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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/10/21 10:44:32」(JST)

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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.^{[citation needed]}

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.

External links

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

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. D型肝炎ウイルス感染の治療および予防 treatment and prevention of hepatitis d virus infection
2. 高IgD症候群：病態生理 hyperimmunoglobulin d syndrome pathophysiology

English Journal

An encouraging progress report on the treatment of progeria and its implications for atherogenesis.

Oshima J1, Hisama FM2, Martin GM2.
Circulation.Circulation.2014 Jul 1;130(1):4-6. doi: 10.1161/CIRCULATIONAHA.114.010648. Epub 2014 May 2.
PMID 24795391

Impact of farnesylation inhibitors on survival in Hutchinson-Gilford progeria syndrome.

Gordon LB1, Massaro J2, D'Agostino RB Sr2, Campbell SE2, Brazier J2, Brown WT2, Kleinman ME2, Kieran MW2; Progeria Clinical Trials Collaborative.
Circulation.Circulation.2014 Jul 1;130(1):27-34. doi: 10.1161/CIRCULATIONAHA.113.008285. Epub 2014 May 2.
BACKGROUND: Hutchinson-Gilford progeria syndrome is an ultrarare segmental premature aging disease resulting in early death from heart attack or stroke. There is no approved treatment, but starting in 2007, several recent single-arm clinical trials administered inhibitors of protein farnesylation ai
PMID 24795390

Progeria: a rare genetic premature ageing disorder.

Sinha JK, Ghosh S, Raghunath M1.
The Indian journal of medical research.Indian J Med Res.2014 May;139(5):667-74.
Progeria is characterized by clinical features that mimic premature ageing. Although the mutation responsible for this syndrome has been deciphered, the mechanism of its action remains elusive. Progeria research has gained momentum particularly in the last two decades because of the possibility of r
PMID 25027075

Japanese Journal

The farnesyltransferase inhibitor lonafarnib induces CCAAT/enhancer-binding protein homologous protein-dependent expression of death receptor 5, leading to induction of apoptosis in human cancer cells

SUN SY
J Biol Chem 282, 18800-18809, 2007
NAID 80018479911

Related Pictures

First-ever drug trial reverses some signs of aging in progeria - Vector Lonafarnib by aseem Drug Shows Promise Against Rapid-Aging Disease - Photo Journal - WSJ Lonafarnib • ARZNEI-NEWS.de Great News For The Progeria Community | DNA Science Blog Determinants of Health and Disease (7.295) Srunphut Pukma - ppt video online download Results of Phase 2 study of lonafarnib in HDV published Treatment - SaterScience

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リンク元	「nib」「上皮成長因子受容体阻害薬」「ロナファーニブ」

「nib」

Lonafarnib
Names
	IUPAC name 4-(2-(4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-yl)-1-piperidinyl)-2-oxoethyl)-1-piperidinecarboxamide
	Other names Sarasar (US), SCH 66336
Identifiers
CAS Registry Number	193275-84-2
ChEMBL	ChEMBL298734
ChemSpider	130645
	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 ;
IUPHAR/BPS	8024
Jmol-3D images	Image
KEGG	D04768
PubChem	148195
	SMILES O=C(N)N5CCC(CC(=O)N4CCC([C@@H]3c1c(Br)cc(Cl)cc1CCc2cc(Br)cnc23)CC4)CC5 ;
UNII	IOW153004F
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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