Nkọwa ngwaahịa
Retatrutide bụ peptide agonist ọhụrụ nke na-ezubere onye na-anabata glucagon (GCGR), nnabata insulinotropic polypeptide na-anabata glucose (GIPR), na onye na-anabata glucagon dị ka peptide-1 (GLP-1R). Retatrutide na-arụ ọrụ GCGR, GIPR, na GLP-1R mmadụ nwere ụkpụrụ EC50 nke 5.79, 0.0643, na 0.775 nM, n'otu n'otu, na òké GCGR, GIPR, na GLP-1R nwere ụkpụrụ EC50 nke 2.32, 0.0.41, na Ọ na-eje ozi dị ka ngwá ọrụ nyocha dị mkpa na ọmụmụ banyere oke ibu na nsogbu metabolic.
Retatrutide na-arụ ọrụ nke ọma n'ụzọ mgbaàmà GLP-1R ma na-akpali mmepụta insulin dabere na glucose site n'ime ma GIP na GLP-1 ndị na-anabata ya. Nke a peptide sịntetik na-egosipụta ikike hypoglycemic nwere ike ma mepụta ya dị ka ihe mgbochi ọrịa shuga maka ụdị ọrịa shuga 2 (T2D). Ọ na-akwalite mwepụta insulin ma na-ebelata glucagon secretion na-adabere na glucose.
Na mgbakwunye, egosipụtara na Retatrutide na-egbu oge mkpofu afọ, na-ebelata ma ibu ọnụ na ọkwa glucose postprandial, belata oriri oriri, ma na-ebute oke ibu ahụ na ndị nwere T2D.
Ọrụ ndu
Retatrutide (LY3437943) bụ otu peptide nwere conjugated lipid nke na-arụ ọrụ dị ka agonist dị ike nke GCGR mmadụ, GIPR na GLP-1R. E jiri ya tụnyere glucagon mmadụ na GLP-1, Retatrutide na-egosipụta ike dị ala na GCGR na GLP-1R (0.3 × na 0.4 ×, n'otu n'otu) mana na-egosipụta ike nke ọma (8.9 ×) na GIPR ma e jiri ya tụnyere glucose-based insulinotropic polypeptide (GIP).
Usoro nke Omume
N'ime ọmụmụ ihe metụtara oke ọrịa shuga nwere nephropathy, nchịkwa Retatrutide belatara nke ukwuu albuminuria yana mmụba nzacha glomerular. A na-ekwu na mmetụta nchebe a sitere na ịgbalite ụzọ mgbaàmà GLP-1R/GR, nke na-eme ka ihe mgbochi mkpali na mgbochi apoptotic na anụ ahụ akwara.
Retatrutide na-agbanwekwa permeability glomerular ozugbo, na-eme ka ikike itinye uche na mmamịrị dịkwuo mma. Nchoputa nke mbu na-egosi na, ma e jiri ya tụnyere ọgwụgwọ ọrịa akụrụ na-adịghị ala ala nke dị ka ACE inhibitors na ARBs, Retatrutide na-emepụta mbelata nke ukwuu na albuminuria mgbe naanị izu anọ gasịrị. Ọzọkwa, ọ egosipụtala ịdị irè dị ukwuu n'ibelata ọbara mgbali systolic karịa ndị na-egbochi ACE ma ọ bụ ARB, na-enweghị mmetụta ọjọọ ọ bụla a hụrụ.
Mmetụta dị n'akụkụ
Mmetụta kachasị emetụta Retatrutide bụ eriri afọ na ọdịdị, gụnyere ọgbụgbọ, afọ ọsịsa, vomiting, na afọ ntachi. Mgbaàmà ndị a na-adịkarị nwayọọ ma na-agafeghị oke ma na-edozi ya site na mbelata dose. Ihe dị ka 7% nke isiokwu ahụ kọkwara mmetụta nke nrịanrịa akpụkpọ ahụ. A hụrụ mmụba nke obi obi na izu 24 n'ime ìgwè ndị dị elu, nke mesịrị laghachi na ọkwa mmalite.