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I-Elafibranor (GFT505) Powder-The New Drug for NASH Treatment Study

Yini i-Elafibranor (GFT505)?

I-Elafibranor (GFT505) powder (923978-27-2), ngumuthi wokuhlola ocwaningo lwawo oluqhubekayo. Ngokuyinhloko, ukutadisha nokuthuthukiswa kwayo yiGenfit kusekelwe ekusebenzeni kwe- I-Elafibranor (GFT505powder (923978-27-2) ekulweni nezifo ezinjenge-non-alcoholic fat onesifo sesibindi, i-dyslipidemia, ukumelana ne-insulin, kanye nesifo sikashukela.

 

I-Elafibranor (GFT505) indlela yokusebenza

I-Elafibranor (GFT505) powder iyindlela yokwelashwa ngomlomo esebenza kuma-subtypes amathathu e-PPAR. Kubandakanya i-PPARa, i-PPARd, ne-PPARg. Kodwa-ke, isebenza ikakhulu nge-PPARa.

Indlela yokusebenza ye-Elafibranor iyinkimbinkimbi njengoba ifaka ngokuhlukile ama-cofactors ku-receptor yenuzi. Ngenxa yalokhu, lokhu kuholela ekwenziweni umehluko kofuzo kanye nomphumela webhayoloji.

I-Elafibranor (GFT505) powder iyakwazi ukukhomba nokuphrinta umsebenzi okhethiwe we-nuclear receptor modulator (SNuRMs). Ngenxa yalokho, inikeza ukusebenza okuthuthukile ngemiphumela emibi encishisiwe.

Womabili ama-molecule we-multimodal ne-pluripotent akhombisile ukuthi ayasebenza ekulweni nezimo ezahlukahlukene. Kubandakanya ukumelana ne-insulin nesifo sikashukela, ukuvuvukala, ukukhuluphala ngokweqile, ne-lipid triad, okubonakala ngokwanda kwe-cholesterol ye-HDL kanye nokwehliswa kwe-cholesterol ye-LDL ne-triglycerides.

Umehluko phakathi kwendlela yokusebenza ye-Elafibranor kanye namanye amakhemikhali akhomba ama-PPAR ku-NASH (nonalcoholic steatohepatitis) iqiniso lokuthi ayikhombisi noma yimuphi umsebenzi we-PPARy wemithi.

Ngenxa yalokho, I-Elafibranor abasebenzisi abayitholi imiphumela emibi engafuneki ehlotshaniswa nokwenza kusebenze kwe-PPARy. Imiphumela emibi enjalo ifaka phakathi; ukugcinwa kwe-fluid, i-edema, kanye nesisindo sazo zonke ezikhulisa ubungozi bomuntu ekuhluphekeni kwenhliziyo.

 

I-Elafibranor (GFT505) yesifundo sokwelashwa kweNash

NASH (nonalcoholic steatohepatitis) yisifo sesibindi esiholela ekuvukeleni nasekuwohlokeni kwama-hepatocyte kanye nokuqoqwa kwamafutha aziwa nangokuthi ngamaconsi e-lipid. Imvamisa, izimo ezithile zezempilo ezifana nesifo se-metabolic syndrome, uhlobo lwesibili sikashukela, kanye nokukhuluphala ngokweqile kuyimbangela yokuqala ye-nonalcoholic steatohepatitis (NASH), kanye nesifo sesibindi esinamafutha angenalo utshwala (NAFLD).

 

I-Elafibranor (GFT505) Powder-The New Drug for NASH Treatment Study

 

Namuhla, abantu abaningi bahlushwa yilesi sifo esibulalayo. Ingxenye ethusayo ngakho ukuthi kungaholela ku-cirrhosis, isimo esenza isibindi singakwazi ukusebenza. Kungathuthuka futhi kumdlavuza wesibindi futhi kwezinye izimo, kubangele ukufa.

Izindaba ezidabukisayo nge-NASH (nonalcoholic steatohepatitis) ukuthi ayikhethi ubudala futhi iyaqhubeka nokuthinta wonke umuntu. Okubi kakhulu ukuthi izimpawu zesifo zingabonakaliswa, futhi umuntu kungenzeka angazi ukuthi baphethwe yilesi sifo kuze kube yilapho sesithuthuke kamuva.

Ukulimala nokulimala okulethwe yi-NASH (i-nonatocoholic steatohepatitis) futhi kungaholela ezinkingeni zenhliziyo namaphaphu. Njengoba abantu abaningi manje behlushwa yilesi simo esivela ezifweni zesibindi esinamafutha angenalo utshwala, abacwaningi bafuna ezinye izindlela zokwelashwa ngaphandle kokufakelwa kwesibindi.

Enye yezidakamizwa ezifundelwa ukwelashwa kwe-NASH yi-Elafibranor (GFT505) powder (923978-27-2). Kuze kube manje, kukhombisile ukudala imiphumela emihle ezicini ezimbili eziphambili zalesi sifo, ie, ukubhalaza nokuvuvukala. Ubuhle obunayo ukuthi iyabekezeleleka kakhulu futhi ngeke yenze umuntu ahlupheke nganoma iyiphi imiphumela emibi. Kungenxa yalesi sizathu ukuthi i-US Food and Drug Administration inikeze ukubizwa okusheshayo kwalesi sidakamizwa Ukwelashwa kwe-NASH.

Njengamanje, i-Elafibranor (GFT505) powder isesivivinyo somtholampilo weSigaba 3, esibizwa nangokuthi yi-RESOLVE IT.

HLOLA-IT

Ucwaningo lomhlaba wonke oluqale kwikota yokuqala yonyaka we-2016, olwenziwe ngokungahleliwe, olulawulwa yi-placebo ku-ratio 2: 1 kanye ne-blind-blind. Iziguli ezibambe iqhaza kulolu cwaningo yilabo abahlushwa yi-NASH (NAS> = 4) ne-fibrosis (F2 noma i-F3 izigaba lapho ukulimala kwesibindi sekuvele khona. Kuwo wonke lolu cwaningo, iziguli zizonikezwa ngomthamo we-Elafibranor (GFT505) I-120mg noma i-placebo kanye ngosuku.

Iziguli eziyinkulungwane zokuqala ezizobhaliswa zizosiza ukukhombisa ukuthi ngabe i-NASH iyelapheka nge-Elafibranor (GFT505) ngaphandle kwe-fibrosis ebhebhetheka uma kuqhathaniswa nalabo abaphathwa nge-placebo.

Iqembu lokuqala labhaliswa ngo-Ephreli 2018, kanti ukucutshungulwa kwemiphumela kuzobikwa ngasekupheleni kuka-2019. Imininingwane ebikiwe izonquma ukuthi ngabe i-Elafibranor ivunywa yini yi-US Food and Drug Administration njengoba ithola imvume yezomthetho yi-European Medicines Agency, kahle eyaziwa ngokuthi i-EMA ngo-2020.

Ucwaningo luqhubekele phambili ngoDisemba 2018 lapho i-Data Safety Monitoring Board (DSMB) ivuma ukuqhubeka kwecala ngaphandle kokushintshwa. Lokho kwakungemva kokubuyekezwa kwangaphambi kokuhlelwa kwedatha yokuphepha eyenziwe ngemuva kwezinyanga ezingamashumi amathathu.

 

I-Elafibranor (GFT505) Powder-The New Drug for NASH Treatment Study

 

Imiphumela yocwaningo lwangaphambi kokuhlola kanye nezifundo zokwelapha ekwelashweni kwe-NASH

Ukusebenza nokuphepha kwe-Elafibranor ekwelashweni kwe-NASH kuhlolwe esikhathini esedlule ngokusebenzisa izinhlobo zezifo eziningi. Esigabeni 5a 2a, kwenziwa izilingo ezahlukahlukene kubantu abahlukahlukene beziguli ezinesifo se-metabolic. Kubandakanya labo abane-type 2 diabetes noma i-pre-diabetes kanye ne-atherogenic dyslipidemia. Ngesikhathi kwenziwa ucwaningo, kwabonwa ukuthi u-Elafibranor wakhuphula isikhundla;

  • Inciphise ingozi yokuhlushwa yizinkinga zenhliziyo
  • Amamaki ancishisiwe wokulimala kwesibindi
  • Izici zokulwa nokuvuvukala
  • Ukwanda kokuzwela kwe-insulin
  • I-glucose homeostasis
  • Iphrofayili ye-lipidoprotective lipid.

Isivivinyo sesigaba 2b esaqalwa ngonyaka we-2012 sasiyisivivinyo esikhulu kakhulu sangaphakathi kanye nocwaningo lwangempela lokuqala olwenziwa e-NASH. Kungaleso sikhathi lapho u-Elafibranor athola khona umbono ophakanyisiwe we-FDA wokuqedwa kwe-NASH ngaphandle kokukhula kwe-Fibrosis. "Lokho bekuyiso isiphetho esiyinhloko sokuqulwa kwecala 3 lesigaba esisaqhubekayo.

Kwaqashelwa ukuthi iziguli ezathola ukwelashwa kwe-NASH nge-Elafibranor zaphawula ukuthuthuka kwezimpawu zokungasebenzi kwesibindi njenge-ALP, GGT, ne-ALT. Ngokuhlolwa kwamaphuzu wesibili, kube nokuqaphelisisa ukuthi isilinganiso sika-Elafibranor (GFT505) esingu-120mg sinikeze imiphumela yokwelashwa ezicini zobungozi be-cardiometabolic ezihambisana ne-NASH, Zazihlanganisa;

  • Imiphumela yokulwa nokuvuvukala
  • Ukuthuthukiswa kokuzwela kwe-insulin kanye ne-glucose metabolism ezigulini ezinesifo sikashukela
  • Thuthukisa amazinga we-lipoproteins kanye ne-plasma lipids.
Ukusebenza kwe-Elafibranor ekwelapheni i-NASH yezingane

Izinga izingane ezihlushwa ukukhuluphala ngalo likhuphuke kakhulu, okwenza kwaba nokukhathazeka ngezempilo okukhona. Ocwaningweni olwenziwe ngonyaka we-2016, kwaqapheleka ukuthi NAFLD(isifo sesibindi esinamafutha) singena ku-10-20% wabantu bezingane. Iphinde yabonisa ukuthi i-NAFLD yezingane izoba imbangela ehamba phambili yokwehluleka kwesibindi, izifo zesibindi, kanye nokufakwa kwesibindi ezinganeni nasebusheni.

NgoJanuwari 2018 kwaba nokwethulwa ngokusemthethweni kohlelo lwezingane lwe-NASH kucatshangelwa ukuthi i-Elafibranor ukuphela komuthi okhombise ukuthi uyasebenza ekwelashweni kwe-NASH kubantu abadala futhi usesigabeni sokuthuthuka ekwelapheni izingane.

Ngabe i-Elafibranor ingasetshenziswa kanye nezinye izidakamizwa ekwelashweni kwe-NASH?

Sekuvele kucacile ukuthi i-Elafibranor iyasebenza ekwelashweni kwe-NASH lapho isetshenziswa yodwa. Kodwa-ke, ngenxa yenkinga yokugula, ingasetshenziswa kanye nezinye izidakamizwa ekuphathweni kwesibindi i-fibrosis, i-NASH, kanye nokugula kwabo okubambisene.

 

I-Elafibranor (GFT505) okunye ukusetshenziswa

Ekwelashweni kwezifo ze-cholstasis

I-cholestasis yisimo esidalwa ukukhubazeka ekwakhiweni kwenyongo nokugeleza kwayo nge-gallbladder ne-duodenum. Kungaholela ekwandeni kwesifo se-systemic nesifo sesibindi, ukwehluleka kwesibindi, kanye nesidingo sokufakelwa kwesibindi. Ucwaningo olwenziwe emtholampilo lwenziwe lwabonisa ukuthi i-Elafibranor (GFT505) powder inciphisa omaka bamakhemikhali e-plasma yingakho kufakazela ukuthi ingasiza ekwelapheni isifo se-cholestasis.

Diabetes

Isifo sikashukela yisimo esidalwa ukuthi sinoshukela omningi noma ushukela egazini. Ithinta cishe abantu abangamakhulu amane emhlabeni jikelele. Umuntu uba nesifo sikashukela sohlobo 2 uma imizimba yabo ingakwazi ukukhiqiza nokusebenzisa i-insulin ngokujwayelekile.

Ucwaningo olwenziwe ku-elafibranor lukhombisa ukuthi kunciphisa ukuqhubeka kohlobo lwesifo sikashukela ngezindlela ezimbili. Owokuqala ngukuthuthuka kwe-glucose metabolism emzimbeni.

Kuphinde kuthuthukise ukuzwela kwe-insulin emisipha nasezithanjeni zangaphakathi.

 

I-Elafibranor (GFT505) Powder-The New Drug for NASH Treatment Study

 

Isiphetho

Ucwaningo lwe-Elafibranor luza njengezindaba ezinhle kunoma ngubani ophethwe yi-NASH. Njengoba sekunikezwe ngomlomo iziguli ezingaphezu kwamakhulu ayisishiyagalombili kuze kube manje futhi kukhombisa ukuthi kuyasiza, kunethemba lokuthi abantu ngeke besadinga ukufakelwa isibindi.

Kwakungekho Ukusebenzisana kwezidakamizwa kwe-Elafibranor itholakale nge-sitagliptin, simvastatin, noma i-warfarin, ekhombisa ukuthi ingasetshenziswa kanye nezinye izidakamizwa ngokuphepha. I-Elafibranor ibekezeleleke kahle emzimbeni futhi ayikhombisi imiphumela emibi.

 

Okubhekwayo

  1. Izindlela Zokuhumusha Zokuhumusha kwisifo sikashukela, i-Obesity, neNonalcoholic Fatty, ehlelwe ngu-Andrew J. Krentz, uChristian Weyer, uMarcus Hompesch, uSpringer Nature, ikhasi 261
  2. Ama-PPAR ku-Cellular and - i-Whole Body Energy Metabolism ahlelwe nguWalter Wahli, uRob Tee, ngo-457-470
  3. I-Obesity and Gastroenterology, Indaba Yemitholampilo yaseGastroenterology yaseNyakatho, i-Octavia Pickett-Blakely, uLinda A. Lee, ikhasi 1414-1420

 

Okuqukethwe

 

 

2019-07-23 supplements
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