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Etalocib

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Etalocib
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
LY293111
VML 295
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
UNII
  • 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)[画像:check]Y
    Key:YFIZRWPXUYFCSN-UHFFFAOYSA-N[画像:check]Y
  • Fc1ccc(cc1)c4c(O)cc(OCCCOc3cccc(Oc2ccccc2C(=O)O)c3CCC)c(c4)CC
Properties
C33H33FO6
Molar mass 544.619g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25°C [77°F], 100kPa).
Chemical compound

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

  1. 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.
  2. 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.
  3. "Etalocib". Adisinsight. Retrieved 31 January 2017.


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