Retatrutide wani sabon peptide na roba ne wanda aka tsara don kunna masu karɓa guda uku a lokaci guda waɗanda ke cikin glucose homeostasis da ma'aunin makamashi: glucagon receptor (GCGR), mai karɓar insulinotropic polypeptide mai dogaro da glucose (GIPR) da glucagon-like peptide-1 receptor (GLP- 1R) (Finan et al., 2023, The New England Journal of Medicine).Ta hanyar yin niyya ga waɗannan masu karɓa, retatrutide yana yin kwaikwayon tasirin ligands na endogenous, glucagon, GIP da GLP-1, waɗanda suke da hormones waɗanda ke daidaita glucose metabolism da nauyin jiki a cikin kyallen takarda daban-daban, kamar su pancreas, hanta, kwakwalwa, adipose tissue da gastrointestinal tract. fili (Drucker, 2023, Nature).
Ba kamar ligands na endogenous ba, waɗanda ke da ɗan gajeren rabin rayuwa, raguwa mai sauri ta hanyar dipeptidyl peptidase-4 (DPP-4) enzyme da abubuwan da ba a so, irin su hypoglycemia da tashin zuciya (Drucker, 2023, Nature), an ƙirƙira retatrutide don shawo kan waɗannan. iyakoki.Retatrutide shine peptide fusion wanda ya ƙunshi gyare-gyaren jerin glucagon da ke da alaƙa da tsarin GLP-1 da aka gyara ta hanyar jerin GIP (Finan et al., 2023, The New England Journal of Medicine).Canje-canjen sun haɗa da maye gurbin amino acid da sharewa waɗanda ke haɓaka kwanciyar hankali, ƙarfi da zaɓi na peptide don masu karɓa guda uku (Finan et al., 2023, The New England Journal of Medicine).
Retatrutide ya nuna kaddarorin magunguna na ban mamaki da ingantaccen magani a cikin kiba da nau'in ciwon sukari na 2 a cikin ilimin kimiya da na asibiti.A cikin nau'ikan dabbobi na kiba da ciwon sukari, retatrutide ya nuna babban tasiri akan rage matakan glucose na jini, haɓaka haɓakar insulin, murkushe glucagon, jinkirta zubar da ciki, rage cin abinci da nauyin jiki idan aka kwatanta da guda ɗaya ko dual agonists na masu karɓa guda uku (Gault et al. al., 2023, Ciwon sukari, Kiba da Metabolism; Coskun et al., 2023a, Kwayoyin Halitta).Retatrutide kuma ya inganta bayanin martaba na lipid, aikin hanta, kumburi da sigogi na zuciya a cikin waɗannan dabbobin (Gault et al., 2023, Ciwon sukari, Kiba da Metabolism; Coskun et al., 2023a, Molecular Metabolism).
A cikin gwaje-gwajen asibiti na ɗan adam, retatrutide kuma ya nuna sakamako mai ban sha'awa a cikin masu kiba da masu ciwon sukari.An yi haƙuri da Retatrutide da kyau kuma ya nuna tasirin dogaro da kashi akan rage matakan glucose na jini, haɓaka haɓakar insulin, danne ɓoyayyun glucagon da rage ci a cikin binciken lokaci na 1 wanda ya ƙunshi masu sa kai masu lafiya da marasa lafiya da ke da nau'in ciwon sukari na 2 (Coskun et al., 2023b, Ciwon sukari Care ).Retatrutide ya samu har zuwa 17.5% yana nufin raguwar nauyi a cikin makonni 24 idan aka kwatanta da placebo a cikin binciken lokaci na 2 wanda ya shafi marasa lafiya da kiba da kiba.Wannan asarar nauyi yana tare da haɓakawa a cikin sarrafa glycemic, bayanin martaba na lipid, aikin hanta da ingancin rayuwa (Sakamakon matakin retatrutide na Lilly 2 da aka buga a cikin The New England Journal of Medicine ya nuna kwayar binciken da aka samu har zuwa 17.5% yana nufin rage nauyi a cikin makonni 24 a ciki). manya masu kiba da kiba., 2023).Har ila yau, Retatrutide yana da ingantaccen bayanin martaba na aminci ba tare da wani mummunan al'amuran da suka faru ba ko abubuwan da suka faru na hypoglycemia.
Hoto 1. Retatrutide (LY3437943) yana hana glycated haemoglobin A1c (HbA1c) darajar (A) da nauyin jiki (B) a tsawon lokaci.
(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, labari mai sau uku GIP, GLP-1, da kuma glucagon receptor agonist a cikin mutanen da ke da nau'in ciwon sukari na 2: wani lokaci na 1b, multicentre, makafi biyu, mai sarrafa wuribo, bazuwar, gwajin kashi da yawa. Lancet.
Retatrutide a halin yanzu yana ƙarƙashin haɓaka ta Eli Lilly da Kamfanin a matsayin sabon ɗan takarar magani don kiba da nau'in ciwon sukari na 2.Yana wakiltar wata sabuwar hanya don ƙaddamar da masu karɓa da yawa da ke da hannu a cikin metabolism na glucose da ma'aunin makamashi tare da kwayoyin halitta guda ɗaya.Retatrutide ya nuna ingantaccen inganci a cikin ƙirar dabba da gwajin ɗan adam tare da ingantaccen bayanin martaba da aminci.Ana buƙatar ƙarin karatu don tabbatar da fa'idodinsa na dogon lokaci da haɗarin haɗari a cikin manyan mutane da yawa.Retatrutide na iya ba da sabon zaɓi ga marasa lafiya waɗanda ke fama da kiba da ciwon sukari kuma suna buƙatar ƙarin ingantattun jiyya.
Mu masu sana'a ne na polypeptide a kasar Sin, tare da shekaru masu yawa na kwarewa a cikin samar da polypeptide.Hangzhou Taijia Biotech Co., Ltd. ƙwararren ƙwararren masana'anta ne na polypeptide, wanda zai iya samar da dubun dubatan polypeptide albarkatun ƙasa kuma ana iya keɓance shi gwargwadon buƙatu.Ingancin samfuran polypeptide yana da kyau sosai, kuma tsabta zai iya kaiwa 98%, wanda masu amfani suka gane a duk faɗin duniya. Barka da tuntuɓar mu.