<p>Enasidenib in the treatment of relapsed/refractory acute myeloid leukemia: an evidence-based review of its place in therapy</p>

Abstract

Introduction: Acute myeloid leukemia (AML) remains a disease with high mortality, especially for older patients and those with relapsed/refractory (R/R) disease. With recent advances in molecular testing, targeting particular leukemogenic mutations such as those occurring in isocitrate dehydrogenase (IDH) became possible. Enasidenib is a new small-molecule inhibitor of mutant isocitrate dehydrogenase-2 (IDH2). Aim: The objective of this article is to review the evidence for the use of enasidenib in R/R AML, as well as to outline future directions of enasidenib therapy. Evidence Review: Enasidenib was approved in August 2017, after a successful Phase I/II trial showing an overall response rate (ORR) of 40.3% in R/R disease, with 19.3% of patients achieving complete remission (CR). Enrollees in the trial were mostly older adults. The most prominent toxicities were hyperbilirubinemia and IDH-differentiation syndrome (IDH-DS), though the drug was generally well tolerated and the maximum tolerated dose was not reached. A Phase III trial is currently ongoing. Conclusion: Enasidenib provides a new therapeutic option for patients with R/R AML. Further studies are ongoing to ascertain its role in combination with other agents and newly diagnosed disease.

Isocitrate dehydrogenase inhibitors in acute myeloid leukemia

“…Enasidenib (Idhifa®) is an oral selectively allosteric inhibitor of IDH2 mutation developed by Celgene Corporation under a global exclusive license from Agios Pharmaceuticals. It shows more powerful inhibitory effects on IDH2 R172K rather than IDH1 R140Q (ORR, 53.3% vs. 35.4%; CR, 24.4% vs. 17.7%) mutation, although it has inhibitory effects on both the mutations [52]. FDA has approved enasidenib for the treatment of adult R/R AML with IDH2 mutations on 1 August 2017.…”

Can a metabolism-targeted therapeutic intervention successfully subjugate SARS-COV-2? A scientific rational

“…As shown in Table 2 [ 21 , [160] , [161] , [162] , [163] , [164] , [165] , [166] , [167] , [168] , [169] , [170] , [171] , [172] , [173] , [174] , [175] , [176] , [177] , [178] , [179] , [180] , [181] , [182] , [183] , [184] , [185] , [186] , [187] , [188] , [189] , [190] , [191] , [192] , [193] , [194] , [195] , [196] , [197] , [198] , [199] , [200] , [201] , [202] , [203] , [204] , [205] , [206] , [207] ], there are many Krebs cycle inhibitors with antiviral properties. Here, metformin, according to its well-established and favorable side effect profile and antiviral activity [ [208] , [209] , [210] , [211] , [212] , [213] , [214] , [215] ], seems to be a promising compound.…”

Pediatric acute myeloid leukemias treatment: current scientific view

“…Первые результаты для AG120 у пациентов с рецидивом ОМЛ доказали эффективность, анало гичную ингибитору IDH2, с частотой ПО или ПО с ча стичным гематологическим восстановлением 30,4 %. Исследований применения этих препаратов у детей в настоящее время нет [89].…”