AASraw tsim NMN thiab NRC hmoov hauv qhov ntau!

TAK-438

TAK438, tseem hu ua Vonoprazan Fumarate, yog ib yam tshuaj tshiab rau kev kho cov kab mob kua qaub nrog lub tswv yim tshiab ntawm kev nqis tes ua hu ua potassium-sib tw acid blockers (P-CABs) uas sib tw tiv thaiv kev khi ntawm potassium ions rau H +, K + -ATPase ( kuj tseem hu ua proton twj tso kua mis) hauv cov kauj ruam kawg ntawm kev mob plab gastric secretion hauv gastric parietal hlwb, tswj lub plab zom plab. Nws muab cov kua qaub ua kom muaj zog thiab ua kom ntev li ntawm cov tshuaj zais cia cov nyhuv.

Hauj lwm yam khoom

Cov yam ntxwv yooj yim

khoom npe TAK-438
CAS Number 1260141-27-2
molecular Formula C21H20FN3O6S
Mis Lub Cev 461.46
Synonyms Vonoprazan Fumarate;
TAK-438;
1260141-27-2;
Vonoprazan fumurate;
TAK438.
tsos Dawb rau hmoov zoo dawb
Cia thiab Ua Haujlwm Qhuav, tsaus thiab nyob rau hauv 0 - 4 C rau lub sij hawm luv (hnub mus rau lub lis piam) lossis -20 C rau lub sij hawm ntev (hli txog xyoo).

 

TAK-438 Cov lus piav qhia

TAK438, tseem hu ua Vonoprazan Fumarate, yog ib yam tshuaj tshiab rau kev kho cov kab mob kua qaub nrog lub tswv yim tshiab ntawm kev nqis tes ua hu ua potassium-sib tw acid blockers (P-CABs) uas sib tw tiv thaiv kev khi ntawm potassium ions rau H +, K + -ATPase ( kuj tseem hu ua proton twj tso kua mis) hauv cov kauj ruam kawg ntawm kev mob plab gastric secretion hauv gastric parietal hlwb, tswj lub plab zom plab. Nws muab cov kua qaub ua kom muaj zog thiab ua kom ntev li ntawm cov tshuaj zais cia cov nyhuv.

Hauv kev kuaj quav rau lub plab zom mov, TAK-438 kev kho tau ua rau lub sijhawm ntev dua thiab muaj zog acid tsim cov kev txwv. Qhov cuam tshuam loj ntawm TAK-438 ntawm cov kua qaub ua kom zoo li cuam tshuam nrog lub plab pias plab parietal cell physiology.

 

TAK-438 Mechanism of Action

TAK-438 (Vonoprazan fumarate) yog pyrole derivative thiab potassium-sib tw acid blocker (P-CAB) uas muaj kev sib tw los tiv thaiv cov kab mob potassium-khi qhov chaw ntawm pais plab H (+), K (+) - ATPase, ib qho tseem ceeb enzyme hauv kev ua. ntawm pais plab acid secretion. Cov kab ke tuaj yeem sib sau ua ke hauv cov kua qaub hauv thaj chaw thiab yuav tsum muab lub sijhawm ntev dua ntawm kev thaiv vim yog muaj kuab pKa txog 9.06.

Hauv kev kuaj quav rau lub plab zom mov, TAK-438 kev kho tau ua rau lub sijhawm ntev dua thiab muaj zog acid tsim cov kev txwv. Qhov cuam tshuam loj ntawm TAK-438 ntawm cov kua qaub ua kom zoo li cuam tshuam nrog lub plab pias plab parietal cell physiology.

 

TAK-438 Daim Ntawv Thov

TAK-438 (Vonoprazan fumarate lossis Vonoprazan) yog cov tshuaj tshiab rau kev kho cov kabmob muaj feem cuam nrog kev tiv thaiv kab mob tshiab nrog kev ua haujlwm tshiab hu ua potassium-sib tw acid blockers (P-CABs) uas sib tw tiv thaiv kev khi ntawm potassium ions rau H +, K + -ATPase (tseem hu ua proton twj tso kua mis) hauv cov kauj ruam kawg ntawm pais plab acid secretion hauv pais plab parietal hlwb. Cov tshuaj no tau pom zoo hauv Nyij Pooj rau kev kho cov kab mob ntsig txog acid, nrog rau lub plab zom mov, mob plab duodenal, reflux esophagitis thiab Adjunct rau Helicobacter pylori kev tshem tawm nyob rau hauv tus neeg mob Helicobacter pylori gastritis.

 

TAK-438 Cov Kev Cuam Tshuam & Ceeb Toom

Cov kev mob tshwm sim zoo nrog:

▪ raws plab,

▪ xeev siab thiab ntuav,

▪ cem quav,

Mob plab,

Rash daim tawv nqaij ua pob,

Burn kub siab.

 

Tsis yog txhua yam mob tshwm sim ntawm TAK438. Xav paub ntau ntxiv, nug koj tus kws kho mob lossis kws muag tshuaj. Hu koj tus kws kho mob rau cov lus qhia kho mob txog cov kev mob tshwm sim. Koj yuav qhia txog tej kev phiv rau FDA ntawm 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. Kev tshawb pom ntawm tshiab pyrrole derivative 1- [5- (2-fluorophenyl) -1- (pyridin-3-ylsulfonyl) -1H-pyrrol-3-yl] -N-methylmethanamin e fumarate (TAK-438) yog cov tshuaj tua kab mob potassium. blocker (P-CAB). J Med Chem. 2012 Tsib Hlis 10; 55 (9): 4446-56. doi: 10.1021 / jm300318t. Epub 2012 Apr 30. PubMed PMID: 22512618.

[2] Kondo M, Kawamoto M, Hasuoka A, Kajino M, Inatomi N, Tarui N. Kev ntsuas siab tshaj ntawm cov pa roj carbon ntau-tiv thaiv cov kua qaub. J Biomol Ntsuam Xyuas. 2012 Lub Ob Hlis; 17 (2): 177-82. doi: 10.1177 / 1087057111421004. Epub 2011 Sep 22. PubMed PMID: 21940711.

[3] Shin JM, Inatomi N, Munson K, Strugatsky D, Tokhtaeva E, Vagin O, Sachs G. Cov yam ntxwv ntawm cov paj hlwb tshiab-kev sib tw acid blocker ntawm lub plab H, K-ATPase, 1- [5- (2- fluorophenyl) -1- (pyridin-3-ylsulfonyl) -1H-pyrrol-3-yl] -N-methylmethanamin e monofumarate (TAK-438). J Pharmacol Exp Ther. 2011 Nov; 339 (2): 412-20. doi: 10.1124 / jpet.111.185314. Epub 2011 Aug 9. PubMed PMID: 21828261; PubMed Central PMCID: PMC3199995.

[4] Hori Y, Matsukawa J, Takeuchi T, Nishida H, Kajino M, Inatomi N. Ib txoj kev tshawb fawb sib piv cov nyhuv antisecretory ntawm TAK-438, cov tshuaj tshiab potassium-sib tw acid blocker, nrog lansoprazole hauv cov tsiaj. J Pharmacol Exp Ther. 2011 Jun; 337 (3): 797-804. doi: 10.1124 / jpet.111.179556. Epub 2011 Mar 16. PubMed PMID: 21411494.

[5] Matsukawa J, Hori Y, Nishida H, Kajino M, Inatomi N. Ib txoj kev sib piv ntawm cov qauv kev nqis tes ntawm TAK-438, tshiab tshiab cov tshuaj potassium-kev sib tw acid blocker, thiab lansoprazole hauv thawj kab lis kev cai luav gastric qog. Cov Tshuaj Biochem. 2011 Tsib Hlis 1; 81 (9): 1145-51. doi: 10.1016 / j.bcp.2011.02.009. Epub 2011 Mar 1. PubMed 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 (TAK-438), yog ib qho tshiab thiab muaj cov muaj zog potassium-sib tw acid blocker rau kev kho mob ntawm cov kua qaub. J Pharmacol Exp Ther. Xyoo 2010 Oct; 335 (1): 231-8. doi: 10.1124 / jpet.110.170274. Epub 2010 Jul 12. PubMed PMID: 20624992.