РАДИАЦИЯ И РИСК
Бюллетень Национального радиационно-эпидемиологического регистра
c 1992 года

Аналоги соматостатина, меченные радионуклидами, для терапии онкологических заболеваний. Обзор

DOI: 10.21870/0131-3878-2022-31-2-76-96

Тищенко В.К.1, Петриев В.М.1,2, Крылов В.В.1, Власова О.П.1,3, Шегай П.В.3, Иванов С.А.1, Каприн А.Д.3

«Радиация и риск». 2022. Том 31. № 2, с.76-96

Сведения об авторах

Тищенко В.К. – вед. науч. сотр., д.б.н.
Петриев В.М. – зав. лаб., д.б.н., проф. НИЯУ МИФИ. Контакты: 249035, Калужская обл., Обнинск, ул. Королёва, 4. Тел.: (484) 399-71-00; e-mail: Этот адрес электронной почты защищен от спам-ботов. У вас должен быть включен JavaScript для просмотра. .
Крылов В.В. – зав. отд., д.м.н.
Власова О.П. – вед. науч. сотр., к.б.н.
Иванов С.А. – директор, д.м.н., проф. РАН. МРНЦ им. А.Ф. Цыба – филиал ФГБУ «НМИЦ радио-логии» Минздрава России.
Шегай П.В. – зам. ген. директора, к.м.н.
Каприн А.Д. – ген. директор, акад. РАН, д.м.н., проф. ФГБУ «НМИЦ радиологии» Минздрава России.

1 МРНЦ им. А.Ф. Цыба – филиал ФГБУ «НМИЦ радиологии» Минздрава России, Обнинск
2 Национальный исследовательский ядерный университет «МИФИ», Москва
3 ФГБУ «НМИЦ радиологии» Минздрава России, Москва

Аннотация

В настоящее время основным требованием к радионуклидной терапии онкологических заболеваний является специфическое воздействие на опухолевые клетки с минимальной токсичностью в отношении здоровых тканей. Молекулярная основа селективной противоопухолевой терапии обеспечивается сверхэкспрессией соматостатиновых рецепторов (ССТр) на клеточной мембране различных опухолей и их метастазов. Природный соматостатин не может быть использован в качестве векторной молекулы для доставки радионуклидов ввиду короткого периода полураспада в крови (1-3 мин). Синтетические аналоги соматостатина пептидной природы, меченные терапевтическими радионуклидами (радиопептиды), также обладают высоким сродством с ССТр и улучшенной фармакокинетикой по сравнению с соматостатином, и потому представляют огромный интерес для направленной терапии рака, именуемой пептид-рецепторной радионуклидной терапией (ПРРТ). В обзоре представлена информация о наиболее значимых на сегодняшний день аналогах соматостатина, меченных радионуклидами 111In, 90Y, 177Lu, для терапии опухолей со сверхэкспрессией ССТр. Приведены данные об эффективности лечения и профиле токсичности ПРРТ, проводимой с различными поколениями радио-фармацевтических лекарственных препаратов (РФЛП), нацеленных на ССТр, включая рандомизированное контролируемое исследование NETTER-1. Кроме того, обсуждаются некоторые стратегии оптимизации ПРРТ, такие как тандемная терапия, внутриартериальный способ введения РФЛП, модификация препаратов для оптимизации фармакокинетики, а также разработка новых препаратов, содержащих альфа-излучающие радионуклиды, или являющихся антагонистами ССТр.

Ключевые слова
аналоги соматостатина, радиопептиды, пептид-рецепторная радионуклидная терапия, соматостатиновые рецепторы, производные октреотида, радиофармацевтический лекарственный препарат (РФЛП), DOTATOC, DOTATATE, нейроэндокринные опухоли.

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