Lonafarnib

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
CAS Number	193275-84-2 N
3D model (Jmol)	Interactive image
ChEBI	CHEBI:47097 N
ChEMBL	ChEMBL298734 Y
ChemSpider	130645 Y
ECHA InfoCard	100.204.509
IUPHAR/BPS	8024
KEGG	D04768 Y
PubChem	148195
UNII	IOW153004F Y
InChI InChI=1S/C27H31Br2ClN4O2/c28-20-12-19-2-1-18-13-21(30)14-22(29)24(18)25(26(19)32-15-20)17-5-9-33(10-6-17)23(35)11-16-3-7-34(8-4-16)27(31)36/h12-17,25H,1-11H2,(H2,31,36)/t25-/m1/s1 Y Key: DHMTURDWPRKSOA-RUZDIDTESA-N Y InChI=1/C27H31Br2ClN4O2/c28-20-12-19-2-1-18-13-21(30)14-22(29)24(18)25(26(19)32-15-20)17-5-9-33(10-6-17)23(35)11-16-3-7-34(8-4-16)27(31)36/h12-17,25H,1-11H2,(H2,31,36)/t25-/m1/s1 Key: DHMTURDWPRKSOA-RUZDIDTEBQ
SMILES C=12CCC=3C=C(C=C(C3[C@H](C1N=CC(=C2)Br)C4CCN(CC4)C(=O)CC5CCN(CC5)C(N)=O)Br)Cl
Properties
Chemical formula	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).
N verify (what is YN ?)
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

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 2015-01-14). PMID 17667598. 
2. ↑ "Lonafarnib". NCI Drug Dictionary. National Cancer Institute. 
3. ↑ 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

• Laminopathy

External links

• "Experimental Drug Is First To Help Kids With Premature-Aging Disease", NPR, September 24, 2012