RO4929097

Chemical compound From Wikipedia, the free encyclopedia

RO4929097 (RG-4733) is a gamma secretase inhibitor being studied as an anti-cancer drug.[1] Targeting gamma secretase inhibits NOTCH signaling, which is upregulated in many forms of cancer.[2] The drug was initially developed by Roche for the treatment of Alzheimer's disease, but current research focuses on cancer.[3] Production was halted in 2010, but began again in 2014.[4]

CAS Number
PubChem CID
ChemSpider
UNII
Quick facts Identifiers, CAS Number ...
RO4929097
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
FormulaC22H20F5N3O3
Molar mass469.412 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
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Research

Over 35 phase I and II clinical trials have been performed, but no phase III trials have yet commenced.[5] Phase II studies have investigated the use of RO4929097 in ovarian cancer,[6] renal cell carcinoma in patients that were unsuccessful on anti-VEGF treatments,[7] metastatic pancreatic cancer,[8] advanced brain tumors,[9] and relapsed non-small cell lung cancer.[10]

Other planned clinical trials were terminated, because the drug became unavailable.[11]

References

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