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Dactolisib
Names
	Preferred 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; RTB101
Identifiers
CAS Number	915019-65-7 ;
3D model (JSmol)	Interactive image;
ChEMBL	ChEMBL1879463 ;
ChemSpider	10151099 ;
IUPHAR/BPS	7950;
KEGG	D10552;
PubChem CID	11977753;
UNII	RUJ6Z9Y0DT ;
CompTox Dashboard (EPA)	DTXSID10238599 ;
	InChI InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3 Key: JOGKUKXHTYWRGZ-UHFFFAOYSA-N ;
	SMILES N#CC(c6ccc(N5c4c(cnc3ccc(c1cc2ccccc2nc1)cc34)N(C5=O)C)cc6)(C)C;
Properties
Chemical formula	C30H23N5O
Molar mass	469.548 g·mol−1
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). verify (what is ?) Infobox references

Dactolisib (codenamed NVP-BEZ235 and BEZ-235, also known as RTB101) 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) had initially reported results, but was later terminated because insufficient normal tissue tolerance to the drug.^[7] A phase I clinical trial of BEZ235 in patients with advanced renal cell carcinoma had to be terminated prematurely due to toxicity and a lack of clinical efficacy .^[8] Another Phase Ib study on patients with various solid cancers found severe normal tissue toxicity as well when BEZ235/Dactolisib was administered in combination with the mTOR inhibitor Everolimus. The authors concluded that the combination of both drugs demonstrated limited efficacy and tolerance. BEZ235 systemic exposure increased in a dose-proportional manner while oral bioavailability was quite low, which may be related to gastrointestinal-specific toxicity .^[9] A phase I study of BEZ-235 to treat acute lymphoid leukaemia was initiated in 2012, but no results were published since then.^[10]

A phase 2a randomized, placebo-controlled clinical trial published in 2018 showed that everolimus in combination with dactolisib decreased the rate of reported infections in an elderly population.^[11]