Luminespib Explained

Luminespib (INN,[1] 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[2] and licensed to Novartis.[3] From 2011 to 2014 it was in Phase II clinical trials.[4] [5] Chemically it is a resorcinylic isoxazole amide[5]

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.[6] [7] [8] [9]

A related compound, NVP-HSP990, was abandoned by Novartis in 2012 after it failed to show efficacy in an early clinical trial.[5]

See also

Notes and References

  1. Web site: WHO Drug Information. International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 70. World Health Organization. 16 July 2016. 297–8.
  2. Web site: Structure-based design of cancer therapeutics . The Institute of Cancer Research . 2011-10-25 . https://web.archive.org/web/20110625222638/http://icr.ac.uk/about_us/annual_research_report/9719.pdf . 2011-06-25 . dead .
  3. Web site: AUY922 . Vernalis . dead. https://web.archive.org/web/20110929015547/http://www.vernalis.com/development/oncology/auy922 . 2011-09-29 .
  4. News: Small caps: Vernalis drug fillip . Financial Times . July 19, 2011.
  5. Sidera, K. . Patsavoudi, E. . HSP90 inhibitors: current development and potential in cancer therapy. . Recent Patents on Anti-Cancer Drug Discovery. 9 . 1 . 1–20 . Jan 2014 . 23312026 . 10.2174/15748928113089990031 .
  6. 10.1186/bcr1996 . NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models . 2008 . Jensen . Michael . Schoepfer . Joseph . Radimerski . Thomas . Massey . Andrew . Guy . Chantale T . Brueggen . Josef . Quadt . Cornelia . Buckler . Alan . Cozens . Robert . Breast Cancer Research . 10 . 2 . R33 . 18430202 . 2397535 . free .
  7. 10.1158/1535-7163.MCT-09-0683 . Mechanistic Evaluation of the Novel HSP90 Inhibitor NVP-AUY922 in Adult and Pediatric Glioblastoma . 2010 . Gaspar . N. . Sharp . S. Y. . Eccles . S. A. . Gowan . S. . Popov . S. . Jones . C. . Pearson . A. . Vassal . G. . Workman . P. . Molecular Cancer Therapeutics . 9 . 5 . 1219–1233 . 20457619 . 2875164 .
  8. 21508365 . 2011 . Okui . T . Shimo . T . Hassan . NM . Fukazawa . T . Kurio . N . Takaoka . M . Naomoto . Y . Sasaki . A . Antitumor effect of novel HSP90 inhibitor NVP-AUY922 against oral squamous cell carcinoma . 31 . 4 . 1197–204 . Anticancer Research .
  9. 10.1158/0008-5472.CAN-07-5256 . NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis . 2008 . Eccles . S. A. . Massey . A. . Raynaud . F. I. . Sharp . S. Y. . Box . G. . Valenti . M. . Patterson . L. . De Haven Brandon . A. . Gowan . S. . Cancer Research . 68 . 8 . 2850–2860 . 18413753 . free .

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