Luminespib

Chemical Compound
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References

Luminespib (INN,<ref>

WHO Drug Information. International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 70(link). {{{website}}}. World Health Organization.

</ref> 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<ref>

Structure-based design of cancer therapeutics(link). {{{website}}}. The Institute of Cancer Research.

</ref> and licensed to Novartis.<ref>

AUY922(link). {{{website}}}. Vernalis.

</ref> From 2011 to 2014 it was in Phase II clinical trials.<ref>

Small caps: Vernalis drug fillip(link). {{{website}}}. Financial Times. July 19, 2011.

</ref><ref name=Sidera2014rev>,

 HSP90 inhibitors: current development and potential in cancer therapy., 
 Recent Pat. Anticancer Drug Discov., 
 
 Vol. 9(Issue: 1),
 pp. 1–20,
 DOI: 10.2174/15748928113089990031,
 PMID: 23312026,
 
 
 Full text,</ref>  Chemically it is a resorcinylic isoxazole amide<ref name=Sidera2014rev/>

Luminespib is an inhibitor of heat shock protein 90 (Hsp90),<ref name=Brough/> 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.<ref>,

 NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models, 
 Breast Cancer Research, 
 2008,
 Vol. 10(Issue: 2),
 pp. R33,
 DOI: 10.1186/bcr1996,
 PMID: 18430202,
 PMC: 2397535,</ref><ref>, 
 Mechanistic Evaluation of the Novel HSP90 Inhibitor NVP-AUY922 in Adult and Pediatric Glioblastoma, 
 Molecular Cancer Therapeutics, 
 2010,
 Vol. 9(Issue: 5),
 pp. 1219–1233,
 DOI: 10.1158/1535-7163.MCT-09-0683,
 PMID: 20457619,
 PMC: 2875164,</ref><ref>, 
 Antitumor effect of novel HSP90 inhibitor NVP-AUY922 against oral squamous cell carcinoma, 
 Anticancer Research, 
 2011,
 Vol. 31(Issue: 4),
 pp. 1197–204,
 
 PMID: 21508365,</ref><ref>, 
 NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis, 
 Cancer Research, 
 2008,
 Vol. 68(Issue: 8),
 pp. 2850–2860,
 DOI: 10.1158/0008-5472.CAN-07-5256,
 PMID: 18413753,</ref>

A related compound, NVP-HSP990, was abandoned by Novartis in 2012 after it failed to show efficacy in an early clinical trial.<ref name=Sidera2014rev/>

See also

• Hsp90 inhibitors

References

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