GLEEVEC(imatinib
mesylate)20095http://www.pharma.us.novartis.com/product/pi/pdf/gleevec_tabs.pdf
05/27/2009 05/27/2009 02/10/2009 12/19/2008 09/26/2008
09/26/2008 09/26/2008 04/30/200809/13/2007 10/30/2006 10/19/2006
10/19/2006 10/19/2006 10/19/2006 10/19/2006 09/27/2006 05/31/2006
10/20/200500805/19/2005 05/18/2005 03/14/2005 06/23/2004 12/08/200
05/20/2003 04/18/2003000
2001 ----------------------------------------------------Ph+ CML
(1.1) XX/2009GIST (1.9) 09/2008GIST (1.10) 12/2008GIST (2.8)
09/2008GIST (2.8) 12/2008(2.9) 09/2008(5.4)(5.5)(5.9)
09/2008-------------------------------------------------------1(Ph+
CML)2(Ph+ CML)(BC)(AP)(CP)-(1.2)3-Ph+CML(1.3)4(Ph+ ALL)
(1.4)5/(MDS/MPD)PDGFR()(1.5)6(ASM)D816V
c-Kitc-Kit(1.6)7(HES)/FIP1L1-PDGFR([Flu orescence in situ
hybridization,
FISH]CHIC2)(CEL)HES/FIP1L1PDGFRCEL(1.7)8/(DFSP)(1.8)9Kit
(CD117)/(GIST)(1.9)10Kit(CD117)GIST(1.10)--------------------------------------------1Ph+
CML CP(2.1)400 mg/dayPh+ CML APBC(2.1)600 mg/day2Ph+ CML(2.2)340
mg//day260 mg//day3Ph+ ALL(2.3)600 mg/day4/(2.4)400
mg/day5ASM(2.5)100 mg/day400 mg/day6HES/CEL(2.6)100 mg/day400
mg/day7DFSP(2.7)800 mg/day8/GIST(2.8)400 mg/dayGIST(2.8)400
mg/day9(2.9)400 mg/day(2.9)300 mg/day400 mg600 mg800 mg400 mg2800
mg400 mg-------------------------------------------()100 mg400 mg
(3)-------------------------------------------------------------(4)-----------------------------------------------1(5.1,
6.1,
6.11)2221(5.2)3(5.3)4(5.4)5CMLGIST3/4GISTGIGI(5.5)6(5.6)7(HESMDS/MPDASM)/(5.7)8
(Stevens-Johnson) (5.8)9TSH(5.9).10(5.10)11(5.11,
8.1)-------------------------------------------------------------(>30%)(6.16.11)
Novartis Pharmaceuticals
Corporation1-888-669-6682FDA1-800-FDA-1088www.fda.gov/medwatch
-------------------------------------------------------------1CYP3A4CmaxAUC
(2.9, 7.1)2CYP3A4CmaxAUC (7.2)3CYP3A4CmaxAUC( 7.3)4[warfarin]
(7.3)5[acetaminophen](7.5)-----------------------------------------------2(8.4)
1 1.1 (Ph+ CML)
1.2- (IFN)Ph+ CML(BC)(AP)(CP)-
1.3 Ph+ CML-Ph+ CML
1.4 Ph+ (ALL)
1.5/(MDS/MPD)/PDGFR()
1.6(ASM)D816V c-Kitc-Kit
1.7(HES)/(CEL)FIP1L1-PDGFR([FISH]CHIC2)/HES/CELFIP1L1-PDGFR.
1.8 (DFSP)/
1.9 Kit+ (GIST)Kit(CD117)/
1.10 GISTKit(CD117)GIST
2 400 mg600 mg1800 mg400 mg21- 112(100 mg50 mL400 mg200 mL)800
mg400 mg
2.1Ph+ CML CP, APBCCML400 mg/day600 mg/dayCML400 mg600 mg600
mg800 mg(400 mg2) ()36-12
2.2 Ph+ CMLPh+ CML340 mg//day(600 mg)Ph+ CML-260 mg//day
2.3 Ph+ ALL/Ph+ ALL600 mg/day
2.4 MDS/MPDMDS/MPD400 mg/day
2.5 ASMD816V c-KitASM400 mg/dayc-KitASM400
mg/dayASMFIP1L1-PDGFR100 mg/day()100 mg400 mg
2.6 HES/CELHES/CEL400 mg/dayFIP1L1-PDGFRHES/CEL100 mg/day()100
mg400 mg
2.7 DFSPDFSP800 mg/day
2.8 GIST/GIST400 mg/day800 mg(400 mg2)GIST400 mg/day1
2.9 CYP3A4CYP3A4
([dexamethasone][phenytoin](carbamazepine)(rifampin)(rifabutin)(rifapentin)[rifampacin](Phenobarbital))CYP3A450%[(7.1)].
25% [ (8.6)]
(CrCL = 20-39 mL/min)50%(CrCL = 40-59 mL/min)600 mg400 mg
100 mg/day[(8.7)]
2.10 If elevations in >3 (IULN) >5 IULN
