Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 Kubushakashatsi bukoreshwa gusa
Semaglutide, kugurishwa munsi yizinaOzempic,WegovynaRybelsus, ni animiti igabanya ubukanaikoreshwa mu kuvuraubwoko bwa diyabetenaimiti irwanya umubyibuho ukabijeigihe kirekiregucunga ibiro, byakozwe naNovo Nordiskmuri 2012. Semaglutide ni aGLP-1 reseptor agonist, bivuze ko yigana ibikorwa byumuntuincretin glucagon-isa na peptide-1(GLP-1), bityo kwiyongerainsulinegusohora no kwiyongeraisukari mu marasoguta no gutera imbereglycemic.Ingaruka mbi zirimo isesemi, kuruka, impiswi, kubabara mu nda, no kuribwa mu nda. Ukuboza 2017, verisiyo yatewe inshinge yitwa Ozempic yaremewe.Muri Nzeri 2019, hemejwe verisiyo ishobora gufatwa ku munwa (Rybelsus), maze muri Kamena 2021, inshinge nyinshi yagurishijwe ku izina rya Wegovy kugira ngo imicungire y'ibiro birebire ku bantu bakuru yemejwe na AmerikaUbuyobozi bushinzwe ibiryo n'ibiyobyabwenge(FDA).Muri Mutarama 2023, FDA yahaye Novo Nordisk uruhushya rwo kuvugurura ikirango kugirango yerekane ko Rybelsus yo mu kanwa ishobora gukoreshwa nka aubuvuzi bwa mberekubantu bakuze barwaye diyabete yo mu bwoko bwa 2-bivuze mubantu batigeze bafata undi muti wa diyabete. Muri 2020, semaglutide yari imiti ya 129 ikunze kwandikwa muri Amerika, hamwe na miliyoni zirenga 4 zandikiwe. Synonyme: Rybelsus, Ozempic, NN9535, OG217SC, Kubushakashatsi bukoreshwa gusa.
Igikorwa cyibinyabuzima
| Ibisobanuro | Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), glucagon ikora nka peptide 1 (GLP-1) analogue, ni aGLP-1agonist hamwe nubushobozi bwo kuvura diyabete yo mu bwoko bwa 2 (T2DM). |
| Intego | GLP-1 |
| Muri vitro | Semaglutide yatoranijwe nkibyiza rimwe mukandida buri cyumweru.Semaglutide ifite insimburangingo ebyiri za aside amine ugereranije na GLP-1 yumuntu (Aib8, Arg34) kandi ikomoka kuri lysine 26. GLP-1R ifitanye isano na semaglutide (0.38 ± 0.06 nM) yagabanutse inshuro eshatu ugereranije na liraglutide, naho alubumu ya albumin. ni Byiyongereye. |
| Muri vivo | Plasma igice cyubuzima ni 46.1 h muri mini-ingurube ikurikira ubuyobozi bwa iv, naho semaglutide ifite MRT ya 63,6 h nyuma yo kwipimisha ingurube. |
Porotokole (uhereye ku gitabo)
| Ubushakashatsi bwakagari: | Line Imirongo y'utugari:BHK selile Kwibanda:0.01 pM - 0.1 μM Time Igihe cyo Kwiyongera:3 h ● Uburyo:Alikoti ikonje ya selile ya BHK yerekana hGLP-1R na CRE firefly luciferase (clone FCW467-12A / KZ10-1) irashwanyaguzwa, yozwa kabiri muri PBS, ihagarikwa muri buffer.Ingirabuzimafatizo zashyizwe mu isahani 96-nziza kuri selile 5000 / neza mubunini bwa 50 μL.Ibicuruzwa bigomba gupimwa bivangwa muri buffer hamwe na 50 μL aliquot yimuriwe ku isahani irimo selile kugirango igere kumurongo wa 1 × 10-14- 1 × 10-7M. Isahani yashizwemo 3h kuri 5% CO2kuri 37 ° C.Isahani yemerewe guhagarara ku bushyuhe bwicyumba kuminota 15 mbere yo kongeramo 100 μL ya stabilite yongeyeho reagent.Isahani irapfundikijwe kugirango irinde urumuri kandi ihinda umushyitsi mucyumba cya min 30.Isahani isomwa mubikoresho bya TopCount NXT. |
Gukemura (25 ° C)
| Muri vitroIcyiciro: | DMSO | 3 mg / mL(0,73 mM) |
| Ethanol | Kudashobora gukemuka | |
| Amazi | Kudashobora gukemuka |
Amakuru yimiti
| Uburemere bwa molekile | 4113.58 | ||
| Inzira | C187H291N45O59 | ||
| URUBANZA No. | 910463-68-2 | ||
| Ububiko | Imyaka 3 | -20 ° C. | ifu |
| Imyaka 2 | -80 ° C. | muri solve | |
| Kohereza | Kohereza ubushyuhe bwicyumba(Impungenge zubuntu: ibicuruzwa nibyiza kuri 37 ℃ byibura icyumweru.) | ||
Amakuru Yikigereranyo
| Umubare wa NCT | Gushaka abakozi | Gutabara | Ibisabwa | Abaterankunga / Abafatanyabikorwa | Itariki yo gutangiriraho | Ibyiciro |
| NCT05537233 | Kugeza ubu | Ibiyobyabwenge: Semaglutide | Ibiyobyabwenge: Placebo | Ubwoko bwa 1 Diyabete | Umubyibuho ukabije | Kaminuza ya Colorado Denver | Fondasiyo yubushakashatsi bwa Diyabete | Mutarama 1 2023 | Icyiciro cya 2 |
| NCT04885634 | Kugeza ubu | Ibiyobyabwenge: Semaglutide Ibicuruzwa byatewe | Ibiyobyabwenge: Placebo | Fibrillation Atrial | Umubyibuho ukabije n'umubyibuho ukabije | Axel Brandes | Ibitaro bya Herlev na Gentofte | Ibitaro bya Hillerod Danemark | Ibitaro bya Svendborg | Ibitaro byo mu majyepfo y’iburengerazuba bwa Jutland | Ibitaro bya kaminuza ya Odense | Ukwakira 2022 | Icyiciro cya 3 |
| NCT05579977 | Gushaka abakozi | Ibiyobyabwenge: PF-07081532 | Ibindi: Placebo | Ibiyobyabwenge: Rybelsus | Indwara ya Diyabete | Umubyibuho ukabije | Pfizer | Ukwakira 27 2022 | Icyiciro cya 2 |
| NCT05254314 | Gushaka abakozi | Ibiyobyabwenge: Injira ya Semaglutide 2.4mg buri cyumweru | Ibindi: Placebo | Asima | Ikigo cy’ubuvuzi cya kaminuza ya Vanderbilt | Ikigo cy’igihugu gishinzwe allergie n’indwara zanduza (NIAID) | Ku ya 7 Nzeri 2022 | Icyiciro cya 2 |
| NCT05478252 | Gushaka abakozi | Ibiyobyabwenge: Semaglutide J | Ibiyobyabwenge: Semaglutide B. | Indwara ya Diyabete Ubwoko bwa 2 | Novo Nordisk A / S. | Kanama 3 2022 | Icyiciro cya 3 |
(amakuru yaturutsehttps://clinicaltrials.gov, ivugururwa kuri 2022-11-29)
