Dactolisib

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Dactolisib
Dactolisib.svg
Ball-and-stick model of the BEZ235 molecule
Names
IUPAC name
2-Methyl-2-{4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl]phenyl}propanenitrile
Other names
NVP-BEZ235; BEZ-235
Identifiers
3D model (JSmol)
ChemSpider
KEGG
Properties
C30H23N5O
Molar mass 469.55 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references

Dactolisib (codenamed NVP-BEZ235 and BEZ-235) is an imidazoquinoline derivative acting as a PI3K inhibitor.[1] It also inhibits mTOR.[2] It is being investigated as a possible cancer treatment.[3]

It has been shown to be toxic to Waldenström's macroglobulinemia cells.[4]

It was the first PI3K inhibitor to enter clinical trials, in 2006.[5]

A phase IB/II clinical trial for locally advanced or metastatic HER2 negative breast cancer has completed.[6]

A phase II clinical trial for advanced pancreatic neuroendocrine tumors (pNET) has reported results.[7]

References[edit]

  1. ^ Liu, TJ; Koul, D; LaFortune, T; Tiao, N; Shen, RJ; Maira, SM; Garcia-Echevrria, C; Yung, WKA (11 August 2009). "NVP-BEZ235, a Novel Dual Phosphatidylinositol 3-kinase/Mammalian Target of Rapamycin Inhibitor, Elicits Multifaceted Antitumor Activities in Human Gliomas". Molecular Cancer Therapeutics. 8 (8): 2204–10. PMC 2752877Freely accessible. PMID 19671762. doi:10.1158/1535-7163.MCT-09-0160. 
  2. ^ Awasthi, N; Yen, PL; Schwarz, MA; Schwarz, RE (March 2012). "The Efficacy of a Novel, Dual PI3K/mTOR Inhibitor NVP-BEZ235 to Enhance Chemotherapy and Antiangiogenic Response in Pancreatic Cancer". Journal of Cellular Biochemistry. 113 (3): 784–91. PMID 22020918. doi:10.1002/jcb.23405. 
  3. ^ Maira, SM; Stauffer, F; Schnell, C; García-Echeverría, C (1 February 2009). "PI3K Inhibitors for Cancer Treatment: Where Do We Stand?" (PDF). Biochemical Society Transactions. 37 (1): 265–72. PMID 19143644. doi:10.1042/BST0370265. Retrieved 16 July 2016. 
  4. ^ Sacco, A; Roccaro, A; Ghobrial, IM (November 2010). "Role of Dual PI3/Akt and mTOR Inhibition in Waldenström's Macroglobulinemia". Oncotarget. 1 (7): 578–82. PMC 3248138Freely accessible. PMID 21317453. doi:10.18632/oncotarget.101105. 
  5. ^ "A Phase I/II Study of BEZ235 in Patients with Advanced Solid Malignancies Enriched by Patients with Advanced Breast Cancer". ClinicalTrials.gov. Retrieved 16 July 2016. 
  6. ^ Phase Ib/II Trial of BEZ235 With Paclitaxel in Patients With HER2 Negative, Locally Advanced or Metastatic Breast Cancer
  7. ^ BEZ235 Phase II Trial in Patients With Advanced Pancreatic Neuroendocrine Tumors (pNET) After Failure of mTOR Inhibitor Therapy.