Etalocib
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| Names | 
| Preferred IUPAC name 25-Ethyl-14-fluoro-22-hydroxy-82-propyl-3,7,9-trioxa-1,10(1),2(1,4),8(1,3)-tetrabenzenadecaphane-102-carboxylic acid | 
| Other names LY293111VML 295
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| Identifiers | 
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InChI=1S/C33H33FO6/c1-3-9-25-29(12-7-13-30(25)40-31-11-6-5-10-26(31)33(36)37)38-18-8-19-39-32-21-28(35)27(20-22(32)4-2)23-14-16-24(34)17-15-23/h5-7,10-17,20-21,35H,3-4,8-9,18-19H2,1-2H3,(H,36,37)  YKey: YFIZRWPXUYFCSN-UHFFFAOYSA-N  Y
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Fc1ccc(cc1)c4c(O)cc(OCCCOc3cccc(Oc2ccccc2C(=O)O)c3CCC)c(c4)CC
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| Properties | 
|  | C33H33FO6 | 
| Molar mass | 544.619 g·mol−1 | 
| Except where otherwise noted, data are given for materials in their standard state  (at 25 °C [77 °F], 100 kPa).Infobox references | 
Etalocib is a drug candidate that was under development for the treatment of various types of cancer.[1] It acts as a leukotriene B4 receptor antagonist and a PPARγ agonist.[2]
Clinical trials were conducted measuring efficacy for treatment of non-small cell lung cancer and pancreatic cancer and the inflammatory conditions asthma, psoriasis, and ulcerative colitis, but were suspended due to lack of efficacy.[3]
References
- ^ Jänne, P. A.; Paz-Ares, L; Oh, Y; Eschbach, C; Hirsh, V; Enas, N; Brail, L; von Pawel, J (2014). "Randomized, double-blind, phase II trial comparing gemcitabine-cisplatin plus the LTB4 antagonist LY293111 versus gemcitabine-cisplatin plus placebo in first-line non-small-cell lung cancer". Journal of Thoracic Oncology. 9 (1): 126–31. doi:10.1097/JTO.0000000000000037. PMID 24346102.
- ^ Adrian, T. E.; Hennig, R; Friess, H; Ding, X (2008). "The Role of PPARgamma Receptors and Leukotriene B(4) Receptors in Mediating the Effects of LY293111 in Pancreatic Cancer". PPAR Research. 2008: 827096. doi:10.1155/2008/827096. PMC 2631651. PMID 19190780.
- ^ "Etalocib". Adisinsight. Retrieved 31 January 2017.
 
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| Receptor (ligands)
 | | BLTTooltip Leukotriene B4 receptor | | BLT1Tooltip Leukotriene B4 receptor 1 | 
Antagonists: 20-Carboxy-LTB4AmelubantCGS-23131 (LY-223982)CGS-25019CCP-105696CP-195543LY-293111MoxilubantONO-4057RG-14893RP-69698SB-209247SC-53228TicolubantU-75302ZK-158252
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 | BLT2Tooltip Leukotriene B4 receptor 2 | 
Antagonists: CP-195543LY-255283ZK-158252
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 | CysLTTooltip Cysteinyl leukotriene receptor | | CysLT1Tooltip Cysteinyl leukotriene receptor 1 | 
Antagonists: AblukastBAYu9773BAYu9916BAYx7195CinalukastFPL-55712ICI-198615IralukastLY-170680MasilukastMK-571MontelukastONO-1078PobilukastPranlukastRitolukastSKF-104353SR-2640SulukastTipelukastTomelukastVerlukastZafirlukastZD-3523
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 | CysLT2Tooltip Cysteinyl leukotriene receptor 2 | 
Antagonists: BAYu9773BAYu9916
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 | CysLTETooltip Cysteinyl leukotriene receptor E |  | 
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| Enzyme (inhibitors)
 | | 5-LOXTooltip Arachidonate 5-lipoxygenase | 
FLAPTooltip Arachidonate 5-lipoxygenase-activating protein inhibitors: AM-103AM-679BAYx1005MK-591MK-886
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 | 12-LOXTooltip Arachidonate 12-lipoxygenase |  | 
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 | 15-LOXTooltip Arachidonate 15-lipoxygenase |  | 
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 | LTA4HTooltip Leukotriene A4 hydrolase |  | 
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 | LTB4HTooltip Leukotriene B4 ω-hydroxylase |  | 
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 | LTC4STooltip Leukotriene C4 synthase |  | 
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 | LTC4HTooltip Leukotriene C4 hydrolase |  | 
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 | LTD4Tooltip Leukotriene D4 hydrolase |  | 
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| Others |  | 
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See alsoReceptor/signaling modulatorsProstanoid signaling modulators
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| PPARαTooltip Peroxisome proliferator-activated receptor alpha |  | 
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| PPARδTooltip Peroxisome proliferator-activated receptor delta | 
Antagonists: FH-535GSK-0660GSK-3787
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| PPARγTooltip Peroxisome proliferator-activated receptor gamma | 
Antagonists: FH-535GW-9662SR-202T-0070907
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| Non-selective |  | 
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See alsoReceptor/signaling modulators
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