Retatrutide waa peptide synthetic novel kaas oo loogu talagalay in uu si isku mid ah u dhaqaajiyo saddex reseptors oo muhiim ah oo ku lug leh gulukoosta homeostasis iyo dheelitirka tamarta: glucagon receptor (GCGR), gulukoos-ku-tiirsan insulinotropic polypeptide receptor (GIPR) iyo glucagon-like peptide-1 reseptor (GLP- 1R) (Finan et al., 2023, The New England Journal of Medicine).Iyada oo la beegsanayo soo-dhoweeyayaashan, retatrutide waxay u ekaanaysaa saamaynta isku-xidhka xayndaabkooda, glucagon, GIP iyo GLP-1, kuwaas oo ah hormoonno nidaamiya dheef-shiid kiimikaadka gulukooska iyo miisaanka jidhka ee unugyada kala duwan, sida beeryarada, beerka, maskaxda, unugyada adipose iyo caloosha caloosha. jidka (Drucker, 2023, Dabeecadda).
Si ka duwan ligands endogenous, kuwaas oo leh nus-nolosho gaaban, hoos u dhac degdeg ah by dipeptidyl peptidase-4 (DPP-4) enzyme iyo waxyeellooyin aan loo baahnayn, sida hypoglycemia iyo lallabbo (Drucker, 2023, Nature), retatrutide ayaa loo habeeyay si looga gudbo kuwan. xaddidid.Retatrutide waa peptide fiyuus ah oo ka kooban isku xigxiga glucagon wax laga beddelay oo ku xidhan taxanaha GLP-1 ee wax laga beddelay iyada oo loo marayo taxanaha GIP (Finan et al., 2023, The New England Journal of Medicine).Wax ka beddelka waxaa ka mid ah beddelka amino acids iyo tirtiridda kuwaas oo kor u qaadaya xasilloonida, awoodda iyo xulashada peptide ee saddexda soo-qaadayaasha (Finan et al., 2023, The New England Journal of Medicine).
Retatrutide waxay muujisay sifooyinka dawooyinka ee cajiibka ah iyo waxtarka daaweynta ee buurnaanta iyo nooca 2 ee sonkorowga ee daraasadaha hore iyo kiliinikada.Noocyada xayawaanka ee buurnaanta iyo sonkorowga, retatrutide waxay muujisay saameyn sare oo ku saabsan hoos u dhigista heerarka gulukooska dhiigga, kicinta dheecaanka insulinta, xakamaynta dheecaanka glucagon, dib u dhigista faaruqinta caloosha, yaraynta qaadashada cuntada iyo miisaanka jidhka marka la barbar dhigo hal ama dual agonists ee saddexda soo-qaadayaasha (Gault et et al. al., 2023, Sonkorowga, buurnaanta iyo dheef-shiid kiimikaadka; Coskun et al., 2023a, Dheef-shiid kiimikaad).Retatrutide waxay sidoo kale wanaajisay astaanta dufanka, shaqada beerka, caabuqa iyo xuduudaha wadnaha iyo xididada xayawaankan (Gault et al., 2023, Sonkorowga, Cayilka iyo dheef-shiid kiimikaadka; Coskun et al., 2023a, Metabolism Molecular).
Tijaabooyin caafimaad oo biniaadmi ah, retatrutide ayaa sidoo kale muujisay natiijooyin rajo leh oo ku saabsan bukaannada cayilan iyo sonkorowga.Retatrutide si fiican ayaa loo dulqaatay waxayna muujisay saamaynta qiyaasta ku-tiirsanaanta hoos u dhigista heerarka gulukooska dhiigga, kicinta dheecaanka insulin, xakamaynta dheecaanka glucagon iyo yaraynta rabitaanka cuntada ee daraasadda 1 ee ku lug leh tabaruceyaal caafimaad qaba iyo bukaanada qaba nooca 2 ee sonkorowga (Coskun et al., 2023b, Care Diabetes) ).Retatrutide waxay gaadhay ilaa 17.5% celcelis ahaan dhimista miisaanka toddobaadyada 24 marka la barbar dhigo placebo ee daraasadda wejiga 2 ee ku lug leh bukaannada cayil iyo cayilan.Miisaan darradan waxaa weheliya hagaajinta kontoroolka glycemic, astaanta dufanka, shaqada beerka iyo tayada nolosha (Natiijooyinka wajiga Lilly 2 ee retatrutide ee lagu daabacay joornaalka New England Journal of Medicine ayaa muujinaya molecule-ka baadhista ee la gaarey ilaa 17.5% macnaheedu waa dhimista miisaanka 24 toddobaad dadka waaweyn ee leh buurnaanta iyo cayilka., 2023).Retatrutide sidoo kale waxay lahayd astaan badbaado oo wanaagsan iyada oo aan la soo sheegin dhacdooyin xun oo halis ah ama xaalad hypoglycemia ah oo la soo sheegay.
Jaantus 1. Retatrutide (LY3437943) waxay joojisaa hemoglobin glycated A1c (HbA1c) qiimaha (A) iyo miisaanka jidhka (B) waqti ka dib.
(Urva S, Coskun T, Loh MT, Du Y, Thomas MK, Gurbuz S, Haupt A, Benson CT, Hernandez-Illas M, D'Alessio DA, Milicevic Z. LY3437943, sheeko saddexle GIP, GLP-1, iyo glucagon receptor agonist ee dadka qaba nooca 2-aad ee sonkorowga: wajiga 1b, xarun badan, laba-indhoole, placebo-control, randomized, tijaabin qiyaasta kor u kaca. 2022 Nov 26;400(10366):1869-1881.
Retatrutide hadda waxaa ku hoos jira horumarinta Eli Lilly iyo Shirkadda oo ah musharax daroogo cusub oo cayilka iyo nooca 2 ee sonkorowga.Waxay ka dhigan tahay hab cusub oo lagu beegsanayo reseptors badan oo ku lug leh dheef-shiid kiimikaadka gulukooska iyo dheelitirka tamarta oo leh hal unug.Retatrutide waxay muujisay waxtarka cajiibka ah ee moodooyinka xayawaanka iyo tijaabooyinka bini'aadamka ee leh astaamaha badbaadada iyo dulqaadka wanaagsan.Daraasado dheeraad ah ayaa loo baahan yahay si loo xaqiijiyo faa'iidooyinkeeda mustaqbalka fog iyo khataraha ka iman kara dadka waaweyn iyo kuwa kala duwan.Retatrutide waxaa laga yaabaa inay siiso ikhtiyaar cusub bukaanada la halgamaya cayilka iyo sokorowga oo u baahan daaweyn waxtar leh.
Waxaan nahay soo saaraha polypeptide ee Shiinaha, oo leh dhowr sano oo waayo-aragnimo ah oo bislaaday wax soo saarka polypeptide.Hangzhou Taijia Biotech Co., Ltd. waa xirfadle soo saaraha alaabta ceeriin polypeptide, kaas oo ku siin kara tobanaan kun oo polypeptide alaabta ceeriin iyo sidoo kale loo habayn karaa iyadoo loo eegayo baahiyaha.Tayada alaabada polypeptide waa mid aad u fiican, nadiifintuna waxay gaari kartaa 98%, taas oo ay aqoonsadeen isticmaalayaasha adduunka oo dhan. Ku soo dhawow inaad nala tashato.