Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 Bakeng sa tšebeliso ea lipatlisiso feela
Semaglutide, e rekisoang tlas'a mabitso a marang-rangOzempic,WegovyleRybelsus,ke amoriana oa antidiabeticse sebedisoang bakeng sa kalafo yamofuta oa 2 lefu la tsoekerele joalo kamoriana o thibelang botenyabakeng sa nako e teleletaolo ya boima, e ntlafalitsoeng keNovo Nordiskka 2012. Semaglutide ke aGLP-1 receptor agonist, ho bolelang hore e etsisa ketso ea mothoincretin glucagon-joaloka peptide-1(GLP-1), ka hona e eketsehainsulinho ruruha le ho eketsehatsoekere e malingho lahla le ho ntlafatsataolo ea glycemic.Litla-morao li kenyelletsa ho nyekeloa ke pelo, ho hlatsa, letšollo, bohloko ba ka mpeng le ho pipitlela. Ka December 2017, mofuta oa ente e bitsoang Ozempic o ile oa amoheloa.Ka Loetse 2019, mofuta o ka nkuoang ka molomo (Rybelsus) o ile oa amoheloa, mme ka Phuptjane 2021, ente ea tekanyetso e phahameng e rekisoang tlasa lebitso la Wegovy bakeng sa taolo ea boima ba nako e telele ho batho ba baholo e ile ea amoheloa ke US.Tsamaiso ea Lijo le Lithethefatsi(FDA).Ka Pherekhong 2023, FDA e ile ea fa Novo Nordisk tumello ea ho nchafatsa leibole ho bontša hore Rybelsus ea molomo e ka sebelisoa e lephekolo ea pelebakeng sa batho ba baholo ba nang le lefu la tsoekere la mofuta oa 2-e bolelang ho batho ba e-s'o noe meriana e 'ngoe ea lefu la tsoekere. Ka 2020, semaglutide e ne e le meriana ea 129 e sebelisoang haholo United States, e nang le litaelo tse fetang limilione tse 4. Litlhaloso tse tšoanang: Rybelsus, Ozempic, NN9535, OG217SC, Bakeng sa tšebeliso ea lipatlisiso feela.
Mosebetsi oa Likokoana-hloko
| Tlhaloso | Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), analogue ea nako e telele e kang glucagon-joaloka peptide 1 (GLP-1),GLP-1 receptoragonist e nang le monyetla oa ho phekola lefu la tsoekere la mofuta oa 2 mellitus (T2DM). |
| Lipheo | GLP-1 receptor |
| In vitro | Semaglutide e khethoa e le mokhethoa ea nepahetseng hang ka beke.Semaglutide e na le li-substitutes tse peli tsa amino acid ha li bapisoa le GLP-1 ea motho (Aib8, Arg34) 'me e nkiloeng ho lysine 26. The GLP-1R affinity ea semaglutide (0.38 ± 0.06 nM) e fokotsehile ka makhetlo a mararo ha e bapisoa le liraglutide, athe albumin affinity ea eketseha. |
| Ka vivo | Bophelo ba halofo ea plasma ke 46.1 h ho li-mini-pigs tse latelang tsamaiso ea iv, 'me semaglutide e na le MRT ea 63.6 h ka mor'a sc dosing ho likolobe tse nyenyane. |
Protocol (ho tloha ho litšupiso)
| Lipatlisiso ka Mehala: | ● Mela ea lisele:Lisele tsa BHK ● Maikutlo:0.01 pM - 0.1 μM ● Nako ea ho Incubation:3 h ● Mokhoa:Li-aliquots tse hatselitsoeng tsa lisele tsa BHK tse hlalosang bobeli ba hGLP-1R le CRE firefly luciferase (clone FCW467-12A/KZ10-1) lia qhibiliha, li hlatsuoa habeli ho PBS, 'me li emisoa ka har'a assay buffer.Lisele li kenngoa ka har'a lipoleiti tsa liliba tse 96 liseleng tse 5000 / seliba ka bongata ba 50 μL.Metsoako e lokelang ho lekoa e hlapollotsoe ka har'a assay buffer mme 50 μL aliquot e fetisetsoa poleiting e nang le lisele ho fihlela likhakanyo tsa ho qetela tsa 1 × 10.−14− 1 × 10−7M. Letlapa le kenngoa ka 3 h ho 5% CO2ka mocheso oa 37 ° C.Letlapa le ne le lumelloa ho ema mocheso oa kamore bakeng sa metsotso e 15 pele ho eketsa 100 μL ea steadylite hammoho le reagent.Letlapa le koahetsoe ho e sireletsa khanyeng le ho sisinyeha mocheso oa kamore bakeng sa 30 min.Letlapa le baloa ka sesebelisoa sa TopCount NXT. |
Sollubility (25°C)
| In vitroSehlopha: | DMSO | 3 mg/mL(0.73 mM) |
| Ethanol | E sa qhibidihang | |
| Metsi | E sa qhibidihang |
Boitsebiso ba Lik'hemik'hale
| Boima ba Molek'hule | 4113.58 | ||
| Foromo | C187H291N45O59 | ||
| Nomoro ea CAS. | 910463-68-2 | ||
| Polokelo | 3 lilemo | -20°C | phofo |
| lilemo tse 2 | -80°C | ka solvent | |
| Ho tsamaisa ka sekepe | Ho romelloa ha mocheso oa kamore(Ha ho na matšoenyeho a boleng: sehlahisoa se hantle ho 37 ℃ bonyane beke e le 1.) | ||
Tlhahisoleseding ea Teko ea Tleliniki
| Nomoro ea NCT | Ho hira batho | Ho kenella | Maemo | Motšehetsi/Basebelisi | Letsatsi la qalo | Mekhahlelo |
| NCT05537233 | Ha e so thaothe | Lithethefatsi: Semaglutide|Lithethefatsi: Placebo | Mofuta oa 1 oa Lefu la tsoekere | Botenya | Univesithi ea Colorado Denver | Motheo oa Patlisiso ea Bacha ba lefu la tsoekere | La 1 Pherekhong 2023 | Mokhahlelo oa 2 |
| NCT04885634 | Ha e so thaothe | Lithethefatsi: Semaglutide Injectable Product|Lithethefatsi: Placebo | Atrial Fibrillation|Botenya bo feteletseng le Botenya | Axel Brandes|Sepetlele sa Herlev le Gentofte|Sepetlele sa Hillerod Denmark|Sepetlele sa Svendborg|Sepetlele sa South West Jutland|Sepetlele sa Univesithi ea Odense | Mphalane 2022 | Mokhahlelo oa 3 |
| NCT05579977 | Ho thaotha | Lithethefatsi: PF-07081532|E 'ngoe: Placebo|Lithethefatsi: Rybelsus | Lefu la tsoekere mellitus | Botenya | Pfizer | La 27 Mphalane 2022 | Mokhahlelo oa 2 |
| NCT05254314 | Ho thaotha | Lithethefatsi: Semaglutide Pen Injector 2.4mg beke le beke | Tse ling: Placebo | Asma | Setsi sa Bongaka sa Univesithi ea Vanderbilt|Setsi sa Naha sa Allergy le Mafu a tšoaetsanoang (NIAID) | La 7 Loetse 2022 | Mokhahlelo oa 2 |
| NCT05478252 | Ho thaotha | Lithethefatsi: Semaglutide J | Lithethefatsi: Semaglutide B | Mofuta oa 2 oa lefu la tsoekere mellitus | Novo Nordisk A/S | La 3 Phato 2022 | Mokhahlelo oa 3 |
(data ho tsoa hohttps://clinicaltrials.gov, e ntlafalitsoeng ka 2022-11-29)
