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 ;
3D model (JSmol)	Interactive image;
ChEBI	CHEBI:47097 ;
ChEMBL	ChEMBL298734 ;
ChemSpider	130645 ;
ECHA InfoCard	100.204.509
IUPHAR/BPS	8024;
KEGG	D04768 ;
PubChem CID	148195;
UNII	IOW153004F ;
CompTox Dashboard (EPA)	DTXSID90172927 ;
	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 Key: DHMTURDWPRKSOA-RUZDIDTESA-N ; 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).
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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 halogenated 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.

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 2019-08-20). PMID 17667598.
“The FTI Drug Lonafarnib”, Progeria Research Foundation. Accessed October 3, 2017.
"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.

External links

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

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[pmid17667598-1] 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 2019-08-20). 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 3776537. PMID 23897869.

Lonafarnib

References

See also

External links