Retatrud 20 mg

▎ Retatrutid Structure

Source: PubChem

Sequence: YA⊃1;QGTFTSDYSI-L⊃2;LDKK⁴AQA⊃1;AFIEYLLEGGPSSGAPPPS⊃3; Molecular Formula: C 221H 342N 46O68 Molecular Luj: 4731 g / mol CAS Nr .: 2381089-83-2 PubChem CID: 171390338 Synonyms: LY3437943

▎ Retatrutid Research

Kev tshawb fawb keeb kwm ntawm Retatrutid yog dab tsi?

Kev tshawb fawb keeb kwm yav dhau los ntawm Retatrutid yog ze ze rau cov teeb meem loj thoob ntiaj teb ntawm kev rog thiab ntshav qab zib, nrog rau cov kev txwv ntawm cov tshuaj kho mob uas twb muaj lawm: rog rog thiab ntshav qab zib ua rau muaj kev hem thawj rau pej xeem kev noj qab haus huv, nrog rau cov neeg rog rog hauv ntiaj teb tau kwv yees mus txog 4.005 billion los ntawm 2035 thiab tus naj npawb ntawm cov neeg mob ntshav qab zib nce mus rau 592 lab, ua rau muaj kev noj qab haus huv thoob ntiaj teb. Multi-target receptor agonist peptides tau tshwm sim los ua ib qho kev daws teeb meem, muaj peev xwm tiv thaiv kev rog rog, kho ntshav qab zib, thiab zam cov kev mob tshwm sim ntawm cov tshuaj uas twb muaj lawm, ua rau lawv muaj qhov sib txawv hauv kev txhim kho kev rog thiab kev kho mob ntshav qab zib.

Yuav ua li cas yog lub mechanism ntawm kev txiav txim ntawm Retatrutid?

Regulating zog metabolism los ntawm multi-receptor activation

Retatrutid yog triple receptor agonist tsom rau cov piam thaj-dependent insulinotropic polypeptide receptor (GIPR), glucagon-zoo li peptide-1 receptor (GLP-1R), thiab glucagon receptor (GCGR). Nws ib txhij activates peb receptors, tswj lub zog metabolism los ntawm ntau txoj kev.

GIPR agonist kev txiav txim: 

GIP yog ib qho tshuaj insulin-secreting hauv plab hnyuv secreted los ntawm plab hnyuv K hlwb thiab tso tawm tom qab noj mov. Retatrutid activates GIPR, txhawb kev tsim cov tshuaj insulin, ua kom cov tshuaj insulin rhiab heev, thiab yog li pab lub cev nqus tau zoo dua thiab siv cov piam thaj, yog li txo cov ntshav qabzib. Tsis tas li ntawd, GIP tuaj yeem cuam tshuam cov roj metabolism los ntawm kev tswj hwm adipocyte muaj nuj nqi thiab txo cov rog rog ^[1].

GLP-1R agonist kev ua haujlwm: 

GLP-1 yog peptide hormone secreted los ntawm txoj hnyuv L hlwb. Tom qab ua kom GLP-1R, Retatrutid tsim ntau yam txiaj ntsig. Nws tuaj yeem ua rau cov tshuaj insulin tso tawm hauv cov piam thaj hauv cov ntshav, yog li txo cov ntshav qab zib. Nws tuaj yeem ncua lub plab zom mov, ua kom satiety, thiab txo cov khoom noj. GLP-1R agonism kuj tseem tuaj yeem ua rau lub hauv nruab nrab lub paj hlwb, tswj kev qab los noj mov thiab lub zog sib npaug, yog li pab kom poob phaus ^[2].

GCGR agonist cuam tshuam: 

Glucagon feem ntau ua rau cov ntshav qabzib nce ntxiv, tab sis raws li kev cuam tshuam ntawm Retatrutid, GCGR agonism ua rau muaj kev cuam tshuam sib txawv. Nws txhawb nqa glycogenolysis thiab gluconeogenesis hauv daim siab. Raws li kev sib xyaw ua ke ntawm Retatrutid, lub cev tsis muaj kev nce qib hauv cov ntshav qabzib yooj yim tab sis hloov kho lub zog metabolism kom nce rog, yog li ua tiav qhov poob phaus thiab txhim kho cov metabolism. GCGR agonism kuj tseem tuaj yeem cuam tshuam rau lub siab lipid metabolism, txo cov rog hauv siab ^[3].

Cov teebmeem ntawm Metabolism-Related Physiological Processes

Los ntawm tib lub sijhawm ua haujlwm ntawm peb qhov receptors, Retatrutid cuam tshuam rau ntau yam metabolism hauv lub cev.

Kev tswj cov ntshav qabzib: 

Los ntawm kev ua kom GIPR thiab GLP-1R los txhawb cov insulin secretion, thiab tswj GCGR kom tsim nyog, Retatrutid tuaj yeem txo cov ntshav qabzib. Nws cov nyhuv hypoglycemic tau tshaj tawm thaum cov ntshav qabzib nce siab, thaum nws tsis zoo li ua rau hypoglycemia thaum cov ntshav qabzib zoo li qub, uas muaj txiaj ntsig zoo rau kev tswj ntshav qabzib hauv cov neeg mob ntshav qab zib ^[4].

Kev tswj qhov hnyav: 

Retatrutid qhia tau hais tias muaj txiaj ntsig zoo hauv kev tswj qhov hnyav. Los ntawm kev ua kom GLP-1R, nws ua rau lub plab zom mov qeeb, ua kom satiety, thiab txo cov zaub mov noj; los ntawm kev tswj cov roj metabolism, nws txhawb kev rog rog thiab kev siv zog, yog li ua tiav qhov hnyav. Cov kev sim tshuaj ntsuam xyuas tau pom tias cov neeg mob rog rog lossis rog rog tau kho nrog Retatrutid muaj kev poob ceeb thawj hauv ib lub sijhawm ^[5,6].

Lipid tswj: 

Kev kho mob Retatrutid txhim kho cov neeg mob lipid profile. Nws txo qis triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), thiab tsawg-density lipoprotein cholesterol (VLDL-C), thaum tseem tswj hwm apolipoproteins, xws li txo qis apolipoprotein B (apoB) thiab apolipoprotein C-III (apoarticles nrog cov qib III). atherosclerosis thiab txhawb kev mob plawv ^[7].

Txhim kho hepatic lipid metabolism: 

Rau cov neeg mob uas tsis yog-alcoholic fatty siab kab mob (NAFLD) cuam tshuam nrog metabolic dysfunction, Retatrutid ho txo ​​cov rog rog. Hauv kev sim tshuaj ntsuam xyuas, cov neeg mob kho nrog ntau koob tshuaj ntawm Retatrutid pom qhov txo qis hauv daim siab rog cov ntsiab lus piv rau cov hauv paus ntsiab lus, qhia tias Retatrutid muaj kev tswj xyuas zoo ntawm daim siab cov roj metabolism, uas muaj txiaj ntsig zoo rau kev txhim kho daim siab ua haujlwm ^[3].

Daim duab 1 Retatrutid's mechanisms of action ^[8].

Cov ntawv thov ntawm Retatrutid yog dab tsi?

Kev kho mob rog rog: 

Kev rog rog dhau los ua qhov teeb meem tseem ceeb hauv ntiaj teb kev noj qab haus huv, cuam tshuam nrog kev pib thiab kev loj hlob ntawm ntau yam kab mob. Retatrutid tau pom tias muaj txiaj ntsig zoo hauv kev kho mob rog. Cov neeg mob rog rog kho nrog Retatrutid tau ntsib qhov txo qis hauv lub cev hnyav. Hauv kev tshawb fawb 48-lub lim tiam Phase 2 kev rog rog, cov neeg mob kho nrog 8mg thiab 12mg ntawm Retatrutid tau ntsib qhov hnyav ntawm 22.8% thiab 24.2%, feem. Hauv lwm Theem 2 ob-dig muag, randomized, placebo-tswj sim, cov neeg mob nyob rau hauv ntau pab pawg tau ntsib qhov sib txawv ntawm qhov hnyav ntawm 24 lub lis piam thiab 48 lub lis piam. Cov pab pawg 12mg tau ua tiav qhov hnyav ntawm 24.2% ntawm 48 lub lis piam, thaum pawg placebo tsuas pom qhov txo qis ntawm -2.1%. Retatrutid zoo txo ​​lub cev hnyav hauv cov neeg mob rog, muab cov cuab yeej tshiab thiab muaj zog rau kev kho mob rog. Retatrutid therapy rau kev rog rog tsis tsuas yog txo lub cev hnyav xwb tab sis kuj tseem tuaj yeem txhim kho lwm yam teeb meem kev noj qab haus huv uas cuam tshuam nrog kev rog, xws li txo cov kev ntxhov siab ntawm kev sib koom tes thiab txo cov tsos mob ntawm kev rog rog los ntawm kev poob phaus; Kev txo qhov hnyav kuj tseem tuaj yeem pab txhim kho kev rog rog xws li pw tsaug zog apnea ^[3,6].

Kev kho mob ntshav qab zib hom 2: 

Hom 2 mob ntshav qab zib mellitus yog ib hom kab mob metabolic uas tshwm sim los ntawm kev tiv thaiv insulin thiab tsis txaus cov tshuaj insulin. Retatrutid muaj peev xwm siv tau rau kev kho mob ntshav qab zib hom 2. Nws txhawb kev tsim cov tshuaj insulin los ntawm kev ua kom lub GLP-1 receptor, txhim kho insulin tsis kam, thiab txo cov ntshav qabzib. Nws cov txiaj ntsig txo qhov hnyav kuj tseem pab txhim kho tus mob ntawm cov neeg mob ntshav qab zib hom 2, vim kev rog rog yog qhov tseem ceeb ntawm kev pheej hmoo rau hom 2 mob ntshav qab zib, thiab kev poob phaus tuaj yeem txhim kho insulin rhiab heev, ntxiv kev pab tswj ntshav qabzib. Hauv kev tshawb fawb txog cov neeg mob ntshav qab zib hom 2, Retatrutid ua rau poob ceeb thawj thiab qhov tseem ceeb txo qis hauv qib hemoglobin A1c (HbA1c), nrog HbA1c txo qis los ntawm 1.64% piv rau cov placebo. Qhov no qhia tau hais tias Retatrutid tsis tsuas yog tswj cov ntshav qab zib kom zoo xwb tab sis kuj txhim kho tag nrho cov neeg mob ntshav qab zib hom 2 los ntawm ntau lub tswv yim, suav nrog kev poob phaus, yog li txhim kho lawv lub neej zoo ^[6].

Tsis-alcoholic fatty siab kab mob (NAFLD) kev kho mob: 

NAFLD yog ib qho metabolic stress-induced daim siab raug mob zoo sib xws nrog insulin tsis kam thiab genetic susceptibility, encompassing ib spectrum ntawm tej yam kev mob xws li tsis-alcoholic yooj yim fatty siab, tsis-alcoholic steatohepatitis, thiab lwm yam cirrhosis. Retatrutid qhia tau hais tias muaj peev xwm zoo hauv kev kho NAFLD. Hauv kev sib piv, ob qhov muag tsis pom kev, kev sim tshuaj placebo nrog cov neeg koom nrog cov kab mob metabolic tsis ua haujlwm cuam tshuam nrog cov kab mob siab rog thiab lub siab rog cov ntsiab lus ≥10%, ntawm 24 lub lis piam, qhov nruab nrab tus txheeb ze hloov pauv hauv daim siab rog cov ntsiab lus los ntawm lub hauv paus yog qhov sib txawv thoob plaws hauv pawg Retatrutid koob tshuaj: -81.4% hauv pawg 8mg 20% thiab 8mg. hauv pawg placebo. Qhov no qhia tau hais tias Retatrutid tuaj yeem txo cov rog hauv siab, uas yog qhov tseem ceeb rau kev txhim kho daim siab pathology ntawm NAFLD cov neeg mob. Nws tuav cov lus cog tseg raws li qhov kev xaiv kho tshiab rau NAFLD, uas tuaj yeem ua rau muaj kab mob qeeb zuj zus thiab txo qhov kev pheej hmoo ntawm cov teeb meem loj xws li cirrhosis ^[3].

Xaus

Retatrutid qhia tau hais tias muaj peev xwm los txhim kho cov kab mob hepatic pathological ntawm NAFLD cov neeg mob, ua haujlwm los ntawm ntau lub tswv yim suav nrog kev tswj hwm lub zog metabolism, txhim kho insulin tsis kam, tiv thaiv kab mob, thiab hloov kho lipid metabolism.

Hais Txog Tus Sau

Cov ntaub ntawv hais saum toj no yog txhua yam tshawb fawb, kho thiab sau los ntawm Cocer Peptides.

Scientific Journal Author

Rosenstock, J yog ib tus kws tshaj lij uas nws txoj haujlwm tau txuas nrog ntau lub tsev muaj koob npe, suav nrog University of Texas Southwestern Medical Center, University of Texas Dallas, thiab Canadian VIGOR Center. Nws txoj kev tshawb fawb nthuav dav ntau yam xws li Endocrinology & Metabolism, General & Internal Medicine, Cardiovascular System & Cardiology, Pharmacology & Pharmacy, thiab Kev Tshawb Fawb & Kev Siv Tshuaj. Nws qhov txiaj ntsig zoo tshaj plaws rau kev kawm hauv zej zog tau ua rau nws tau txais kev lees paub thoob plaws, raws li tau pom los ntawm nws qhov kev xaiv rov ua dua li 'Tus Kws Tshaj Lij Tshaj Lij Tshaj Lij Tshaj Plaws hauv Kev Kho Mob' los ntawm 2017 txog 2024, qhia txog nws txoj haujlwm tseem ceeb thiab muaj txiaj ntsig zoo hauv kev tshawb fawb kho mob. Rosenstock J tau teev nyob rau hauv qhov kev siv ntawm cov ntaub ntawv pov thawj [4].

▎ Cov Lus Qhia Tseem Ceeb

[1] Brzozowska P, Frańczuk A, Nowińska B, et al. Retatrutid - revolutionary nyuam qhuav tsim GLP agonist - cov ntaub ntawv tshuaj xyuas [J]. Zoo hauv Kev Ua Si, 2024.DOI: 10.12775/qs.2024.15.52125.

[2] Doggrell S A. Retatrutid qhia kev cog lus hauv kev rog (thiab ntshav qab zib hom 2)[J]. Cov Lus Qhia Txog Kev Tshawb Fawb Txog Tshuaj, 2023,32(11): 997-1001.DOI: 10.1080/13543784.2023.2283020.

[3] Sanyal AJ, Kaplan LM, Frias JP, et al. Triple hormone receptor agonist Retatrutid rau metabolic dysfunction-associated steatotic siab kab mob: ib theem randomized 2a sim [J]. Xwm Txheej, 2024,30:2037-2048.DOI:10.1038/s41591-024-03018-2.

[4] Rosenstock J, Frias J, Jastreboff AM, et al. Retatrutid, GIP, GLP-1 thiab glucagon receptor agonist, rau cov neeg mob ntshav qab zib hom 2: ib qho randomised, ob-dig muag, placebo thiab active-tswj, parallel-pab pawg, theem 2 sim ua nyob rau hauv teb chaws USA [J]. Lancet, 2023,402(10401):529-544.DOI:10.1016/S0140-6736(23)01053-X.

[5] Jastreboff AM, Kaplan LM, Frías JP, et al. Triple-hormone-Receptor Agonist Retatrutid for Obesity - Phase 2 Trial [J]. New England Journal of Medicine, 2023,389(6:514-526.DOI:10.1056/NEJMoa2301972.

[6] Lopez DC, Pajimna JT, Milan MD, et al. 7792 Kev Ua Tau Zoo ntawm Retatrutid rau Kev Txo Nyhav thiab Nws Cov Teebmeem Cardiometabolic Ntawm Cov Neeg Laus: Kev Ntsuam Xyuas Txheej Txheem thiab Meta-Analysis[J]. Phau ntawv Journal of the Endocrine Society, 2024,8(1):163-749.DOI:10.1210/jendso/bvae163.749.

[7] Nicholls S, Pirro V, Lin Y, et al. Triple-hormone receptor agonist Retatrutid ho txhim kho lipoprotein thiab apolipoprotein profiles hauv cov neeg koom nrog rog lossis rog [J]. European Heart Journal, 2024,45(1):666-1501.DOI:10.1093/eurheartj/ehae666.1501.

[8] Katsi V, Koutsopoulos G, Fragoulis C, et al. Retatrutid-A Game Changer in Obesity Pharmacotherapy: Biomolecules [Z]. 2025: 15.DOI: 10.3390 / biom15060796.

Tag nrho cov kab lus thiab cov ntaub ntawv ntawm cov khoom lag luam muab rau ntawm lub vev xaib no tsuas yog rau cov ntaub ntawv tshaj tawm kev tshaj tawm thiab cov hom phiaj kev kawm.  

Cov khoom muab rau hauv lub vev xaib no yog npaj tshwj xeeb rau kev tshawb fawb hauv vitro. Kev tshawb fawb hauv vitro (Latin: * hauv iav *, lub ntsiab lus hauv iav) yog ua los ntawm tib neeg lub cev. Cov khoom no tsis yog tshuaj, tsis tau txais kev pom zoo los ntawm US Food and Drug Administration (FDA), thiab yuav tsum tsis txhob siv los tiv thaiv, kho, lossis kho txhua yam mob, kab mob, lossis mob. Nws raug txwv nruj raws li txoj cai los qhia cov khoom no rau hauv tib neeg lossis tsiaj lub cev hauv txhua daim ntawv.