Chapter title |
Enasidenib
|
---|---|
Chapter number | 9 |
Book title |
Small Molecules in Hematology
|
Published in |
Recent results in cancer research Fortschritte der Krebsforschung Progrès dans les recherches sur le cancer, January 2018
|
DOI | 10.1007/978-3-319-91439-8_9 |
Pubmed ID | |
Book ISBNs |
978-3-31-991438-1, 978-3-31-991439-8
|
Authors |
Alwin Krämer, Tilmann Bochtler, Krämer, Alwin, Bochtler, Tilmann |
Abstract |
Enasidenib is an orally available, selective, potent, small molecule inhibitor of mutant isocitrate dehydrogenase 2 (IDH2). Neomorphic mutations in IDH2 are frequently found in both hematologic malignancies and solid tumors and lead to the production of the oncometabolite (R)-2-hydroxyglutarate. Increased levels of (R)-2-hydroxyglutarate cause histone and DNA hypermethylation associated with blocked differentiation and tumorigenesis. In PDX mice transplanted with human IDH2-mutant acute myeloid leukemia cells, enasidenib treatment led to normalization of (R)-2-hydroxyglutarate serum levels, differentiation of leukemic blasts and increased survival. Early clinical data in patients with relapsed/refractory IDH2-mutant acute myeloid leukemia show that enasidenib is well tolerated and induces durable complete remissions as a single agent in about 20% of cases. One notable drug-related adverse effect is differentiation syndrome. On the basis of these results the compound has recently been approved for the treatment of relapsed/refractory IDH2-mutant acute myeloid leukemia in the USA. Although no data are available yet, clinical trials on the treatment of patients with several types of IDH2-mutant solid tumors including gliomas, chondrosarcomas and cholangiocarcinomas are currently being performed. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 34 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Master | 4 | 12% |
Student > Bachelor | 3 | 9% |
Researcher | 3 | 9% |
Student > Ph. D. Student | 3 | 9% |
Professor > Associate Professor | 2 | 6% |
Other | 2 | 6% |
Unknown | 17 | 50% |
Readers by discipline | Count | As % |
---|---|---|
Medicine and Dentistry | 7 | 21% |
Biochemistry, Genetics and Molecular Biology | 6 | 18% |
Engineering | 2 | 6% |
Chemistry | 1 | 3% |
Pharmacology, Toxicology and Pharmaceutical Science | 1 | 3% |
Other | 0 | 0% |
Unknown | 17 | 50% |