1 kits (10 Vials)
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▎ Bayanin Mazdutide
Mazdutide wani labari ne mai tsayi mai tsayi mai dual agonist na mai karɓar glucagon-kamar peptide-1 (GLP-1R) da mai karɓar glucagon (GCGR), yana ba da hanyoyin aiki daban-daban da ingantaccen ingantaccen magani. A gefe guda, ta hanyar kunna GLP-1R, yana haɓaka haɓakar insulin kuma yana hana sakin glucagon ta hanyar dogaro da glucose, yayin da yake rage zubar da ciki da rage ci, don haka yana daidaita matakan glucose na jini yadda yakamata. A gefe guda, kunna GCGR yana haɓaka lipolysis, yana haɓaka kashe kuzari, da rage tarin kitse na hanta, yana haifar da babban tasiri a sarrafa nauyi. Bayan wadannan, Mazdutide kuma yana taka rawa mai kyau wajen inganta hyperuricemia, daidaita karfin jini, da kuma kula da lafiyar zuciya, yana ba da sabon zaɓi mai ban sha'awa don kula da nau'in ciwon sukari na 2, kiba, da cututtukan da ke da alaƙa.
▎ Tsarin Mazdutide
Source: PubChem |
Jeri: AEGTFTSDVSSYLEGQAAKFIAWLVKGRG Tsarin kwayoyin halitta: C 207H 317N 45O65 Nauyin Kwayoyin: 4476g/mol Lambar CAS: 2259884-03-0 PubChem CID: 167312357 Ma'ana: GLXC-26803 |
▎ Binciken Mazdutide
Menene asalin binciken Mazdutide?
Fitaccen batu na kiba a duniya da cututtuka masu alaƙa:
Kiba da kiba sun ƙara tsananta ƙalubalen lafiyar jama'a a duniya. A cewar World Obesity Atlas, adadin masu kiba a duniya ya kai miliyan 764 a shekarar 2020 kuma ana sa ran zai haura biliyan 1 nan da shekarar 2030. Kiba na iya haifar da matsaloli masu yawa na kiwon lafiya, irin su cututtukan zuciya da jijiyoyin jini da ciwon sukari na 2, wadanda ke matukar shafar ingancin rayuwar mutum da albarkatun kiwon lafiya a duniya. Wannan ya sa masu bincike su binciko ingantattun hanyoyin magani, musamman sabbin magunguna.
Tushen haɓakar magunguna na tushen incretin:
Tun lokacin da aka gabatar da manufar incretin a cikin 1932, bincike mai alaƙa yana ci gaba a hankali. A cikin 1987, an gano GLP-1 a matsayin mabuɗin mai sarrafa ƙwayar insulin a cikin pancreas, kuma an haɓaka tsarin jiyya don nau'in ciwon sukari na 2 dangane da incretin. A cikin 2005, exenatide, farkon GLP-1 agonist mai karɓa na duniya (GLP-1RA), an amince da shi don tallatawa, yana shimfida tushe mai ƙarfi da tushe mai amfani don bincike da haɓaka sabbin magunguna na tushen incretin kamar Mazdutide. Mazdutide shine analog na mammalian oxyntomodulin (OXM). A matsayin sabon-ƙarni mai dual agonist wanda ke niyya GLP-1R da GCGR, yana da na'ura ta musamman na ayyuka biyu da kuma faffadan bege a cikin maganin asarar nauyi da cututtukan da ke da alaƙa.
Menene tsarin aikin Mazdutide?
Tasirin Agonistic akan mai karɓar glucagon-kamar peptide-1 (GLP-1):
GLP-1 wani hormone ne na hanji wanda zai iya inganta siginar insulin kuma ya hana fitar da glucagon ta hanyar dogara ga glucose, ta haka ne rage matakan glucose na jini [1] . A matsayin GLP-1 agonist mai karɓar mai karɓa, Mazdutide yana kwaikwayon aikin GLP-1, yana haɓaka haɓakar insulin da rage sakin glucagon, wanda ke taimakawa daidaita glucose na jini. Haka kuma, GLP-1 agonists mai karɓa na iya jinkirta zubar da ciki, haɓaka satiety, da rage cin abinci, wanda ke da fa'ida don sarrafa nauyi [1, 2].
Tasirin Agonistic akan mai karɓar glucagon:
Glucagon na iya haɓaka rushewar glycogen hanta da gluconeogenesis, wanda ke haifar da haɓakar glucose na jini. Mazdutide, ta hanyar kunna mai karɓar glucagon, na iya daidaita al'amuran da yawa na metabolism na glucose, samun kyakkyawan tsari na glucose na jini. Glucagon kuma yana haɓaka lipolysis, yana taimakawa rage tarin kitse da ƙananan nauyin jiki [1, 2].
Tasirin tsari akan hawan jini:
Mazdutide na iya rage duka systolic da diastolic hawan jini. A gefe guda, yana rage karfin jini ta hanyar daidaita glucose da lipid metabolism da inganta aikin endothelial na jijiyoyin jini; a gefe guda, yana iya rinjayar hanyoyin daidaita karfin jini kamar tsarin renin-angiotensin.
Menene takamaiman tsarin Mazdutide don asarar nauyi?
Tsarin glucose na jini da metabolism:
A matsayin mai dual agonist na glucagon-kamar peptide-1 (GLP-1) da masu karɓar glucagon, ɗayan tasirin ilimin lissafin jiki da yawa na GLP-1 shine daidaita matakan glucose na jini. Yana inganta ƙwayar insulin, yana hana ƙwayar glucagon, yana rage glucose na jini [1] , yana jinkirta zubar da ciki, yana ƙaruwa, kuma yana rage cin abinci. Glucagon, a gefe guda, yana haɓaka lipolysis da amfani da makamashi. Sabili da haka, Mazdutide yana kunna duka masu karɓa kuma yana daidaita matakan glucose na jini don cimma asarar nauyi. Nazarin ya nuna cewa Mazdutide na iya rage nauyin jiki, hawan jini (systolic da diastolic), jimlar cholesterol, triglycerides, low-density lipoprotein, da high-density lipoprotein matakan [3] , yana nuna cewa zai iya haifar da asarar nauyi da kuma inganta cututtukan da ke da alaka da kiba.
Tasiri kan ci da kuzari:
Mazdutide na iya samun asarar nauyi ta hanyar rinjayar ci da kuzari. A wasu gwaje-gwaje na asibiti, mahalarta sun fuskanci halayen gastrointestinal kamar rage cin abinci bayan amfani da Mazdutide [3] . Ana iya haifar da wannan ta hanyar aikin kai tsaye na Mazdutide akan gastrointestinal tract ko ta hanyar tsari ta tsarin kulawa na tsakiya. Ba tare da la'akari da tsarin ba, rage cin abinci da illa masu illa na gastrointestinal zai rage yawan kuzari da inganta asarar nauyi. Bugu da ƙari, Mazdutide na iya rinjayar ci ta hanyar daidaita masu watsawa da kuma hormones a cikin kwakwalwa. Misali, GLP-1 na iya yin aiki akan hypothalamus don daidaita ma'aunin ci da kuzari [4].
Menene takamaiman hanyoyin aikin Mazdutide don daidaita glucose na jini?
Ƙarfafa ƙwayar insulin:
Glucagon-kamar peptide-1 (GLP-1) agonists masu karɓa na iya tayar da ƙwayar insulin. A matsayin mai dual agonist na GLP-1 da masu karɓar glucagon, Mazdutide na iya kunna mai karɓar GLP-1 don ƙaddamar da ƙwayoyin sel na sel na pancreatic don ɓoye insulin. Insulin shine babban hormone don rage glucose na jini, wanda zai iya haɓaka sel don ɗaukar glucose da rage matakan glucose na jini [1]..
Hana fitar da glucagon:
A lokaci guda, Mazdutide na iya yin aiki akan mai karɓar glucagon don hana fitar da glucagon. Glucagon da insulin suna gaba da juna a cikin tsarin glucose na jini, kuma rage fitar da shi yana taimakawa wajen rage glucose na jini [1]..
Tsarin metabolism na glucose:
Mazdutide na iya daidaita metabolism na glucose a matakai da yawa don aiwatar da tasirin sa na hypoglycemic, kamar yana shafar metabolism na glucose a cikin hanta, tsoka, da kyallen takarda. A cikin hanta, yana rage rushewar hanta glycogen da gluconeogenesis, yana rage samar da glucose na jini; a cikin ƙwayar tsoka, yana inganta haɓakawa da amfani da glucose; a cikin adipose tissue, yana daidaita metabolism na lipid, yana rage sakin fatty acids kyauta, kuma a kaikaice yana shafar glucose na jini [1, 3]..
Tasiri kan ci da kuzari:
Nazarin ya gano cewa Mazdutide na iya rage ci da kuzari, mai yiwuwa ta yin aiki a kan masu karɓa a cikin tsarin juyayi na tsakiya da kuma daidaita hanyar siginar ci. Rage cin abinci na iya rage tushen glucose na jini kuma yana taimakawa sarrafa matakan glucose na jini [3, 5].

Canji daga asali a cikin nauyin jiki da kewayen kugu.
a.Kashi na canji daga asali a cikin nauyin jiki akan lokaci. b. Canja daga asali a cikin nauyin jiki akan lokaci.
Source:PubMed [2]
Menene aikace-aikacen Mazdutide?
Jiyya na nau'in ciwon sukari na 2:
Wani bazuwar, makafi biyu, gwajin gwaji na mataki na 2 na wuribo ya nuna cewa Mazdutide, wani agonist dual agonist da ake gudanarwa kowane mako na glucagon-kamar peptide 1 (GLP-1) da masu karɓar glucagon, ya nuna inganci da aminci ga marasa lafiya na kasar Sin masu fama da ciwon sukari na 2 [1].
Aikace-aikace a cikin asarar nauyi:
Bincike a kan marasa lafiya da kuma ba tare da ciwon sukari ba: Bita na yau da kullum da bincike-bincike ya nuna cewa Mazdutide na iya rage nauyin jikin manya tare da ko ba tare da ciwon sukari ba [3] . Binciken ya haɗa da gwaje-gwajen sarrafawa guda bakwai tare da jimlar mahalarta 680. Sakamakon ya nuna cewa idan aka kwatanta da placebo, Mazdutide ya haifar da raguwa mai mahimmanci a cikin nauyin jiki (ma'anar bambanci [MD] = -6.22%, 95% tazarar amincewa [CI]: -8.02% zuwa -4.41%, I⊃2; = 90.0%) (Nalisa DL, 2024). Ƙungiya da ƙididdiga na meta-regression sun gano cewa marasa lafiya ba tare da ciwon sukari suna da asarar nauyi mai yawa ba, kuma marasa lafiya da aka yi musu magani na makonni 24 sun fi girma rage nauyi idan aka kwatanta da waɗanda aka yi wa 12 - 20 makonni [3]..
Aikace-aikace a cikin manya na kasar Sin masu kiba ko kiba:
Binciken tsakiyar lokaci na bazuwar, kashi biyu (ƙananan kashi har zuwa 6mg da babban kashi 9mg), makafi biyu, gwajin gwaji na Phase 2 wanda aka gudanar a cikin manya na kasar Sin tare da kiba ko kiba ya nuna cewa Mazdutide yana da lafiya kuma yana da tasiri a cikin wannan yawan yayin lokacin jiyya na mako 24, yana kawo gagarumin hasara mai ma'ana ta asibiti [2] . A cikin binciken, manya da kiba (BMI ≥ 24 kg / m²) tare da hyperphagia da / ko aƙalla ɗaya daga cikin cututtukan da ke da alaƙa da kiba, ko manya da kiba (BMI ≥ 28 kg / m²) An ba da izini don karɓar Mazdutide mako-mako a allurai na 3.5mg. Sakamakon ya nuna cewa daga asali zuwa mako na 24th, ma'anar canjin kashi a cikin nauyin jiki shine -6.7% (kuskuren daidaitattun 0.7) a cikin 3mg Mazdutide kungiyar, -10.4% (0.7) a cikin 4.5mg kungiyar, -11.3% (0.7) a cikin 6mg kungiyar, da kuma 1.7) a cikin 0.0% Idan aka kwatanta da placebo, bambancin jiyya ya kasance daga -7.7% zuwa -12.3% (duk p <0.0001) [2].
A ƙarshe, a matsayin sabon agonist dual- target agonist, ta hanyoyi da yawa kamar daidaita glucose na jini, haɓaka metabolism na mai, da hana ci abinci, Mazdutide na iya haɓaka matakan glucose na jini yadda ya kamata na marasa lafiya masu fama da ciwon sukari na 2 da kuma taimakawa masu kiba su rasa nauyi. Yana shigar da sabon kuzari a cikin maganin cututtukan da ke haifar da rayuwa kuma ana tsammanin zai rage nauyin kiba da cututtukan da ke da alaƙa a duniya.
Game da Marubuci
Abubuwan da aka ambata a sama duk bincike ne, gyara su kuma Cocer Peptides ne suka haɗa su.
Mawallafin Jaridar Kimiyya
Zhang B ƙwararren malami ne wanda ke da alaƙa da shahararrun ƙungiyoyi. Wadannan sun hada da Kwalejin Kiwon Lafiya ta Peking Union, Kwalejin Kimiyyar Kiwon Lafiya ta kasar Sin - Kwalejin Kiwon Lafiya ta Peking Union, - Asibitin Abota na Japan, Guizhou Equipment Mfg Polytech, Jami'ar Shanghai Jiao Tong, Jami'ar Utara Malaysia, Cibiyar Fasaha ta Yingkou, Jami'ar Zhejiang, da Asibitin Kwalejin Kiwon Lafiya ta Peking Union. Irin waɗannan bambance-bambancen haɗin kai na cibiyoyi suna nuna faffadan iliminsa da na bincike.
Dangane da bincike, Zhang B yana da nau'ikan batutuwa masu yawa. Kwarewarsa ya haɗa da Endocrinology & Metabolism, General & Internal Medicine, Oncology, Cardiovascular System & Cardiology, da Radiology, Medicine Nuclear & Medical Imaging. Ayyukansa a waɗannan fagagen suna nuna zurfin iliminsa da gagarumar gudunmawar haɓaka ilimin likitanci da inganta ayyukan kiwon lafiya. An jera Zhang B a cikin ambaton ambaton [1].
▎ Abubuwan da suka dace
[1] Zhang B, Cheng Z, Chen J, et al. Inganci da Tsaron Mazdutide a cikin Majinyatan Sinawa Masu Ciwon sukari Na 2: Bazuwar, Makafi Biyu, Gwajin Mataki na 2 Mai Sarrafa Wuri[J]. Kula da ciwon sukari, 2024,47 (1): 160-168.DOI: 10.2337 / dc23-1287.
[2] Ji L, Jiang H, Cheng Z, et al. Gwajin gwaji na mazdutide na zamani na 2 a cikin manya masu kiba na kasar Sin ko manya masu kiba[J]. Sadarwar yanayi, 2023,14 (1).DOI:10.1038/s41467-023-44067-4.
[3] Nalisa DL, Cuboia N, Dyab E, et al. Inganci da amincin Mazdutide akan asarar nauyi tsakanin masu ciwon sukari da marasa ciwon sukari: nazari na yau da kullun da meta-bincike na gwaje-gwajen da aka sarrafa bazuwar[J]. Iyakoki a cikin Ilimin Ilimin Halittu, 2024,15.
[4] Morris A. Ƙirƙirar hanyoyin asara nauyi [J]. Nature Reviews Endocrinology, 2020,16(7):343.DOI:10.1038/s41574-020-0374-4.
[5] Ji L, Gao L, Jiang H, et al. Aminci da inganci na GLP-1 da glucagon receptor dual agonist mazdutide (IBI362) 9 MG da 10 MG a cikin manya na kasar Sin masu kiba ko kiba: Bazuwar, sarrafa wuribo, yawan hawan-hawan kashi 1b gwaji [J]. Eclinicalmedicine, 2022,54:101691.DOI:10.1016/j.elinm.2022.101691.
DUKKANIN LABARI DA BAYANIN KYAUTATAWA DA AKE BAYAR A WANNAN SHAFIN KAWAI DOMIN WATSA BAYANI NE DA MANUFOFIN ILIMI.
Kayayyakin da aka bayar akan wannan gidan yanar gizon an yi niyya ne kawai don binciken in vitro. Binciken in vitro (Latin: *a cikin gilashi*, ma'ana a cikin gilashin gilashi) ana gudanar da shi a wajen jikin mutum. Waɗannan samfuran ba magunguna ba ne, Hukumar Abinci da Magunguna ta Amurka (FDA) ba ta amince da su ba, kuma dole ne a yi amfani da su don hanawa, magani, ko warkar da kowane yanayi na likita, cuta, ko cuta. Doka ta haramta shigar da waɗannan samfuran cikin jikin mutum ko dabba ta kowace hanya.