1 ngwa (10 Vials)
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▎ Nyochaa Retatrutid
Retatrutid bụ ọgwụ peptide ọhụrụ. Dị ka agonist atọ na-anabata ya, ọ na-arụ ọrụ na glucagon-dị ka peptide-1 (GLP-1), glucose-based insulinotropic polypeptide (GIP), na ndị na-anabata glucagon n'otu oge. Ọ na-enyere ndị mmadụ n'otu n'otu aka ifelata site n'ịchịkwa agụụ nke ukwuu, ịkwalite afọ ojuju, igbochi agụụ, na ịba ụba ume ike.
Na mgbakwunye, Retatrutid nwekwara ike melite ọtụtụ ihe ngosi ihe egwu cardiometabolic, dị ka ọbara mgbali elu, hemoglobin glycated, glucose ọbara na-ebu ọnụ, insulin, mkpokọta cholesterol, cholesterol lipoprotein dị ala, na triglycerides. Ọ na-enwekwa mmetụta dị mma na ndị ọrịa nwere ọrịa imeju na-adịghị egbu egbu, na-eme ka abụba imeju nke ọtụtụ ndị sonyere na-alaghachi na nkịtị.
E jiri ya tụnyere otu agonists ma ọ bụ nke abụọ, Retatrutid na-achịkwa glucose ọbara, ịdị arọ ahụ, wdg site n'ọtụtụ akụkụ site n'ime ka ndị na-anabata GLP-1, GIP na glucagon (GCG) rụọ ọrụ n'otu oge. N'ịkọwapụta, ọ nwere ike imeziwanye nsogbu metabolic karịa ma nwee uru pụrụ iche na akụkụ ndị dị ka mbelata ibu, mbelata steatosis imeju, na ịhazi ọkwa glucose ọbara.
Omume mmekọrịta nke ọtụtụ ndị na-anabata Retatrutid na-eme ka ọ dị irè karịa GLP-1 agonists na-anabata ma ọ bụ abụọ agonists na-achịkwa metabolism na ịchịkwa ibu ahụ, na-enye nhọrọ ọgwụgwọ ọhụrụ maka ndị ọrịa nwere oke ibu na ụdị ọrịa shuga 2.
▎ Nnyocha Retatrutid
Kedu ihe ndabere nyocha nke Retatrutid?
Ibu ibu aghọwo otu n'ime ihe ịma aka ahụike ọha ama ama na ọha mmadụ nke oge a. Ọ nwere ike ibute ọtụtụ nsogbu ahụike dịka ọrịa shuga mellitus ụdị 2, ọrịa obi, ọbara mgbali elu, dyslipidemia, na ọrịa imeju na-adịghị egbu egbu. Site na mmụba na-aga n'ihu na mmụba nke oke ibu, a na-enwewanye mkpa ngwa ngwa maka ọgwụgwọ ọhụrụ nke nwere ike ijikwa oke ahụ nke ọma ma melite ọnọdụ ahụike [1] . Ọ bụ ezie na ntinye aka n'ụdị ndụ, dị ka mmega ahụ na-abawanye na njikwa nri, bụ isi ihe na-eme ka ọ ghara ịdị arọ, ọ na-esiri ọtụtụ ndị ọrịa buru oke ibu ike ịnọgide na-ebufu ibu ogologo oge.
Retatrutid, dị ka agonist atọ na-anabata ihe, nwere ike ime ihe na glucagon-dị ka peptide-1 nnabata.
GLP-1R), onye na-anabata insulinotropic polypeptide na-anabata glucose (GIPR), na onye na-anabata glucagon (GCGR). Usoro ihe omume nke ọtụtụ ndị na-anabata ya na-enye ya nnukwu uru n'ọhịa nke ịbelata ibu. E jiri ya tụnyere ọgwụ na-ebelata ibu nke na-eme naanị otu onye na-anabata ya, Retatrutid nwere ike ịhazi usoro metabolic nke anụ ahụ n'ụzọ zuru ezu [1] . Retatrutid na-enweta oke ibu site n'ịchịkwa ọtụtụ ndị na-anabata homonụ, ọ bụghị naanị na-egosi arụmọrụ dị ịrịba ama kamakwa na-enwe mmetụta dị nro nke eriri afọ. Na mgbakwunye, dị ka onye na-anabata agonist ugboro atọ, Retatrutid nwere mmetụta mbelata ịdị arọ dị ike karị yana ọnụ ọgụgụ dị ukwuu nke ndị ọdabara ma e jiri ya tụnyere ọgwụ ọhụrụ ọnwụ arọ ndị ọzọ.
Kedu ihe bụ Retatrutid?
Retatrutid bụ glucagon na-eme ogologo oge dị ka peptide-1 (GLP-1) agonist nnabata. A na-emezi ya ma kwalite ya dabere na usoro nke GLP-1 eke, ọ nwere ike jikọta ma rụọ ọrụ GLP-1 onye na-anabata ya, na-arụ ọrụ physiological dị ka nke GLP-1 eke, dị ka ịkwalite secretion insulin, igbochi glucagon secretion, na-egbu oge ịpụsị gastric, ibelata agụụ, wdg.
Kedu ihe bụ usoro Retatrutid?
Usoro omume nke Retatrutid sitere na mmetụta agonist ya na ọtụtụ ndị na-anabata ya. Nke mbụ, mmetụta ya na-akpata ya na onye na-anabata glucagon-dị ka peptide-1 (GLP-1R) nwere ike ime ka mmepụta insulin dịkwuo elu, na-egbochi glucagon secretion, na-ebelata ọkwa glucose ọbara, ma n'otu oge ahụ na-egbu oge nkwụsị nke gastric, na-abawanye satiety, ma belata oriri [2] . Nke abuo, mmetụta agonist ya na onye na-anabata insulinotropic polypeptide (GIPR) na-adabere na glucose nwere ike ịkwalite mmepụta insulin, mee ka ojiji glucose dịkwuo elu, ma na-emetụta abụba abụba, na-egbochi lipolysis na ịkwalite njikọ abụba [2] . Ọzọkwa, mmetụta agonistic nke Retatrutid na onye na-anabata glucagon (GCGR) na-akwalitekarị glycogenolysis na gluconeogenesis na imeju, na-abawanye ọkwa glucose ọbara. Otú ọ dị, n'okpuru ọrụ nke Retatrutid, mmetụta a na-ebuli glucose na-ebelata site na mmetụta nke abụọ ndị ọzọ na-anabata ya, na-akwalite lipolysis na ibelata mkpokọta abụba [2] . Ụdị omume a nwere ọtụtụ ebumnuche nwere ike ịdị irè karịa n'ịgwọ oke ibu karịa otu agonists nnabata.
Site n'otu oge na-eme ka ndị nnata atọ a rụọ ọrụ, Retatrutid nwere ike ịmepụta mmetụta dị iche iche nke usoro metabolic ma mepụta mmetụta ọgwụgwọ na oke ibu na ọrịa ndị metụtara ya. N'ihe banyere ịhazi ọkwa glucose ọbara, ebe ọ bụ na ịgbalite GLP-1R na GIPR na-akwalite secretion insulin ma na-egbochi glucagon secretion, na ntinye nke GCGR na-emebi site na mmetụta nke abụọ ndị ọzọ na-anabata ya, Retatrutid nwere ike ịhazi ọkwa glucose ọbara nke ọma, nke dị oke mkpa maka ọgwụgwọ ụdị ọrịa shuga 22 . N'ihe banyere ibelata mkpokọta abụba, ịgbalite GCGR na-akwalite lipolysis ma belata mkpokọta abụba, ebe ịgbalite GLP-1R na-abawanye satiety ma belata oriri nri, na-ebelata njikọ abụba [1] . Na mgbakwunye, Retatrutid nwekwara mmetụta dị mma na ọrịa imeju na-adịghị egbu egbu. Ọ nwere ike ibelata abụba dị n'imeju ma melite ọrụ imeju.


HbA1c, arọ ahụ, ọbara mgbali elu, na lipids Data bụ ụzọ opekata mpe-squares (ya na mpe mpe mpe mpe mpe mpe mpe mpe mpe mpe mpe mpe mperi na-egosi SE) site na nhazi nyocha nrụpụta ọrụ, belụsọ na amataghi ya.
Isi mmalite: PubMed [4]
N'akụkụ dị aṅaa ka Retatrutid na-egosi mmetụta ya?
Retatrutid na-egosipụta mmetụta dị ukwuu n'ọtụtụ akụkụ
Mmetụta ọnwụ dị oke mkpa: Retatrutid egosipụtala mmetụta ọnwụ dị oke arọ n'ọtụtụ ule ụlọ ọgwụ. Dịka ọmụmaatụ, n'ime ọmụmụ ụlọ ọgwụ metụtara ndị okenye 338 (Jastreboff AMM, 2023), ndị ọrịa a na-emeso ya na doses dị iche iche nke Retatrutid nwetara nnukwu ibu ibu na izu 48. N'ime ha, ndị ọrịa nọ na 12mg dose otu tụfuru 24.2% nke ịdị arọ ahụ ha, na ọnụ ọgụgụ dị elu nke ndị ọrịa nwetara oke ibu na ogo dị iche iche. Dịka ọmụmaatụ, n'etiti ndị ọrịa na-anata 4mg, 8mg, na 12mg doses, 92%, 100%, na 100% nke ndị ọrịa, n'otu n'otu, tụfuru 5% ma ọ bụ karịa nke ahụ ha. N'ọmụmụ ihe ọzọ [3] , ule abụọ a na-achịkwa nke na-agụnye ndị ọrịa 353 nwere ụdị ọrịa shuga mellitus nke 2 gosiri na e jiri ya tụnyere placebo, Retatrutid nwere ike ibelata arọ ahụ nke ndị ọrịa site na 11.89kg, ma belata haemoglobin glycated (HbA1C). Na mgbakwunye, na nnwale nke ndị okenye nwere oke ibu na-enweghị ọrịa shuga, Retatrutid kpatara mbelata ịdị arọ 24.2% na ndị ọrịa, na 83% nke ndị ọrịa tụfuru 15% ma ọ bụ karịa nke ahụ ha na izu 48. Nsonaazụ ndị a na-egosi na Retatrutid nwere ikike dị ukwuu na mbelata ibu.
Ọgwụgwọ nke ụdị ọrịa shuga mellitus nke 2: Retatrutid na-egosikwa ụfọdụ ike na ọgwụgwọ ụdị ọrịa shuga mellitus nke 2. N'ime ule ụfọdụ ụlọ ọgwụ, Retatrutid egosila mbelata nke haemoglobin glycated (HbA1c) yana mbelata ibu nke dabere na dose. Dịka ọmụmaatụ, n'otu nyocha, na ndị ọrịa nwere ụdị ọrịa shuga mellitus nke 2, Retatrutid gosipụtara mmetụta nchịkwa glucose ọbara dị ukwuu. E jiri ya tụnyere placebo, haemoglobin glycated belatara site na 1.64% [3] . Tụkwasị na nke a, n'ime usoro 2 nke a na-ahụ anya, nke kpuru ìsì, na-arụ ọrụ na-arụ ọrụ na-arụ ọrụ, ụdị anụmanụ nwere ụdị ọrịa shuga mellitus 2, mgbe ha nwetasịrị ọgwụgwọ Retatrutid, gosipụtara mbelata dị ukwuu na ọkwa hemoglobin glycated, na ịdị arọ ahụ ha na-ebelatakwa n'ụzọ dabere na dose [4] . Enwere ike ịsị na nke a bụ nsonaazụ zuru oke nke ọgwụ na GLP-1, GCGR, na GIPR, nke na-eme ka metabolism glucose dịkwuo elu na nguzozi ike.
Mmelite nke ihe ize ndụ nke obi: Retatrutid nwere ike ọ bụghị naanị ibelata ibu ahụ kamakwa melite ihe egwu obi, dị ka profaịlụ lipid serum na ọkwa hemoglobin glycated. Nke a na-egosi njikọ chiri anya pathophysiological n'etiti oke ibu na ọrịa obi, na Retatrutid nwere ike melite ahụike obi nke ndị ọrịa buru ibu site na ọtụtụ ụzọ. Dịka ọmụmaatụ, ibelata ọkwa na-abụghị HDL-C, apoB, na LDLP nwere ike ibelata ihe ize ndụ nke atherosclerosis; Mbelata ọkwa hemoglobin glycated nwere ike imezi njikwa glucose ọbara n'ime ndị ọrịa nwere ọrịa shuga, si otú ahụ belata ihe ize ndụ nke nsogbu obi obi [3, 5, 6]..
Ọgwụgwọ nke ọrịa imeju abụba na-adịghị egbu egbu (NAFLD): Retatrutid bụ peptide nke na-anabata glucagon receptor (GCGR), glucose-based insulinotropic polypeptide receptor (GIPR), na glucagon-dị ka peptide-1 receptor (GLP-1R). Nnyocha egosiwo na Retatrutid nwere ikike ịgwọ ọrịa imeju abụba na-adịghị egbu egbu. N'ime otu ọmụmụ, a na-eduzi ule a na-achịkwaghị achịkwa, nke kpuru ìsì abụọ, ebe a na-achịkwa placebo maka izu 48 na ndị na-eso ya nwere ọrịa imeju abụba na-emetụta metabolic dysfunction na abụba imeju nke ≥10%. Nsonaazụ gosiri na n'ime izu 24, nkezi mgbanwe mgbanwe na abụba imeju site na ntọala nke ndị sonyere na-eji usoro dị iche iche nke Retatrutid (1mg, 4mg, 8mg, na 12mg) bụ -42.9%, -57.0%, -81.4%, na -82.4%, n'otu n'otu, ebe nke ahụ nọ na placebo bụ + 7.3 % . Nke a na-egosi na Retatrutid nwere ike inwe mmetụta ọgwụgwọ dị ukwuu na ọrịa imeju na-adịghị egbu egbu.
Na mmechi, dị ka akwụkwọ akụkọ atọ agonist receptor, Retatrutid na-egosi nnukwu ikike na ọgwụgwọ oke ibu na ọrịa ndị metụtara ya. Ọ nwere ike ịhazi metabolism nke mmadụ site n'ọtụtụ akụkụ site na ịgbalite onye na-anabata glucagon, onye na-anabata insulinotropic polypeptide na-adabere na glucose, yana onye na-anabata glucagon dị ka peptide-1, na-eme ka njikwa glucose ọbara dịkwuo mma, na-ebelata ibu ahụ, na ịhazi metabolism lipid. Mpụta nke Retatrutid ewetala nhọrọ ọgwụgwọ ọhụrụ maka ndị ọrịa nwere oke ibu, ụdị ọrịa shuga mellitus 2, wdg. A na-atụ anya na ọ ga-emebi njedebe nke ọgwụ agonist otu onye na-anabata ya, na-enye ngwa ọgụ siri ike maka idozi nsogbu ndị siri ike nke oke ibu na ọrịa metabolic, na-akwalite mmepe mmepe nke ngalaba ahụike metụtara ya, meziwanye ndụ ndị ọrịa, ma belata ibu ahụike ọha.
Banyere Onye dere ya
Ihe niile a kpọtụrụ aha n'elu bụ Cocer Peptides na-enyocha, dezie ma chịkọta ya.
Onye ode akwụkwọ akụkọ sayensị
Rosenstock J bụ ọkà mmụta nwere mmetụta dị ukwuu na ngalaba ahụike, na-arụkọ ọrụ ọnụ na ụlọ ọrụ dịka Mahadum Texas Southwestern Medical Center na Mahadum Texas Dallas. Ọ na-eduzi nyocha na ụlọ ọrụ dịka Canadian VIGOR Center na Veloc Clin Res Ctr Med City.
Nchoputa ya gbasara endocrinology na metabolism, sistemu obi obi na akwara obi, pharmacology, na nnwale nnwale, na-elekwasị anya na ọrịa shuga, oke ibu, na ọgwụgwọ ndị metụtara ya na mmepe ọgwụ. J Rosenstock enwetawo ihe ịga nke ọma dị ịrịba ama na nkà mmụta ọgwụ, n'ịbụ onye a na-akpọ onye nyocha nke ukwuu site na 2017 ruo 2024. Nke a na-egosipụta mmetụta dị elu na nkwanye ùgwù sara mbara nke ọrụ ya. Site na mmekorita ya na ụlọ ọrụ nyocha dị iche iche, ọ tụgharịrị nke ọma nchọpụta nchọpụta bụ isi n'ime ngwa ụlọ ọgwụ, na-erite uru ndị ọrịa nwere ọrịa metabolic na ọrịa obi na ịkwalite sayensị ahụike. A na-edepụta Rosenstock J n'akwụkwọ ntụaka [4].
▎ Okwu ndị dị mkpa
[1] Kaur M, Misra S. Ntụleghachi nke nyocha ọgwụ retatrutide, onye nnọchi anya agonist atọ nke akwụkwọ akụkọ maka ọgwụgwọ oke ibu [J]. Akwụkwọ akụkọ European nke Clinical Pharmacology, 2024,80 (5): 669-676.DOI: 10.1007 / s00228-024-03646-0.
[2] Jastreboff AM, Kaplan LM, Frias JP, et al. Triple-Hormone-Receptor Agonist Retatrutid maka oke ibu - Ọnwụnwa nke 2 [J]. Akwụkwọ akụkọ ọgwụ New England, 2023,389 (6): 514-526.DOI: 10.1056/NEJMoa2301972.
[3] Lopez DC, Pajimna JT, Milan MD, et al. 7792 arụmọrụ nke Retatrutid maka Mbelata ibu na Mmetụta Cardiometabolic ya n'etiti ndị okenye: Nyochaa usoro na Meta-Analysis[J]. Akwụkwọ akụkọ nke Endocrine Society, 2024,8 (1): 163-749.DOI: 10.1210/jendso/bvae163.749.
[4] Rosenstock J, Frias J, Jastreboff AM, et al. Retatrutid, GIP, GLP-1 na glucagon agonist receptor, maka ndị nwere ụdị ọrịa shuga 2: ihe na-adịghị ahụkebe, ndị ìsì abụọ, placebo na ndị na-arụ ọrụ na-achịkwa, otu-otu, nnwale 2 nke emere na USA[J]. Lancet, 2023,402 (10401):529-544.DOI:10.1016/S0140-6736(23)01053-X.
[5] Nicholls S, Pirro V, Lin Y, et al. Agonist retatrutide na-anabata homonụ atọ na-eme ka profaịlụ lipoprotein na apolipoprotein dịkwuo mma na ndị sonyere nwere oke ibu ma ọ bụ oke ibu[J]. Akwụkwọ akụkọ obi European, 2024,45.DOI:10.1093/eurheartj/ehae666.1501.
[6] Ray A. Retatrutid: agonist atọ incretin nnabata maka njikwa oke ibu [J]. Echiche ndị ọkachamara na ọgwụ nyocha, 2023,32 (11): 1003-1008.DOI: 10.1080/13543784.2023.2276754.
[7] Sanyal AJ, Kaplan LM, Frias JP, et al. agonist Triple hormone receptor agonist retatrutide maka ọrịa ọrịa imeju steatotic metụtara metabolic dysfunction: usoro 2a na-enweghị usoro [J]. Ọgwụ okike, 2024,30 (7): 2037-2048.DOI:10.1038/s41591-024-03018-2.
Edemede na ozi ngwaahịa niile enyere na webụsaịtị a bụ naanị maka mgbasa ozi na ebumnuche mmụta.
Ngwaahịa ndị enyere na webụsaịtị a bụ naanị maka nyocha in vitro. A na-eme nyocha in vitro (Latin: * na iko *, nke pụtara na ihe eji enyo) na mpụga ahụ mmadụ. Ngwaahịa ndị a abụghị ọgwụ, ndị US Food and Drug Administration (FDA) akwadoghị ya, ha agaghịkwa eji ya gbochie, gwọọ, ma ọ bụ gwọọ ọnọdụ ahụike ọ bụla, ọrịa, ma ọ bụ ọrịa. Iwu amachibidoro nke ọma iwebata ngwaahịa ndị a n'ime ahụ mmadụ ma ọ bụ anụmanụ n'ụdị ọ bụla.