Ibisobanuro ku bicuruzwa
Retatrutide nigitabo cya gatatu cyitwa agonist peptide yibasira reseptor ya glucagon (GCGR), reseptor ya glucose iterwa na insulineotropique polypeptide (GIPR), hamwe na glucagon imeze nka peptide-1 (GLP-1R). Retatrutide ikora GCGR, GIPR, na GLP-1R ifite EC50 ifite agaciro ka 5.79, 0.0643, na 0.775 nM, hamwe nimbeba GCGR, GIPR, na GLP-1R ifite EC50 ifite agaciro ka 2.32, 0.191, na 0.794 nM. Ikora nkigikoresho cyingenzi cyubushakashatsi mukwiga umubyibuho ukabije nindwara ya metabolike.
Retatrutide ikora neza inzira ya GLP-1R yerekana inzira kandi igatera glucose iterwa na glucose isohoka ikora kuri reseptor ya GIP na GLP-1. Iyi peptide ya syntetique yerekana hypoglycemic ikomeye kandi yakozwe nkurwego rwo kurwanya diyabete ya Diyabete yo mu bwoko bwa 2 (T2D). Itera gusohora insuline kandi igahagarika ururenda rwa glucagon muburyo buterwa na glucose.
Byongeye kandi, Retatrutide yerekanwe kudindiza ubusa gastrica, kugabanya urugero rwa glucose ndetse no nyuma ya glucose nyuma yo kugabanuka, kugabanya ibiryo, no gutera ibiro byinshi mumubiri kubantu bafite T2D.
Igikorwa cyibinyabuzima
Retatrutide (LY3437943) ni peptide imwe ya lipide-conjugated peptide ikora nka agonist ikomeye ya muntu GCGR, GIPR, na GLP-1R. Ugereranije na glucagon kavukire ya kimuntu na GLP-1, Retatrutide yerekana imbaraga nkeya kuri GCGR na GLP-1R (0.3 × na 0.4 ×,) ariko ikerekana imbaraga zongerewe imbaraga (8.9 ×) kuri GIPR ugereranije na glucose iterwa na insulineotropique polypeptide (GIP).
Uburyo bwibikorwa
Mu bushakashatsi bujyanye n'imbeba za diyabete hamwe na nepropatique, ubuyobozi bwa Retatrutide bwagabanije cyane albuminuria kandi byongera umuvuduko wo kuyungurura isi. Izi ngaruka zo gukingira ziterwa no gukora inzira ya GLP-1R / GR iterwa n'inzira yerekana ibimenyetso, ihuza ibikorwa byo kurwanya inflammatory na anti-apoptotique mubice byimpyiko.
Retatrutide nayo ihindura muburyo butaziguye glomerular, ikongerera ubushobozi inkari. Ubushakashatsi bwibanze bwerekana ko, ugereranije nubuvuzi busanzwe bwindwara zimpyiko nka ACE inhibitor na ARBs, Retatrutide itanga igabanuka ryinshi rya albuminuria nyuma yibyumweru bine gusa bivuwe. Byongeye kandi, yerekanye imbaraga nyinshi mukugabanya umuvuduko wamaraso wa systolique kuruta ACE inhibitor cyangwa ARBs, nta ngaruka mbi zagaragaye.
Ingaruka Zuruhande
Ingaruka zikunze kugaragara kuri Retatrutide ni gastrointestinal muri kamere, harimo isesemi, impiswi, kuruka, no kuribwa mu nda. Ibi bimenyetso mubisanzwe byoroheje kandi biringaniye kandi bikunda gukemurwa no kugabanya ibipimo. Hafi ya 7% by'amasomo nabo bavuze ko bumva uruhu. Ubwiyongere bw'umutima bwagaragaye mu byumweru 24 mu matsinda menshi, nyuma yaje gusubira mu rwego rw'ibanze.