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EA-438-TAK

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TAK438, eo hape e tsejoang ka hore ke Vonoprazan Fumarate, ke moriana o mocha oa ho phekola maloetse a amanang le asiti ka mokhoa o mocha oa ts'ebetso o bitsoang potasiamo-tlholisano ea li-acid blockers (P-CABs) e qothisanang lehlokoa le ho thibela tlamo ea li-ion tsa potasiamo ho H +, K + -ATPase ( eo hape e tsejoang e le pompo ea proton) mohatong oa hoqetela oa secha sa gastric acid liseleng tsa parietal, e laola ho boloka sephiri sa asiti. E fana ka phello ea thibelo ea acid e matla le e tšoarellang.

Tlhaloso ea Sehlahisoa

Litšobotsi tsa Motheo

Name Product TAK-438 phofo
Nomoro ea CAS 1260141-27-2
Molecular Formula C21H20FN3O6S
Boima ba 'mele 461.46
Li-synonyms Fumarate ea Vonoprazan;
TAK-438 phofo;
1260141-27-2;
Vonoprazan fumurate;
TAK438.
Ponahalo Tšoeu ho ea phofo e tšoeu
Ho Boloka le ho Sebetsana E omme, e lefifi ebile e le 0 - 4 C ka nako e khuts'oane (matsatsi ho isa ho libeke) kapa -20 C nako e telele (likhoeli ho isa ho lilemo).

 

Tlhaloso ea phofo ea TAK-438

TAK438, eo hape e tsejoang ka hore ke Vonoprazan Fumarate, ke moriana o mocha oa ho phekola maloetse a amanang le asiti ka mokhoa o mocha oa ts'ebetso o bitsoang potasiamo-tlholisano ea li-acid blockers (P-CABs) e qothisanang lehlokoa le ho thibela tlamo ea li-ion tsa potasiamo ho H +, K + -ATPase ( eo hape e tsejoang e le pompo ea proton) mohatong oa hoqetela oa secha sa gastric acid liseleng tsa parietal, e laola ho boloka sephiri sa asiti. E fana ka phello ea thibelo ea acid e matla le e tšoarellang.

Ka litšoelesa tse ntlafalitsoeng tsa ka mpeng, kalafo ea phofo ea TAK-438 e hlahisitse tšitiso e telele le e matla ea sebopeho sa asiti. Phello ea thibelo ea phofo ea TAK-438 ka sephiri sa asiti e bonahala e amahanngoa le gastric parietal cell physiology.

 

TAK-438 phofo Mokhoa oa Khato

TAK-438 phofo (Vonoprazan fumarate) ke sehlahisoa sa pyrole le potasiamo ea tlholisano ea acid blocker (P-CAB) e qothisanang lehlokoa le ho thibela sebaka sa potasiamo sa H (+), K (+) - ATPase, enzyme ea bohlokoa ho mokhoa oa ho boloka sephiri sa asiti. Motsoako o ka bokellana libakeng tsa asiti mme o lokela ho fana ka nako e telele ea thibelo ka lebaka la pKa ea alkaline ea 9.06.

Ka litšoelesa tse ntlafalitsoeng tsa ka mpeng, kalafo ea phofo ea TAK-438 e hlahisitse tšitiso e telele le e matla ea sebopeho sa asiti. Phello ea thibelo ea phofo ea TAK-438 ka sephiri sa asiti e bonahala e amahanngoa le gastric parietal cell physiology.

 

Kopo ea TAK-438 ea phofo

TAK-438 phofo (Vonoprazan fumarate kapa Vonoprazan) ke moriana o mocha oa ho phekola maloetse a amanang le asiti ka mokhoa o mocha oa tšebetso o bitsoang potasiamo-tlholisano ea li-acid blockers (P-CABs) e qothisanang lehlokoa le ho thibela tlamo ea li-ion tsa potasiamo ho H +, K + - ATPase (e tsejoang hape e le pompo ea proton) mohatong oa hoqetela oa sephiri sa asiti ea ka mpeng liseleng tsa parietal tsa ka mpeng. Lithethefatsi li amoheloa Japane bakeng sa kalafo ea maloetse a amanang le asiti, ho kenyelletsa le seso sa ka mpeng, seso sa duodenal, reflux esophagitis le Adjunct ho Helicobacter pylori eradication tabeng ea Helicobacter pylori gastritis.

 

Litla-morao tsa phofo ea TAK-438 le Temoso

Litla-morao tse tloaelehileng li kenyeletsa:

▪ letšollo,

▪ ho nyekeloa ke pelo le ho hlatsa,

▪ ho sokela,

▪ bohloko ba mpeng,

▪ lekhopho letlalong,

▪ ho nyekeloa ke pelo.

 

Tsena ha se litla-morao tsohle tsa TAK438. Bakeng sa tlhaiso-leseling e batsi, botsa ngaka kapa setsebi sa metsoako. Bitsa ngaka ea hau bakeng sa likeletso tsa bongaka mabapi le litla-morao. U ka tlaleha litla-morao ho FDA ho 1-800-FDA-1088.

 

Reference

[1] Arikawa Y, Nishida H, Kurasawa O, Hasuoka A, Hirase K, Inatomi N, Hori Y, Matsukawa J, Imanishi A, Kondo M, Tarui N, Hamada T, Takagi T, Takeuchi T, Kajino M. Ho sibolloa ha sehlahisoa sa pyrrole se tsoang ho 1- [5- (2-fluorophenyl) -1- (pyridin-3-ylsulfonyl) -1H-pyrrol-3-yl] -N-methylmethanamin e fumarate (TAK-438 phofo) e le tlholisano ea potasiamo acid blocker (P-CAB). J Med Chem. 2012 Mots'eanong 10; 55 (9): 4446-56. doi: 10.1021 / jm300318t. Epub 2012 Apr 30. E fetotsoe PMID: 22512618.

[2] Kondo M, Kawamoto M, Hasuoka A, Kajino M, Inatomi N, Tarui N. Tlhatlhobo e phahameng ea li-block tsa acid e nang le tlholisano ka potasiamo. Sesebelisoa sa J Biomol. 2012 Hlakola; 17 (2): 177-82. doi: 10.1177 / 1087057111421004. Epub 2011 Sep 22. E fetotsoe PMID: 21940711.

[3] Shin JM, Inatomi N, Munson K, Strugatsky D, Tokhtaeva E, Vagin O, Sachs G. Sebopeho sa potasiamo ea tlholisano ea acid e thibelang gastric H, K-ATPase, 1- [5- (2-) fluorophenyl) -1- (pyridin-3-ylsulfonyl) -1H-pyrrol-3-yl] -N-methylmethanamin e monofumarate (phofo ea TAK-438). J Pharmacol Phekolo ea Ther. 2011 Nov; 339 (2): 412-20. doi: 10.1124 / jpet.111.185314. Epub 2011 Aug 9. E fetotsoe PMID: 21828261; E fetotsoe PMCID e bohareng: PMC3199995.

[4] Hori Y, Matsukawa J, Takeuchi T, Nishida H, Kajino M, Inatomi N. Phuputso e bapisoang le phello ea antisecretory ea phofo ea TAK-438, e nang le potasiamo ea tlholisano ea potassium e nang le lansoprazole liphoofolong. J Pharmacol Phekolo ea Ther. 2011 Jun; 337 (3): 797-804. doi: 10.1124 / jpet.111.179556. Epub 2011 Mar 16. E fetotsoe PMID: 21411494.

[5] Matsukawa J, Hori Y, Nishida H, Kajino M, Inatomi N. Phuputso e bapisoang ka mekhoa ea tšebetso ea phofo ea TAK-438, pokello ea asiti ea tlholisano ea potasiamo le lansoprazole liphatsong tsa mantlha tsa mmutla. Biochem Pharmacol. 2011 Mots'eanong 1; 81 (9): 1145-51. doi: 10.1016 / j.bcp.2011.02.009. Epub 2011 Mar 1. E fetotsoe PMID: 21371447.

[6] Hori Y, Imanishi A, Matsukawa J, Tsukimi Y, Nishida H, Arikawa Y, Hirase K, Kajino M, Inatomi N. 1- [5- (2-Fluorophenyl) -1- (pyridin-3-ylsulfonyl) -1H-pyrrol-3-yl] -N-methylmethanamin e monofumarate (phofo ea TAK-438), bukana ea thibelo ea asiti ea potasiamo e matla bakeng sa kalafo ea mafu a amanang le acid. J Pharmacol Phekolo ea Ther. 2010 Mphalane; 335 (1): 231-8. doi: 10.1124 / jpet.110.170274. Epub 2010 Jul 12. E fetotsoe PMID: 20624992.