NVP-AUY-922; AUY922; VER-52296
3D model (JSmol)
|Molar mass||465.55 g·mol−1|
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
|what is ?)(|
Luminespib (INN, previously known as NVP-AUY922) is an experimental drug candidate for the treatment of cancer. It was discovered through a collaboration between The Institute of Cancer Research and the pharmaceutical company Vernalis and licensed to Novartis. From 2011 to 2014 it was in Phase II clinical trials. Chemically it is a resorcinylic isoxazole amide
Luminespib is an inhibitor of heat shock protein 90 (Hsp90), which is a chaperone protein that plays a role in the modification of a variety of proteins that have been implicated in oncogenesis. Luminespib has shown promising activity in preclinical testing against several different tumor types.
A related compound, NVP-HSP990, was abandoned by Novartis in 2012 after it failed to show efficacy in an early clinical trial.
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- Jensen, Michael; Schoepfer, Joseph; Radimerski, Thomas; Massey, Andrew; Guy, Chantale T; Brueggen, Josef; Quadt, Cornelia; Buckler, Alan; Cozens, Robert (2008). "NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models". Breast Cancer Research. 10 (2): R33. doi:10.1186/bcr1996. PMC . PMID 18430202.
- Gaspar, N.; Sharp, S. Y.; Eccles, S. A.; Gowan, S.; Popov, S.; Jones, C.; Pearson, A.; Vassal, G.; Workman, P. (2010). "Mechanistic Evaluation of the Novel HSP90 Inhibitor NVP-AUY922 in Adult and Pediatric Glioblastoma". Molecular Cancer Therapeutics. 9 (5): 1219–1233. doi:10.1158/1535-7163.MCT-09-0683. PMC . PMID 20457619.
- Okui, T; Shimo, T; Hassan, NM; Fukazawa, T; Kurio, N; Takaoka, M; Naomoto, Y; Sasaki, A (2011). "Antitumor effect of novel HSP90 inhibitor NVP-AUY922 against oral squamous cell carcinoma". Anticancer research. 31 (4): 1197–204. PMID 21508365.
- Eccles, S. A.; Massey, A.; Raynaud, F. I.; Sharp, S. Y.; Box, G.; Valenti, M.; Patterson, L.; De Haven Brandon, A.; Gowan, S. (2008). "NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis". Cancer Research. 68 (8): 2850–2860. doi:10.1158/0008-5472.CAN-07-5256. PMID 18413753.
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