Awọn Abuda Ipilẹ

ọja orukọ	TAK-438
CAS Number	1260141-27-2
molikula agbekalẹ	C21H20FN3O6S
Ilana iwuwo	461.46
Awọn Synonyms	Vonoprazan Fumarate; TAK-438; 1260141-27-2; Vonoprazan fumurate; TAK438.
irisi	Funfun si pipa-funfun lulú
Ifipamọ ati mimu	Gbẹ, okunkun ati ni 0 - 4 C fun igba kukuru (awọn ọjọ si awọn ọsẹ) tabi -20 C fun igba pipẹ (awọn oṣu si ọdun).

 

TAK-438 Apejuwe

TAK438, ti a tun mọ ni Vonoprazan Fumarate, jẹ oogun tuntun fun atọju awọn aisan ti o ni acid pẹlu ilana aramada ti iṣe ti a pe ni awọn oluṣeto acid ifigagbaga ti potasiomu (P-CABs) eyiti o ni idije dena didapọ awọn ions potasiomu si H +, K + -ATPase ( tun mọ bi fifa proton) ni igbesẹ ikẹhin ti yomijade ti acid inu inu awọn sẹẹli parietal inu, awọn idari yomijade ti inu. O pese ipa idena yomijade ti acid lagbara ati atilẹyin.

Ninu awọn keekeke ti inu ti aṣa, itọju TAK-438 yorisi ni idena ilana iṣelọpọ gigun ati okun. Ipa idiwọ ti TAK-438 lori yomijade acid dabi ẹni pe o ni nkan ṣe pẹlu fisioloji ẹyin parietal cell.

 

TAK-438 Iṣaṣe ti Ise

TAK-438 (Vonoprazan fumarate) jẹ itọsẹ pyrole kan ati oludena acid ifigagbaga ti potasiomu (P-CAB) eyiti o ni idiwọ ṣe idiwọ aaye isopọ potasiomu ti H (+), K (+) - ATPase, enzymu bọtini kan ninu ilana ti iṣan acid inu. Apopọ le ṣajọ ni awọn agbegbe acid ati pe o yẹ ki o pese akoko gigun ti idinamọ nitori pKa ipilẹ ti 9.06.

Ninu awọn keekeke ti inu ti aṣa, itọju TAK-438 yorisi ni idena ilana iṣelọpọ gigun ati okun. Ipa idiwọ ti TAK-438 lori yomijade acid dabi ẹni pe o ni nkan ṣe pẹlu fisioloji ẹyin parietal cell.

 

Ohun elo TAK-438

TAK-438 (Vonoprazan fumarate tabi Vonoprazan) jẹ oogun tuntun fun titọju awọn aisan ti o ni acid pẹlu ilana aramada ti iṣe ti a pe ni awọn oludibo acid ifigagbaga ti potasiomu (P-CABs) eyiti o ni idije dena didapọ awọn ions potasiomu si H +, K + -ATPase (tun mọ bi fifa proton) ni igbesẹ ikẹhin ti yomijade acid acid ninu awọn sẹẹli parietal inu. A fọwọsi oogun naa ni ilu Japan fun itọju awọn arun ti o ni ibatan acid, pẹlu ọgbẹ inu, ọgbẹ duodenal, reflux esophagitis ati Adjunct si iparun Helicobacter pylori ninu ọran Helicobacter pylori gastritis.

 

TAK-438 Awọn ipa Ipa & Ikilọ

Awọn ipa ẹgbẹ ti o wọpọ pẹlu:

▪ gbuuru,

▪ inu ati eebi,

▪ àìrígbẹyà,

Pain irora inu,

Rash awọ ara,

▪ ibinujẹ.

 

Iwọnyi kii ṣe gbogbo awọn ipa ẹgbẹ ti o ṣeeṣe ti TAK438. Fun alaye diẹ sii, beere lọwọ dokita rẹ tabi oniwosan oogun. Pe dokita rẹ fun imọran iṣoogun nipa awọn ipa ẹgbẹ. O le ṣe ijabọ awọn ipa ẹgbẹ si FDA ni 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. Awari ti Itanran pyrrole ti o ni itọsẹ 1- [5- (2-fluorophenyl) -1- (pyridin-3-ylsulfonyl) -1H-pyrrol-3-yl] -N-methylmethanamin e fumarate (TAK-438) gege bi acid ifigagbaga potasiomu ohun amorindun (P-CAB). J Med Chem. 2012 Oṣu Kẹwa 10; 55 (9): 4446-56. ṣe: 10.1021 / jm300318t. Epub 2012 Oṣu Kẹrin 30. PubMed PMID: 22512618.

[2] Kondo M, Kawamoto M, Hasuoka A, Kajino M, Inatomi N, Tarui N. Ṣiṣayẹwo ṣiṣiparọ giga ti awọn idiwọ acid ifigagbaga ti potasiomu. J Iboju Biomol. 2012 Kínní; 17 (2): 177-82. ṣe: 10.1177 / 1087057111421004. Epub 2011 Oṣu Kẹsan 22. PubMed PMID: 21940711.

[3] Shin JM, Inatomi N, Munson K, Strugatsky D, Tokhtaeva E, Vagin O, Sachs G. Ihuwasi ti aratuntun olomi-ifigagbaga acid ifigagbaga ti inu 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. Oṣu kọkanla 2011; 339 (2): 412-20. ṣe: 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. Iwadi kan ti o ṣe afiwe ipa ti antisecretory ti TAK-438, iwe-akọọlẹ acid-ifigagbaga acid-ifigagbaga, pẹlu lansoprazole ninu awọn ẹranko. J Pharmacol Exp Ther. Oṣu Kẹwa 2011; 337 (3): 797-804. ṣe: 10.1124 / jpet.111.179556. Epub 2011 Mar 16. PubMed PMID: 21411494.

[5] Matsukawa J, Hori Y, Nishida H, Kajino M, Inatomi N. Iwadi afiwera lori awọn ipo iṣe ti TAK-438, aramada amuludun ifigagbaga potasiomu-ifigagbaga, ati lansoprazole ni akọkọ keekeke ti o jẹ ehoro ikun inu. Biochem Pharmacol. 2011 Oṣu Karun 1; 81 (9): 1145-51. ṣe: 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), iwe-akọọlẹ ati amulo acid ifigagbaga potasiomu-ifigagbaga fun itọju awọn aisan ti o ni ibatan acid. J Pharmacol Exp Ther. Oṣu Kẹwa Ọdun 2010; 335 (1): 231-8. ṣe: 10.1124 / jpet.110.170274. Epub 2010 Jul 12. PubMed PMID: 20624992.

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