Tirzepatide (GLP-2) 20 mg

▎ Tirzepatide Structure

Source: PubChem

Ib ntus: Tyr-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{Aib}-Leu-Asp-Lys-Ile-Ala-Gln-{diacid-C20-gamm a-Glu-(AEEA)2-Lys}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2 Molecular Formula: C 225H 348N 48O68 Molecular Luj: 4813 g / mol CAS Nr .: 2023788-19-2 PubChem CID: 163285897 Synonyms: Zepbound; Mounjaro

▎ Kev Tshawb Fawb Tirzepatide

Kev tshawb fawb keeb kwm ntawm Tirzepatide yog dab tsi?

Kev tshawb fawb keeb kwm yav dhau los ntawm Tirzepatide feem ntau yog los ntawm kev tshawb nrhiav cov tshuaj kho cov metabolism thiab kev thov rau cov tshuaj tswj qhov hnyav. Cov tshuaj kho cov tshuaj metabolism hauv ib txwm muaj kev txwv, thaum GLP-1 receptor agonists pom tau tias muaj txiaj ntsig zoo hauv kev txhim kho cov ntshav qabzib, ua rau cov kws tshawb fawb los tsim cov tshuaj zoo dua qub ntawm tib chav kawm. Raws li GIP / GLP-1 dual receptor agonist, Tirzepatide tuaj yeem tswj cov ntshav qabzib zoo dua. Kev nce thoob ntiaj teb ntawm cov neeg rog rog thiab rog rog tau ua kom tswj tau qhov hnyav uas xav tau kev kho mob sai. GLP-1 receptor agonists muaj qhov hnyav-txo cov teebmeem, ua rau lawv lub hom phiaj rau kev poob phaus. Tirzepatide tau txais kev pom zoo vim nws qhov txiaj ntsig zoo-poob qhov tshwm sim.

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

Dual receptor agonist ua haujlwm: 

Tirzepatide yog dual glucagon-zoo li peptide-1 (GLP-1) thiab qabzib-dependent insulinotropic polypeptide (GIP) receptor agonist [1,2] (Wong E, 2023; Kumar D, 2022). GLP-1 thiab GIP yog ob qho tib si cov tshuaj hormones incretin uas tsim hauv txoj hnyuv, ua lub luag haujlwm tseem ceeb hauv kev tswj cov piam thaj hauv tsev. Tirzepatide ua rau muaj kev sib koom ua ke los ntawm ib txhij ua kom GLP-1 thiab GIP receptors, yog li tswj cov ntshav qabzib.

Kev tswj hwm ntawm insulin thiab glucagon secretion: 

Nws ua rau cov tshuaj insulin ntau ntxiv thiab tso tawm thaum txo glucagon tso tawm hauv cov piam thaj-dependant. Thaum cov ntshav qabzib nce siab, Tirzepatide txhawb nqa pancreatic β-hlwb kom tso cov tshuaj insulin, txhawb nqa cov piam thaj thiab siv, yog li txo cov ntshav qabzib; Tib lub sijhawm, nws inhibits pancreatic α-hlwb los ntawm kev zais glucagon, txo qis cov piam thaj hauv siab, txo qis cov ntshav qabzib ntxiv, thiab tswj kev yoo mov thiab cov ntshav qabzib tom qab ^[1,3].

Lwm yam mechanisms ntawm kev ua: 

Tirzepatide kuj txhawb kev satiety, uas tej zaum yuav cuam tshuam rau kev ua kom GLP-1 receptors, ua haujlwm ntawm lub hauv nruab nrab lub paj hlwb, thiab cuam tshuam cov chaw tswj kev noj qab haus huv, ua rau cov neeg mob txo cov zaub mov noj thiab yog li pab kom poob phaus. Nws kuj tseem ncua lub plab khoob, ncua sij hawm cov zaub mov tseem nyob hauv plab thiab maj mam nkag mus rau hauv txoj hnyuv me, yog li tiv thaiv kev nce siab hauv cov ntshav qabzib ntau ^[1].

Daim duab 1 Mechanism of action of T irzepatide ^[6].

Dab tsi yog daim ntawv thov ntawm T irzepatide?

Kev kho mob ntawm hom 2 metabolism: 

Tirzepatide tau pom zoo rau kev kho mob ntawm cov neeg laus cov neeg mob uas muaj hom 2 metabolism raws li kev noj haus thiab kev tawm dag zog. Qhov kev sim SURPASS tau pom tias Tirzepatide txo qis hemoglobin A1c (HbA1c) ntau ntau, nrog kev txo qis ntawm -1.87% mus rau -2.59% (-20 txog -28 mmol / mol). Nws kuj tseem ua kom pom kev tswj glycemic zoo dua piv rau qee yam GLP-1 receptor agonists, xws li semaglutide 1 mg hauv SUPRASS-2 mus sib hais. Tsis tas li ntawd, nws tuaj yeem txo qhov hnyav ntawm lub cev, nrog rau qhov hnyav li ntawm -6.2 txog -12.9 kg hauv kev tshawb fawb soj ntsuam, tshwj xeeb tshaj yog rau cov neeg mob uas muaj hom 2 metabolism uas feem ntau muaj teeb meem rog lossis rog ^[1,4].

Kev kho mob rog: 

Txij li thaum Tirzepatide txhawb kev satiety, txo cov zaub mov kom tsawg, thiab txhawb kev poob phaus, nws muaj peev xwm kho tus nqi rau cov neeg mob rog. Cov kev tshawb fawb pom tau tias nws tuaj yeem txo qhov hnyav ntau dua 20%, txhim kho cov neeg mob cov txheej txheem metabolic, thiab ua txoj kev kho tshiab rau kev rog rog, pab cov neeg mob rog rog thiab txo qhov kev pheej hmoo ntawm ntau yam kab mob cuam tshuam nrog kev rog ^[1,2].

Txo kev pheej hmoo ntawm kab mob plawv: 

Cov neeg mob uas muaj hom 2 metabolism feem ntau ntsib kev pheej hmoo ntawm cov kab mob plawv. Ntxiv nrog rau kev txo qis ntshav qab zib thiab qhov hnyav, Tirzepatide muaj txiaj ntsig zoo rau cov kab mob plawv, suav nrog txo cov ntshav siab, txo qis cov rog hauv cov hlab ntsha, thiab txo qis cov ntshav triglyceride, yog li pab txo qis kev pheej hmoo ntawm cov kab mob plawv thiab txhim kho cov neeg mob cov hlab plawv ^[4].

Muaj peev xwm kho mob rau cov uas tsis yog-alcoholic steatohepatitis (NASH): 

Tirzepatide muaj peev xwm kho tau los ntawm NASH. Los ntawm kev txhim kho insulin rhiab heev thiab tswj cov piam thaj thiab lipid metabolism, nws tuaj yeem txo qis hepatic steatosis thiab o, muab cov lus qhia tshiab rau kev kho NASH ^[5].

Xaus

Raws li GIP / GLP-1 dual receptor agonist, Tirzepatide tau pom tias muaj txiaj ntsig zoo hauv kev kho cov metabolism thiab cov teeb meem metabolic. Los ntawm kev tswj hwm cov tshuaj insulin thiab glucagon secretion, ncua lub plab zom mov, thiab ua kom muaj kev txaus siab, nws txo qis hemoglobin A1c qib thiab txo cov neeg mob hnyav. Tsis tas li ntawd, cov tshuaj pab txhim kho cov kab mob plawv xws li qib lipid thiab ntshav siab thiab ua kom pom qhov ua tau zoo ntawm cov tsis muaj dej cawv steatohepatitis.

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

De Block C yog txuam nrog University of Antwerp thiab nws cov koom haum cuam tshuam hauv Belgium, suav nrog Inflamed Ctr Excellence, University Hospital Antwerp (UZA thiab Univ Hosp Antwerp), thiab Infla Med Ctr Excellence. Nws txoj kev tshawb fawb nthuav dav ntau yam kev qhuab qhia, xws li Endocrinology & Ntshav Qab Zib, qhov uas nws tsom mus rau cov tshuaj hormones thiab cov kab mob metabolic; Gastroenterology & Hepatology, tshawb nrhiav digestive thiab daim siab kab mob; General & Internal Medicine, hais txog kev kuaj mob thiab kev tswj xyuas cov kab mob hauv lub cev; Khoom noj khoom haus & Dietetics, tshawb xyuas cov khoom noj khoom haus thiab nws cov teebmeem kev noj qab haus huv; thiab Urology & Nephrology, kawm txog pathology thiab kev kho mob ntawm cov kab mob urinary thiab raum. Nws yog ib tug kws tshawb fawb uas muaj txiaj ntsig zoo rau ntau yam kev kho mob. De Block C tau teev nyob rau hauv qhov kev siv ntawm cov ntaub ntawv pov thawj [4].

▎ Cov Lus Qhia Tseem Ceeb

[1] Wong E, Cope R, Dima L, et al. Tirzepatide: Dual Glucose-dependent Insulinotropic Polypeptide thiab Glucagon-zoo li Peptide-1 Agonist rau Kev Tswj Xyuas Hom 2 Ntshav Qab Zib Mellitus [J]. American Journal of Therapeutics, 2023,30(1):e26-e35.DOI:10.1097/MJT.0000000000001588.

[2] Kumar D, Harshidha D, Mousigan M, et al. Kev Qhia Txog Tirzepatide, Kev Kho Mob Ob Lub Hom Phiaj rau Ntshav Qab Zib thiab Kev rog [J]. International Journal of Innovative Research & Growth, 2022,7:983.DOI:10.5281/zenodo.7420605.

[3] Sweta, Gupta S, Bansal S, et al. Tirzepatide ib qho tshiab los tiv thaiv ntshav qab zib molecule nthuav tawm dual kev ua haujlwm [J]. Discover Public Health, 2024,21(1):75.DOI:10.1186/s12982-024-00200-2.

[4] De Block C, Bailey C, Wysham C, et al. Tirzepatide rau kev kho mob ntawm cov neeg laus nrog hom 2 metabolism: Ib qho kev pom endocrine [J]. Diabetes Obesity & Diabetes, 2023,25(1):3-17.DOI:10.1111/dom.14831.

[5] Sood A, Kaur P, Syed O, et al. Revolutionizing metabolism hauv kev saib xyuas: nthuav tawm Tirzepatide lub peev xwm hauv kev tswj glycemic thiab dhau [J]. Kws tshuaj ntsuam xyuas ntawm Clinical Pharmacology, 2024,17(3):235-246.DOI:10.1080/17512433.2024.2310070.

[6] Grover-Páez F, Gomez A, Suárez A, et al. Los ntawm txoj hauv kev glycocentric hauv tus neeg mob uas muaj hom 2 metabolism hauv mellitus mus rau kev kho mob ntau yam hauv nruab nrog cev thiab kev txo qis hauv cov txiaj ntsig neuro-nephro-cardiovascular.[M]//2023.DOI: 10.5772/intechopen.1002363.

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.