Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 Kugwiritsa ntchito kafukufuku kokha
Semaglutide, ogulitsidwa pansi pa mayina amtunduOzempic,WegovyndiRybelsus,ndi amankhwala antidiabeticamagwiritsidwa ntchito pochizamtundu 2 shugandi ngatimankhwala oletsa kunenepa kwambirikwa nthawi yayitalikasamalidwe kulemera, opangidwa ndiNovo Nordiskmu 2012. Semaglutide ndiGLP-1 receptor agonist, kutanthauza kuti amatsanzira zochita za munthuincretin glucagon-ngati peptide-1(GLP-1), potero ikuwonjezekainsulinkatulutsidwe ndi kuwonjezekashuga wamagazikukonza ndi kukonzaglycemic control.Zotsatira zake ndi monga nseru, kusanza, kutsegula m'mimba, kupweteka m'mimba, ndi kudzimbidwa. Mu Disembala 2017, mtundu wa jakisoni wotchedwa Ozempic unavomerezedwa.Mu Seputembara 2019, mtundu womwe ungamwe pakamwa (Rybelsus) udavomerezedwa, ndipo mu June 2021, jekeseni wapamwamba kwambiri wogulitsidwa pansi pa dzina la Wegovy pakuwongolera kulemera kwanthawi yayitali mwa akulu adavomerezedwa ndi US.Food and Drug Administration(FDA).Mu Januware 2023, FDA idapatsa Novo Nordisk chilolezo kuti akonzenso zolembera kuti awonetse kuti Rybelsus yapakamwa itha kugwiritsidwa ntchito ngati mankhwala.chithandizo choyambakwa akuluakulu omwe ali ndi matenda a shuga a mtundu wa 2-kutanthauza anthu omwe sanamwepo mankhwala ena a shuga. Mu 2020, semaglutide inali mankhwala a 129 omwe amagwiritsidwa ntchito kwambiri ku United States, okhala ndi mankhwala opitilira 4 miliyoni. Mawu ofanana ndi mawuRybelsus, Ozempic, NN9535, OG217SC, Kugwiritsa ntchito kafukufuku kokha.
Ntchito Zachilengedwe
| Kufotokozera | Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), analogue ya glucagon-ngati peptide 1 (GLP-1) yanthawi yayitali, ndiGLP-1 cholandiliraagonist yemwe amatha kuchiza matenda amtundu wa 2 mellitus (T2DM). |
| Zolinga | GLP-1 cholandilira |
| Mu vitro | Semaglutide imasankhidwa kukhala woyenera kamodzi pa sabata.Semaglutide ili ndi zigawo ziwiri za amino acid poyerekeza ndi GLP-1 yaumunthu (Aib8, Arg34) ndipo imachokera ku lysine 26. GLP-1R yogwirizana ndi semaglutide (0.38 ± 0.06 nM) imachepetsedwa katatu poyerekeza ndi liraglutide, pamene albumin affinity chikuwonjezeka. |
| Mu vivo | Theka la moyo wa plasma ndi 46.1 h mu nkhumba zazing'ono pambuyo pa kayendetsedwe ka iv, ndipo semaglutide ili ndi MRT ya 63.6 h pambuyo pa sc dosing kwa mini-ngulube. |
Protocol (kuchokera muzofotokozera)
| Kafukufuku wa Ma cell: | ● Mizere yam'manja:Maselo a BHK ● Kuyikira Kwambiri:0.01 pm - 0.1 μM ● Nthawi Yoyalitsira:3 h ● Njira:Ma Aliquot owuma a ma cell a BHK omwe amawonetsa hGLP-1R ndi CRE firefly luciferase (clone FCW467-12A/KZ10-1) amasungunuka, kutsukidwa kawiri mu PBS, ndikuyimitsidwa mu assay buffer.Ma cell amakutidwa mu mbale 96-zitsime pa ma cell 5000 / bwino mu voliyumu ya 50 μL.Ma Compounds omwe ayesedwe amachepetsedwa mu assay buffer ndipo 50 μL aliquot imasamutsidwa ku mbale yomwe ili ndi ma cell kuti ifike pakuyesa komaliza kwa 1 × 10.−14− 1 × 10−7M. Mbaleyi imakulungidwa kwa 3 h pa 5% CO2pa 37 °C.Mbaleyo idaloledwa kuyima kutentha kwa mphindi 15 musanawonjezere 100 μL ya steadylite kuphatikiza reagent.Chophimbacho chimaphimbidwa kuti chitetezeke ku kuwala ndikugwedezeka kutentha kwa mphindi 30.Mbaleyi imawerengedwa mu chida cha TopCount NXT. |
Kusungunuka (25°C)
| Mu vitroGulu: | DMSO | 3 mg/mL(0.73 mm) |
| Ethanol | Zosasungunuka | |
| Madzi | Zosasungunuka |
Zambiri Zamankhwala
| Kulemera kwa Maselo | 4113.58 | ||
| Fomula | C187H291N45O59 | ||
| CAS No. | 910463-68-2 | ||
| Kusungirako | 3 zaka | -20 ° C | ufa |
| zaka 2 | -80 ° C | mu zosungunulira | |
| Manyamulidwe | Kutumiza kutentha kwachipinda(Zopanda nkhawa zamtundu: chinthucho ndi chabwino pa 37 ℃ kwa sabata imodzi.) | ||
Zambiri Zoyeserera Zachipatala
| Nambala ya NCT | Kulembera anthu ntchito | Kulowererapo | Zoyenera | Othandizira/Othandizira | Tsiku loyambira | Magawo |
| NCT05537233 | Osalemba ntchito | Mankhwala: Semaglutide|Mankhwala: Placebo | Type 1 Diabetes | Kunenepa | University of Colorado Denver | Juvenile Diabetes Research Foundation | Januware 1, 2023 | Gawo 2 |
| NCT04885634 | Osalemba ntchito | Mankhwala: Semaglutide Injectable Product | Mankhwala: Placebo | Atrial Fibrillation|Kunenepa Kwambiri ndi Kunenepa Kwambiri | Axel Brandes|Chipatala cha Herlev ndi Gentofte|Chipatala cha Hillerod Denmark|Chipatala cha Svendborg|Chipatala cha South West Jutland|Chipatala cha Yunivesite ya Odense | Okutobala 2022 | Gawo 3 |
| NCT05579977 | Kulemba anthu ntchito | Mankhwala: PF-07081532|Zina: Placebo|Mankhwala: Rybelsus | Diabetes Mellitus | Kunenepa Kwambiri | Pfizer | Okutobala 27, 2022 | Gawo 2 |
| NCT05254314 | Kulemba anthu ntchito | Mankhwala: Semaglutide Pen Injector 2.4mg sabata | Zina: Placebo | mphumu | Vanderbilt University Medical Center|National Institute of Allergy and Infectious Diseases (NIAID) | Seputembara 7, 2022 | Gawo 2 |
| NCT05478252 | Kulemba anthu ntchito | Mankhwala: Semaglutide J| Mankhwala: Semaglutide B | Type 2 shuga mellitus | Malingaliro a kampani Novo Nordisk A/S | Ogasiti 3, 2022 | Gawo 3 |
(data kuchokerahttps://clinicaltrials.gov, kusinthidwa pa 2022-11-29)
