TirzepatideCAS 2023788-19-2 yog ib qho tshiab dual receptor agonist ntawm glucagon zoo li peptide -1 receptor (GLP-1) thiab qabzib nyob ntawm insulinotropic peptide (GIP, tseem hu ua gastric inhibitory peptide), muab tshuaj ib zaug ib lim tiam . GLP-1 thiab GIP ob leeg koom nrog enterotropin, uas yog peptide secreted los ntawm tib neeg plab hnyuv mucosa. Cov qub tuaj yeem khi rau cov receptors ntawm pancreatic islet hlwb thiab txhawb kev tsim cov tshuaj insulin, yog li tsim cov teebmeem hypoglycemic. Nws tuaj yeem ncua kev ua pa ntawm plab thiab inhibit qhov qab los noj mov, yog li tswj qhov hnyav; Cov tom kawg muaj cov haujlwm xws li inhibiting gastric acid thiab pepsin secretion, stimulating insulin tso tawm, inhibiting gastric peristalsis thiab tshem tawm, thiab tuaj yeem ntxiv qhov kev txiav txim ntawm GLP-1 receptor agonists. Tirzepatide koom ua ke ob qho kev txhawb nqa insulin rau hauv ib qho molecule, sawv cev rau cov chav kawm tshiab ntawm cov tshuaj rau kev kho mob ntshav qab zib hom 2.
Cov molecule no muaj peptide caj qaum ntawm 39 amino acids thiab ib sab saw ntawm cov residue Lys20. Tawm ntawm 39 amino acids, 37 yog ib txwm tam sim no (los yog encoded), thiab ob yog tsis muaj nyob, nrog tsis coding amino isobutyric acid residues nyob rau ntawm txoj hauj lwm 2 thiab 13.
TirzepatideCAS 2023788-19-2 muaj ib ntu zoo sib xws rau semaglutide, thiab lys sab saw nyob rau hauv ib ntu yog hloov nrog PEG, uas yog ib pab pawg neeg ua haujlwm ntawm peptides thiab tuaj yeem ua kom cov dej solubility ntawm qhov sib lawv liag. Lub ntsiab physiological muaj nuj nqi ntawm Tirzepatide yog qabzib nyob rau hauv insulin kev noj haus polypeptide (GIP) thiab glucagon zoo li peptide-1 (GLP-1) receptor dual agonist, uas yog tsim los rau kev kho mob ntawm hom 2 mob ntshav qab zib thiab tau nkag mus. theem kho mob.
Txoj kev tshawb fawb SURPASS yog ib qho kev sim loj randomized tswj kev soj ntsuam txhawm rau ntsuas qhov ua tau zoo thiab kev nyab xeeb ntawm tilporide hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus (T2DM). Ntawm lawv, cov txiaj ntsig ntawm SURPASS-2 [1] yog qhov kev txhawb siab tshaj plaws thaum piv rau lub taub hau nrog smeglutide. Txoj kev tshawb no piv cov teebmeem hypoglycemic ntawm tirposide 5mg (n=470), 10mg (n=469), thiab 15mg (n=469) nrog smeglutide 1mg (n{ {12}}). Cov txiaj ntsig tau pom tias piv rau theem pib HbA1c (8.3%), telposide txo cov neeg kawm 'HbA1c los ntawm qhov nruab nrab ntawm 2.0%, 2.2%, thiab 2.3%, thaum smeglutide txo qis los ntawm qhov nruab nrab ntawm 1.9%; Nyob rau hauv cov nqe lus ntawm kev poob phaus, piv rau lub hauv paus qhov hnyav hauv Chemicalbook (207 phaus), telposide ua rau qhov hnyav poob ntawm 17 phaus, 21 phaus, thiab 25 phaus rau cov neeg koom, thaum smeglutide yog 13 phaus. Qhov kev sim no tau pom tias telposide nthuav tawm cov txiaj ntsig zoo tshaj plaws ntawm hypoglycemic thiab lub peev xwm poob phaus piv rau smeglutide. Lwm qhov kev tshawb fawb loj tau nrhiav 2539 cov neeg laus uas muaj tsawg kawg ib qho teeb meem rog rog (tsis suav nrog ntshav qab zib), lub cev qhov hnyav (BMI) Ntau dua lossis sib npaug li 30kg / m2 lossis Ntau dua lossis sib npaug li 27kg / m2. Txhua tus neeg koom nrog tau muab faib ua qhov sib npaug sib npaug rau hauv telposide 5mg, 10mg, 15mg thiab placebo pawg. Cov txiaj ntsig tau pom tias ntawm 72 lub lis piam, qhov hnyav ntawm txhua pab pawg tau txo qis los ntawm 16.1kg, 22.2kg, 23.6kg, thiab 2.4kg, feem. Qhov kev poob phaus ntawm tirposide yog piv rau qhov poob phaus phais.
Telpolotide muaj cov kab ke zoo sib xws rau semaglutide, nrog rau lys sab chains hauv cov kab ke hloov nrog PEG, uas yog cov pab pawg ua haujlwm ntawm peptides thiab tuaj yeem ua kom cov dej solubility ntawm qhov sib lawv liag. Tilpodide, uas feem ntau yog siv los tsim cov tshuaj chemobooks, yog ob tus agonist ntawm cov piam thaj nyob ntawm insulin noj zaub mov polypeptide (GIP) thiab glucagon zoo li peptide -1 (GLP-1) receptor. Nws yog tsim los rau kev kho mob ntshav qab zib hom 2 thiab tau nkag mus rau theem kho mob.
TirzepatideCAS 2023788-19-2 yog ib tug dual agonist ntawm qabzib nyob rau hauv insulinotropic peptide (GIP) receptors thiab glucagon zoo li peptide-1 (GLP-1) receptors, muaj peev xwm ua kom qab los noj mov, calorie ntau ntau, thiab kev ua haujlwm hauv metabolic.
Piv txwv li, peb lub cev zoo li lub Hoobkas raug, thiab GIP thiab GLP -1 yog ob tus neeg ua haujlwm muaj peev xwm hauv lub Hoobkas no.
GIP zoo li tus kws tshaj lij tswj cov suab thaj ntse, nws pab tswj cov ntshav qab zib thaum nws siab thiab tsis txhob cia nws nce siab; Thaum cov ntshav qab zib tsis zoo los yog qis, nws yuav pab ua kom cov ntshav qab zib nce ntxiv thiab tiv thaiv peb kom tsis txhob muaj ntshav qab zib.
Kev tshawb fawb tau pom tias telopoptide ua kom ruaj khov thiab kho qhov tseem ceeb txo qis hauv glycated hemoglobin thiab lub cev hnyav, nrog kev txo qis ntau dua li txhua cov tshuaj tswj hwm - placebo, 1mg ntawm sitagliptin txhaj, titrated insulin diglutide, thiab titrated insulin glargine.
Yolanda
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