Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 Don amfani da bincike kawai
Semaglutide, ana sayar da su a ƙarƙashin sunayen alamarOzempic,WegovykumaRybelsus, wanimaganin ciwon sukariamfani da magani nanau'in ciwon sukari na 2kuma kamar yaddamaganin rage kibana dogon lokacisarrafa nauyi, ci gabanNovo Nordiska shekarar 2012. Semaglutide shine aGLP-1 agonist mai karɓa, ma'ana yana kwaikwayon aikin ɗan adamincretin glucagon-kamar peptide-1(GLP-1), don haka yana ƙaruwainsulinasiri da karuwasukarin jinizubarwa da ingantawasarrafa glycemic.Abubuwan da ke haifar da cutar sun hada da tashin zuciya, amai, gudawa, ciwon ciki, da maƙarƙashiya. A cikin Disamba 2017, an amince da sigar allurar mai suna Ozempic.A watan Satumba na 2019, an yarda da sigar da za a iya ɗauka ta baki (Rybelsus), kuma a cikin Yuni 2021, Amurka ta amince da allurar mafi girma da aka sayar a ƙarƙashin sunan Wegovy don sarrafa nauyi na dogon lokaci a cikin manya.Gudanar da Abinci da Magunguna(FDA).A cikin Janairu na 2023, FDA ta ba Novo Nordisk izini don sake fasalin lakabin don nuna cewa ana iya amfani da Rybelsus na baka azamanmagani na farkoga manya masu nau'in ciwon sukari na 2-ma'ana a cikin mutanen da ba su taɓa shan wani maganin ciwon sukari ba. A cikin 2020, semaglutide shine magani na 129 da aka fi ba da izini a Amurka, tare da fiye da takardun magani miliyan 4. Makamantu: Rybelsus, Ozempic, NN9535, OG217SC, Don amfani da bincike kawai.
Ayyukan Halittu
| Bayani | Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), wani dogon aiki glucagon-kamar peptide 1 (GLP-1), analogue ne.GLP-1 mai karɓaagonist tare da yuwuwar maganin nau'in ciwon sukari na 2 (T2DM). |
| Makasudi | GLP-1 mai karɓa |
| In vitro | An zaɓi Semaglutide azaman mafi kyawun ɗan takara sau ɗaya kowane mako.Semaglutide yana da maye gurbin amino acid guda biyu idan aka kwatanta da ɗan adam GLP-1 (Aib8, Arg34) kuma an samo shi a lysine 26. GLP-1R alaƙar semaglutide (0.38 ± 0.06 nM) ya ragu sau uku idan aka kwatanta da liraglutide, yayin da alaƙar albumin. yana karuwa. |
| A cikin vivo | Rabin rabin rayuwar plasma shine 46.1 h a cikin ƙananan aladu bayan gudanar da iv, kuma semaglutide yana da MRT na 63.6 h bayan sc dosing zuwa ƙananan aladu. |
Protocol (daga tunani)
| Binciken Kwayoyin Halitta: | ● Layukan salula:Kwayoyin BHK ● Mahimmanci:0.01 pm - 0.1 μM ● Lokacin Fitowa:3 h ku ● Hanya:Daskararre aliquots na sel BHK waɗanda ke bayyana duka hGLP-1R da CRE firefly luciferase (clone FCW467-12A/KZ10-1) ana narke, an wanke su sau biyu a cikin PBS, kuma an dakatar da su a cikin buffer assay.An jera ƙwayoyin sel zuwa faranti 96-rijiya a sel 5000 / rijiyar a cikin ƙarar 50 μL.Abubuwan da za a gwada ana diluted su a cikin buffer assay da 50 μL aliquot canjawa wuri zuwa farantin da ke ɗauke da sel don isa ga ƙima na ƙarshe na 1 × 10-14- 1 × 10-7M. Ana shigar da farantin don 3 h a 5% CO2da 37 ° C.An ba da izinin farantin ya tsaya a dakin da zafin jiki na mintuna 15 kafin ƙara 100 μL na steadylite da reagent.An rufe farantin don kare shi daga haske kuma a girgiza a cikin dakin da zafin jiki na minti 30.Ana karanta farantin a cikin kayan aikin TopCount NXT. |
Solubility (25°C)
| In vitroBatch: | DMSO | 3 mg/ml(0.73 mM) |
| Ethanol | Mara narkewa | |
| Ruwa | Mara narkewa |
Bayanan Kimiyya
| Nauyin Kwayoyin Halitta | 4113.58 | ||
| Formula | C187H291N45O59 | ||
| CAS No. | 910463-68-2 | ||
| Adanawa | shekaru 3 | -20°C | foda |
| shekaru 2 | -80°C | a cikin sauran ƙarfi | |
| Jirgin ruwa | jigilar da zafin jiki(Kyakkyawan damuwa kyauta: samfurin yana da kyau a 37 ℃ na akalla sati 1.) | ||
Bayanan Gwaji na asibiti
| Lambar NCT | daukar ma'aikata | Tsangwama | Sharuɗɗa | Masu Tallafawa/Masu Haɗin kai | Ranar farawa | matakai |
| Saukewa: NCT05537233 | Har yanzu ba a dauki ma'aikata ba | Drug: Semaglutide|Magunguna: Placebo | Nau'in Ciwon Suga Na 1|Kiba | Jami'ar Colorado Denver | Gidauniyar Binciken Ciwon Ciwon Yara na Yara | Janairu 1, 2023 | Mataki na 2 |
| NCT04885634 | Har yanzu ba a dauki ma'aikata ba | Drug: Semaglutide Samfurin Injectable | Magunguna: Placebo | Atrial Fibrillation|Kiba da Kiba | Axel Brandes | Asibitin Herlev da Gentofte | Asibitin Hillerod Denmark | Asibitin Svendborg | Asibitin Kudu maso Yamma Jutland | Asibitin Jami'ar Odense | Oktoba 2022 | Mataki na 3 |
| Saukewa: NCT0557997 | Daukar ma'aikata | Drug: PF-07081532|Sauran: Placebo|Magunguna: Rybelsus | Ciwon sukari Mellitus|Kiba | Pfizer | Oktoba 27, 2022 | Mataki na 2 |
| Saukewa: NCT05254314 | Daukar ma'aikata | Drug: Semaglutide Pen Injector 2.4mg kowane mako | Wani: Placebo | Asma | Cibiyar Kiwon Lafiya ta Jami'ar Vanderbilt | Cibiyar Nazarin Allergy da Cututtuka (NIAID) | Satumba 7 2022 | Mataki na 2 |
| Saukewa: NCT05478252 | Daukar ma'aikata | Drug: Semaglutide J|Magunguna: Semaglutide B | Nau'in ciwon sukari na 2 | Novo Nordisk A/S girma | Agusta 3, 2022 | Mataki na 3 |
(data dagahttps://clinicaltrials.govAn sabunta ta 2022-11-29)
