Lonafarnib
 | |
| Names | |
|---|---|
| IUPAC name
4-(2-{4-[(11R)-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]piperidin-1-yl}-2-oxoethyl)piperidine-1-carboxamide | |
| Other names
Sarasar (US), SCH 66336 | |
| Identifiers | |
193275-84-2  | |
| 3D model (Jmol) | Interactive image |
| ChEBI | CHEBI:47097 |
| ChEMBL | ChEMBL298734  |
| ChemSpider | 130645 |
| ECHA InfoCard | 100.204.509 |
| 8024 | |
| KEGG | D04768 |
| PubChem | 148195 |
| UNII | IOW153004F |
| |
| |
| Properties | |
| C27H31Br2ClN4O2 | |
| Molar mass | 638.82164 |
| Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| verify (what is ?) | |
| Infobox references | |
Lonafarnib is a farnesyltransferase inhibitor (FTI) that is being investigated in a human clinical trial as a potential treatment for progeria.[1]
Lonafarnib is a synthetic tricyclic derivative of carboxamide with antineoplastic properties.[2] As such, it is used primarily for cancer treatment. For those with progeria, research has shown that the drug reduces the prevalence of stroke and transient ischemic attack, and the prevalence and frequency of headaches while taking the medication.[3] A phase II clinical trial was completed in 2012, which showed that a cocktail of drugs that included lonafarnib and two other drugs, met clinical efficacy endpoints that improved the height and diminished the rigidity of the bones of progeria patients.
References
- ↑ Liu G, Marrinan CH, Taylor SA, et al. (2007). "Enhancement of the antitumor activity of tamoxifen and anastrozole by the farnesyltransferase inhibitor lonafarnib (SCH66336)". Anticancer Drugs. 18 (8): 923–31. doi:10.1097/CAD.0b013e3280c1416e (inactive 2015-01-14). PMID 17667598.
- ↑ "Lonafarnib". NCI Drug Dictionary. National Cancer Institute.
- ↑ Ullrich, N. J.; Kieran, M. W.; Miller, D. T.; Gordon, L. B.; Cho, Y.-J.; Silvera, V. M.; Giobbie-Hurder, A.; Neuberg, D.; Kleinman, M. E. (2013). "Neurologic features of Hutchinson–Gilford progeria syndrome after lonafarnib treatment". Neurology. 81 (5): 427–30. doi:10.1212/WNL.0b013e31829d85c0. PMC 3776537
. PMID 23897869.
See also
External links
- "Experimental Drug Is First To Help Kids With Premature-Aging Disease", NPR, September 24, 2012
This article is issued from Wikipedia - version of the 11/17/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.