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Зитига — Zytiga (Абиратерон)

Зитига (Абиратерон)

Зитига — Zytiga (Абиратерон)

Андроген-чувствительный рак предстательной железы реагирует на терапию, понижающую уровень андрогенов. Антиандрогенная терапия с использованием агонистов ЛГРГ (лютеинизирующего гормона рилизинг-гормон) или орхиэктомия, ослабляет синтез андрогенов в яичках, но не влияет на синтез андрогенов надпочечниками и в опухоли. Препарат Зитига, в составе которого действующее вещество абиратерона ацетат, снижает концентрацию тестостерона и других андрогенов в сыворотке крови до уровней, которые ниже достигнутых при применении агонистов ЛГРГ или после орхиэктомии. Это является результатом избирательного ингибирования фермента CYP-17, необходимого для биосинтеза андрогенов. Использование препарата Зитига в сочетании с агонистами ЛГРГ (или орхиэктомией) понижает уровень тестостерона в сыворотке крови до уровня ниже порога определения. Простатспецифический антиген (ПСА) служит биомаркером у пациентов с раком предстательной железы.

Категория:

Описание

Андроген-чувствительный рак предстательной железы реагирует на терапию, понижающую уровень андрогенов. Антиандрогенная терапия с использованием агонистов ЛГРГ (лютеинизирующего гормона рилизинг-гормон) или орхиэктомия, ослабляет синтез андрогенов в яичках, но не влияет на синтез андрогенов надпочечниками и в опухоли. Препарат Зитига, в составе которого действующее вещество абиратерона ацетат, снижает концентрацию тестостерона и других андрогенов в сыворотке крови до уровней, которые ниже достигнутых при применении агонистов ЛГРГ или после орхиэктомии. Это является результатом избирательного ингибирования фермента CYP-17, необходимого для биосинтеза андрогенов. Использование препарата Зитига в сочетании с агонистами ЛГРГ (или орхиэктомией) понижает уровень тестостерона в сыворотке крови до уровня ниже порога определения. Простатспецифический антиген (ПСА) служит биомаркером у пациентов с раком предстательной железы.

Показания к применению

Препарат Зитига в комбинации с преднизоном или преднизолоном показан:

  • для терапии взрослых мужчин с метастатическим кастрационно-резистентным раком предстательной железы, с отсутствием симптомов или с легкой симптоматикой после неудачной антиандрогенной терапии, которым клинически пока не показана химиотерапия;
  • для терапии метастатического кастрационно-резистентного рака предстательной железы у взрослых мужчин, прогрессирующего во время или после применения химиотерапии на основе доцетаксела.

Состав

Одна таблетка содержит

  • активное вещество — абиратерона ацетат 250 мг,
  • вспомогательные вещества: лактозы моногидрат, целлюлоза микрокристаллическая, натрия кроскармеллоза, повидон (K29/K32), натрия лаурилсульфат, кремния диоксид коллоидный безводный, магния стеарат.

Фармакодинамика

В условиях in vivo абиратерона ацетат преобразуется в абиратерон, ингибитор синтеза андрогенов. Абиратерон избирательно подавляет фермент 17α-гидроксилазу/C17,20-лиазу (CYP-17). Данный фермент экспрессируется и необходим для синтеза андрогенов в надпочечниках, яичках и клетках опухоли предстательной железы. CYP-17 катализирует преобразование прегненолона и прогестерона путем 17α-гидроксилирования и разрыва связи C17, 20 в предшественники тестостерона: дегидроэпиандростерон и андростендион. Ингибирование активности CYP-17 также сочетается усилением синтеза минералокортикоидов в надпочечниках.

Зитига снижает концентрацию тестостерона и других андрогенов в сыворотке ниже показателей, которые возможно получить на фоне применения агонистов люлиберина или после орхидэктомии. Это возникает из-за избирательного ингибирования фермента CYP-17, требуемого для синтеза андрогенов. Концентрация ПСА служит биомаркером у пациентов с раком предстательной железы.

Анальгетический эффект. Количество больных, у которых отмечался паллиативный анальгетический результат, была достоверно выше при использовании препарата Зитига, по сравнению с группой плацебо. Кроме того, по сравнению с больными, получавшими плацебо, у меньшей части больных, получавших препарат Зитига отмечалось прогрессирование болевого синдрома.

Риск развития костных осложнений. В сравнении с группой плацебо, у меньшей части больных, применявших препарат Зитига, отмечались случаи поражения костной ткани, к которым были отнесены спинальная компрессия, патологический перелом, паллиативное облучение кости, хирургическое лечение кости.

Фармакокинетика

Фармакокинетика абиратерона ацетата и абиратерона была изучена на здоровых лицах, пациентах с поздними стадиями метастатического рака предстательной железы и неонкологических больных с почечной или печеночной недостаточностью. В условиях in vivo абиратерона ацетат быстро превращается в абиратерон, который является ингибитором синтеза андрогенов.

Абсорбция.

После перорального приёма абиратерона ацетата натощак, время достижения максимальной концентрации в плазме крови составляет 2 часа.

По сравнению с приёмом препарата натощак, приём абиратерона ацетата с пищей приводит к 10-кратному увеличению площади под кривой «концентрация-время» (AUC) и 17-кратному увеличению максимальной концентрации (Cmax) абиратерона в зависимости от содержания жира в пище. Учитывая вероятное разнообразие приема пищи, применение препарата с пищей обладает способностью оказывать разнообразное системное влияние. Поэтому, препарат Зитига нельзя принимать во время еды.

Распределение

Взаимодействие меченного 14C-абиратерона с белками плазмы крови человека составляет 99.8%. Кажущийся объём распределения составляет 5.630 л, что свидетельствует о том, что абиратерон широко распределяется в периферических тканях.

Метаболизм

При пероральном приёме 14C-абиратерона ацетата в капсулах, абиратерона ацетат гидролизируется до абиратерона, который в дальнейшем метаболизируется, включая процессы сульфатирование, гидроксилирование и окисление, главным образом, в печени. Большая часть циркулирующего 14C-абиратерона ацетата (примерно 92%) обнаруживается в форме метаболитов абиратерона. Из 15 поддающихся обнаружению метаболитов, 2 основных метаболита, абиратерона сульфат и N-оксид абиратерона сульфат, дают 43% общей радиоактивности каждый.

Выведение.

По данным проведенных исследований с участием здоровых добровольцев, средний период полувыведения абиратерона в плазме составляет приблизительно 15 часов. После перорального приёма меченного 14C-абиратерона ацетата в дозе 1000 мг, около 88% радиоактивной дозы выводилось через кишечник и 5% почками. Основными веществами, представленными в кале, являются неизмененный абиратерона ацетат и абиратерон (приблизительно 55% и 22% принятой дозы соответственно).

Пациенты с печеночной недостаточностью.

Фармакокинетика абиратерона ацетата исследовалась на больных с легкой и умеренной степенью печеночной недостаточности (класс А и В по классификации Чайлд-Пью соответственно) и на здоровых лицах. Системное влияние абиратерона ацетата после однократного применения внутрь в дозе 1 г увеличивалось приблизительно на 11% у пациентов с легкой степенью печеночной недостаточности и на 260% у пациентов с умеренной степенью печеночной недостаточности. Средний период полувыведения абиратерона увеличивался приблизительно до 18 ч у больных с легкой степенью печеночной недостаточности и приблизительно до 19 ч у больных с умеренной степенью печеночной недостаточности. Коррекция дозы препарата для больных, с легкой степень печеночной недостаточности не требуется. Зитига не рекомендуется назначать больным с умеренной или тяжелой степенью печеночной недостаточности (класс B или C по Чайлд-Пью), потому что в этом случае невозможно предсказать необходимую коррекцию дозы. Препарат Зитига с осторожностью применяют у больных с нарушениями функции печени умеренной степени, только если польза от лечения явно перевешивает возможный риск. Зитига нельзя назначать пациентам с тяжелой недостаточностью функции печени. Больным, у которых в прoцессе терапии препаратом развилась гепатотоксичность, может потребоваться временная отмена препарата и коррекция дoзы.

Пациенты с почечной недостаточностью.

Фармакокинетику абиратерона сравнивали у больных с терминальной стадией почечной недостаточности, получающих стандартную схему гемодиализа, и у больных с нормальной функцией почек. Системное воздействие абиратерона ацетата после приема внутрь в дозе 1 г у больных с терминальной стадией почечной недостаточности, получающих гемодиализ, не увеличивалось. Рекомендуется с осторожностью назначать препарат больным, больным раком предстательной железы с нарушением функции почек тяжелой степени, поскольку клинические данные о применении препарата Зитига у таких больных отсутствуют.

Клиническая эффективность и безопасность

в ходе двух рандомизированных плацебо-контролируемых многоцентровых клинических исследований 3 фазы (исследования 301 и 302) была установлена эффективность. В исследовваниях принимали участие больные с метастатическим кастрационно-резистентным раком предстательной железы. В исследование 302 были включены пациенты, ранее не получавшие доцетаксел; тогда как в исследование 301 были включены пациенты, ранее уже получавшие доцетаксел. Больные ранее применяли аналог ЛГРГ или им была ранее проведена орхиэктомия. В группе активного применения препарата, Зитига назначался в дозе 1000 мг в сутки в сочетании с низкой дозой преднизона или преднизолона в дозировке 5 мг 2 раза в сутки. Больные контрольной группы получали плацебо и низкую дозу преднизона или преднизолона в дозировке 5 мг 2 раза в сутки.

Изменения сывороточной концентрации ПСА сами по себе не всегда предопределяют клиническую эффективность. Поэтому, пациентам в обоих исследованиях рекомендовалось продолжать назначенную терапию, до тех пор пока не будут достигнуты критерии прекращения терапии, указанные для соответствующего исследования.

В обоих исследованиях не допускалось использование спиронолактона, потому что спиронолактон взаимодействует с рецепторами андрогена и может увеличивать уровни ПСА.

Фармацевтические характеристики

Таблетки овальной формы, с двояковыпуклой поверхность. Таблетки от белого до почти белого цвета. Имеется гравировка на одной стороне «АА250».

Упаковка, срок годности, условия хранения

По 120 таблеток помещены в банки из полиэтилена высокой плотности и закупорены крышками из полиэтилена высокой плотности, с защитой от вскрытия. Одна банка вместе с инструкцией по применению помещена в пачку картонную.

Хранить при температуре не выше 30°С в защищенном от света и влаги месте. Хранить в недоступном для детей месте.

Срок годности 2 года.

Не использовать по истечении срока годности.

 

 

 

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