первый день.

Неларабин и арабинофуранозилгуанина выводятся частично почками. Среднее количество, выводимое почками, составляет для неларабина и арабинофуранозилгуанина соответственно, 5.3% и 23.2% от введенной дозы в течение 24 ч после инфузий неларабина в первый день. Почечный клиренс составляет в среднем 16.4 л/ч для неларабина и 4.9 л/ч — для арабинофуранозилгуанина.

Фармакокинетика в особых клинических случаях

Главные фармакокинетические параметры у детей сходны с таковыми у взрослых.

Нет отличий в основных фармакокинетических параметрах у пожилых пациентов.

В клинические исследования входили пациенты с клиренсом более 80 мл/мин, с нарушением функции почек легкой степени и умеренной степени тяжести. Средний клиренс ара-Г на 7% ниже у пациентов с умеренными нарушениями функции почек. Различий в эффективности и безопасности препарата не отмечено.

Для пациентов с нарушением функции печени нет данных.

Показания

препарата Атрианс

  • У пациентов c рефрактерными к химиотерапии или рецидивирующими заболеваниями:
  • T-клеточный острый лимфобластный лейкоз;
  • T-клеточная лимфобластная лимфома.

Фармацевтические характеристики

50 мл — флаконы стеклянные (6) — пачки картонные.

Раствор для инфузий прозрачный, бесцветный, без видимых механических включений. Раствор упакован в стеклянные флаконы по 50 мл, по 6 флаконов упаковано в пачку картонную.

Упаковка, срок годности,

условия хранения

При температуре до 30°С, в местах недоступных для детей. При температуре выше 30°С раствор стабилен в течение 8 часов.

Срок годности — 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.

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

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