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1kits (Ebipipa 10) .
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▎ Enzimba ya Retatrutide
Ensibuko: PubChem |
Omutendera: YA⊃1;QGTFTSDYSI-L⊃2;LDKK4AQA⊃1;AFIEYLLEGGPSSGAPPPS⊃3; Ensengekera ya molekyu: C 221H 342N 46O68 Obuzito bwa molekyu: 4731 g/mol Ennamba ya CAS: 2381089-83-2 PubChem CID: 171390338. Enkola y’okukuuma eddagala lino Ebigambo ebikwatagana:LY3437943 |
▎ Okunoonyereza ku Retatrutide
Retatrutide y’egenda mu maaso n’okunoonyereza etya?
Ensibuko y’okunoonyereza eya Retatrutide ekwatagana nnyo n’ensonga z’ensi yonna ezeeyongera okuba ez’amaanyi ez’omugejjo n’enkyukakyuka mu mubiri, awamu n’obuzibu bw’eddagala erijjanjaba eririwo: omugejjo n’okukyusakyusa mu mubiri biba bya bulabe nnyo eri obulamu bw’abantu, ng’omuwendo gw’abagejjulukuka mu nsi yonna gusuubirwa okutuuka ku buwumbi 4.005 mu mwaka gwa 2035 ate omuwendo gw’abalwadde b’enkyukakyuka mu mubiri gweyongera okutuuka ku 592 obukadde, ekivaamu ensaasaanya ennene mu by’obulamu mu nsi yonna olw’enkyukakyuka y’emmere. Multi-target receptor agonist peptides zivuddeyo nga solution, ezisobola okuziyiza omugejjo, okujjanjaba metabolism, n’okwewala obutwa obuva mu ddagala eririwo, ekizifuula omuze mu kukola obujjanjabi bw’omugejjo n’okukyusakyusa metabolism.
Enkola ya Retatrutide ekola ki?
Okulungamya enkyukakyuka y’amasoboza okuyita mu kukola kw’amasoboza amangi
Retatrutide ye agonist ey’okukwata ebitundu bisatu ng’etunuulira ekirungo ekikwata insulinotropic polypeptide ekisinziira ku glucose (GIPR), ekirungo kya glucagon-like peptide-1 receptor (GLP-1R), n’ekirungo kya glucagon receptor (GCGR). Mu kiseera kye kimu kikola ebitundu bino ebisatu ebikwata, ne kitereeza enkyukakyuka y’amasoboza okuyita mu makubo agawera.
Ekikolwa kya GIPR agonist:
GIP busimu obufulumya insulini mu byenda obufulumizibwa obutoffaali bwa K obw’ekyenda ne bufulumizibwa oluvannyuma lw’okulya. Retatrutide ekola GIPR, n’etumbula okufulumya insulini, n’eyamba okuwulira insulini, era bwe kityo n’eyamba omubiri okunyiga obulungi n’okukozesa glucose, bwe kityo ne kikendeeza ku mutindo gwa glucose mu musaayi. Okugatta ku ekyo, GIP eyinza okukwata ku nkyukakyuka y’amasavu ng’etereeza enkola y’obutoffaali bw’amasavu n’okukendeeza ku kukuŋŋaanyizibwa kw’amasavu [1]..
Enkola ya GLP-1R agonist:
GLP-1 ye hormone ya peptide efulumizibwa obutoffaali bwa L obw’ekyenda. Oluvannyuma lw’okukola GLP-1R, Retatrutide ekola emigaso egy’enjawulo. Kiyinza okusitula okufulumya insulini mu ngeri eyeesigama ku bungi bwa glucose, bwe kityo ne kikendeeza ku sukaali mu musaayi. Kiyinza okulwawo okufulumya amazzi mu lubuto, okwongera okukkuta n’okukendeeza ku mmere gy’olya. GLP-1R gonism era eyinza okukola ku busimu obw’omu makkati, okutereeza okwagala okulya n’okutebenkeza amaanyi, bwe kityo ne kiyamba mu kugejja [2]..
Ebikolwa bya GCGR agonist:
Glucagon mu bujjuvu ayongera ku glucose mu musaayi, naye wansi w’okufugibwa Retatrutide, GCGR gonism ekola ebikolwa eby’enjawulo. Kitumbula glycogenolysis ne gluconeogenesis mu kibumba. Wansi w’ebikolwa bya Retatrutide byonna awamu, omubiri tegufuna kweyongera kwangu mu miwendo gya glucose mu musaayi wabula mu kifo ky’ekyo gutereeza enkyukakyuka y’amaanyi okwongera okumenya amasavu, bwe kityo ne kituuka ku kugejja n’okulongoosa mu nkyukakyuka y’emmere. GCGR agonism era eyinza okukosa enkyukakyuka y’amasavu mu kibumba, okukendeeza ku kukuŋŋaanyizibwa kw’amasavu mu kibumba [3]..
Ebikosa Enkola z’Emibiri Ezekuusa ku Ssukaali
Nga ekola mu kiseera kye kimu ku bikwata ebisatu ebyogeddwako waggulu, Retatrutide ekwata ku nkola z’omubiri eziwera ezikwata ku nkyukakyuka y’emmere.
Okulungamya glucose mu musaayi:
Nga ekola GIPR ne GLP-1R okutumbula okufulumya insulini, n’okulungamya obulungi GCGR, Retatrutide esobola okukendeeza ku glucose mu musaayi. Ekikolwa kyayo eky’okukendeeza sukaali kyeyoleka nga glucose mu musaayi alinnye, so nga tekisuubirwa kuleeta kukendeeza sukaali mu musaayi nga glucose mu musaayi ali wa bulijjo, ekintu eky’omugaso mu kufuga glucose mu musaayi mu balwadde ba sukaali [4]..
Enzirukanya y’obuzito:
Retatrutide eraga obulungi obw’amaanyi mu kuddukanya obuzito. Nga ekola GLP-1R, ekendeeza ku kufulumya amazzi mu lubuto, eyongera okukkuta, n’okukendeeza ku mmere gy’olya; nga kitereeza enkyukakyuka y’amasavu, kitumbula okumenya amasavu n’okukozesa amaanyi, bwe kityo ne kituuka ku kugejja. Okugezesebwa mu malwaliro kulaga nti abalwadde abagejjulukuka oba abagejjulukuka abajjanjabwa n’eddagala lya Retatrutide bafuna okugejja okw’amaanyi mu kiseera ekigere [5,6]..
Okulungamya amasavu:
Obujjanjabi bwa Retatrutide bulongoosa amasavu g’abalwadde. Kikendeeza ku triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), ne low-density lipoprotein cholesterol (VLDL-C) emiwendo, ate nga era kitereeza apolipoproteins, gamba ng’okukendeeza ku apolipoprotein B (apoB) ne apolipoprotein C -III (apoC-III) emiwendo, bwe kityo ne kikendeeza ku muwendo gw’obutundutundu bwa lipoprotein obukwatagana nga balina okuzimba emisuwa n’okutumbula obulamu bw’emisuwa n’emisuwa [7]..
Okulongoosa mu nkyukakyuka y’amasavu mu kibumba:
Ku balwadde abalina obulwadde bw’ekibumba obutali bwa mwenge (NAFLD) obukwatagana n’obutakola bulungi mu nkyukakyuka y’emmere, Retatrutide ekendeeza nnyo amasavu mu kibumba. Mu kugezesebwa okukwatagana, abalwadde abajjanjabiddwa ne dose ez’enjawulo eza Retatrutide baalaga okukendeera okw’amaanyi mu masavu mu kibumba bw’ogeraageranya n’okusooka, ekiraga nti Retatrutide erina ekikolwa ekirungi eky’okulungamya ku nkyukakyuka y’amasavu mu kibumba, eky’omugaso mu kulongoosa enkola y’ekibumba [3]..
Ekifaananyi 1 Enkola za Retatrutide ez’okukola [8]..
Enkola za Retatrutide ze ziruwa?
Obujjanjabi bw’omugejjo:
Omugejjo gufuuse ensonga enkulu ey’ebyobulamu mu nsi yonna, ekwatagana nnyo n’okutandika n’okukulaakulana kw’endwadde ez’enjawulo ezitawona. Retatrutide eraga nti ekola bulungi mu kujjanjaba omugejjo. Abalwadde abagejjulukuka abajjanjabwa n’eddagala lya Retatrutide baafuna okukendeera okw’amaanyi mu buzito bw’omubiri. Mu kunoonyereza okwamala wiiki 48 ku mugejjo ogwa Phase 2, abalwadde abajjanjabiddwa n’eddagala lya Retatrutide erya 8mg ne 12mg baafuna okukendeera kw’obuzito ebitundu 22.8% ne 24.2%. Mu kugezesebwa okulala okwa Phase 2 double-blind, randomized, placebo-controlled trial, abalwadde mu bibinja bya dose ez’enjawulo baafuna diguli ez’enjawulo ez’okugejja ku wiiki 24 ne wiiki 48. Ekibinja kya 12mg kyatuuka ku kugejja ebitundu 24.2% ku wiiki 48, ate ekibinja kya placebo kyalaba okukendeera kwa -2.1% kwokka. Retatrutide ekendeeza bulungi ku buzito bw’omubiri mu balwadde abagejjulukuka, n’ewa ekintu ekipya era eky’amaanyi mu kujjanjaba omugejjo. Obujjanjabi bwa Retatrutide ku mugejjo tebukoma ku kukendeeza ku buzito bwa mubiri wabula buyinza n’okulongoosa ensonga endala ez’ebyobulamu ezikwatagana n’omugejjo, gamba ng’okukendeeza ku situleesi y’okusitula ebinywa n’okumalawo obubonero bw’endwadde z’ennyondo ezeekuusa ku mugejjo nga tuyita mu kugejja; okukendeeza ku buzito nakyo kiyinza okuyamba okulongoosa ebizibu ebiva ku mugejjo nga okusannyalala mu tulo [3,6]..
Obujjanjabi bw’okukyusakyusa emmere ey’ekika kya 2:
Enkyukakyuka y’emmere ey’ekika eky’okubiri bulwadde bwa bulijjo obutawona obumanyiddwa olw’okuziyiza insulini n’obutafulumya insulini emala. Retatrutide erina omugaso oguyinza okukozesebwa mu kujjanjaba enkyukakyuka y’omubiri ey’ekika eky’okubiri. Kisitula okufulumya insulini nga kikola ekirungo kya GLP-1 receptor, kiyamba okuziyiza insulini, n’okukendeeza ku glucose mu musaayi. Ebikolwa byayo eby’okukendeeza ku buzito era biyamba okulongoosa embeera y’abalwadde b’omubiri ogw’ekika eky’okubiri, kubanga omugejjo nsonga nkulu mu bulabe eri enkyukakyuka y’omubiri ey’ekika eky’okubiri, era okugejja kuyinza okutumbula okuwulira kwa insulini, okwongera okuyamba mu kufuga glucose mu musaayi. Mu kunoonyereza okwali kuzingiramu abalwadde abalina ekika kya 2 metabolism, Retatrutide yaleeta okugejja ennyo n’okukendeera okw’amaanyi mu miwendo gya hemoglobin A1c (HbA1c), nga HbA1c yakendeera ebitundu 1.64% bw’ogeraageranya ne placebo. Kino kiraga nti Retatrutide tekoma ku kufuga bulungi miwendo gya glucose mu musaayi wabula era etereeza embeera okutwalira awamu ey’abalwadde abalina enkyukakyuka y’omubiri ey’ekika eky’okubiri ng’eyita mu nkola eziwera, omuli okugejja, bwe kityo n’eyongera ku mutindo gw’obulamu bwabwe [6]..
Obujjanjabi bw’obulwadde bw’ekibumba obutaliimu masavu (NAFLD):
NAFLD buvune bw’ekibumba obuva ku situleesi y’enkyukakyuka y’emmere obukwatagana ennyo n’okuziyiza insulini n’okukwatibwa obuzaale, nga buzingiramu embeera ez’enjawulo omuli ekibumba eky’amasavu amangi ekitali kya mwenge, obulwadde bw’ekibumba obutali bwa mwenge, n’obulwadde bwa cirrhosis obukwatagana nabyo. Retatrutide eraga obusobozi obusuubiza mu bujjanjabi bwa NAFLD. Mu kugezesebwa okwa randomized, double-blind, placebo-controlled trial okwali kuzingiramu abeetabye mu kugezesebwa n’obulwadde bw’amasavu mu kibumba obukwatagana n’obutakola bulungi mu mubiri n’amasavu mu kibumba ≥10%, ku wiiki 24, enkyukakyuka eya wakati mu masavu mu kibumba okuva ku ntandikwa yali ya njawulo nnyo mu bibinja bya dose ya Retatrutide: -81.4% mu kibinja kya 8mg, -82.4% mu 12 mg ekibinja, ne +0.3% mu kibinja kya placebo. Kino kiraga nti Retatrutide esobola bulungi okukendeeza ku masavu mu kibumba, ekintu ekikulu ennyo mu kulongoosa endwadde z’ekibumba ez’abalwadde ba NAFLD. Kisuubiza ng’enkola empya ey’obujjanjabi eri NAFLD, eyinza okukendeeza ku kukula kw’obulwadde n’okukendeeza ku bulabe bw’ebizibu eby’amaanyi nga cirrhosis [3]..
Mu bufunzi
Retatrutide eraga obusobozi obusuubiza mu kulongoosa embeera y’obulwadde bw’ekibumba mu balwadde ba NAFLD, ng’ekola okuyita mu nkola eziwera omuli okulungamya enkyukakyuka y’amaanyi, okulongoosa obuziyiza bwa insulini, ebikolwa ebiziyiza okuzimba, n’okukyusakyusa enkyukakyuka y’amasavu.
Ebikwata ku Muwandiisi
Ebintu ebyogeddwako waggulu byonna binoonyerezeddwako, birongooseddwa era ne bikung’aanyizibwa kkampuni ya Cocer Peptides.
Omuwandiisi wa Scientific Journal
Rosenstock, J mumanyi wa njawulo era omulimu gwe gukwatagana nnyo n’amatendekero ag’ekitiibwa agawerako, omuli University of Texas Southwestern Medical Center, University of Texas Dallas, ne Canadian VIGOR Centre. Okunoonyereza kwe kukwata ku bintu bingi nga Endocrinology & Diabetes, General & Internal Medicine, Cardiovascular System & Cardiology, Pharmacology & Pharmacy, ne Research & Experimental Medicine. Ebintu ebyewuunyisa bye yakola mu abasomesa bimufudde okusiimibwa ennyo, nga bwe kiragibwa okusunsulwa enfunda eziwera nga 'Highly Cited Researcher in the field of Clinical Medicine' okuva mu 2017 okutuuka mu 2024, ekiraga ekifo kye eky'amaanyi n'obuyinza bwe obw'amaanyi mu kunoonyereza ku by'obujjanjabi. Rosenstock J awandiikiddwa mu kiwandiiko ekijuliziddwa [4].
