ʻO Elafibranor (GFT505) ka pauma (923978-27-2), he lāʻau hoʻāʻo ia e hoʻomau ʻia nei kāna noiʻi. ʻO ka mea nui, kāna aʻo ʻana a me kāna hoʻomohala ʻana e Genfit ma muli o ka hopena o Elafibranor (GFT505) ka lehu (923978-27-2) i ka hakakā ʻana i nā maʻi e like me ka maʻi leka ʻona ʻole o ka maʻi wai, ka dyslipidemia, ke kūʻē o ka insulin, a me ka maʻi diabetes.
ʻO Elafibranor (GFT505) ka pauka kahi lapaʻau waha e hana ana ma nā subtypes PPAR ʻekolu. Hoʻokomo pū lākou iā PPARa, PPARd, a me PPARg. Eia naʻe, hana nui ia ma PPARa.
He paʻakikī ka hana a Elafibranor o ka hana no ka mea ʻokoʻa ka loaʻa ʻana o nā cofactors i ka receptor nukelea. ʻO ka hopena, alakaʻi kēia i ka hoʻoponopono ʻokoʻa o nā genes a me ka hopena biological.
Hiki i ka Elafibranor (GFT505) pauka ke ʻike a hōʻike ʻana i ka hana modulator receptor nukelea (SNuRMs) hana. A ʻo kahi hopena, hāʻawi ia i ka hoʻomaikaʻi maikaʻi me nā hopena i hōʻemi ʻia.
Ua hōʻike ʻia nā molekila multimodal a me ka pluripotent e kū pono i ka hakakā ʻana i nā ʻano like ʻole. Hoʻopili lākou i ka kū'ē o ka insulin a me ka maʻi diabetes, ka uihue, nā momona, a me ka lipid triad, ka mea i hōʻike ʻia e ka hoʻonui ʻana o ka kolamu HDL a me ka hoʻohaʻahaʻa i ka kolamu LDL a me ka triglycerides.
ʻO ka ʻokoʻa ma waena o ka hana a ka Elafibranor o ka hana a me nā hui ʻē aʻe i hoʻokumu i nā PPAR ma NASH (stealhepatitis nonalcoholic) ʻo ia ka mea ʻaʻole hōʻike i kahi hana PPARy pharmacological.
Ma ka hopena, Elafibranor ʻaʻoleʻike nā mea hoʻohana i nā hopena i makemake ʻole ʻia e pili pū ana me ka hoʻolaʻa PPARy. Loaʻa nā hopena maikaʻi; ka paʻa o ke kahe, edema, a me ke kaupaona loaʻa nā mea a pau e hoʻonui i ka pilikia i ka ʻehaʻeha o ka puʻuwai.
NASH (nonalcoholic steatohepatitis) kahi maʻi akepaʻa e alakaʻi ai i ka mumū a me ka hoʻohaʻahaʻa ʻana o nā hepatosit a me ka hōʻiliʻili ʻana o ka momona i ʻike ʻia he lipid droplets. ʻO ka maʻamau, ʻo kekahi mau ʻano olakino e like me ka maʻi metabolic, ʻano 2 diabetes, a me ka momona ke kumu helu ʻekahi o ka steatohepatitis nonalcoholic (NASH), a me nā maʻi akepaʻa momona ʻole (NAFLD).
I kēia mau lā, nui ka poʻe e ʻeha nei i kēia maʻi make. ʻO ka ʻōlelo hopohopo e pili ana i ia mea hiki iā ia ke alakaʻi i ka cirrhosis, kahi kūlana e hiki ai i ka ʻōpū ke hana. Hiki nō hoʻi iā ia ke holomua i ka maʻi paleka kōpaʻa a ma kekahi mau mea, kahi e make ai.
ʻO ka nūhou kaumaha e pili ana iā NASH (stealhepatitis nonalcoholic) ʻaʻole ia e koho i ka makahiki a hoʻomau i ka hopena i nā mea āpau. ʻO ka mea ʻoi aku ka maikaʻi, ʻo nā hōʻailona o ka maʻi hiki ke asimtomatik, a ʻaʻole paha e ʻike kekahi ke ʻeha nei lākou i ka maʻi a hiki i kona neʻe ʻana i kahi pae hope.
ʻO ka ʻili a me ka mumū i lawe ʻia e NASH (steatohepatitis hauole ʻole) hiki iā ia ke alakaʻi i ka maʻi puʻuwai a me ka hanu. Me nā poʻe he nui e ʻehaʻeha nei i kēia ʻano mai ke kumu mai o ka maʻi akepaʻa momona ʻole ʻona, ʻimi nā mea noiʻi i nā koho lapaʻau ʻē aʻe ma mua o kahi transplant ake.
ʻO kekahi o nā lāʻau lapaʻau e noiʻi nei no ka mālama ʻana iā NASH ʻo ia ʻo Elafibranor (GFT505) pauma (923978-27-2). I kēia manawa, hōʻike ia i nā hopena kūpono i nā hiʻohiʻona koʻikoʻi ʻelua o ka maʻi, ʻo ia hoʻi, ballooning a me ka ʻūhā. ʻO ka nani me ia e hiki ke ahonui a ʻaʻole iki e hana i kekahi e hoʻopiʻi i kekahi hopena ʻaoʻao. ʻO ia ke kumu i hāʻawi ai ka US Food and Drug Administration i kahi ʻano wikiwiki i kēia lāʻau lapaʻau no ka Hoʻohana ʻia NASH.
I kēia manawa, ʻo Elafibranor (GFT505) ka pauka i ka Phase 3 hoʻokolohua hoʻokolohua, a kapa ʻia hoʻi RESOLVE IT.
He noi honua ia i hoʻomaka i ka hapaha mua o 2016, ka mea i randomized, placebo-kāohi ʻia i ka lakio 2: 1 a me ka makapō makapō. ʻO nā mea maʻi e pili ana i kēia noi ʻana ʻo ia ka poʻe e ʻeha mai ka NASH (NAS> = 4) a me ka fibrosis (F2 a i ʻole F3 pae e ʻike nui ʻia ai ka hōʻino o ke ake. 505mg a i ʻole placebo hoʻokahi manawa i kēlā me kēia lā.
ʻO nā mea maʻi he hoʻokahi kaukani e hoʻopaʻa inoa ʻia e kōkua e hōʻike inā hiki ke mālama ʻia ʻo NASH me Elafibranor (GFT505) me ka ʻole o ka fibrosis ʻoi aku ka maikaʻi ke hoʻohālikelike ʻia me nā mea i mālama ʻia me ka placebo.
ʻO ka cohort mua i kau inoa ʻia ma ʻApelila 2018, a e hōʻike ʻia ka loiloi o nā hopena i ka hopena o ka makahiki 2019. E hōʻike ka ʻikepili i ka ʻōlelo a loaʻa ʻo Elafibranor e ʻae ʻia e ka US Food and Drug Administration ma ke ʻano he ʻae ʻia me ka hoʻokele ʻia e ka European Medicines Agency, maikaʻi. kaulana ia Ea e 2020.
Ua hele i mua ka ʻike ma ka mahina ʻo Dekemaba 2018 i ka manawa o ka Data Safety Monitoring Board (DSMB) i kākoʻo ai i ka hoʻomau ʻana o ka hoʻokolokolo me ka ʻole o kahi hoʻololi. ʻO ia ma hope o ka loiloi mua i hoʻolālā ʻia e pili ana i ka ʻike palekana ma hope o kanakolu mau mahina.
ʻO ka maikaʻi a me ka palekana oElafibranor i ka mālama ʻana i ka NASH i loiloi ʻia i ka wā ma mua ma o nā ʻano maʻi like ʻole. I ka mahele 5a 2a, ua hana ʻia nā hoʻokolohua like ʻole ma nā lehulehu like ʻole o nā mea maʻi e ʻehaʻeha nei i ka maʻi metabolic. Hoʻopili ʻia ia me kēlā me kēia ʻano me ka maʻi diabetes 2 a i ʻole pre-diabetes a me atherogenic dyslipidemia. I loko o ke aʻo ʻana, ua ʻike ʻia ua hoʻolaha ʻo Elafibranor;
ʻO ka hōʻike 2b ʻoi i hoʻokumu ʻia ma ka makahiki 2012 ʻo ia ka hoʻokūkū interventional nui loa a me ka hoʻāʻo mua hoʻokele honua mua e hana ʻia ma NASH. Ma laila ua loaʻa iā Elafibranor i ka FDA e kuhikuhi i ka hopena o ka "Hoʻolālā NASH me ka ʻole o ka hoʻomakeke ʻana o Fibrosis." ʻO ia ka manaʻo nui no ka hoʻokolokolo honua 3 e hoʻomau nei.
Ua ʻike ʻia nā mea maʻi i loaʻa i ka lāʻau ʻo NASH me Elafibranor i hōʻike i ka hoʻomaikaʻi ʻana i nā māka kīnā o ke ake e like me ALP, GGT, a me ALT. Ma o ka loiloi ʻana i nā hopena lua, aia kahi mea i ʻike ʻia ʻo Elafibranor (GFT505) mahele lāʻau 120mg i hāʻawi i nā hopena therapeutic ma nā mea pilikia cardiometabolic e pili ana me NASH, ua hui pū lākou;
Ua hoʻonui nui ʻia ka nui o nā keiki e loaʻa ana i ka obesity, me ka ulu ʻana ka hopohopo olakino. Ma kahi noiʻi i hana ʻia ma ka makahiki 2016, ua nānā 'ia NAFLD(maʻi ʻalekona momona momona ʻole) pili iā 10-20% o ka heluna pediatric. Hōʻike hou ia ʻo ka NAFLD pediatric ke kumu nui o ka hōʻino ʻole o ke ake, nā pathology o ke ake, a me ka implantation ate i nā keiki a me nā ʻōpio.
I Ianuali 2018 ua hoʻokumu ʻia kahi papahana official NASH pediatric me ka noʻonoʻo ʻo Elafibranor wale nō ka lāʻau i hōʻoia i ka maikaʻi ma ka mālama ʻana i ka NASH i nā mākua a aia i ke kahua hoʻomohala i ka mālama ʻana i nā keiki.
Ua maopopo ka maikaʻi o Elafibranor i ka mālama ʻana i ka NASH ke hoʻohana ʻia iā ia iho. Eia nō naʻe, ma muli o ka paʻakikī o ka maʻi, hiki ke hoʻohana pū ʻia me nā lāʻau ʻē aʻe i ka mālama ʻana i ka fibrosis ate, NASH, a me kā lākou mau maʻi maʻi pū.
ʻO Cholestasis kahi kūlana i hoʻokumu ʻia e ka hoʻopilikia i ka hoʻokumu ʻia ʻana o ka bile a me kona kahe ma o ka gallbladder a me ka duodenum. Hiki iā ia ke alakaʻi i ka hōʻino ʻana o ka maʻi ʻōnaehana a me nā maʻi ate, ka hōʻeha o ke ake, a me ka pono no ka hoʻoliʻiliʻi ate. Ua hōʻike ʻia kahi noiʻi lapaʻau i hōʻike ʻia ʻo Elafibranor (GFT505) ka pauka e hoʻēmi i nā kaha biochemical i ka plasma no laila e hōʻike nei he hiki ke pono i ka mālama ʻana i ka maʻi cholestasis.
ʻO ka maʻi hakahaka he kūlana ia e loaʻa i ka nui o ke kō a me ke koko i loko o ke koko. Hoʻopilikia ʻia ia ma kahi o ʻehā mau miliona poʻe i ka honua. Hoʻokumu kekahi i ka maʻi diabetes type 2 inā ʻaʻole hiki i ko lākou kino ke hana a hoʻohana i ka insulin maʻamau.
Hōʻike ka noiʻi i hana ʻia ma elafibranor e hoʻemi ana i ka holomua o ka maʻi ʻano 2 i ʻelua ala. ʻO ka mea ma o ka hoʻomaikaʻi ʻana o ka glucose glucose i loko o ke kino.
Hoʻonui pū ia i ka hoʻoliʻiliʻi ʻana o nā inanini ma nā uaua a me nā kiko peripheral.
ʻO ka loiloi Elafibranor he mea maikaʻi maikaʻi i kēlā me kēia mea e loaʻa nei i ka maʻi NASH. Ke lawelawe waha ʻia ʻana ma mua o ʻewalu haneli mau mea maʻi a hiki i kēia lā a ke hōʻike nei he mea pono ia, ke lana nei ka manaʻo ʻaʻole e loaʻa hou i nā kānaka i kahi hoʻoliʻiliʻi ate.
ʻAʻole Hoʻopili i nā lāʻau lapaʻau Elafibranor ʻike ʻia me sitagliptin, simvastatin, a i ʻole warfarin, e hōʻike ana hiki ke hoʻohana pū ʻia me nā lāʻau ʻē aʻe me ka palekana. ʻAe maikaʻi ʻo Elafibranor i ke kino a hōʻike ʻole i nā hopena ʻē aʻe.
Paukū ma:
Kauka Liang
Co-hoʻokumu, alakaʻi alakaʻi o ka ʻoihana o ka ʻoihana; Loaʻa ʻo PhD mai ke Kulanui ʻo Fudan i ka kemika kemika. Ma mua o ʻeiwa mau makahiki o ka ʻike i ke kahua synthetic organic o ka chemistry lāʻau. ʻIke waiwai i ka kemika kombinatorial, kemika lāʻau a me ka synthesist custom a me ka hoʻokele papahana.
E hoʻomaopopo '
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