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Experimental cancer drugs
RO4929097
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    RO4929097

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    RO4929097
    RO4929097.svg
    Identifiers
    • 2,2-Dimethyl-N-[(10S)-9-oxo-8-azatricyclo[9.4.0.02,7]pentadeca-1(15),2,4,6,11,13-hexaen-10-yl]-'N′-(2,2,3,3,3-pentafluoropropyl)propanediamide
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    CompTox Dashboard (EPA)
    Chemical and physical data
    Formula C22H20F5N3O3
    Molar mass 469.412 g·mol−1
    3D model (JSmol)
    • O=C1Nc2ccccc2c2c(C1NC(=O)C(C(=O)NCC(C(F)(F)F)(F)F)(C)C)cccc2
    • InChI=1S/C22H20F5N3O3/c1-20(2,18(32)28-11-21(23,24)22(25,26)27)19(33)30-16-14-9-4-3-7-12(14)13-8-5-6-10-15(13)29-17(16)31/h3-10,16H,11H2,1-2H3,(H,28,32)(H,29,31)(H,30,33)/t16-/m0/s1
    • Key:OJPLJFIFUQPSJR-INIZCTEOSA-N

    RO4929097 (RG-4733) is a gamma secretase inhibitor being studied as an anti-cancer drug. Targeting gamma secretase inhibits NOTCH signaling, which is upregulated in many forms of cancer. The drug was initially developed by Roche for the treatment of Alzheimer's disease, but current research focuses on cancer. Production was halted in 2010, but began again in 2014.

    Research

    Over 35 phase I and II clinical trials have been performed, but no phase III trials have yet commenced. Phase II studies have investigated the use of RO4929097 in ovarian cancer,renal cell carcinoma in patients that were unsuccessful on anti-VEGF treatments, metastatic pancreatic cancer, advanced brain tumors, and relapsed non-small cell lung cancer.

    Other planned clinical trials were terminated, because the drug became unavailable.


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