Описание
Дакоген (Dacogen) — противоопухолевый препарат, антиметаболит. Препарат обладает узконаправленным химиотерапевтическим действием, назначается при миелодиспластическом синдроме (МДС).
Дакоген содержит в себе действующее вещество децитабин, обладающее способностью реактивизировать опухолевые гены-ингибиторы, за счет чего улучшается дееспособность клеток-предшественников к созреванию и делению. Результатом действия является восстановление элементов крови (тромбоцитов, лейкоцитов и эритроцитов). Децитабин (5-аза-2′-деоксицитидин) — аналог нуклеозида цитозина, который в малых дозах избирательно подавляет активность ДНК-метилтрансферазы, что приводит к гипометилированию промоторов генов-супрессоров, их реактивации, индукции клеточной дифференциации или к «старению» клеток с последующей их запрограммированной гибелью (апоптоз). В высоких концентрациях (>10-4 М) децитабин оказывает выраженное цитотоксическое воздействие.
Состав
- Активное вещество: децитабин 50 мг;
- Вспомогательные вещества: натрия гидроксид, калия дигидрофосфат. При необходимости корректировки pH лиофилизата, используются 1-М раствор кислоты хлористоводородной или 1-М раствор натрия гидроксида.
Показания
препарата Дакоген
- Миелодиспластический синдром (МДС) всех типов у ранее леченых и нелеченых больных, в т.ч.: первичный и вторичный;
- впервые диагностированный острый миелолейкоз (ОМЛ-1);
- острый миелолейкоз вторичного типа (ОМЛ 2).
Фармакодинамика
Децитабин (5-аза-2′-деоксицитидин) — аналог нуклеозида цитозина, который в малых дозах избирательно подавляет активность ДНК-метилтрансферазы, функции которой связаны с контролем генной экспрессии через процессы метилирования и деметилирования. Показано, что метилирование промоторного участка гена подавляет транскрипцию. Деметилирование ДНК восстанавливает экспрессию гена. Активизация гена супрессорами ДНК-метилирования, в частности децитабином, может выражаться в индукции дифференциации, необходимом эффекте в терапии миелодиспластического синдрома и других злокачественных новообразований крови, активации генов опухолевой ингибиции и других генов, эффект которых может быть распространен на многие виды новообразований.
Зафиксированные комплексы фермент ДНК — метилтрансферазы и 5-аза-деоксицитидина способны вызвать апоптозную гибель, когда клетка выходит из цикла синтеза ДНК и стимулируется цикл клеточной изоляции и митотической блокировки. Также могут быть результатом эффектов децитабина и альтернативные механизмы, такие как преодоление лекарственной резистентности, облегчение иммунных ответов, индуцирование апоптоза.
Децитабин действует в S-фазу клеточного цикла. До S-фазы клетки должны дойти самостоятельно, чтобы эффект децитабина проявился максимально.
Фармакокинетика
У 14 онкологических пациентов, получавших препарат в дозе 15 мг/м2 путем 3-часовой в/в инфузии с постоянной скоростью каждые 8 часов в течение 3 последовательных дней, была изучена фармакокинетика децитабина.
Всасывание
У пациентов с поздними стадиями крупных опухолей при инфузии децитабина в дозе 100 мг/м2 в течение 1 часа концентрация препарата в плазме крови во время в/в введения повышалась, а после этого снижалась двухфазно (средняя Cmax в плазме крови составляет 0.459±0.100 мкг/мл, средняя AUC — 408±88 нг х ч/мл). У пациентов с поздними стадиями крупных опухолей при 72-часовой в/в введения препарата дакогена в дозе 20, 25 или 30 мг/м2/сут AUC составляет 543±158, 743±98 и 743±124 нг х ч/мл соответственно.
Распределение
Фармакокинетика децитабина соответствует многокамерной модели распределения периода полувыведения в терминальной фазе выведения примерно 0.78 часа. Концентрация в плазме крови составляет 77 нг/мл, AUC составляет 157 нг × ч/мл. Кумуляции препарата при указанной схеме применения не наблюдалось. При введении Дакогена 23 больным путем 1-часовой инфузии ежедневно в течение 5 последовательных дней получены аналогичные данные по фармакокинетике.
После в/в инфузии Vd препарата в равновесном состоянии составляет примерно 70 л/м2, что показывает на проникновение препарата в периферические ткани организма. Связывание препарата с белками плазмы крови крайне низкое (<1%). Кроме того, децитабин плохо связывается с P-гликопротеином. Vd децитабина в равновесном состоянии составляет примерно 4.59±1.42 л/кг. Связывание с белками плазмы крови пренебрежимо мало (<1%).
Метаболизм
Децитабин в клетках подвергается фосфокиназами последовательному фосфорилированию до соответствующего трифосфата, встраивающегося затем с помощью ДНК-полимеразы в ДНК. По данным in vitro известно о том, что Р450 не участвует в метаболизме препарата дакогена. Ведущий путь метаболизма вещества, по всей вероятности, связан с деаминированием в печени цитидин-деаминазой, а также в гранулоцитах, плазме крови и в эпителии кишечника. In vivo метаболиты децитабина однозначно не идентифицированы к настоящему времени.
Выведение
Менее 1% дозы децитабина выводится с мочой в неизмененном виде, что позволяет предположить, что вещество удаляется главным образом в виде метаболитов. У пациентов с поздними стадиями крупных опухолей прив/в инфузии препарата, в дозе 100 мг/м2 в течение 1 часа, общий клиренс препарата составляет 126±21 мл/мин/кг, что превышает печеночный кровоток. Что показывает о вкладе внепеченочного метаболизма в выведение децитабина. Среднее T1/2 в терминальной фазе выведения составляет примерно 35±5 мин.
Фармакокинетика в особых клинических случаях
У пациентов с нарушениями функции почек и печени фармакокинетика децитабина не изучена. Не проводились исследования зависимости фармакокинетики от пола, возраста и расы пациента.
Фармацевтические характеристики
Лиофилизат для приготовления раствора для инфузий 50 мг
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Лиофилизат, содержащий в одном флаконе 50 мг децитабина, помещенный в прозрачный стеклянный флакон (тип I) объемом 20 мл с бромбутил-резиновым ограничителем диаметром 20 мм и одноразовой алюминиевой крышкой. Каждый флакон вместе с инструкцией по медицинскому применению помещен в картонную упаковку.
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