LSD1/KDM1A inhibitors in clinical trials: advances and prospects
Top Cited Papers
Open Access
- 4 December 2019
- journal article
- review article
- Published by Springer Science and Business Media LLC in Journal of Hematology & Oncology
- Vol. 12 (1), 1-14
- https://doi.org/10.1186/s13045-019-0811-9
Abstract
Histone demethylase LSD1 plays key roles during carcinogenesis, targeting LSD1 is becoming an emerging option for the treatment of cancers. Numerous LSD1 inhibitors have been reported to date, some of them such as TCP, ORY-1001, GSK-2879552, IMG-7289, INCB059872, CC-90011, and ORY-2001 currently undergo clinical assessment for cancer therapy, particularly for small lung cancer cells (SCLC) and acute myeloid leukemia (AML). This review is to provide a comprehensive overview of LSD1 inhibitors in clinical trials including molecular mechanistic studies, clinical efficacy, adverse drug reactions, and PD/PK studies and offer prospects in this field.Keywords
Funding Information
- National Natural Science Foundation of China (81703326, 81973177, 81773580)
- Science and Technology Department of Henan Province (182102310123)
- Postdoctoral Research Foundation of China (2018M630840, 2019T120641)
- Guangdong Key Laboratory for Translational Cancer Research of Chinese Medicine (2018B030322011)
- the open fund of state key laboratory of Pharmaceutical Biotechnology, Nan-jing University, China (KF-GN-201902)
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