Chemistry:RO4929097
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| Formula | C22H20F5N3O3 |
| Molar mass | 469.412 g·mol−1 |
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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]
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
- ↑ "Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties". Cancer Research 69 (19): 7672–80. October 2009. doi:10.1158/0008-5472.CAN-09-1843. PMID 19773430.
- ↑ "Gamma-secretase/Notch signalling pathway inhibitor RO4929097". NCI Drug Dictionary. National Cancer Institute. https://www.cancer.gov/publications/dictionaries/cancer-drug/def/gamma-secretase-inhibitor-ro4929097.
- ↑ "RO4929097". IUPHAR/BPS Guide to PHARMACOLOGY. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7338.
- ↑ "RG 4733". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800027906.
- ↑ "Search for: RO4929097 - List Results - ClinicalTrials.gov". https://clinicaltrials.gov/ct2/results?term=RO4929097.
- ↑ Clinical trial number NCT01175343 for "RO4929097 in Treating Patients With Recurrent and/or Metastatic Epithelial Ovarian Cancer, Fallopian Tube Cancer, or Primary Peritoneal Cancer" at ClinicalTrials.gov
- ↑ Clinical trial number NCT01141569 for "A Study of RO4929097 in Patients With Advanced Renal Cell Carcinoma That Have Failed Vascular Endothelial Growth Factor (VEGF)/Vascular Endothelial Growth Factor Receptor (VEGFR) Therapy" at ClinicalTrials.gov
- ↑ Clinical trial number NCT01232829 for "Gamma Secretase Inhibitor RO4929097 in Previously Treated Metastatic Pancreas Cancer" at ClinicalTrials.gov
- ↑ Clinical trial number NCT01122901 for "Gamma-Secretase/Notch Signalling Pathway Inhibitor RO4929097 in Treating Patients With Recurrent or Progressive Glioblastoma" at ClinicalTrials.gov
- ↑ Clinical trial number NCT01070927 for "An Exploratory Study of RO4929097 in Patients With Recurrent or Refractory Non-Small Cell Lung Cancer" at ClinicalTrials.gov
- ↑ Clinical trial number NCT01216787 for "RO4929097 in Treating Patients With Stage IIIB, Stage IIIC, or Stage IV Melanoma That Can Be Removed by Surgery" at ClinicalTrials.gov
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