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

Yintoni iElafibranor (GFT505)?

I-Elafibranor (GFT505) powder (923978-27-2), sisiyobisi esilingayo esophando sisaqhubayo. Ngokuyintloko, ukufundwa kwayo kunye nokukhula kwayo yiGenfit kusekwe ekusebenzeni kwe I-Elafibranor (GFT505) powder (I-923978-27-2) ekulweni nezifo ezifana nesibindi esinamafutha angenasiselo sinxilisayo, idyslipidemia, ukumelana ne-insulin, kunye neswekile.

Indlela yokusebenza ye-Elafibranor (GFT505)

I-Elafibranor (GFT505) ipowder yonyango lomlomo olusebenza kwii-subtypes ezintathu ze-PPAR. Babandakanya i-PPARa, i-PPARd, kunye ne-PPARg. Nangona kunjalo, isebenza ikakhulu kwi-PPARa.

Indlela ye-Elafibranor yesenzo iyinkimbinkimbi njengoko ngokwahlukileyo kuthatha i-cofactors kwi-receptor yenyukliya. Ngenxa yoko, oku kukhokelela kummiselo owahlukileyo wemfuza ngokunjalo nefuthe lebhayiloji.

I-Elafibranor (GFT505) ipowder iyakwazi ukuphawula kunye nokuprinta imisebenzi ekhethiweyo ye-receptor modator yenyukliya (SNuRMs). Ngenxa yoko, inika ukuphuculwa okusebenzayo kunye nemiphumo emibi encinci.

Zombini iimolekyuli ze-multimodal kunye ne-pluripotent ziye zibonakalise ukuba ziyasebenza ekulweni iimeko ezahlukeneyo. Babandakanya ukumelana ne-insulin kunye neswekile, ukuvuvukala, ukutyeba kakhulu, kunye ne-lipid triad, ephawuleka ngokunyuka kwe-cholesterol ye-HDL kunye nokwehliswa kwe-cholesterol ye-LDL kunye ne-triglycerides.

Umahluko phakathi kwendlela yokusebenza ye-Elafibranor kunye nezinye iicomputer ezijolise kwii-PPARs kwi-NASH (i-nonato alcoholic steatohepatitis) yeyokuba ayibonisi misebenzi ye-PPARy ye-pharmacological.

Nje ngeziphumo, Elafibranor Abasebenzisi abafumani ziphumo ebezingalindelekanga ezinxulumene nokusebenza kwe-PPARy. Iziphumo ebezingalindelekanga zibandakanya; ukugcinwa kwamanzi, i-edema, kunye nobunzima bokufumana ubunzima obukhulisa umngcipheko umntu ekubandezelekeni kwentliziyo.

I-Elafibranor (GFT505) yesifundo sonyango sika-Nash

I-NASH ((nonalcoholic steatohepatitis) sisifo sesibindi esikhokelela ekutyhafeni nasekuthambekeni kwehepatocytes kunye nokuqokelelwa kwamafutha okwaziwa ngokuba ziipipid Droplets. Ngokwesiqhelo, iimeko ezithile zempilo ezinje ngesifo se-metabolic, uhlobo lweswekile yesi-2, kunye nokukhuluphala zizinto ezingunobangela wokuqala wesifo esine-non-alcoholic steatohepatitis (NASH), kunye nesifo esingesosiselo esinamafutha esibindi (NAFLD).

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

Namhlanje, abantu abaninzi banesi sifo esibulalayo. Icandelo elothusayo malunga nalo kukuba kungakhokelela kwisifo sokuqina kwesibindi, imeko esenza isibindi singakwazi ukusebenza. Inokuqhubela phambili nomhlaza wesibindi kwaye kwezinye iimeko, ibangela ukufa.

Iindaba ezilusizi malunga ne-NASH (i-nonato alcohol's steatohepatitis) kukuba ayichaphazeli ubudala kwaye iyaqhubeka ichaphazela wonke umntu. Okubi nangakumbi, iimpawu zezifo zinokuba zi-asymptomatic, kwaye umntu angaze azi ukuba bahlaselwa sesi sifo de abe uqhubele phambili kwinqanaba elilandelayo.

Ukuqhekeka kunye nosulelo oluziswe yi-NASH (i-non-alcoholic steatohepatitis) inokukhokelela kwintlungu yentliziyo kunye nemiphunga. Ngabantu abaninzi ngoku abanesi sifo esivela kwisifo esinamafutha angenasiselo sinxilisayo, abaphandi bafuna ezinye iindlela zonyango ngaphandle kokudluliselwa kwisibindi.

Elinye lala machiza afundelwa unyango lwe-NASH yi-Elafibranor (GFT505) powder (923978-27-2). Ukuza kuthi ga ngoku, ibonisile ukuba ibangela iimpembelelo ezilungileyo kwiimpawu ezimbini eziphambili zesifo, oko kukuthi, ukuhla kwebala nokuvuvukala. Ubuhle kunye nayo kukuba kuyanyamezeleka kwaye ayifane yenze umntu ahlupheke ngayo nayiphi na imiphumo. Kungenxa yesi sizathu ukuba iU.S. Food and Drug Administration inike umkhombandlela wegama ngokukhawuleza Unyango lwe-NASH.

Okwangoku, i-Elafibranor (GFT505) ipoda ikwinqanaba lesi-3 sovavanyo lwezonyango, ekwabizwa ngokuba yi-ISONKA.

HLOLA-IT

Sisifundo esenziwa kwihlabathi liphela esiqale kwikota yokuqala ka-2016, esingakhethiweyo, silawulwa yi-placebo kulungelelaniso 2: 1 kunye nokungaboni kabini. Izigulana ezibandakanyekayo kolu phononongo zizo ezinesifo se-NASH (NAS> = 4) kunye ne-fibrosis (F2 okanye F3 amanqanaba apho umonakalo wesibindi sele uqaphelekile. Kuyo lonke uphando, abaguli banokulawulwa nge-Elafibranor (GFT505) dosage I-120mg okanye i-placebo kube kanye ngosuku.

Isigulana sokuqala esingenakubhaliswa siya kunceda ukubonisa ukuba ngaba i-NASH iyanyangeka nge-Elafibranor (GFT505) ngaphandle kokuya ngokuba mandundu xa kuthelekiswa nonyango lwe-placebo.

I-cohort yokuqala yabhaliswa ngo-Epreli ngo-2018, kwaye uhlalutyo lweziphumo luya kuxelwa emva konyaka ka-2019. Idatha echaziweyo iyakucacisa ukuba i-Elafibranor ivunywa yi-US Food and Drug Administration njengoko ifumana imvume kwi-Arhente yaMayeza aseYurophu, yaziwa ngokuba yi-EMA ngo-2020.

Uphononongo luye lwaya phambili ngoDisemba ngo-2018 xa iBhodi yoLawulo loKhuseleko lweDatha (i-DSMB) ixhasa ukuqhubeka kwelingo ngaphandle kotshintsho. Oko kwakungemva kophononongo olwacwangciswa kwangaphambili kwidatha yokhuseleko olwenziwe emva kweenyanga ezingamashumi amathathu.

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

Iziphumo zesikolo sangaphambi kokuqala kunye nezifundo zeklinikhi kunyango lwe-NASH

Ukusebenza ngokukhuselekileyo nokukhuselekileyo kwe-Elafibranor kunyango lwe-NASH kuvavanywe ngaphambili kwiimodeli zesifo ezininzi. Kwinqanaba le-5a le-2a, iimvavanyo ezahlukeneyo zenziwa kwiqela labantu abagula sisifo se-metabolic. Kubandakanya abo banesifo seswekile 2 okanye isifo seswekile kunye dyslipidemia yesifo seswekile. Ngexesha lesifundo, kwabonwa ukuba i-Elafibranor iyakhuthaza;

  • Ukuncitshiswa komngcipheko wokubandezeleka kwimicimbi yentliziyo
  • Ukucitshiswa kweempawu zokulimala kwesibindi
  • Iipropathi ezichasene nokuvuvukala
  • Ukunyuka kokuziva kwe-insulin
  • Iglucose homeostasis
  • Iprofayile ye-lipidoprotective lipid.

Uvavanyo lwesigaba 2b olwaqaliswa ngo-2012 lolona vavanyo longenelelo lukhulu kunye nolona luhlobo lokuqala lokufunda olwenziwe kwi-NASH. Kulapho u-Elafibranor afumana umbono ophakanyisiweyo we-FDA wokupheliswa kwesigqibo se-NASH ngaphandle kokuya nokuba mandundu kwe-Fibrosis.

Kwaqwalaselwa ukuba abaguli abafumene unyango lwe-NASH nge-Elafibranor baqaphela ukuphuculwa kokumakishwa kokusebenza kwesibindi njenge-ALP, GGT, kunye ne-ALT. Ngokuvavanywa kokuphela kwexesha lesibini, kwabonwa ukuba i-Elafibranor (GFT505) ithamo le-120mg inika iziphumo zonyango kumngcipheko we-cardiometabolic ehambelana ne-NASH, Babandakanya;

  • Iziphumo ezichasene nokuvuvukala
  • Ukuphuculwa kokuziva kwe-insulin kunye ne-glucose metabolism kwizigulana ezinesifo seswekile
  • Ukuphucula amanqanaba e-lipoproteins kunye neeplasma lipids.
Ukusebenza kwe-Elafibranor kunyango lwe-NASH yabantwana

Umgangatho apho abantwana babandezeleka ngenxa yokukhuluphala inyuke kakhulu, iyenza inkxalabo yezempilo. Kuphando olwenziwe ngo-2016, kwajongwa ukuba NAFLD(isifo esingesosiselo esinamafutha esibindi) ichaphazela malunga ne-10-20% yabantwana. Ibonise kwakhona ukuba i-NAFLD yabantwana iya kuba yeyona nto iphambili yokungaphumeleli kwesibindi, i-pathology yesibindi, kunye nokufakwa kwesibindi kubantwana nakwishumi elivisayo.

NgoJanuwari ka-2018 bekusekwe ngokusesikweni inkqubo ye-NASH yabantwana inengqondo yokuba i-Elafibranor kuphela kwesiyobisi esiye saqinisekisa ukuba siyasebenza kunyango lwe-NASH kubantu abadala kwaye kukwinqanaba lophuhliso kunyango lwabantwana.

Ngaba i-Elafibranor ingasetyenziswa kunye namanye amachiza kunyango lwe-NASH?

Sele kucacile ukuba i-Elafibranor iyasebenza kunyango lwe-NASH xa isetyenziswa ngokwayo. Nangona kunjalo, ngenxa yokungaxhomekeki kwesi sigulo, singasetyenziswa kunye namanye amachiza kulawulo lwe-fibrosis yesibindi, i-NASH, kunye nokusebenzisana kwabo ngokubambisana.

I-Elafibranor (GFT505) ezinye izixhobo

Kunyango wesifo se-cholstasis

Ikholestasis yimeko ebangelwa kukungonwabi ekumiselweni kwe-bile kunye nokuhamba kwayo kwi-gallbladder kunye ne-duodenum. Inokukhokelela ekoneni kwesifo senkqubo yesiqhelo kunye nesifo sesibindi, ukungaphumeleli kwesibindi, kunye nemfuno yokufakelwa kwesibindi. Uphononongo lweklinikhi olwenziwe lubonise ukuba i-Elafibranor (GFT505) ipowder inciphisa uphawu lwe-biochemical kwi-plasma engqina ukuba lunokuba luncedo kunyango lwesifo se-cholestasis.

Diabetes

Iswekile yimeko ebangelwa kukuba neswekile eninzi okanye iswekile egazini. Ichaphazela phantse amakhulu amane ezigidi zabantu kwihlabathi liphela. Umntu uphuhlisa uhlobo lweswekile yesibini xa imizimba yabo ingakwazi ukuvelisa kwaye isebenzise i-insulin ngokwesiqhelo.

Uphando olwenziwe kwi-elafibranor lubonisa ukuba kunciphisa ukuqhubela phambili kwesifo seswekile 2 ngeendlela ezimbini. Eyokuqala kukuphuculwa kwe-glucose metabolism emzimbeni.

Ikwaphucula ubuntununtunu be-insulin kwezihlunu nakwizihlunu zomzimba.

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

isiphelo

Isifundo se-Elafibranor siza njengeendaba ezilungileyo kuye nabani na ogula yi-NASH. Ukuba sinikezelwe ngomlomo kwizigulana ezingaphaya kwamakhulu asibhozo ukuza kuthi ga ngoku kwaye zibonise ukuba ziluncedo, sinethemba lokuba abantu abasayi kuphinda batshintshelwe kwisibindi.

Kwakungekho Ukuhlangana kweziyobisi ze-Elafibranor ifunyenwe i-sitagliptin, i-simvastatin, okanye i-warfarin, ebonisa ukuba inokusetyenziswa kunye namanye amachiza ngokukhuselekileyo. I-Elafibranor inyamezelekile emzimbeni kwaye ayibonisi nayiphi na imiphumo emibi.

Ucaphulo

  1. Iindlela zoPhando zokuGuqulela kwisifo seswekile, ukukhuluphala, kunye neNonalcoholic Fatty, ehlelwe nguAndrew J. Krentz, uChristian Weyer, uMarcus Hompesch, uSpringer weSimo, iphepha 261
  2. Ii-PPARs kwiCellular kunye ne-umzimba wonke weMetabolism ehlelwe nguWalter Wahli, uRachel Tee, 457-470
  3. Ukutyeba kakhulu kunye neGastroenterology, umba weKliniki ye-Gastroenterology yaseNyakatho, i-Octavia Pickett-Blakely, uLinda A. Lee, iphepha 1414-1420

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2019-07-23 nezongezo
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