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. 2018 Sep 12;78(14):1509–1516. doi: 10.1007/s40265-018-0978-3

Features and properties of Ivosidenib

Alternative names AG-120; Tibsovo®
Class Antineoplastics, cyclobutanes, nitriles, pyridines, pyrrolidines, small molecules
Mechanism of Action Isocitrate dehydrogenase 1 inhibitor
Route of Administration Oral
Pharmacodynamics Selective, small molecule inhibitor of isocitrate dehydrogenase R132 mutants, resulting in the inhibition of mutant isocitrate dehydrogenase enzyme and decreased 2-hydroxyglutarate levels
Pharmacokinetics Rapidly absorbed (median time to peak plasma concentration ≈ 3 h)
Terminal elimination half-life 93 h
Adverse events in patients with acute myeloid leukaemia
 Any-grade treatment-emergent Diarrhoea, leucocytosis, febrile neutropenia, nausea, fatigue, dyspnoea, prolongation of the QT interval, peripheral oedema, anaemia, pyrexia, cough
 Grade ≥ 3 treatment-related Prolongation of QT interval, isocitrate dehydrogenase differentiation syndrome
ATC codes
 WHO ATC code L01X-X (Other antineoplastic agents)
 EphMRA ATC code L1X9 (All other antineoplastics)
Chemical Name (2S)-N-[(1S)-1-(2-Chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl]-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide