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

Chii chinonzi Elafibranor (GFT505)?

Elafibranor (GFT505) poda (923978-27-2), mushonga wekuyedza uyo kutsvagisa kwake kuchiri kuenderera. Kunyanya, kudzidza kwayo uye kukura kweGenfit kunoenderana nebasa re 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 kurapwa nemuromo kunoshanda pane ese matatu PPAR subtypes. Zvinosanganisira PPARa, PPARd, uye PPARg. Nekudaro, inonyanya kuita paPPARa.

Iyo Elafibranor mashandiro ekuita akaoma sezvo iwo musiyano unotora ma cofactors kune nyukiliya receptor. Semhedzisiro, izvi zvinotungamira kumusiyano wekutungamira kwemarudzi pamwe nemhedzisiro yezvibereko.

Elafibranor (GFT505) poda inokwanisa kuona uye kukanganisa basa rinosarudza renyukireya receptor modulator (SNuRMs) basa. Nekuda kweizvozvo, inopa yakanyatsoshanda pamwe nekuderedzwa mativi.

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 uripakati pesimba reElafibranor rekuita uye remamwe makomponi anotarisana nePPARs muNASH (nonalcoholic steatohepatitis) inyaya yekuti hairatidze chero chinhu chemishonga PPARy.

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 nekuora kwehepatocytes pamwe nekuunganidzwa kwemafuta ayo anozivikanwawo se lipid madonhwe. Kazhinji, mamwe mamiriro ehutano senge metabolic syndrome, Type 2 chirwere cheshuga, uye kufutisa ndizvo zvinokonzeresa zvisiri zvechinwiwa chinonzi steatohepatitis (NASH), uye chirwere chisina mafuta chinodhaka chiropa (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 dzinoshungurudza nezve NASH (nonalcoholic steatohepatitis) ndeyekuti haisi kutora pazera uye inoramba ichibata munhu wese. Zvakatonyanya kunetsa, zviratidzo zvechirwere zvinogona kunge zviri asymptomatic, uye mumwe anogona kusamboziva kuti ari kurwara nechirwere kudzamara zvasvika padanho rinotevera.

Kukuvadza uye kuzvimba kwakaunzwa neNASH (isina kunwa doro steatohepatitis) inogona zvakare kukonzera kunetseka kwemoyo nemapapu. Nevanhu vazhinji ikozvino vanotambura nechirwere ichi chinobva kune isiri yekudhakwa mafuta echiropa chirwere, vanotsvaga vanotsvaga nzira dzekurapwa kunze kwekutapurirana kwechiropa.

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 muPase 3 kliniki kuyedzwa, zvakare yakanzi DZVISVANYAI.

RUDZIVA-IT

Icho chidzidzo chepasi rose chakatanga mukota yekutanga ye 2016, iyo yakasarudzika, placebo-inodzorwa muchiyero 2: 1 uye mapofu-maviri. Varwere vane chekuita nechidzidzo ichi ndevaya vanorwara neNASH (NAS> = 4) uye fibrosis (F2 kana F3 nhanho umo kukuvara kwechiropa kwatova pachena. Muongororo yose iyi, varwere vanogona kunge vachirapwa pamwe neElafibranor (GFT505) dosage 120mg kana placebo kamwe chete pazuva.

Varwere vane chiuru chekutanga kunyoreswa vachabatsira kuratidza kana NASH ichirapwa neElafibranor (GFT505) isina kuwanda fibrosis kana ichienzaniswa nevaya vakarapwa 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

Iko kushanda uye kuchengeteka kweElafibranor mukurapa kweNASH kwakaongororwa munguva yakapfuura kuburikidza nemhando dzakawanda dzechirwere. Muchikamu che5a 2a, miedzo yakasiyana-siyana yakaitwa pane dzakasiyana nhamba dzevarwere vane chirwere che metabolic. Izvo zvaisanganisira avo vane Type 2 chirwere cheshuga kana pre-chirwere cheshuga uye atherogenic dyslipidemia. Munguva yekudzidza, zvakaonekwa kuti Elafibranor inosimudzira;

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 neElafibranor vakacherekedza kuvandudzwa kwechiitiko chekusagadzikana kwechiropa chakadai sa ALP, GGT, uye ALT. Kuburikidza nekuongororwa kwechipiri ekupedzisira, pakanga paine kucherechedzwa kuti Elafibranor (GFT505) dhigiridzo 120mg yakapa kurapa kwezvirwere zvecardiometabolic njodzi zvinhu zvinosangana neNASH, Vakasanganisira;

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% yevana vechidiki. Yakaratidza zvakare kuti NAFLD yevana ichave iri kutungamira kwechiropa kukundikana, chiropa pathology, pamwe nekuiswa kwechiropa muvana nepwere.

Muna Ndira 2018 pakanga paine kuvhurwa kwepamutemo kwehurongwa hwebeleti yeNASH vachifunga kuti Elafibranor ndiye chete mushonga wakaratidza kuti unobudirira mukurapa kweNASH mune vanhu vakuru uye uri muchikamu chekuvandudza mukurapa kwevana.

Elafibranor inogona kushandiswa pamwe chete nemamwe madhiragi mukurapa kweNASH?

Izvo zvatova pachena kuti Elafibranor inoshanda mukurapa kweNASH painoshandiswa pachayo. Nekudaro, nekuda kwekuoma kwechirwere, chinogona kushandiswa pamwe chete nemamwe madhiragi mukutonga kwechiropa fibrosis, NASH, pamwe nemubatanidzwa wavo.

Elafibranor (GFT505) zvimwe zvinoshandiswa

Mune cholstasis chirwere kurapwa

Cholestasis chimiro chinokonzerwa nekusagadzikana mukuumbwa kwe bile uye inoyerera kuburikidza nemarara uye duodenum. Izvo zvinogona kutungamira pakuwedzera kwechirwere che systemic uye chirwere chechiropa, kushomeka kwechiropa, uye kunyange kudikanwa kwekushandurwa kwechiropa. Kuongororwa kwekiriniki kunoitwa kwakaratidza kuti Elafibranor (GFT505) poda inodzora mamakisi emakemikari ari muplasma nekudaro achiratidza kuti inogona kubatsira mukurapa 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.

Kutsvaga kwakaitwa pane elafibranor kunoratidza kuti kunodzora kufambira mberi kwechirwere cheshuga chechipiri munzira mbiri. Yekutanga ndeye kuburikidza nekuvandudzwa kweglucose metabolism mumuviri.

Izvo zvakare zvinogadzirisa insulin kunzwa mukati memasuru uye zvinopararira tishu.

mhedziso

Iyo Elafibranor yekudzidza inouya senge nhau dzakanaka kunaani ari kurwara neNASH. Kubva tapihwa nemuromo kune vanopfuura mazana masere varwere kusvika parizvino uye zvichiratidza kuti zvinobatsira, kune tariro yekuti vanhu havachafanirwa kutapudzirwazve chiropa.

Pakanga pasina Elafibranor kudyidzana kwezvinodhaka yakawanikwa ne sitagliptin, simvastatin, kana warfarin, izvo zvinoratidza kuti inogona kushandiswa pamwe chete nemamwe madhiragi zvisina ngozi. Elafibranor inoshivirirwa zvakanaka mumuviri uye hairatidze mhedzisiro.

References

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

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