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1kits （10Ibikoresho）
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Imiterere ya Retatrutide
Inkomoko: PubChem |
Urukurikirane: YA⊃1; QGTFTSDYSI-L⊃2; LDKK⁴AQA⊃1; AFIEYLLEGGPSSGAPPPS⊃3; Inzira ya molekulari: C 221H 342N 46O.68 Uburemere bwa molekuline: 4731 g / mol Numero ya CAS: 2381089-83-2 PubChem CID: 171390338 Synonyme ： LY3437943 |
Research Retatrutide Ubushakashatsi
Ni ubuhe bushakashatsi bwakozwe na Retatrutide?
Ubushakashatsi bwakozwe na Retatrutide bufitanye isano rya bugufi n’ibibazo bikomeje kwiyongera ku isi by’umubyibuho ukabije na metabolisme, ndetse n’imbogamizi z’imiti isanzwe ivura: umubyibuho ukabije na metabolisme bibangamira ubuzima rusange bw’abaturage, aho umubare w’abatuye umubyibuho ukabije ku isi uteganijwe kugera kuri miliyari 4.005 muri 2035 kandi umubare w’abarwayi ba metabolism ukaba wiyongereye kugera kuri miliyoni 592. Peptide nyinshi zakira reseptor agonist peptide yagaragaye nkigisubizo, gishobora gukumira umubyibuho ukabije, kuvura metabolisme, no kwirinda ingaruka ziterwa nuburozi bwibiyobyabwenge bihari, bigatuma biba inzira yo guteza imbere umubyibuho ukabije no kuvura metabolism.
Nubuhe buryo bwibikorwa bya Retatrutide?
Kugenzura ingufu za metabolisme binyuze mumikorere myinshi-yakira
Retatrutide ni reseptor eshatu agonist yibasira glucose-iterwa na insulineotropic polypeptide reseptor (GIPR), reseptor ya glucagon imeze nka peptide-1 (GLP-1R), na glucagon reseptor (GCGR). Irakora icyarimwe ikora reseptors eshatu, igenga ingufu za metabolisme binyuze munzira nyinshi.
Igikorwa cya GIPR agonist:
GIP ni imisemburo yo mu mara isohora insuline isohora ingirabuzimafatizo K yo mu mara ikarekurwa nyuma yo kurya. Retatrutide ikora GIPR, igatera gusohora insuline, ikongerera insuline, bityo igafasha umubiri kurushaho kwinjiza no gukoresha glucose, bityo bikagabanya urugero rwa glucose yamaraso. Byongeye kandi, GIP irashobora guhindura metabolisme yibinure muguhindura imikorere ya adipocyte no kugabanya ibinure [1].
GLP-1R ibikorwa bya agonist:
GLP-1 ni imisemburo ya peptide isohoka mu ngirabuzimafatizo L. Nyuma yo gukora GLP-1R, Retatrutide itanga ingaruka zitandukanye zingirakamaro. Irashobora gutuma insuline isohoka muburyo bwa glucose bushingiye ku kwibanda, bityo bikagabanya urugero rwisukari mu maraso. Irashobora gutinza ubusa gastrica, kongera guhaga, no kugabanya ibiryo. Agonism ya GLP-1R irashobora kandi gukora kuri sisitemu yo hagati yo hagati, igenga ubushake bwo kurya no kuringaniza ingufu, bityo igafasha kugabanya ibiro [2].
Ingaruka za GCGR agonist:
Glucagon isanzwe yongera glucose yamaraso, ariko bitewe na Retatrutide, agonism ya GCGR itanga ingaruka zitandukanye. Itera glycogenolysis na gluconeogenezi mu mwijima. Ingaruka ziterwa na Retatrutide, umubiri ntiwiyongera muburyo bworoshye bwamaraso ya glucose ahubwo ugenga metabolisme yingufu kugirango wongere ibinure, bityo ugabanye ibiro kandi utezimbere metabolism. Agonism ya GCGR irashobora kandi kugira ingaruka kuri metabolisme ya hepatike, kugabanya ibinure bya hepatike [3].
Ingaruka kuri Diyabete ifitanye isano na Physiologique
Mugukorera icyarimwe icyarimwe kuri reseptors eshatu zavuzwe haruguru, Retatrutide igira ingaruka kumikorere myinshi ya metabolism ijyanye na physiologique.
Amaraso ya glucose:
Mugukoresha GIPR na GLP-1R kugirango uteze imbere gusohora insuline, no kugenzura neza GCGR, Retatrutide irashobora kugabanya urugero rwa glucose yamaraso. Ingaruka ya hypoglycemic igaragara iyo glucose yamaraso izamutse, mugihe bidashoboka gutera hypoglycemia mugihe glucose yamaraso ari ibisanzwe, ifasha mugukumira glucose yamaraso kubarwayi ba diyabete [4].
Gucunga ibiro:
Retatrutide yerekana imikorere ikomeye mugucunga ibiro. Mugukoresha GLP-1R, itinda gusiba gastric, ikongera guhaga, kandi igabanya ibiryo; muguhindura metabolisme yibinure, itera kugabanuka kwamavuta no gukoresha ingufu, bityo bikagabanuka. Igeragezwa rya Clinical ryerekanye ko abarwayi bafite umubyibuho ukabije cyangwa ufite ibiro byinshi bavuwe na Retatrutide bagabanuka cyane mu gihe runaka [5,6].
Amabwiriza ya Lipid:
Kuvura Retatrutide biteza imbere imyirondoro yabarwayi. Igabanya triglyceride (TG), cholesterol ya lipoprotein nkeya (LDL-C), hamwe na cholesterol ya lipoprotein nkeya cyane (VLDL-C), mu gihe kandi igenga apolipoproteine, nko kugabanya apolipoproteine B (apoB) hamwe na apolipoproteine C -III (apoC). aterosklerose no guteza imbere ubuzima bw'umutima n'imitsi [7].
Kunoza metabolisme ya hepatike:
Ku barwayi bafite indwara y’umwijima idafite inzoga (NAFLD) ifitanye isano n’imikorere mibi ya metabolike, Retatrutide igabanya cyane ibinure byumwijima. Mu bigeragezo bijyanye n’amavuriro, abarwayi bavuwe bafite dosiye zitandukanye za Retatrutide bagaragaje igabanuka rikabije ry’amavuta y’umwijima ugereranije n’ibanze, byerekana ko Retatrutide igira ingaruka nziza ku mikorere y’amavuta y’umwijima, ifasha mu kunoza imikorere y’umwijima [3].
Igishushanyo 1 Uburyo bwa Retatrutide bwibikorwa [8].
Ni ubuhe buryo bukoreshwa muri Retatrutide?
Kuvura umubyibuho ukabije:
Umubyibuho ukabije wabaye ikibazo gikomeye cy’ubuzima rusange ku isi, gifitanye isano rya hafi no gutangira no gutera indwara zitandukanye zidakira. Retatrutide yerekanye akamaro gakomeye mukuvura umubyibuho ukabije. Abarwayi bafite umubyibuho ukabije bavuwe na Retatrutide bagabanutse cyane ku buremere bw'umubiri. Mu byumweru 48 icyiciro cya 2 cy’umubyibuho ukabije, abarwayi bavuwe na 8mg na 12mg za Retatrutide bagabanutse ibiro 22.8% na 24.2%. Mu kindi cyiciro cya 2 gihumye-gihumye, giteganijwe, kigenzurwa na platbo, abarwayi bo mumatsinda atandukanye ya dose bahuye nibiro bitandukanye byo gutakaza ibiro mubyumweru 24 nibyumweru 48. Itsinda rya 12mg ryageze ku gutakaza ibiro 24.2% mu byumweru 48, mugihe itsinda rya placebo ryabonye gusa kugabanuka -2.1%. Retatrutide igabanya neza uburemere bwumubiri kubarwayi bafite umubyibuho ukabije, itanga igikoresho gishya kandi gikomeye cyo kuvura umubyibuho ukabije. Ubuvuzi bwa Retatrutide kumubyibuho ukabije ntibugabanya ibiro byumubiri gusa ahubwo bushobora no kunoza ibindi bibazo byubuzima bujyanye numubyibuho ukabije, nko kugabanya imihangayiko itera hamwe no kugabanya ibimenyetso byindwara ziterwa numubyibuho ukabije binyuze mu kugabanya ibiro; kugabanya ibiro birashobora kandi gufasha kunoza ibibazo biterwa n'umubyibuho ukabije nko gusinzira [3,6].
Ubwoko bwa 2 bwo kuvura metabolism:
Ubwoko bwa 2 metabolism ni indwara isanzwe idakira ya metabolike irangwa no kurwanya insuline no gusohora kwa insuline bidahagije. Retatrutide ifite agaciro gakoreshwa muburyo bwo kuvura ubwoko bwa metabolism. Itera imisemburo ya insuline ikora reseptor ya GLP-1, igahindura insuline, kandi ikagabanya urugero rwa glucose. Ingaruka zayo zo kugabanya ibiro nazo zifasha kunoza imiterere yabarwayi ba metabolisme yo mu bwoko bwa 2, kubera ko umubyibuho ukabije ari ikintu cy’ingaruka zikomeye ziterwa na metabolism yo mu bwoko bwa 2, kandi kugabanya ibiro birashobora kongera insuline ya insuline, bikanafasha mu kurwanya glucose yamaraso. Mu bushakashatsi bwakozwe n’abarwayi bafite metabolism yo mu bwoko bwa 2, Retatrutide yatumye ibiro bigabanuka cyane ndetse n’igabanuka rikabije rya hemoglobine A1c (HbA1c), HbA1c yagabanutseho 1,64% ugereranije na placebo. Ibi byerekana ko Retatrutide itagenzura neza glucose yamaraso gusa ahubwo inatezimbere muri rusange abarwayi bafite metabolism yo mu bwoko bwa 2 hakoreshejwe uburyo bwinshi, harimo no kugabanya ibiro, bityo bikazamura imibereho yabo [6].
Indwara y'umwijima idafite inzoga (NAFLD):
NAFLD ni imvune ziterwa n'umwijima ziterwa n'umwijima zifitanye isano rya bugufi no kurwanya insuline no kwandura indwara, bikubiyemo ibintu bitandukanye birimo umwijima w'amavuta utarimo inzoga, umwijima udafite inzoga, na cirrhose. Retatrutide yerekana ubushobozi butanga ubuvuzi bwa NAFLD. Mu igeragezwa ryateganijwe, rihumye-rihumye, rigenzurwa na platbo ryitabiriwe n’abitabiriye bafite indwara ziterwa n’umwijima ziterwa n’umwijima hamwe n’ibinure by’umwijima ≥10%, mu byumweru 24, impinduka zigereranijwe zijyanye n’ibinure by’umwijima bivuye ku murongo w’ibanze byari bitandukanye cyane mu matsinda ya dose ya Retatrutide: -81.4% mu itsinda rya 8mg, -82.4% mu itsinda rya mg 12, na + 0.3% mu itsinda rya placebo. Ibi byerekana ko Retatrutide ishobora kugabanya neza ibinure byumwijima, bifite akamaro kanini mugutezimbere indwara yumwijima yabarwayi ba NAFLD. Ifite amasezerano nk'uburyo bushya bwo kuvura NAFLD, bishobora kudindiza iterambere ry’indwara no kugabanya ibyago by’ingaruka zikomeye nka cirrhose [3].
Umwanzuro
Retatrutide yerekana imbaraga zitanga icyizere cyo kuzamura indwara y’umwijima y’abarwayi ba NAFLD, ikora binyuze mu buryo bwinshi burimo kugenzura ingufu za metabolisme, kunoza insuline, ingaruka zo kurwanya inflammatory, no guhindura metabolisme ya lipide.
Ibyerekeye Umwanditsi
Ibikoresho byavuzwe haruguru byose byakorewe ubushakashatsi, byahinduwe kandi byakozwe na Cocer Peptides.
Umwanditsi w'ikinyamakuru
Rosenstock, J ni intiti y’indashyikirwa umwuga we ufitanye isano rya bugufi n’ibigo byinshi bizwi, birimo kaminuza y’ubuvuzi ya kaminuza ya Texas y’Amajyepfo y’Uburengerazuba, Kaminuza ya Texas Dallas, n’ikigo cya VIGOR cyo muri Kanada. Ubushakashatsi bwe bwibanze ku bice byinshi nka Endocrinology & Diabete, Ubuvuzi rusange & Imbere mu Gihugu, Sisitemu Yumutima & Cardiology, Pharmacology & Pharmacy, na Research & Experimental Medicine. Umusanzu we udasanzwe mu muryango w’amasomo watumye amenyekana cyane, nk'uko bigaragazwa n’uko yahisemo inshuro nyinshi nka 'Umushakashatsi wavuzwe cyane mu bijyanye n’ubuvuzi bwa Clinical ' kuva 2017 kugeza 2024, agaragaza umwanya afite n’uruhare rukomeye mu bushakashatsi bw’ubuvuzi. Rosenstock J yanditse kurutonde rwerekana [4].
