Tulaga Autu

Igoa oloa	TAK-438 paʻu
Numera CAS	1260141-27-2
Faiga Faʻavae Molecular	C21H20FN3O6S
Fua Faatatau o le Umi	461.46
Synonyms	Vonoprazan Fumarate; TAK-438 paʻu; 1260141-27-2; Vonoprazan fumurate; TAK438.
Faʻaaliga	Paʻepaʻe i paʻu paʻepaʻe paʻepaʻe
Teuina ma Taulimaina	Faʻamago, pogisa ma i le 0 - 4 C mo se taimi puʻupuʻu (aso i vaiaso) poʻo le -20 C mo se taimi umi (masina i tausaga).

 

TAK-438 paʻu Faʻamatalaga

TAK438, e faʻaigoa foʻi ia Vonoprazan Fumarate, o se vailaʻau fou mo le togafitia o faʻamaʻi e fesoʻotaʻi ma le acid ma se faiga fou o gaioiga e taʻua o le potassium-faatauva poloka poloka (P-CABs) e faʻatauvaʻa taofiofia le fusifusia o potasioni iona i H +, K + -ATPase ( lauiloa foi o le proton pump) i le laʻasaga mulimuli o le gastric acid faʻalilolilo i gastric sela sela, pulea gastric acid faʻalilolilo. E maua ai le malosi ma tumau lagolagoina vaivaiga taofiofia aafiaga.

I le gaosia o manava o le manava, o le TAK-438 paʻu togafitiga na mafua ai le umi ma le malosi o le faʻavaeina o le acid. O le taofiofia o le TAK-438 paʻu i le gaosia o le acid na foliga mai e fesoʻotaʻi ma gastric parietal cell physiology.

 

TAK-438 paʻu Mechanism of Action

TAK-438 efuefu (Vonoprazan fumarate) o se pyrole derivative ma potassium-faatauva poloka poloka (P-CAB) e faatauva poloka le potassium-fusifusia nofoaga o gastric H (+), K (+) - ATPase, o se ki autu i le gaioiga o gastric acid faʻalilolilo. E mafai e le lotoa ona faaputuputu i siosiomaga siosiomaga ma e tatau ona maua ai se umi atu o le taofiofia ona o le alkali pKa o le 9.06.

I le gaosia o manava o le manava, o le TAK-438 paʻu togafitiga na mafua ai le umi ma le malosi o le faʻavaeina o le acid. O le taofiofia o le TAK-438 paʻu i le gaosia o le acid na foliga mai e fesoʻotaʻi ma gastric parietal cell physiology.

 

TAK-438 paʻu Talosaga

TAK-438 paʻu (Vonoprazan fumarate poʻo Vonoprazan) o se vailaʻau fou mo le togafitia o faʻamaʻi e fesoʻotaʻi ma le faʻatinoina o le potassium-faatauva poloka poloka (P-CABs) e faʻatauvaʻa taofiofia le fusifusia o potasi ioni i H +, K + ATPase (lea e taʻua o le proton pump) i le laʻasaga mulimuli o le gastric acid faʻalilolilo i gastric parietal sela. Ua faʻamaonia le vailaʻau i Iapani mo le togafitia o faʻamaʻi e fesoʻotaʻi ma le acid, e aofia ai le papala tau kesi, papala duodenal, reflux esophagitis ma Adjunct i le Helicobacter pylori faʻamamaina i le tulaga o Helicobacter pylori gastritis.

 

TAK-438 paʻu Itu Aafiaga & Lapataiga

O aʻafiaga masani masani aofia ai:

▪ manava tatā,

▪ niniva ma puaʻi,

▪ papala,

▪ tiga o le manava,

▪ paʻu o le paʻu,

▪ susunu o le fatu.

 

E leʻo uma ia ono afaina o le TAK438. Mo nisi faʻamatalaga, fesili i lau fomaʻi poʻo le faletalavai. Valaʻau lau fomaʻi mo fautuaga faʻafomaʻi e uiga i aʻafiaga. E mafai ona e lipotia ni aʻafiaga i le FDA i le 1-800-FDA-1088.

 

Tusitaiala

[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. Discovery of a novel pyrrole derivative 1- [5- (2-fluorophenyl) -1- (pyridin-3-ylsulfonyl) -1H-pyrrol-3-yl] -N-methylmethanamin e fumarate (TAK-438 efuefu) o se potassium-faatauva poloka acid (P-CAB). J Med Chem. 2012 Me 10; 55 (9): 4446-56. faia: 10.1021 / jm300318t. Epub 2012 Ape 30. Faʻasalalau PMID: 22512618.

[2] Kondo M, Kawamoto M, Hasuoka A, Kajino M, Inatomi N, Tarui N. Maualuga siakiina siaki o potassium-faatauva poloka poloka. J Biomol Lau. 2012 Fep; 17 (2): 177-82. faia: 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. Faʻailogaina o se tala o le potassium-faatauva poloka poloka o le gastric H, K-ATPase, 1- [5- (2- fluorophenyl) -1- (pyridin-3-ylsulfonyl) -1H-pyrrol-3-yl] -N-methylmethanamin e monofumarate (TAK-438 efuefu). J Pharmacol Exp Ther. 2011 Nov; 339 (2): 412-20. faia: 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. O se suʻesuʻega faʻatusatusaina o le antisecretory aafiaga o le TAK-438 paʻu, o se tala fou potassium-faatauva acid poloka, ma lansoprazole i manu. J Pharmacol Exp Ther. 2011 Iuni; 337 (3): 797-804. faia: 10.1124 / jpet.111.179556. Epub 2011 Mati 16. PubMed PMID: 21411494.

[5] Matsukawa J, Hori Y, Nishida H, Kajino M, Inatomi N. O se faʻatusatusaga suʻesuʻega i auala o gaioiga o le TAK-438 paʻu, o se tala fou potassium-faatauva acid poloka, ma lansoprazole i muamua galueaina lapisi lapisi lapisi. Biochem Pharmacol. 2011 Me 1; 81 (9): 1145-51. faia: 10.1016 / j.bcp.2011.02.009. Epub 2011 Mati 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 paʻu), o se mea fou ma malosi potassium-faatauva poloka poloka mo le togafitia o acid-fesoʻotaʻi maʻi. J Pharmacol Exp Ther. 2010 Oketopa; 335 (1): 231-8. faia: 10.1124 / jpet.110.170274. Epub 2010 Iulai 12. PubMed PMID: 20624992.

---