LSD1/KDM1A inhibitors in clinical trials: advances and prospects
Guangzhou University of Chinese Medicine · Ministry of Education of the People's Republic of China · +3 more institutions
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.
Citation impact
- FWCI
- 15.72
- Percentile
- 100%
- References
- 126
Authors
3- YFYuan Fang
Guangzhou University of Chinese Medicine, Ministry of Education of the People's Republic of China
- GLGuochao Liao
Guangzhou University of Chinese Medicine, Ministry of Education of the People's Republic of China
- BYBin YuCorresponding
China Pharmaceutical University, Zhengzhou University, Nanjing University
Topics & keywords
- Medicine
- Hematology
- Clinical trial
- Internal medicine
- Medical physics
- Intensive care medicine
- Good health and well-being
Funding
- NNNational Natural Science Foundation of ChinaAwards: 81973177, 81703326, 81773580, 2018B030322011
- CPChina Postdoctoral Science FoundationAwards: KF-GN-201902, M630840, 81703326, 81973177, 81773580, T120641
- NUNanjing UniversityAward: KF-GN-201902
- SKState Key Laboratory of Pharmaceutical BiotechnologyAward: KF-GN-201902
- SAScience and Technology Department of Henan ProvinceAward: 182102310123
- PRPostdoctoral Research Foundation of ChinaAwards: 2018M630840, 2019T120641