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Over Incamake ya Cagrilintide
Cagrilintide ni amyline ebyiri na calcitonine reseptor agonist (DACRA) yakozwe ishingiye kumiterere ya amylin. Ikora ingaruka zayo mugukoresha reseptor ya amylin na reseptor ya calcitonine, bityo bikerekana ubushobozi bwo kugenzura ibipimo bya metabolike nkuburemere bwumubiri hamwe n urugero rwa glucose yamaraso.
Ubushakashatsi niterambere rya Cagrilintide bikomoka kumiterere ya physiologique ya amyline karemano. Amyline isanzwe ni imisemburo isohoka mu ngirabuzimafatizo kandi igira uruhare runini mu guhaga no kugabanya ibiryo. Muri icyo gihe kandi, igira uruhare mu kugena metabolisme y’amaraso binyuze mu buryo butandukanye, nko kubuza irekurwa rya glucagon nyuma y’inyuma ndetse no gutinda gusohora gastric.
Nkikigereranyo kirekire, Cagrilintide ifite igice cyubuzima bwiminsi igera kuri 7 kugeza 8. Ibi byongerewe igice cyubuzima butezimbere cyane uburyo bworoshye bwo kuyobora no kubahiriza abarwayi, bigatuma aribwo buryo bwiza bwo kuvura.
CagrilintideStructure Imiterere ya
Inkomoko: PubChem |
Urukurikirane: Pyr-KCNTATCATQRLAEFLRHSSNNFGPILPPTNVGSNTP CAS: 1415456-99-3 Inzira: C 174H 269N 45O 52S.2 MW 4409 g / mol |
Research Ubushakashatsi bwa Cagrilintide
Ni ubuhe bushakashatsi bwakozwe na Cagrilintide?
Cagrilintide ni amyline ebyiri na calcitonine reseptor agonist (DACRA) yakozwe ishingiye kumiterere ya amylin. Amylin isohorwa na pancreatic islet β selile kandi ikorana na insuline kugirango ikore imirimo itandukanye. Irashobora gutera ibyiyumvo byo guhaga no kugabanya gufata ibiryo, cyane cyane mugukora reseptors mukarere ka postrema munsi yumushinga wa kane. Ibimenyetso by'imitsi byanduzwa imbere yimbere binyuze muri nucleus yinzira yonyine kandi birashobora no kwanduzwa mukarere ka hypothalamic hamwe nandi matsinda ya kirimbuzi binyuze muri nucleus ya parabrachial, bityo bigashimisha ikigo gihaza kandi bikabuza gufata ibiryo [1] . Amylin irashobora kandi kugenga glucose homeostasis mukurinda gusohora kwa insuline na glucagon kugirango ikomeze glucose yamaraso [2] . Muburyo bukubiyemo harimo ingaruka itaziguye ku kirwa cya pancreatic islet α selile no kugenzura mu buryo butaziguye ururenda rwa glucagon binyuze mu bimenyetso by'imitsi muri hypothalamus. Ku barwayi barwaye diyabete, gusenya β selile bituma igabanuka rya amyline. Amylin agira uruhare mu kugena glucose homeostasis mu kubuza gusiba gastrica no kubyara hepatike glucose nyuma yo kugabanuka, kugabanya ihindagurika ryamaraso ya glucose nyuma yinyuma. Irashobora kandi gutinza ubusa gastrica, ikabuza gastrointestinal peristalsis, kongera igihe cyo gutura ibiryo, kandi ikarinda kwiyongera gukabije kwamaraso glucose. Nyamara, igice gito cyubuzima bwa amylin karemano igabanya ikoreshwa ryayo. Nubwo pramlintide iboneka nkumuti wongeyeho, bisaba inshinge eshatu kumunsi, ntibyoroshye kandi bikavamo kutubahiriza nabi [3] . Kugira ngo iki kibazo gikemuke, Cagrilintide yatejwe imbere. Ubushakashatsi niterambere ryayo bishingiye ku gusobanukirwa byimbitse kumikorere ya physiologique ya amyline karemano, igamije kwigana uburyo bwayo bwibikorwa mugihe hagamijwe kunoza imiterere n’imikorere myinshi yibiyobyabwenge kugirango bikemure ivuriro.
Cagrilintide ni iki?
Cagrilintide nigitabo kimaze igihe kinini kigereranya amylin igereranya kandi ifite imbaraga nyinshi, imaze kwerekana umusaruro wambere mukuvura umubyibuho ukabije na diyabete. Yashizwemo amavuta kandi ifite imiterere ihamye kandi ikora igihe kirekire [3] . Amylin arekurwa hamwe na insuline na selile pancreatic β selile kandi bigatera kumva uhaze ukora mukarere ka homeostatike kandi kunezeza ubwonko. Nkikigereranyo, Cagrilintide irashobora kwigana izi ngaruka, itera guhaga kugirango ifashe kugenzura ibiro byumubiri. Muri icyo gihe, nka amyline ebyiri na calcitonine reseptor agonist (DACRA), ikomoka mu mugongo wa amylin kandi ifite uburyo bwihariye mu kugenzura metabolike.

Imiterere yuburyo bwa Cagrinlintide
Inkomoko: Byatangajwe [3]
Nibihe bikorwa bifitanye isano na Cagrilintide?
Mu bigeragezo bivura, Cagrilintide yageze ku musaruro mwiza mu kugabanya ibiro. Kurugero, muri multicenter, idahwitse, impumyi ebyiri, igenzurwa na platbo, kandi igereranya igereranya Icyiciro cya 2 ikigereranyo cyo gushakisha ikigereranyo, ugereranije nitsinda rya placebo, impuzandengo yikigereranyo cyo kugabanya ibiro kuva kuri buri tsinda rya dose ya Cagrilintide (0.3 - 4.5 mg) (6.0% - 10.8%) yari hejuru kurenza iyo mumatsinda ya placebo (3.0%). Kugabanuka ibiro mu itsinda rya 4.5 mg nabyo byari byinshi kuruta ibyo mu itsinda rya liraglutide 3.0 mg (10.8% na 9.0%), byerekana ko bishobora kuba uburyo bwiza bwo gucunga ibiro [4] . Cagrilintide ifite uburyo butandukanye ariko bujyanye nibikorwa ugereranije na GLP-1 reseptor agonist semaglutide. Semaglutid igabanya ubushake bwo kurya, ikongera imisemburo ya insuline, kandi igatinda gusohora gastrica ikora kuri reseptor ya GLP-1 muri hypothalamus, naho Cagrilintide ikomeza kugabanya ubushake bwo gukora reseptor ya amylin. Gukoresha hamwe byombi birashobora gutanga ingaruka zidasanzwe, byongera cyane kugabanya ibiro [5] . Urebye umubyibuho ukabije, ubu buryo bwo kuvura ni ingamba zifatika kandi zifatika.
Ku barwayi barwaye diyabete yo mu bwoko bwa 2, Cagrilintide yerekanye kandi ubushobozi bwiza bwo kugenzura amaraso glucose. Ubushakashatsi ku mavuriro bwerekanye ko bufite umutekano muke mu kuvura umubyibuho ukabije na diyabete yo mu bwoko bwa 2. Kurugero, mugupima kwa muganga abarwayi bafite diyabete yo mu bwoko bwa 2, gukoresha hamwe Cagrilintide hamwe na GLP-1 reseptor agonist semaglutide byagaragaje neza glucose yamaraso no kugabanya ibiro [6] . Urundi rubanza kandi rwerekanye ko rwihanganirwa n’umutekano rwiza iyo rukoreshejwe rwonyine cyangwa rufatanije na semaglutide [6] , kubera ko imiti ihagaze neza ifitanye isano no kwihanganira umutekano.
Byongeye kandi, Cagrilintide yihanganiye neza mubigeragezo byamavuriro. Mu cyiciro cya 2 cyo gushakisha ibipimo, ibipimo byo guhagarika burundu muri buri tsinda rivura byari bisa, ahanini bitewe nibintu bibi. Nyamara, ibintu byakunze kugaragara nabi ni indwara zo munda no gutera inshinge, kandi ibyinshi muri byo byari byoroheje kandi bitagereranywa. Mu igeragezwa ryateganijwe, rigenzurwa Icyiciro cya 1b, kuvura hamwe na Cagrilintide na 2,4 mg semaglutide nabyo byagaragaje kwihanganira umutekano n'umutekano [7] . Ibigeragezo binini kandi birebire birakenewe mugihe kizaza kugirango dusuzume byimazeyo imikorere numutekano byubu buvuzi hamwe.
Cagrilintide izana ibyiringiro bishya byo kuvura umubyibuho ukabije na diyabete yo mu bwoko bwa 2. Itanga uburyo bushya bwo kuvura abarwayi bafite umubyibuho ukabije, cyane cyane abatitabira neza uburyo bwo kubaho kandi ntibakwiriye kubagwa ibibari. Uburyo bwihariye bwibikorwa bitanga ibitekerezo nuburyo bushya bwo kuvura umubyibuho ukabije, kandi birashobora kugira ibyiza byinshi kuruta imiti igabanya ibiro (D'Ascanio AM, 2024). Ikibazo cyatsinzwe cyo gukoresha Cagrilintide na semaglutide (CagriSema) cyerekana ko kuvura intego nyinshi ari ingamba zifatika zo kunoza uburyo bwo kuvura umubyibuho ukabije [6] . Iyi moderi itanga paradizo nshya yo gucunga umubyibuho ukabije kandi ikanazana iterambere ryinshi rya metabolike kubarwayi barwaye diyabete yo mu bwoko bwa 2.
Mu gusoza, nkigitabo gishya cyerekana amylin igereranya, Cagrilintide ifite amahirwe menshi yo kugabanya ibiro no kurwanya glucose yamaraso. Ikora inzira yerekana ibimenyetso byuzuye yigana ibikorwa bya amylin kandi igenga metabolisme nka agoniste ya reseptor ebyiri. Igeragezwa rya Clinical ryerekanye ko Cagrilintide, yonyine cyangwa ifatanije na semaglutide, ishobora kugabanya cyane ibiro byumubiri kandi irihanganirwa. Byongeye kandi, yerekanye kandi ubushobozi bwiza bwo kugenzura amaraso glucose ku barwayi barwaye diyabete yo mu bwoko bwa 2, itanga uburyo bushya bwo kuvura umubyibuho ukabije na diyabete, kuzuza icyuho mu buryo bwo kuvura buriho, cyane cyane ku barwayi batitabira neza ibikorwa by’ubuzima kandi bidakwiriye kubagwa. Ingamba zayo zo kuvura intego nyinshi zitanga ibitekerezo bishya byo gucunga indwara ziterwa na metabolike.
Ibyerekeye Umwanditsi
Ibikoresho byavuzwe haruguru byose byakorewe ubushakashatsi, byahinduwe kandi byakozwe na Cocer Peptides.
Umwanditsi w'ikinyamakuru
Dr. DCW Lau ni umwarimu mu ishuri ry'ubuvuzi rya Cumming, kaminuza ya Calgary, muri Kanada. Ibyifuzo bye mubushakashatsi bikubiyemo endocrinology na metabolism, ubuvuzi rusange n’imbere, sisitemu yumutima nimiyoboro yumutima, umutima rusange, ubuzima rusange bwibidukikije ndetse nubuzima bwakazi, ndetse na onkologiya. Afite kandi imyanya muri serivisi z'ubuzima za Alberta (AHS) na Obesity Canada kandi akora mu kigo cy’ubushakashatsi cya Diabete ya Julia McFarlane. Dr. Lau afite ubunararibonye mu bijyanye na diyabete n'ubushakashatsi bw'umubyibuho ukabije, hamwe n'ibikorwa bye byasohotse mu binyamakuru byigisha nk'ikinyamakuru cyo muri Kanada cya Diyabete. Muganga DCW yanditse kurutonde rwerekana [4].
Imirongo ijyanye
[1] Hansen KE, Murali S, Chave IZ, n'abandi. Glycomacropeptide Ingaruka Guhaza Amylin-Yunganirwa, Ibimenyetso bya Postprandial ya Glucose Homeostasis, na Microbiome ya Fecal mubagore bafite umubyibuho ukabije [J]. Ikinyamakuru cyimirire, 2023,153 (7): 1915-1929.DOI: 10.1016 / j.tjnut.2023.03.014.
[2] Ling W, Huang Y, Qiao Y, n'abandi. Umuntu Amylin: Kuva muri Pathologiya kugeza Physiology na Pharmacology [J]. Ubumenyi bwa poroteyine & Peptide y'ubu, 2019,20 (9): 944-957.DOI: 10.2174 / 13892037206 66 19032811183 3.
[3] Kruse T, Hansen JL, Dahl K, n'abandi. Iterambere rya Cagrilintide, Analogue ikora Amylin [J]. Ikinyamakuru cya chimie yubuvuzi, 2021,64 (15): 11183-11194.DOI: 10.1021 / acs.jmedchem.1c00565.
[4] Lau DCW, Erichsen L, Francisco AM, n'abandi. Rimwe na rimwe cagrilintide yo gucunga ibiro kubantu bafite umubyibuho ukabije n'umubyibuho ukabije: multicentre, randomisme, impumyi-ebyiri, igenzurwa na platbo kandi igenzurwa cyane, igenzura icyiciro cya 2 [J]. Lancet, 2021,398 (10317): 2160-2172.DOI: 10.1016 / S0140-6736 (21) 01751-7.
[5] D'Ascanio AM, Mullally JA, Frishman W H. Cagrilintide: Ikigereranyo cya Amylin Ikora igihe kirekire cyo kuvura umubyibuho ukabije [J]. Indwara z'umutima mu isubiramo, 2024,32 (1): 83-90.DOI: 10.1097 / CRD.0000000000000513.
[6] Frias JP, Deenadayalan S, Erichsen L, n'abandi. Imikorere n'umutekano byafatanyirijwe hamwe rimwe mu cyumweru cagrilintide 2,4 mg hamwe na semaglutide imwe ya buri cyumweru mg 2,4 mg muri diyabete yo mu bwoko bwa 2: multicentre, randomisme, impumyi ebyiri, igenzurwa cyane, igeragezwa ryicyiciro cya 2 [J]. Lancet, 2023,402 (10403): 720-730.DOI: 10.1016 / S0140-6736 (23) 01163-7.
[7] Enebo LB, Berthelsen KK, Kankam M, n'abandi. Umutekano, kwihanganira, farumasi, hamwe na farumasi yubuyobozi bujyanye no gukoresha inshuro nyinshi za cagrilintide hamwe na semaglutide 2,4 mg yo gucunga ibiro: ibizamini byateganijwe, bigenzurwa, icyiciro cya 1b [J]. Lancet, 2021,397 (10286): 1736-1748.DOI: 10.1016 / S0140-6736 (21) 00845-X.
INGINGO ZOSE N'AMAKURU Y’IBICURUZWA BITANZWE KURI URU RUBUGA BISANZWE KUBONA AMAKURU N'INTEGO Z'UBUREZI.
Ibicuruzwa byatanzwe kururu rubuga bigenewe gusa mubushakashatsi bwa vitro. Mu bushakashatsi bwa vitro (Ikilatini: * mu kirahure *, bisobanura mu bikoresho by'ibirahure) bikorwa hanze y'umubiri w'umuntu. Ibicuruzwa ntabwo ari imiti, ntabwo byemejwe n’ikigo cy’Amerika gishinzwe ibiryo n’ibiyobyabwenge (FDA), kandi ntigomba gukoreshwa mu gukumira, kuvura, cyangwa gukiza indwara iyo ari yo yose y’ubuvuzi, indwara, cyangwa indwara. Birabujijwe rwose n'amategeko kwinjiza ibyo bicuruzwa mumubiri wabantu cyangwa inyamaswa muburyo ubwo aribwo bwose.