I-Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 Okokusetshenziswa kocwaningo kuphela
I-Semaglutide, ethengiswa ngaphansi kwamagama ebhrendiOzempic,WegovyfuthiI-Rybelsus,iyiumuthi we-antidiabeticesetshenziselwa ukwelaphauhlobo 2 sikashukelafuthi njengobaimithi yokulwa nokukhuluphala ngokweqileokwesikhathi esideukuphathwa kwesisindo, ithuthukiswe nguI-Novo Nordiskngo-2012. Semaglutide is aI-GLP-1 receptor agonist, okusho ukuthi ilingisa isenzo somuntui-incretin i-glucagon-like peptide-1(GLP-1), ngaleyo ndlela andai-insulinukukhishwa nokwandaushukela egaziniukulahlwa kanye nokwenza ngconoukulawulwa kwe-glycemic.Imiphumela emibi ihlanganisa isicanucanu, ukuhlanza, isifo sohudo, ubuhlungu besisu, nokuqunjelwa. NgoZibandlela wezi-2017, inguqulo yomjovo ebizwa ngokuthi i-Ozempic yavunywa.NgoSepthemba 2019, inguqulo engathathwa ngomlomo (i-Rybelsus) yavunywa, kwathi ngoJuni 2021, umjovo wethamo eliphezulu odayiswe ngaphansi kwegama lomkhiqizo i-Wegovy wokulawula isisindo eside kubantu abadala wagunyazwa yi-US.Ukuphatha Ukudla Nezidakamizwa(FDA).NgoJanuwari ka-2023, i-FDA yanikeza i-Novo Nordisk imvume yokubuyekeza ilebula ukuze ibonise ukuthi i-Rybelsus yomlomo ingasetshenziswa njenge-oral.ukwelashwa komugqa wokuqalakubantu abadala abanesifo sikashukela sohlobo 2-okusho kubantu abangakaze baphuze omunye umuthi wesifo sikashukela. Ngo-2020, i-semaglutide yayiwumuthi we-129 ovame ukunikezwa e-United States, onemiyalelo engaphezu kwezigidi ezi-4. Omqondofana: Rybelsus, Ozempic, NN9535, OG217SC, Okokusetshenziswa kocwaningo kuphela.
Umsebenzi Webhayoloji
| Incazelo | I-Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), i-analogue esebenza isikhathi eside efana ne-glucagon-like peptide 1 (GLP-1), iyi-analogue.I-GLP-1 receptorI-agonist enamandla okwelapha uhlobo 2 lwesifo sikashukela i-mellitus (T2DM). |
| Okuhlosiwe | I-GLP-1 receptor |
| In vitro | I-Semaglutide ikhethwa njengekhandidethi elifanele kanye ngesonto.I-Semaglutide ine-amino acid eshintshwayo emibili uma kuqhathaniswa ne-GLP-1 yomuntu (Aib8, Arg34) futhi ikhishwe ku-lysine 26. Ukuhlangana kwe-GLP-1R kwe-semaglutide (0.38 ± 0.06 nM) kwehle ngokuphindwe kathathu uma kuqhathaniswa ne-liraglutide, kanti i-albin affinity iyanda. |
| Nge-vivo | I-plasma half-life yi-46.1 h ezingulubeni ezincane ezilandela ukuphathwa kwe-iv, futhi i-semaglutide ine-MRT ye-63.6 h ngemva kokukhipha umthamo ezingulubeni ezincane. |
Iphrothokholi (kusuka kunkomba)
| Ucwaningo Lweseli: | ● Olayini beselula:Amaseli e-BHK ● Okugxilwe kukho:0.01 pM - 0.1 μM ● Isikhathi Sokufukamela:3 h ● Indlela:Ama-aliquots aqandisiwe amaseli e-BHK aveza kokubili i-hGLP-1R ne-CRE firefly luciferase (i-clone FCW467-12A/KZ10-1) ayancibilika, awashwe kabili ku-PBS, futhi amiswe ku-assay buffer.Amaseli ahlukaniswa abe amapuleti anemithombo engu-96 kumaseli angu-5000/emthonjeni ngevolumu engu-50 μL.Izithako ezizohlolwa zihlanjululwe ku-assay buffer futhi i-aliquot engu-50 μL idluliselwe epuletini eliqukethe amaseli ukuze kufinyelelwe ekugxilweni kokuhlolwa kokugcina okungu-1 × 10.−14− 1 × 10−7M. Ipuleti lifakwa amahora ama-3 ku-5% CO2ngo-37°C.Ipuleti livunyelwe ukuma endaweni yokushisa yegumbi imizuzu engu-15 ngaphambi kokwengeza u-100 μL we-steadylite plus reagent.Ipuleti limbozwe ukuze livikeleke ekukhanyeni futhi linyakaziswa ekamelweni lokushisa imizuzu engu-30.Ipuleti lifundwa ensimbini ye-TopCount NXT. |
Ukunyibilika (25°C)
| In vitroIqoqo: | I-DMSO | 3 mg/mL(0.73 mM) |
| I-Ethanol | Ayincibiliki | |
| Amanzi | Ayincibiliki |
Ulwazi Lwekhemikhali
| Isisindo samangqamuzana | 4113.58 | ||
| Ifomula | C187H291N45O59 | ||
| Inombolo ye-CAS. | 910463-68-2 | ||
| Isitoreji | 3 iminyaka | -20°C | impushana |
| iminyaka engu-2 | -80°C | ku-solvent | |
| Ukuthumela ngomkhumbi | Ukuthunyelwa kwezinga lokushisa kwegumbi(Ikhwalithi ayinandaba: umkhiqizo muhle ku-37℃ okungenani iviki elingu-1.) | ||
Ulwazi Lwesivivinyo Somtholampilo
| Inombolo ye-NCT | Ukuqasha | Ukungenelela | Izimo | Umxhasi/Abahlanganyeli | Usuku okuqalwa ngalo | Izigaba |
| I-NCT05537233 | Ayikaqashi | Umuthi: Semaglutide|Izidakamizwa: I-Placebo | Type 1 Diabetes|Ukukhuluphala | Inyuvesi yaseColorado Denver|Juvenile Diabetes Research Foundation | Januwari 1 2023 | Isigaba 2 |
| I-NCT04885634 | Ayikaqashi | Umuthi: Umkhiqizo Ojovayo we-Semaglutide|Isidakamizwa: I-Placebo | I-Atrial Fibrillation|Ukukhuluphala Nokukhuluphala | Axel Brandes|Herlev and Gentofte Hospital|Hillerod Hospital Denmark|Svendborg Hospital|Isibhedlela saseNingizimu Ntshonalanga Jutland|Odense University Hospital | Okthoba 2022 | Isigaba sesi-3 |
| NCT05579977 | Ukuqasha | Isidakamizwa: PF-07081532|Okunye: I-Placebo|Isidakamizwa: I-Rybelsus | Isifo sikashukela i-mellitus|Ukukhuluphala | I-Pfizer | Okthoba 27 2022 | Isigaba 2 |
| I-NCT05254314 | Ukuqasha | Umuthi: I-Semaglutide Pen Injector 2.4mg masonto onke|Okunye: I-placebo | Isifuba somoya | I-Vanderbilt University Medical Center|Isikhungo Sikazwelonke Sokungezwani Nomzimba Nezifo Ezithathelwanayo (NIAID) | Septhemba 7 2022 | Isigaba 2 |
| I-NCT05478252 | Ukuqasha | Umuthi: Semaglutide J|Izidakamizwa: Semaglutide B | Isifo sikashukela i-mellitus Type 2 | I-Novo Nordisk A/S | Agasti 3 2022 | Isigaba sesi-3 |
(idatha evela kuhttps://clinicaltrials.gov, ibuyekezwe ngo-2022-11-29)
