- Guide to PHARMACOLOGY
Synonyms: compound 8 [PMID: 20143778] | CUDC101
Compound class: Synthetic organic
Comment: CUDC-101 is an orally available Phase I compound which is multiacting, inhibiting class I/II histone deacetylases (HDACs) but not the class III sirtuins, and the type I receptor tyrosine kinases EGFR and ERBB2 (HER2) . Targeting two pathogenic pathways simultaneously is one of the strategies being evaluated to overcome problems associated with molecular heterogeneity of tumours and the development of drug resistance.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Cai X, Zhai HX, Wang J, Forrester J, Qu H, Yin L, Lai CJ, Bao R, Qian C. (2010)
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
J Med Chem, 53 (5): 2000-9. [PMID:20143778]
2. Galloway TJ, Wirth LJ, Colevas AD, Gilbert J, Bauman JE, Saba NF, Raben D, Mehra R, Ma AW, Atoyan R et al.. (2015)
A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma.
Clin Cancer Res, 21 (7): 1566-73. [PMID:25573383]
3. Shimizu T, LoRusso PM, Papadopoulos KP, Patnaik A, Beeram M, Smith LS, Rasco DW, Mays TA, Chambers G, Ma A et al.. (2014)
Phase I first-in-human study of CUDC-101, a multitargeted inhibitor of HDACs, EGFR, and HER2 in patients with advanced solid tumors.
Clin Cancer Res, 20 (19): 5032-40. [PMID:25107918]