Journal of Modern OncologyJournal of Modern OncologyСовременная онкология1815-14341815-1442LLC Obyedinennaya Redaktsiya8303810.26442/18151434.2021.3.201130CLINICAL ONCOLOGYКЛИНИЧЕСКАЯ ОНКОЛОГИЯReview ArticleRegorafenib in metastatic colorectal cancer: more data for clinical decisionsРегорафениб в лечении метастатического колоректального рака: больше данных для принятия решенийhttps://orcid.org/0000-0002-0342-40076811-8136PetkauVladislav V.ПеткауВладислав Владимирович
Russian Federation

Cand. Sci. (Med.)

канд. мед. наук, доц. каф. онкологии и лучевой диагностики

vpetkau@yandex.ruhttps://orcid.org/0000-0003-3500-096X8420-9600KarimovaAlisa A.КаримоваАлиса Алексеевна
Russian Federation

Cand. Sci. (Pharm.)

канд. фарм. наук, ассистент каф. управления и экономики фармации, фармакогнозии

alice-k2006@yandex.ruAkishinaZinaida V.АкишинаЗинаида Васильевна
Russian Federation

Deputy Chief Doctor

зам. глав. врача по амбулаторно-поликлинической работе, гл. онколог Минздрава Пермского края, засл. врач РФ

zvakishina@list.ruUral State Medical UniversityФГБОУ ВО «Уральский государственный медицинский университет» Минздрава РоссииPerm Regional Oncological DispensaryГБУЗ Пермского края «Пермский краевой онкологический диспансер»1911202123343644112102021Copyright ©; 2021, Consilium MedicumCopyright ©; 2021, ООО "Консилиум Медикум"2021Consilium MedicumООО "Консилиум Медикум"https://creativecommons.org/licenses/by-nc/4.0https://modernonco.orscience.ru/1815-1434/article/view/83038

Regorafenib is a multiple kinase inhibitor. It influences/blocks angiogenesis (VEGFR1-3, TIE2), proliferation (KIT, RET, RAF-1, BRAF), metastatic activity (VEGFR2-3, PDGFR), tumor immunogenicity (CSF1R), tumor microenvironment (PDGFR-α, PDGFR-β, FGFR1-2). Regorafenib has several indications including metastatic colorectal cancer. Efficacy and safety of regorafenib data from clinical trials (CORRECT, CONCUR, CONSIGN) and observational trials from real world (REBECCA, CORRELATE, RECORA, PMS, REGOTAS) are summarized and presented in this issue. State of the matter of molecular-biologic predictors (KRAS, PIK3CA ANG-2, VEGF-A, LDH, CCL5/CCR5, CA 19-9) and radiological predictors (RadioCORRECT and other trials) is highlighted. Regimens with dose modification and its influence on effectiveness and tolerability of regorafenib are described according to the data from ReDOS, RESET, REARRANGE trials. The results from retrospective trials comparing regorafenib and another approved for refractory metastatic colorectal cancer drug trifluridine/tipiracil are presented.

Регорафениб – мультитаргетный ингибитор тирозинкиназ, оказывающий влияние на ангиогенез (VEGFR1-3, TIE2), пролиферацию (KIT, RET, RAF-1, BRAF), метастазирование (VEGFR2-3, PDGFR), опухолевую иммуногенность (CSF1R), микроокружение опухоли (PDGFR-α, PDGFR-β, FGFR1-2). Регорафениб зарегистрирован по нескольким показаниям, в том числе для лечения метастатического колоректального рака. В статье представлены и обобщены данные по эффективности и профилю безопасности препарата, полученные как в клинических исследованиях III фазы (CORRECT, CONCUR, CONSIGN), так и в наблюдательных исследованиях в реальной клинической практике (REBECCA, CORRELATE, RECORA, PMS, REGOTAS). Рассмотрено изучение предикторов ответа, как молекулярно-биологических (KRAS, PIK3CA ANG-2, VEGF-A, ЛДГ, CCL5/CCR5, CA 19-9), так и рентгенологических (исследование RadioCORRECT и др.). Представлены варианты дозирования на основании исследований ReDOS, RESET, REARRANGE. Изучены данные ретроспективных исследований по сравнению регорафениба с другим зарегистрированным для рефрактерного метастатического колоректального рака препаратом трифлуридин/типирацил.

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