Retatrutide ke novel synthetic peptide e etselitsoeng ho kenya tšebetsong ka nako e ts'oanang li-receptor tse tharo tsa bohlokoa tse amehang ho glucose homeostasis le ho leka-lekana ha matla: glucagon receptor (GCGR), glucose-based insulinotropic polypeptide receptor (GIPR) le glucagon-like peptide-1 receptor (GLP- 1R) (Finan et al., 2023, The New England Journal of Medicine).Ka ho shebana le li-receptor tsena, retatrutide e etsisa litlamorao tsa li-endogenous ligands, glucagon, GIP le GLP-1, e leng lihormone tse laolang metabolism ea tsoekere le boima ba 'mele liseleng tse fapaneng, joalo ka manyeme, sebete, boko, lisele tsa adipose le mala. pampitšana (Drucker, 2023, Tlhaho).
Ho fapana le li-endogenous ligands, tse nang le halofo ea bophelo bo khuts'oane, ho senyeha ka potlako ka dipeptidyl peptidase-4 (DPP-4) enzyme le litlamorao tse sa batleheng, joalo ka hypoglycemia le ho nyekeloa ke pelo (Drucker, 2023, Nature), retatrutide e entsoe ho hlola tsena. mefokolo.Retatrutide ke peptide ea fusion e entsoeng ka tatellano e fetotsoeng ea glucagon e hokahantsoeng le tatellano e fetotsoeng ea GLP-1 ka tatellano ea GIP (Finan et al., 2023, The New England Journal of Medicine).Liphetoho li kenyelletsa li-amino acid le ho hlakoloa tse matlafatsang botsitso, matla le khetho ea peptide bakeng sa li-receptor tse tharo (Finan et al., 2023, The New England Journal of Medicine).
Retatrutide e bontšitse thepa e tsotehang ea meriana le katleho ea phekolo ho botenya le lefu la tsoekere la mofuta oa 2 lithutong tsa pele le tsa bongaka.Mehlala ea liphoofolo tsa botenya le lefu la tsoekere, retatrutide e bonts'itse litlamorao tse phahameng ho theola maemo a tsoekere ea mali, ho hlohlelletsa secretion ea insulin, ho hatella secretion ea glucagon, ho lieha ho tsoa ka mpeng, ho fokotsa ho ja lijo le boima ba 'mele ha ho bapisoa le li-agonists tse le 'ngoe kapa tse peli tsa li-receptor tse tharo (Gault et. al., 2023, Lefu la tsoekere, Botenya le Metabolism; Coskun et al., 2023a, Metabolism ea Limolek'hule).Retatrutide e boetse e ntlafalitse boemo ba lipid, ts'ebetso ea sebete, ho ruruha le likarolo tsa pelo ho liphoofolo tsena (Gault et al., 2023, Lefu la tsoekere, Botenya le Metabolism; Coskun et al., 2023a, Molecular Metabolism).
Litekong tsa bongaka tsa batho, retatrutide e boetse e bonts'itse litholoana tse ts'episang ho bakuli ba batenya le ba nang le lefu la tsoekere.Retatrutide e ile ea mamelloa hantle 'me ea bontša litlamorao tse itšetlehileng ka tekanyo ea ho theola tsoekere ea mali, ho hlohlelletsa secretion ea insulin, ho hatella secretion ea glucagon le ho fokotsa takatso ea lijo thutong ea mohato oa 1 e kenyelletsang baithaopi ba phetseng hantle le bakuli ba nang le lefu la tsoekere la mofuta oa 2 (Coskun et al., 2023b, Tlhokomelo ea Lefu la tsoekere). ).Retatrutide e fihletsoeng ho 17.5% e bolela ho fokotsa boima ba 'mele libeke tse 24 ha ho bapisoa le placebo thutong ea mohato oa 2 e amang bakuli ba botenya le boima bo feteletseng.Ho lahleheloa ke boima ba 'mele ho ne ho tsamaisana le ntlafatso ea taolo ea glycemic, profil ea lipid, ts'ebetso ea sebete le boleng ba bophelo (liphetho tsa Lilly's phase 2 retatrutide tse phatlalalitsoeng ho The New England Journal of Medicine li bonts'a molek'hule ea lipatlisiso e fihletsoeng ho 17.5% e bolela ho fokotsa boima ba 'mele libekeng tse 24 batho ba baholo ba nang le botenya le botenya., 2023).Retatrutide e boetse e na le boemo bo botle ba polokeho ntle le liketsahalo tse mpe tse tebileng kapa liketsahalo tsa hypoglycemia.
Setšoantšo sa 1. Retatrutide (LY3437943) e thibela boleng ba glycated hemoglobin A1c (HbA1c) (A) le boima ba 'mele (B) ka nako.
(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, novel triple GIP, GLP-1, le glucagon receptor agonist ho batho ba nang le lefu la tsoekere la mofuta oa 2: teko ea mohato oa 1b, litsi tse ngata, tse foufetseng habeli, tse laoloang ke placebo, tse sa reroang, tse nyolohang ka makhetlo a mangata. Lancet. 2022 Nov 26;400(10366):1869-1881.
Retatrutide hajoale e ntse e ntlafatsoa ke Eli Lilly and Company joalo ka moemeli e mocha oa lithethefatsi bakeng sa botenya le lefu la tsoekere la mofuta oa 2.E emela mokhoa o mocha oa ho shebisa li-receptor tse ngata tse amehang ho metabolism ea tsoekere le ho leka-lekana ha matla ka molek'hule e le 'ngoe.Retatrutide e bontšitse katleho e tsotehang mefuteng ea liphoofolo le litekong tsa batho tse nang le litlaleho tse ntle tsa polokeho le mamello.Lithuto tse ling lia hlokahala ho netefatsa melemo ea eona ea nako e telele le likotsi tse ka bang teng ho baahi ba bangata le ba fapaneng.Retatrutide e ka fana ka khetho e ncha bakeng sa bakuli ba nang le botenya le lefu la tsoekere mme ba hloka kalafo e sebetsang haholoanyane.
Re baetsi ba polypeptide Chaena, ba nang le phihlelo ea lilemo tse 'maloa tlhahiso ea polypeptide.Hangzhou Taijia Biotech Co., Ltd. ke moetsi oa thepa e tala ea polypeptide, e ka fanang ka mashome a likete a lisebelisoa tse tala tsa polypeptide hape e ka etsoa ho latela litlhoko.Boleng ba lihlahisoa tsa polypeptide bo botle haholo, 'me bohloeki bo ka fihla ho 98%, e' nileng ea hlokomeloa ke basebelisi lefatšeng lohle.
