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Research Retatrutid Ubushakashatsi
Ni ubuhe bushakashatsi bwakozwe na Retatrutid?
Umubyibuho ukabije wabaye imwe mu mbogamizi zikomeye z’ubuzima rusange muri sosiyete ya none. Irashobora kubyara ibibazo byinshi byubuzima nka diyabete yo mu bwoko bwa 2 mellitus, indwara zifata umutima, hypertension, dyslipidemia, nindwara zumwijima zidafite inzoga. Hamwe n’ubwiyongere bukabije bw’umubyibuho ukabije, hakenewe byihutirwa ubuvuzi bushya bushobora gucunga neza ibiro by’umubiri no kuzamura ubuzima [1] . Nubwo ibikorwa byubuzima, nko kongera imyitozo ngororamubiri no kugenzura imirire, nizo ngamba zingenzi zo kugabanya ibiro, biragoye cyane kubarwayi benshi bafite umubyibuho ukabije kugira ngo bagabanye ibiro birebire.
Retatrutid, nkibintu bitatu byakira reseptor agonist, irashobora gukora kuri glucagon imeze nka peptide-1 yakira (
GLP-1R), glucose-iterwa na insulinotropic polypeptide reseptor (GIPR), hamwe na glucagon reseptor (GCGR). Ubu buryo bwinshi-bwakirwa bwibikorwa bubaha ibyiza byingenzi murwego rwo kugabanya ibiro. Ugereranije n’imiti igabanya ibiro ikora kuri reseptor imwe gusa, Retatrutid irashobora kurushaho kugenzura imikorere yimikorere yumubiri [1] . Retatrutid igera ku kugabanya ibiro muguhindura imisemburo myinshi ya hormone, ntigaragaza gusa imbaraga zidasanzwe ahubwo inagira ingaruka zoroheje zo munda. Byongeye kandi, nka triple reseptor agonist, Retatrutid ifite ingaruka zikomeye zo kugabanya ibiro hamwe nabantu benshi bakoreshwa ugereranije nindi miti mishya yo kugabanya ibiro.
Retatrutid ni iki?
Retatrutid nigitabo gishya gikora glucagon-isa na peptide-1 (GLP-1) reseptor agonist. Yahinduwe kandi itezimbere hashingiwe kumiterere ya GLP-1 karemano, kandi irashobora guhuza cyane no gukora reseptor ya GLP-1, gukora imirimo ya physiologique isa niy'imiterere ya GLP-1, nko guteza imbere imisemburo ya insuline, kubuza gusohora glucagon, gutinda gusohora gastrica, kugabanya ubushake bwo kurya, n'ibindi. Ifite ibyifuzo byinshi byo kuvura diyabete no gucunga ibiro.
Nubuhe buryo bwo gukora Retatrutid?
Uburyo bwibikorwa bya Retatrutid bituruka ku ngaruka zabwo za agonistic kuri reseptors nyinshi. Ubwa mbere, ingaruka za agonistic kuri reseptor ya glucagon isa na peptide-1 (GLP-1R) irashobora kongera ururenda rwa insuline, ikabuza gusohora glucagon, igabanuka rya glucose yamaraso, kandi icyarimwe igatinda gusohora gastrica, kongera guhaga, no kugabanya ibiryo [2] . Icya kabiri, ingaruka ziterwa na agonistic kuri glucose iterwa na insuline ya insuline ya polypeptide ya reseptor (GIPR) irashobora guteza imbere gusohora insuline, kongera ikoreshwa rya glucose, no kugira ingaruka ku mavuta ya metabolisme, ikabuza lipolysis no guteza imbere ibinure [2] . Byongeye kandi, ingaruka za Agonistic ya Retatrutid kuri reseptor ya glucagon (GCGR) ubusanzwe itera glycogenolysis na gluconeogenezi mu mwijima, bikongera urugero rw'amaraso glucose. Ariko rero, mugikorwa cya Retatrutid, iyi ngaruka yo kuzamura glucose ikurwaho ningaruka zindi reseptors ebyiri, mugihe iteza lipolysis no kugabanya ibinure [2] . Ubu buryo bwibikorwa byinshi birashobora kuba byiza mukuvura umubyibuho ukabije kuruta reseptor agonist.
Mugukora icyarimwe gukora ibyo byakira bitatu, Retatrutid irashobora gukora ingaruka zinyuranye zoguhindura metabolike kandi ikanatanga ingaruka zo kuvura umubyibuho ukabije nindwara zifitanye isano. Mu rwego rwo kugenzura urugero rwa glucose yamaraso, kubera ko ibikorwa bya GLP-1R na GIPR bitera gusohora insuline kandi bikabuza gusohora glucagon, kandi gukora GCGR bikurwaho n’ingaruka z’abandi bakira, Retatrutid irashobora kugabanya neza glucose y’amaraso, ifite akamaro kanini mu kuvura indwara ya diyabete yo mu bwoko bwa 2 [1, 2] . Mu rwego rwo kugabanya kwegeranya ibinure, gukora kwa GCGR bitera lipolysis kandi bikagabanya kwegeranya ibinure, mugihe gukora GLP-1R byongera guhaga no kugabanya gufata ibiryo, bikagabanya no gusanisha amavuta [1] . Byongeye kandi, Retatrutid nayo igira ingaruka nziza ku ndwara zumwijima zidafite inzoga. Irashobora kugabanya ibinure byumwijima no kunoza imikorere yumwijima.
HbA1c, uburemere bwumubiri, umuvuduko wamaraso, na lipide Data ni byibuze-kare bisobanura (hamwe nibibari byerekana SE) uhereye kubisesengura ryakozwe, keretse bivuzwe ukundi.
Inkomoko: PubMed [4]
Ni mu buhe buryo Retatrutid yerekana ingaruka zayo?
Retatrutid yerekana ingaruka zikomeye mubice byinshi
Ingaruka zikomeye zo kugabanya ibiro: Retatrutid yerekanye ingaruka zikomeye zo kugabanya ibiro mubigeragezo byinshi byamavuriro. Kurugero, mubushakashatsi bwamavuriro burimo abantu bakuru 338 (Jastreboff AMM, 2023), abarwayi bavuwe na dosiye zitandukanye za Retatrutid bagize ibiro byinshi mubyumweru 48. Muri bo, abarwayi bo mu itsinda rya dose ya 12mg batakaje 24.2% by'uburemere bw'umubiri wabo, kandi umubare munini w'abarwayi wageze ku gutakaza ibiro ku buryo butandukanye. Kurugero, mubarwayi bahabwa dosiye ya 4mg, 8mg, na 12mg, 92%, 100%, na 100% byabarwayi, batakaje 5% cyangwa birenga ibiro byabo. Mu bundi bushakashatsi [3] , ibigeragezo bibiri byateganijwe byitabiriwe n’abarwayi 353 barwaye diyabete yo mu bwoko bwa 2 bwerekanye ko ugereranije na placebo, Retatrutid ishobora kugabanya cyane ibiro by’umubiri by’abarwayi ku gipimo cya 11.89, kandi ikanagabanya gemoglobine (HbA1C). Byongeye kandi, mu bigeragezo by’abarwayi bakuze bafite umubyibuho ukabije nta diyabete, Retatrutid yateje ibiro 24.2% ku barwayi, naho 83% by’abarwayi batakaje 15% cyangwa birenga ibiro by’umubiri mu byumweru 48. Ibisubizo byerekana ko Retatrutid ifite amahirwe menshi yo kugabanya ibiro.
Kuvura diyabete yo mu bwoko bwa 2: Retatrutid irerekana kandi ubushobozi bumwe na bumwe bwo kuvura diyabete yo mu bwoko bwa 2. Mu bigeragezo bimwe na bimwe by’amavuriro, Retatrutid yerekanye igabanuka rya glycated hemoglobine (HbA1c) hamwe no kugabanya ibiro biterwa no kugabanuka. Kurugero, mubushakashatsi bumwe, kubarwayi barwaye diyabete yo mu bwoko bwa 2, Retatrutid yerekanye ingaruka zikomeye zo kurwanya glucose. Ugereranije na platbo, glycated hemoglobine yagabanutseho 1,64% [3] . Byongeye kandi, mu buryo butemewe, buhumye-buhumyi, umwanya wawo kandi bugenzurwa n’ibikorwa bigereranywa n’itsinda rya 2, icyitegererezo cy’inyamaswa zifite diyabete yo mu bwoko bwa 2 mellitus, nyuma yo kuvurwa na Retatrutid, cyerekanye ko igabanuka rikabije ry’imisemburo ya gemoglobine, kandi uburemere bw’umubiri nabwo bwaragabanutse ku buryo buterwa na dose [4] . Ibi birashobora guterwa ningaruka zuzuye zibiyobyabwenge kuri GLP-1, GCGR, na GIPR, bitezimbere glucose metabolism hamwe nuburinganire bwingufu.
Kunoza ibintu bishobora gutera ingaruka z'umutima-damura: Retatrutid ntishobora kugabanya ibiro byumubiri gusa ahubwo inateza imbere ingaruka ziterwa numutima nimiyoboro yumutima, nka serumu lipid umwirondoro hamwe na glycated hemoglobine. Ibi byerekana isano iri hagati yumubyibuho ukabije nindwara zifata umutima, kandi Retatrutid irashobora guteza imbere ubuzima bwumutima nimiyoboro yabarwayi bafite umubyibuho ukabije binyuze munzira nyinshi. Kurugero, kugabanya urwego rutari HDL-C, apoB, na LDLP birashobora kugabanya ibyago byo kurwara aterosklerose; kugabanya urugero rwa glycated hemoglobine birashobora kunoza glucose yamaraso kubarwayi barwaye diyabete, bityo bikagabanya ibyago byo kurwara umutima nimiyoboro y'amaraso [3, 5, 6].
Kuvura indwara zumwijima zidafite inzoga (NAFLD): Retatrutid nigitabo gishya cyakira reseptor agonist peptide yibasira reseptor ya glucagon (GCGR), glucose iterwa na insuline ya insuline ya polypeptide (GIPR), na glucagon imeze nka peptide-1 (GLP-1R). Ubushakashatsi bwerekanye ko Retatrutid ifite ubushobozi bwo kuvura indwara zumwijima zidafite inzoga. Mu bushakashatsi bumwe, ubushakashatsi bwakozwe ku bushake, buhumye-buhumyi, bugenzurwa na platbo bwakozwe mu byumweru 48 ku bitabiriye amahugurwa bafite imikorere mibi ya metabolike iterwa n’indwara y’umwijima n’amavuta y’umwijima angana na 10%. Ibisubizo byerekanye ko mu byumweru 24, impuzandengo ugereranije n’amavuta y’umwijima uhereye ku murongo fatizo mu bitabiriye amahugurwa bavuwe na dosiye zitandukanye za Retatrutid (1mg, 4mg, 8mg, na 12mg) bari -42,9%, -57.0%, -81.4%, na -82.4%, mu gihe mu itsinda rya placebo bari + 0.3% [7] . Ibi byerekana ko Retatrutid ishobora kugira ingaruka zikomeye zo kuvura indwara zumwijima zidafite inzoga.
Mu gusoza, nkibintu bitatu byakira reseptor agonist, Retatrutid yerekana imbaraga nyinshi mukuvura umubyibuho ukabije nindwara zifitanye isano. Irashobora kugenga metabolisme yumuntu kuva mubice byinshi ikora reseptor ya glucagon, reseptor ya glucose iterwa na insuline ya insuline, na reseptor ya peptide-1, kunoza igenzura rya glucose yamaraso, kugabanya ibiro byumubiri, no kugenzura metabolisme ya lipide. Kugaragara kwa Retatrutid byazanye uburyo bushya bwo kuvura abarwayi bafite umubyibuho ukabije, indwara ya diyabete yo mu bwoko bwa 2, n'ibindi.
Ibyerekeye Umwanditsi
Ibikoresho byavuzwe haruguru byose byakorewe ubushakashatsi, byahinduwe kandi byakozwe na Cocer Peptides.
Umwanditsi w'ikinyamakuru
Rosenstock J ni intiti ikomeye cyane mubuvuzi, ikorana cyane ninzego nka kaminuza yubuvuzi ya kaminuza ya Texas Southwestern na kaminuza ya Texas Dallas. Akora kandi ubushakashatsi mubigo nka Centre ya VIGOR yo muri Kanada na Veloc Clin Res Ctr Med City.
Ubushakashatsi bwe bwibanze kuri endocrinology na metabolism, sisitemu yumutima nimiyoboro yumutima na cardiologiya, farumasi, nubuvuzi bwikigereranyo, yibanda kuri diyabete, umubyibuho ukabije, hamwe nubuvuzi bujyanye no guteza imbere ibiyobyabwenge. J Rosenstock yageze ku ntera ishimishije mu buvuzi bw’amavuriro, yiswe Umushakashatsi wavuzwe cyane kuva 2017 kugeza 2024.Ibyo byerekana ingaruka zikomeye no kumenyekanisha ibikorwa bye. Binyuze ku bufatanye n’ibigo byinshi by’ubushakashatsi, yahinduye neza ibyavuye mu bushakashatsi mu bikorwa by’ubuvuzi, agirira akamaro abarwayi bafite indwara ziterwa na metabolike n’umutima ndetse no guteza imbere ubumenyi bw’ubuvuzi. Rosenstock J yashyizwe ku rutonde rwerekana [4].
