Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 Ukusetyenziswa kophando kuphela
Semaglutide, ezithengiswa phantsi kwamagama eebhrendiOzempic,WegovykwayeRybelsus,yi iiyeza le-antidiabeticesetyenziselwa unyango lweuhlobo lwe-2 yeswekilekwaye njengokoamayeza achasene nokutyebaixesha elideulawulo lobunzima, iphuhliswe nguNovo Nordiskngo-2012. I-Semaglutide yiI-GLP-1 i-receptor agonist, oku kuthetha ukuba ilinganisa isenzo somntuincretin iglucagon-like peptide-1(GLP-1), ngaloo ndlela isandainsulinukukhutshwa kunye nokwandaiswekile yegaziukulahlwa nokuphuculaulawulo lwe-glycemic.Iziphumo ebezingalindelekanga ziquka isicaphucaphu, ukugabha, urhudo, iintlungu zesisu, nokuqhina. NgoDisemba 2017, inguqulo etofwayo ebizwa ngokuba yi-Ozempic yamkelwa.NgoSeptemba ka-2019, inguqulelo enokuthi ithathwe ngomlomo (i-Rybelsus) yamkelwa, kwaye ngoJuni ka-2021, inaliti yedosi ephezulu ethengiswe phantsi kwegama le-brand Wegovy yokulawula ubunzima bexesha elide kubantu abadala yamkelwa yi-US.Ulawulo lokutya kunye neziyobisi(FDA).NgoJanuwari ka-2023, i-FDA yanika uNovo Nordisk imvume yokuhlaziya ilebhile ukubonisa ukuba i-Rybelsus yomlomo ingasetyenziswa njengonyango.unyango lodidi lokuqalakubantu abadala abanesifo sikashukela sohlobo lwe-2-ithetha kubantu abangazange bathathe elinye iyeza leswekile ngaphambili. Ngo-2020, i-semaglutide yayiyeye-129th eqhelekileyo iyeza elimiselweyo e-United States, linemiyalelo engaphezulu kwe-4 yezigidi. Izithethantonye: I-Rybelsus, i-Ozempic, i-NN9535, i-OG217SC, isetyenziselwa uphando kuphela.
Umsebenzi webhayoloji
| Inkcazo | I-Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), i-glucagon-like peptide 1 (GLP-1) analogue, i-analogueI-GLP-1 i-receptorI-agonist enokubakho kunyango lwe-2 yesifo sikashukela (T2DM). |
| Ekujoliswe kuko | I-GLP-1 i-receptor |
| I-In vitro | I-Semaglutide ikhethwa njengeyona nto ifanelekileyo kanye ngeveki.I-Semaglutide ine-amino acid substitutions ezimbini xa kuthelekiswa ne-GLP-1 yomntu (Aib8, Arg34) kwaye ikhutshwe kwi-lysine 26. Ubudlelwane be-GLP-1R be-semaglutide (0.38 ± 0.06 nM) buhla kathathu xa kuthelekiswa ne-liraglutide, kanti i-albumin affinity iyanda. |
| Kwi-vivo | I-plasma-half-life yi-46.1 h kwiingulube ezincinci ezilandela ulawulo lwe-iv, kwaye i-semaglutide ine-MRT ye-63.6 h emva kwe-sc dosing kwiingulube ezincinci. |
Iprothokholi (ukusuka kwireferensi)
| UPhando lweSeli: | ● Imigca yeeseli:Iiseli zeBHK ● Ugxininiso:0.01 pM - 0.1 μM ● Ixesha lokufukamela:3 h ● Indlela:I-aliquots efriziweyo yeeseli ze-BHK ezivakalisa zombini i-hGLP-1R kunye ne-CRE i-firefly luciferase (i-clone FCW467-12A/KZ10-1) iyanyibilika, ihlanjwe kabini kwi-PBS, kwaye imisiwe kwi-assay buffer.Iiseli zicatshulwe kwiipleyiti zequla ezingama-96 kwiiseli ezingama-5000 / kakuhle kumthamo wama-50 μL.Iikhompawundi eziza kuvavanywa zihlanjululwe kwi-assay buffer kunye ne-50 μL ye-aliquot igqithiselwe kwipleyiti equlethe iiseli ukufikelela kwiimvavanyo zokugqibela ze-1 × 10.−14− 1 × 10−7M. Ipleyiti ifakwe kwi-3 h kwi-5% CO2ku-37 °C.Ipleyiti yayivunyelwe ukuma kwiqondo lobushushu begumbi imizuzu eyi-15 ngaphambi kokuba yongeze i-100 μL ye-steadylite kunye ne-reagent.I-plate ihlanganiswe ukuze ikhusele ekukhanyeni kwaye ishukunyiswe kwindawo yokushisa kwe-30 min.Ipleyiti ifundwa kwisixhobo se-TopCount NXT. |
Ukunyibilika (25°C)
| I-In vitroIqela: | I-DMSO | 3 mg/mL(0.73 mM) |
| I-Ethanol | Ayinyibiliki | |
| Amanzi | Ayinyibiliki |
Ulwazi lweMichiza
| Ubunzima beMolekyuli | 4113.58 | ||
| Ifomula | C187H291N45O59 | ||
| Inombolo yeCAS. | 910463-68-2 | ||
| Ugcino | Iminyaka emi-3 | -20°C | umgubo |
| iminyaka eyi-2 | -80°C | kwisinyibilikisi | |
| Ukuhambisa ngenqanawe | Ukuhanjiswa kweqondo lokushisa kwegumbi(Umgangatho wokuxhalaba simahla: imveliso ilungile kwi-37℃ kangangeveki enye.) | ||
Ulwazi lovavanyo lweklinikhi
| Inombolo ye-NCT | Ukugaya abasebenzi | Amanyathelo okungenelela | Iimeko | Umxhasi/abaSebenzisi | Umhla wokuqala | Izigaba |
| NCT05537233 | Awukaqeshwa | Iziyobisi: Semaglutide|Iziyobisi: Placebo | Type 1 Diabetes|Ukutyeba | IYunivesithi yaseColorado iDenver | NgoJanuwari 1 2023 | Inqanaba lesi-2 |
| NCT04885634 | Awukaqeshwa | Iziyobisi: Imveliso ye-Semaglutide Injectable|Iziyobisi: I-Placebo | I-Atrial Fibrillation | Ubunzima kunye nokutyeba kakhulu | Axel Brandes|Isibhedlele saseHerlev kunye neGentofte|Isibhedlele saseHillerod eDenmark|Isibhedlele saseSvendborg|Isibhedlele saseMzantsi Ntshona Jutland|Isibhedlele saseYunivesithi yaseOdense | Okthobha 2022 | Inqanaba lesi-3 |
| NCT05579977 | Ukugaya abasebenzi | Ichiza: PF-07081532|Ezinye: I-Placebo|Iziyobisi: Rybelsus | Seswekile Mellitus|Ukutyeba | Pfizer | Ngo-Oktobha 27 2022 | Inqanaba lesi-2 |
| NCT05254314 | Ukugaya abasebenzi | Iziyobisi: I-Semaglutide Pen Injector 2.4mg ngeveki | Okunye: I-Placebo | Umbefu | IZiko lezoNyango leDyunivesithi yaseVanderbilt|Iziko leSizwe leZifo zokwaliwa kunye neZifo ezosulelayo (NIAID) | NgoSeptemba 7 2022 | Inqanaba lesi-2 |
| NCT05478252 | Ukugaya abasebenzi | Iziyobisi: Semaglutide J | Iziyobisi: Semaglutide B | Uhlobo lwesi-2 lwesifo seswekile | Novo Nordisk A/S | Nge-3 ka-Agasti 2022 | Inqanaba lesi-3 |
(idatha evelahttps://clinicaltrials.gov, ihlaziywe ngo-2022-11-29)
