Elafibranor (GFT505) Powder-Iyo Itsva Dhiraizi YeNASH Kurapwa Kufunda

Chii chinonzi Elafibranor (GFT505)?

Elafibranor (GFT505) poda (923978-27-2), mushonga wekuyedza uyo ongororo ichiri kuenderera. Kunyanya, kudzidza kwayo uye kuvandudzwa naGenfit kunoenderana nekushanda kwe Elafibranor (GFT505) powder (923978-27-2) mukurwisa hosha senge isiri-doro mafuta chiropa chirwere, dyslipidemia, insulin kuramba, uye chirwere cheshuga.

 

Elafibranor (GFT505) mashandiro anoita

Elafibranor (GFT505) poda inorapwa nemuromo inoshanda kumatatu ePPAR madiki. Zvinosanganisira PPARa, PPARd, uye PPARg. Nekudaro, inonyanya kushanda paPARAR.

Iyo Elafibranor mashandiro ekuita akaomarara sezvo anosiyanisa anotora macofactors kune enyukireya receptor. Nekuda kweizvozvo, izvi zvinotungamira mukusiyanisa kudzora kwemajini pamwe nehunhu hwehupenyu.

Elafibranor (GFT505) poda inokwanisa kuzivisa nekupepeta yakasarudzika yenyukireya receptor modulator (SNuRMs) chiitiko. Nekuda kweizvozvo, inopa kuvandudza kushanda pamwe nemhedzisiro yemhedzisiro

Ose mamodemalal uye mazhinji emamorekuru akabvumikisa kuva anoshanda mukurwisa akasiyana mamiriro. Zvinosanganisira insulin kuramba uye chirwere cheshuga, kuzvimba, kufutisa, uye lipid triad, iyo inoratidzwa nekuwedzera kweiyo HDL cholesterol uye kuderera kweLDL cholesterol uye triglycerides.

Musiyano uripo pakati pemaitiro eElafibranor ekuita uye neayo mamwe makomputa anotarisa maPPAR muNASH (nonalcoholic steatohepatitis) inyaya yekuti hairatidze chero chiitiko chemishonga yePPARy.

Semagumo, Elafibranor vashandisi havawani zvisina kudikanwa mhedzisiro iyo yakabatana nePPARy activation. Mhedzisiro dzakadaro dzinosanganisira; kuchengetwa kwemvura, edema, uye uremu uwane zvese izvo zvinowedzera njodzi yemumwe mukutambura nekutadza kwemoyo.

 

Elafibranor (GFT505) yekudzidza kurapwa kweNash

NASH (nonalcoholic steatohepatitis) chirwere chechiropa chinotungamira mukuzvimba nekuwora kwema hepatocyte pamwe nekuunganidzwa kwemafuta ayo anozivikanwa semadonhwe e lipid. Kazhinji, mamwe mamiriro ehutano senge metabolic syndrome, rudzi rwechipiri chirwere cheshuga, uye kufutisa ndiyo honzeri yekutanga yechinhu chisiri chidhakwa steatohepatitis (NASH), uye nonalcoholic fatty chiropa chirwere (NAFLD).

 

 

Nhasi, vanhu vazhinji vari kurwara nechirwere ichi chinouraya. Chikamu chinotyisa nezvacho ndechekuti chinogona kukonzera cirrhosis, mamiriro anoita kuti chiropa chikatadza kushanda. Iyo inogona zvakare kufambira mberi kune chirwere chechiropa uye mune dzimwe nguva, kukonzera rufu.

Nhau dzinosuruvarisa nezve NASH (nonalcoholic steatohepatitis) ndeyekuti haitore zera uye inoramba ichikanganisa munhu wese. Zvakaipisisa, zviratidzo zvechirwere zvinogona kunge zvisina chiratidzo, uye mumwe anogona kusamboziva kuti vari kutambura nechirwere ichi kusvika chaenda padanho repashure.

Kukuvadza uye kuzvimba kwakaunzwa neNASH (isina kunwa doro steatohepatitis) zvinogona zvakare kutungamira kumatambudziko emoyo nemapapu. Nevanhu vazhinji vava kutambura neichi chiitiko chinobva kune isiri-doro doro mafuta chiropa chirwere, vaongorori vari kutsvaga nzira dzekurapa kunze kwekuchinjisa chiropa.

Imwe yemishonga iri kudzidziswa kurapwa kweNASH ndeye Elafibranor (GFT505) poda (923978-27-2). Parizvino, yakaratidza kukonzera zvakanaka mhedzisiro pane maviri makuru echirwere, kureva, kuwaridza mutsipa uye kuzvimba. Runako narwo nderwunoregererwa zvakanyanya uye hazviwanzo kuita kuti mumwe munhu atambure kubva kune chero madhara. Zviri nekuda kweichi chikonzero iyo US Chikafu neDhiza Administration yakapa kukurumidza-kurongedza mazita kune uyu mushonga we Kurapa kweNASH.

Parizvino, Elafibranor (GFT505) poda iri muPhase 3 kiriniki yekuyedzwa, inonziwo SORURVE IT.

RUDZIVA-IT

Icho chidzidzo chepasirese chakatanga mukota yekutanga ya2016, iyo yakasarudzika, placebo-inodzorwa muchiyero 2: 1 uye yakapofumara-mbiri. Varwere vanobatanidzwa muchidzidzo ichi ndevaya vanotambura neNASH (NAS> = 4) uye fibrosis (F2 kana F3 nhanho umo kukuvara kwechiropa kuri kutozivikanwa.Pakati pekudzidza, varwere vanogona kupihwa muyero weElafibranor (GFT505) 120mg kana placebo kamwe chete zuva nezuva.

Vane chiuru chekutanga varwere kunyoreswa zvinobatsira kuratidza kana NASH ichirapika neElafibranor (GFT505) isina kuwedzera fibrosis kana ichienzaniswa neyavanorapwa ne placebo.

Yekutanga cohort yakanyoreswa muna Kubvumbi 2018, uye kuongororwa kwemhedzisiro yacho kuchaonekwa mukupera kwa 2019 Iyo dhata yakataurwa ichaona kuti Elafibranor anotenderwa here neUS Food and Drug Administration sezvo ichiwana mvumo yemamiriro ezvinhu neEuropean Medicines Agency, zvakanaka inozivikanwa seEMA na 2020.

Chidzidzo ichi chakaenda padanho muna Zvita 2018 apo iyo Dhairekitori Yekuongorora Monitoring Board (DSMB) yakagumisa kuenderera mberi kwechero pasina shanduko. Izvo zvaive mushure mekufanorongerwa kuongororwa pane data rekuchengetedza rakaitwa mushure memwedzi makumi matatu.

 

 

Zvawanikwa zvekutanga preclinic uye kliniki zvidzidzo mukurapa kweNASH

Kubudirira uye kuchengeteka kweElafibranor muNASH kurapwa kwakaongororwa munguva yakapfuura kuburikidza nemhando dzakawanda dzezvirwere. Muchikamu che5a 2a, kuyedzwa kwakasiyana siyana kwakaitwa pavanhu vakasiyana vevarwere vane chirwere chemagetsi. Yaisanganisira avo vane mhando 2 chirwere cheshuga kana pre-chirwere cheshuga uye atherogenic dyslipidemia. Munguva yekudzidza, zvakaonekwa kuti Elafibranor akasimudzira;

• Deredzwa njodzi yekutambura kubva kuzvinhu zvemwoyo
• Kuderedzwa mamakisi ekukuvara kwechiropa
• Anti-kuzvimba zvinhu
• Kuwedzera insulin kunzwa
• Glucose homeostasis
• Cardioprotective lipid chimiro.

Muenzaniso we2b yakatangwa muna 2012 ndiyo yaive muyedzo wakakura chose uye wekutanga kudzidza pasi rese kuitiswa paNASH. Ndipo panguva iyo Elafibranor akawana iyo FDA yakakurudzira mhedziso ye "NASH Kugadziriswa pasina kuwedzera kweFibrosis." Ndiyo yaive yekupedzisira gumo redare repasirese rechitatu kutenderera kuchiri kuenderera mberi.

Izvo zvakaonekwa kuti varwere vakawana kurapwa kweNASH naElafibranor vakacherekedza kuvandudzwa kwechiropa kusagadzikana mamaki akadai ALP, GGT, uye ALT. Kuburikidza nekuongororwa kweyechipiri endpoints, paive nekucherechedzwa kwekuti Elafibranor (GFT505) muyero 120mg yakapa ekurapa mhedzisiro pane iyo cardiometabolic njodzi zvinhu zvine hukama neNASH, Ivo vaisanganisira;

• Anti-kuzvimba mhedzisiro
• Kuvandudzwa kwekunzwa insulin uye glucose metabolism mune varwere vane chirwere cheshuga
• Kuvandudza huwandu hwe lipoproteins uye plasma lipids.

Kubudirira kweElafibranor mukurapa kwevana veNASH

Chiyero icho vana vari kutambudzika nekufutisa chakawedzera zvakanyanya, chichiita kuve kunetseka kwehutano kuri kuwedzera. Muchidzidzo chakaitwa muna 2016, zvakacherechedzwa kuti NAFLD(nonalcoholic fatty chiropa chirwere) inobata nezve 10-20% yehuwandu hwevana. Izvo zvakaramba zvichiratidza kuti vana NAFLD ndiyo ichave iri iyo inotungamira chikonzero chechiropa kutadza, chiropa pathology, pamwe nekuisirwa kwechiropa muvana nevechiri kuyaruka.

MunaNdira 2018 pakange paine kuvhurwa kwepamutemo kwechirongwa cheNASH chevana ichifunga kuti Elafibranor ndiwo chete mushonga wakaratidza kuti unoshanda mukurapa kweNASH muvakuru uye uri muchikamu chekusimudzira mukurapa kwevana.

Elafibranor inogona kushandiswa pamwe chete nemamwe madhiragi mukurapa kweNASH?

Izvo zvatove pachena kuti Elafibranor inoshanda mukurapa kweNASH painoshandiswa yega. Zvisinei, nekuda kwekuoma kwechirwere, inogona kushandiswa pamwe chete nemamwe madhiragi mukutungamira kwechiropa fibrosis, NASH, pamwe nehukama hwavo.

 

Elafibranor (GFT505) zvimwe zvinoshandiswa

Mune cholstasis chirwere kurapwa

Cholestasis ndiwo mamiriro anokonzerwa nehurema mukuumbwa kwenyuchi uye kuyerera kwayo kuburikidza nenduru uye duodenum. Zvinogona kutungamira mukuwedzera kwechirwere systemic uye chirwere chechiropa, kukundikana kwechiropa, uye kunyangwe kudiwa kwekuisirwa chiropa. Chidzidzo chekiriniki chakaitwa chakaratidza kuti Elafibranor (GFT505) poda inoderedza makemikari emakemikari muplasma nokudaro zvichiratidza kuti inogona kubatsira pakurapa chirwere che cholestasis.

chirwere cheshuga

Chirwere cheshuha mamiriro ezvinhu anokonzerwa nekuve akawandisa shuga kana glucose muropa. Inobata vanhu vanosvika mazana mana emamiriyoni vanhu pasirese. Mumwe anovandudza rudzi rwechipiri chirwere cheshuga kamwe chete muviri wavo usingakwanise kuburitsa uye kushandisa insulin zvakajairika.

Tsvagiridzo yakaitwa pa elafibranor inoratidza kuti inoderedza kufambira mberi kwerudzi rwechipiri chirwere cheshuga munzira mbiri. Yekutanga ndeye kuburikidza nekuvandudzwa kweshuga metabolism mumuviri.

Izvo zvakare zvinogadzirisa insulin kunzwa mukati memasuru uye zvinopararira tishu.

 

 

mhedziso

Iyo Elafibranor yekudzidza inouya seyenyaya dzakanaka kune chero munhu ari kutambura neNASH. Sezvo zvakapihwa nemuromo kuvarwere vanopfuura mazana masere kusvika zvino uye zvichiratidza kuti zvinobatsira, pane tarisiro yekuti vanhu havachafanirwa kutora chiropa.

Pakanga pasina Elafibranor kudyidzana kwezvinodhaka yakawanikwa ne sitagliptin, simvastatin, kana warfarin, izvo zvinoratidza kuti inogona kushandiswa pamwechete nemimwe mishonga zvisina njodzi. Elafibranor inoregererwa mumuviri uye haina kuratidza chero mhedzisiro.

References

1. Dudziro Dzekutsvagurudza Maitiro mune Chirwere cheshuga, Kufutisa, uye Nonalcoholic Fatty, yakarongedzwa naAndrew J. Krentz, Christian Weyer, Marcus Hompesch, Springer Nature, peji 261
2. PPARs muCellular uye - Ese Muviri Energy Metabolism yakarongedzwa naWalter Wahli, Rachel Tee, 457-470
3. Kufutisa uye Gastroenterology, Chinhu Nyaya yeGastroenterology Kliniki dzeNorth, Octavia Pickett-Blakely, Linda A. Lee, peji 1414-1420

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