Idelalisib

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Idelalisib

Systematic (IUPAC) name
5-Fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]-4(3H)-quinazolinone
Clinical data
Legal status	Investigational
Routes	Oral
Identifiers

ATC code	None
PubChem	CID 11625818
ChemSpider	9800565
Synonyms	GS-1101, CAL-101
Chemical data
Formula	C₂₂H₁₈F N₇O
Mol. mass	415.42 g/mol
SMILES Fc2cccc3\N=C(/N(c1ccccc1)C(=O)c23)[C@@H](Nc4ncnc5ncnc45)CC
InChI InChI=1S/C22H18FN7O/c1-2-15(28-20-18-19(25-11-24-18)26-12-27-20)21-29-16-10-6-9-14(23)17(16)22(31)30(21)13-7-4-3-5-8-13/h3-12,15H,2H2,1H3,(H2,24,25,26,27,28)/t15-/m0/s1 Key:IFSDAJWBUCMOAH-HNNXBMFYSA-N

Idelalisib (codenamed GS-1101 or CAL-101) is a drug under investigation for the treatment of chronic lymphocytic leukaemia. It is in Phase III clinical trials testing drug combinations with rituximab^[1] and/or bendamustine as of 2013. The substance acts as a phosphoinositide 3-kinase inhibitor; more specifically, it blocks P110δ, the delta isoform of the enzyme phosphoinositide 3-kinase.^[2]^[3]

References

↑ Furman, Richard R.; Sharman, Jeff P.; Coutre, Steven E.; Cheson, Bruce D.; Pagel, John M.; Hillmen, Peter; Barrientos, Jacqueline C.; Zelenetz, Andrew D.; Kipps, Thomas J.; Flinn, Ian; Ghia, Paolo; Eradat, Herbert; Ervin, Thomas; Lamanna, Nicole; Coiffier, Bertrand; Pettitt, Andrew R.; Ma, Shuo; Stilgenbauer, Stephan; Cramer, Paula; Aiello, Maria; Johnson, Dave M.; Miller, Langdon L.; Li, Daniel; Jahn, Thomas M.; Dansey, Roger D.; Hallek, Michael; O'Brien, Susan M. (2014). "Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia". New England Journal of Medicine: 140122140218007. doi:10.1056/NEJMoa1315226.
↑ H. Spreitzer (13 May 2013). "Neue Wirkstoffe – Ibrutinib und Idelalisib". Österreichische Apothekerzeitung (in German) (10/2013): 34.
↑ Wu, M.; Akinleye, A.; Zhu, X. (2013). "Novel agents for chronic lymphocytic leukemia". Journal of Hematology & Oncology 6: 36. doi:10.1186/1756-8722-6-36. PMC 3659027. PMID 23680477.

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