Ib Qho Tshiab Ntawm Cov Tshuaj Tiv Thaiv Antihyperglycemic Imeglimin: Cov Txheej Txheem Tshwj Xeeb Muab Peev Xwm Tsis Muaj Peev Xwm, Yuav Sau Tseg Hauv 2021!

Poxel SA yog lub tuam txhab biopharmaceutical chaw ua haujlwm nyob Lyon, Fabkis, mob siab rau kev tsim kho kev kho mob rau cov kab mob metabolic suav nrog hom 2 mob ntshav qab zib thiab tsis muaj cawv cawv (NASH). Tsis ntev los no, lub tuam txhab tau tshaj tawm cov txiaj ntsig ntawm ob txoj kev tshawb fawb los ntawm kev kho lub qhov ncauj tshiab hypoglycemic tus neeg sawv cev imeglimin. Cov kev tshawb nrhiav 2 tau soj ntsuam qhov ua tau ntawm imeglimin sib cuam tshuam nrog ob qhov kev qhia tshuaj hypoglycemic, metformin (metformin) thiab sitagliptin (sitagliptin, DPP-4 inhibitor). Cov txiaj ntsig tau pom tias hauv cov ntsiab lus noj qab haus huv, imeglimin thiab metformin lossis sitagliptin tswj hwm tsis ua rau muaj kev cuam tshuam ntawm cov chaw muag tshuaj sib raug zoo. Cov txiaj ntsig ntawm ob txoj kev tshawb nrhiav tau tshaj tawm hauv online nyob rau hauv phau ntawv xov xwm cawm neeg lub neej 0010010 quot; Clinical Pharmacokinetics 0010010 quot ;. Cov ntawv sau npe yog: Imeglimin Tsis Yog Qhov Yuav Tsum Sib Cuag Hauv Chaw Sib Raug Mob Pharmacokinetic Sib Koom Tes Thaum Ua ke nrog nrog Ob Cov Metformin lossis Sitagliptin hauv Cov Kev Noj Qab Nyob Zoo.

Lub hom phiaj tseem ceeb ntawm ob qho kev tshawb fawb txog kev sib txuas yeeb tshuaj yog los soj ntsuam cov txiaj ntsig ntawm kev rov ua dua ib zaug ntxiv ntawm metformin lossis sitagliptin nrog imeglimin ntawm cov qauv pharmacokinetic ntawm metformin lossis sitagliptin hauv cov ntsiab lus noj qab haus huv. Lub hom phiaj thib ob ntawm ob txoj kev tshawb fawb tau nyab xeeb thiab pom zoo. Cov txiaj ntsig ntawm ob qho kev tshawb fawb hauv tsev kho mob pom tau hais tias imeglimin muaj kev nyab xeeb thiab zoo rau lub siab, thiab tsis muaj kev hloov pauv hauv chav hauv qib ntawm kev siv tshuaj yeeb tshuaj.

David E. Moller, MD, Poxel Tus Thawj Coj Saib Xyuas Kev Tshawb Fawb tau hais tias: "Hom kab mob ntshav qab zib 2 yog hom mob uas yuav tsum tau siv tshuaj kho ntxiv thaum lub sijhawm dhau los. Rau cov neeg mob uas muaj hom ntshav qab zib 2 uas tau txais kev kho mob uas nws cov ntshav qab zib tsis tuaj yeem tswj tau lawm, Kev tswj kom ua tau zoo feem ntau nce mus rau kev sib xyaw nrog kev siv tshuaj nrog cov tshuaj ntawm kev ua. Cov kev nyab xeeb thiab tiv taus qhov nkhaus ntawm imeglimin ua ke nrog metformin lossis sitagliptin tau pom nyob rau hauv cov kev tshawb fawb no thiab ntau lwm yam kev tshuaj xyuas Kev tshawb fawb txog kev siv cov tshuaj sib txawv yog sib xws, suav nrog theem tseem ceeb III TIMES 2 kev sim siab thiab ob txoj kev sim ua ntej II, uas kuj qhia tau tias muaj peev xwm nce kev ua tau zoo. Cov txiaj ntsig no pom hais tias imeglimin yog ib txoj kev kho mob tshiab ntxiv los ntxiv rau cov tshuaj kho mob qog noj ntshav uas twb muaj lawm Cov kev kho mob ntshav qab zib. 0010010 quot;

Dr Sebastien Bolze, tus thawj coj ua haujlwm thiab thawj coj ua haujlwm ntawm Poxel 0010010 # 39; s kev ua haujlwm tsis zoo thiab kev ua haujlwm, hais tias: 0010010 quot; imeglimin yog thawj cov neeg sib tw ntawm cov tshuaj tshiab tshuaj qhov ncauj rau lub caj dab mitochondrial ua pa, uas yog lub hlwb tsim lub zog. Cov txiaj ntsig no tau qhia, Imeglimin yuav tsis ua rau thaj chaw muaj kev hloov pauv hauv cov chaw muag tshuaj ntawm ob txoj tshuaj tseem ceeb hauv cov tsev kho mob ntshav qab zib hauv lub tsev qiv ntawv kho mob. Cov txiaj ntsig tau zoo sib xws nrog rau cov kev xav ua ntej dhau los thiab kev tshawb nrhiav ntev ntev. 0010010 quot;

Tus qauv molecular ntawm imeglimin (Source: Wikipedia)

imeglimin belongs rau chav kawm tshiab ntawm kev npaj tshuaj hauv qhov ncauj hu ua Glimins. Nws yog thawj tus neeg sib tw ua lag luam ntawm chav kawm no los nkag rau txoj kev kho mob. Nws muaj lub tshuab tshwj xeeb ntawm kev nqis tes ua (MOA) thiab lub hom phiaj mitochondrial bioenergetics. Nws yog tib tus neeg lub qhov ncauj hypoglycemic uas tuaj yeem ua rau tag nrho peb lub plab hnyuv siab raum (nplooj siab, leeg, leeg) koom nrog cov ntshav qabzib homeostasis.

imeglimin tau pom tias yuav txo cov ntshav qab zib los ntawm kev ua kom insulin ntau ntxiv, nce insulin rhiab heev, thiab inhibiting gluconeogenesis. Qhov kev ua haujlwm ntawm kev ua haujlwm no muaj lub peev xwm los tiv thaiv kev ua kom tsis txhob ua rau endothelial thiab diastolic dysfunction, thiab muaj cov kev tiv thaiv ntawm microvascular thiab macrovascular cov teeb meem tshwm sim los ntawm ntshav qab zib. Tsis tas li ntawd, imeglimin tseem muaj cov peev xwm tiv thaiv kev ua neej nyob thiab ua haujlwm ntawm β hlwb. Qhov kev coj ua uas tsis txawv txav no muab imeglimin nrog rau qhov tsis muaj peev xwm yuav kho tus kab mob ntshav qab zib hom 2 ntshav qab zib nyob rau yuav luag txhua theem ntawm cov qauv kev kho ntshav qab zib tam sim no, suav nrog kev kho mob ntshav qab zib lossis kho ntxiv rau lwm yam kab mob ntshav qab zib.

Lub imeglimin mechanism yog qhov tshwj xeeb thiab muaj lub peev xwm los pab tswj hom 2 mob ntshav qab zib ntawm txhua theem ntawm tus kab mob

Poxel thiab Sumitomo Pharmaceutical tsim kev sib koom tes koom ua ke nyob rau lub Kaum Hlis 2017 txhawm rau txhim kho thiab ua lag luam imeglimin rau kev kho mob ntawm hom 2 mob ntshav qab zib hauv Nyiv, Suav, Kaus Lim Qab Teb, thiab cuaj lub teb chaws hauv Southeast Asia thiab East Asia. Thaum kawg ntawm xyoo tas los, theem III kev tsim kho kev kho mob ntawm imeglimin rau kev kho mob ntawm hom 2 mob ntshav qab zib tau ua tiav. Lub phiaj xwm tshuaj xyuas qhov ua tau zoo thiab kev nyab xeeb ntawm imeglimin hauv kev kho mob rau cov neeg mob Japanese uas muaj mob ntshav qab zib hom 2 los txhawb qhov kev nyab xeeb thiab ua haujlwm ntawm imeglimin hauv pawg neeg mob sib txawv. Txoj haujlwm no suav nrog peb qhov kev tshawb fawb nyob qib III uas muaj ntau dua li ntawm 1, 100 tus neeg mob. Hauv cov kev tshawb fawb no, imeglimin tau muab tshuaj rau ntawm 1 000 mg ob zaug ib hnub.

Cov txiaj ntsig ntawm TIMES qhov project tau lees paub qhov sib txawv ntawm imeglimin, qhia tias imeglimin muaj qhov ua tau zoo ntawm ob qho kev ua kom nce insulin zais thiab txhim kho insulin rhiab heev, thiab nws pom tias muaj kev cuam tshuam hypoglycemic thaum ua ke nrog tshuaj nrog kev ua tiav ntawm kev ua, suav nrog DPP -4 inhibition Agents, SGLT 2 inhibitors, biguanides, sulfonylurea tshuaj, gleneides, alpha-glucosidase inhibitors, thiazolidine tshuaj, GLP 1 receptor agonists. Raws li cov ntaub ntawv hauv cov txheej txheem, Poxel thiab Sumitomo Cov Tshuaj Noj tau npaj rau kev xa tawm imeglimin 0010010 # 39; s daim ntawv thov kev siv tshuaj tshiab (NDA) hauv Nyij Pooj, uas xav tias yuav xa hauv peb lub hlis thib peb ntawm 2020 thiab yuav nqa cov khoom rau lub khw hauv Nyij Pooj hauv 2021.

Lub Ob Hlis 2018, Roivant Sciences thiab Poxel tau kos npe $ 650 lab pom zoo los tsim thiab ua lag luam imeglimin hauv kev ua lag luam sab nraum cov tebchaws thiab thaj chaw, suav nrog Tebchaws Meskas thiab European Union. Tam sim no, Poxel tab tom ua haujlwm nrog Metavant, lub chaw tsim khoom ntawm Roivant Sciences, kom nce qib imeglimin mus rau theem III qhov project.

imeglimin muaj qhov tshwj xeeb thiab muaj qhov sib txawv thiab kev nyab xeeb zoo thiab kev tiv taus siab. Cov tshuaj muaj peev xwm dhau los ua qhov kev xaiv tseem ceeb tshiab rau kev kho mob los pab cov neeg mob tswj ntshav qab zib hom 2 mob ntshav qab zib nyob rau ntau theem ntawm tus kab mob. （Bioon.com）