Lonafarnib

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Lonafarnib
Lonafarnib.svg
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
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
ECHA InfoCard 100.204.509
KEGG
UNII
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).
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Infobox references

Lonafarnib is a farnesyltransferase inhibitor (FTI) that has been investigated in a human clinical trial as a treatment for progeria, which is an extremely rare genetic disorder in which symptoms resembling aspects of aging are manifested at a very early age.[1][2]

Lonafarnib is a synthetic tricyclic derivative of carboxamide with antineoplastic properties.[3] 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.[4] 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.[citation needed]

References[edit]

  1. ^ 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 2017-01-16). PMID 17667598. 
  2. ^ “The FTI Drug Lonafarnib”, Progeria Research Foundation. Accessed October 3, 2017.
  3. ^ "Lonafarnib". NCI Drug Dictionary. National Cancer Institute. 
  4. ^ 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 3776537Freely accessible. PMID 23897869. 

See also[edit]

External links[edit]