Elafibranor (GFT505) Foda-Sabuwar Magunguna Don Nazarin Jiyya NASH

Menene Elafibranor (GFT505)?

Elafibranor (GFT505) foda (923978-27-2), magani ne na gwaji wanda bincikensa ke ci gaba. Ainihi, karatunsa da haɓakawa ta hanyar Genfit suna dogara ne akan tasirin Elafibranor (GFT505) foda (923978-27-2) a cikin yakar cutuka kamar cututtukan hanta masu yawan maye, dyslipidemia, insulin resistance, da ciwon suga.

 

Elafibranor (GFT505) tsarin aiwatarwa

Elafibranor (GFT505) foda magani ne na baka wanda ke aiki akan ƙananan ƙananan PPAR guda uku. Sun hada da PPARa, PPARd, da PPARg. Koyaya, yafi yin aiki akan PPARa.

Tsarin Elafibranor na aiki yana da rikitarwa yayin da yake banbanta kwastomomi daban daban zuwa ga mai karɓar nukiliya. A sakamakon haka, wannan yana haifar da tsarin bambanci na kwayoyin halitta da kuma tasirin ilimin halitta.

Elafibranor (GFT505) foda yana iya ganowa da kuma bayyana aikin mai karɓar mai karɓar makaman nukiliya (SNuRMs). A sakamakon haka, yana ba da ingantaccen inganci tare da rage tasirin.

Dukansu kwayoyin sunadaran multimodal da sunadarai sun tabbatar suna da tasiri wajen yakar yanayi daban daban. Sun haɗa da juriya na insulin da ciwon sukari, kumburi, kiba, da lipid triad, wanda haɓakar haɓaka HDL cholesterol da rage ƙwayar LDL cholesterol da triglycerides.

Bambanci tsakanin tsarin aikin Elafibranor da na sauran mahaɗan da ke niyyar PPAR a cikin NASH (nonalcohol steatohepatitis) shine gaskiyar cewa baya nuna duk wani aikin PPARy na magunguna.

Saboda, Elafibranor masu amfani ba su fuskantar tasirin sakamako mara amfani wanda ke hade da kunnawar PPARy. Irin waɗannan sakamako masu illa sun haɗa da; riƙewar ruwa, edema, da nauyin jiki waɗanda suke ƙaruwa da haɗarin mutum ga wahala daga bugun zuciya.

 

Elafibranor (GFT505) don nazarin ilimin Nash

NASH (nonalcohol steatohepatitis) cuta ce ta hanta wacce ke haifar da kumburi da lalacewar hepatocytes da haɗuwar kitse wanda kuma ake kira da 'ya'yan leɓon ɓaure. Yawancin lokaci, wasu yanayi na kiwon lafiya kamar cututtukan rayuwa, rubuta ciwon sukari na 2, da kiba sune lamba ta farko na yawan cutar steatohepatitis (NASH), da cututtukan hanta mai haɗari (NAFLD).

 

 

A yau, mutane da yawa suna fama da wannan cutar mai mutuƙar rai. Ban tsoro mai ban tsoro game da shi shine zai haifar da cutar cirrhosis, yanayin da zai sa hanta ta kasa aiki. Hakanan yana iya ci gaba zuwa cutar kansa hanta kuma a wasu halayen, haifar da mutuwa.

Labari mai ban haushi game da NASH (nonalcohol steatohepatitis) shine cewa baya daukar shekaru kuma yana ci gaba da shafar kowa. Mafi munin har yanzu, alamun cutar na iya zama asymptomatic, kuma mutum ba zai taɓa sanin cewa suna fama da cutar ba har sai ta ci gaba zuwa wani mataki na gaba.

NASHI da kumburi da NASH ya kawo (steatohepatitis mara amfani) na iya haifar da cututtukan zuciya da huhu. Tare da mutane da yawa yanzu suna fama da wannan yanayin wanda ya samo asali daga cutar hanta mai haɗari, masu bincike suna neman zaɓuɓɓukan magani ban da dashen hanta.

Ofayan magungunan da ake binciken don maganin NASH shine Elafibranor (GFT505) foda (923978-27-2). Ya zuwa yanzu, ya nuna haifar da tasirin gaske akan manyan halaye guda biyu na cutar, watau ballooning da kumburi. Kyawun da ke tare da ita shi ne cewa yana da haƙurin gaske kuma ba zai sa mutum ya wahala daga kowace wahala ba. Saboda wannan dalili ne cewa Hukumar Abinci da Magunguna ta Amurka ta ba da saurin saurin wannan maganin ga NASH jiyya.

A halin yanzu, Elafibranor (GFT505) foda yana cikin gwajin gwaji na Phase 3, wanda aka laƙaba shi kamar yadda KA YI SHI.

RA'AYIN-IT

Nazari ne na duniya wanda ya fara a farkon kwata na 2016, wanda aka bazu, ana sarrafa placebo a cikin rabo 2: 1 da makaho biyu. Marasa lafiya da ke cikin wannan binciken sune wadanda ke fama da cutar NASH (NAS> = 4) da fibrosis (matakan F2 ko F3 inda cutar hanta ta riga ta zama sananne. Duk cikin binciken, marasa lafiya ko dai za a yi amfani da maganin Elafibranor (GFT505) 120mg ko placebo sau daya a kowace rana.

Marasa lafiya dubu daya da za a yi wa rajista za su taimaka wajen nuna idan za a iya magance NASH tare da Elafibranor (GFT505) ba tare da munin fibrosis ba idan aka kwatanta da waɗanda aka yi wa magani tare da placebo.

An yi rajistar rukunin farko a watan Afrilun 2018, kuma za a ba da rahoton sakamakon za a bayar da rahoto a ƙarshen 2019. Bayanin da aka bayar zai ƙayyade ko Hukumar Kula da Abinci da Abinci ta Amurka ta sami Elafibranor kamar yadda yake samun yardar ƙungiyar Hukumar Kula da Lafiya ta Turai, da kyau. da aka sani da EMA daga 2020.

Binciken ya ci gaba a wani mataki a watan Disamba na shekarar 2018 lokacin da Hukumar Kula da Kula da Lafiya ta Data (DSMB) ta amince da ci gaba da shari’ar ba tare da wani sauyi ba. Hakan ya biyo bayan bita ne da farko akan bayanan aminci da aka yi bayan watanni talatin.

 

 

Sakamakon binciken ƙididdigar asali da na asibiti a cikin jiyya ga NASH

An kimanta inganci da amincinElafibranor a cikin maganin NASH a baya ta hanyar samfurin cuta da yawa. A cikin 5 na 2a, an yi gwaji iri-iri a kan yawan marasa lafiya da ke fama da cututtukan rayuwa. Ya haɗa da waɗanda ke da ciwon sukari na 2 ko pre-ciwon sukari da atherogenic dyslipidemia. A yayin nazarin, an lura cewa Elafibranor ya inganta;

• Rage haɗarin wahala daga al'amuran zuciya
• Rage alamomin rauni na hanta
• Propertiesungiyoyin anti-kumburi
• Sensara ƙwaƙwalwar insulin
• Gulukos homeostasis
• Profile lipid bayanin martaba.

Batun fitarwa na 2b wanda aka ƙaddamar a 2012 shine mafi girman fitinar shiga tsakani da kuma binciken farko na ƙasa da ƙasa da za a yi akan NASH. A lokacin ne Elafibranor ya cimma matsayar FDA ta ba da shawarar karshe game da “NASH Resolution ba tare da ci gaban Fibrosis ba.” Wancan shine babban batun farkon gwaji na duniya na 3 wanda har yanzu yana ci gaba.

An lura cewa marasa lafiyar da suka sami maganin NASH tare da Elafibranor sun lura da ci gaba a cikin alamomin cutar hanta kamar ALP, GGT, da ALT. Ta hanyar kimantawa na mahimman bayanai na biyu, akwai lura cewa Elafibranor (GFT505) sashi na 120mg ya ba da sakamako na warkarwa akan abubuwan haɗarin zuciya da ke haɗuwa da NASH, Sun haɗa da;

• Abubuwan da ke haifar da rigakafi
• Ingantawa cikin ƙwayar insulin da metabolism metabolism a cikin marasa lafiya waɗanda ke da ciwon sukari
• Inganta matakan lipoproteins da plasma lipids.

Tasiri na Elafibranor a cikin kulawa da cututtukan yara na NASH

Yawan yadda yara ke fama da kiba ya karu sosai, wanda hakan ke haifar da damuwa game da lafiyar. A cikin binciken da aka yi a shekarar 2016, an lura da hakan NAFLD(cututtukan hanta mai haɗari) yana shafar kusan 10-20% na yawan yara. Hakan ya kara nuna cewa NAFLD na yara zai zama babban dalilin gazawar hanta, cutar hanta, gami da dasa hanta ga yara da matasa.

A cikin watan Janairun 2018 an gabatar da shirin likitan yara na NASH a hukumance tare da tuna cewa Elafibranor shine kadai magani da ya tabbatar yana da tasiri a maganin NASH a cikin manya kuma yana cikin matakin ci gaba wajen kula da yara.

Shin ana iya amfani da Elafibranor tare da sauran magunguna a cikin maganin NASH?

Ya riga ya bayyana cewa Elafibranor yana da tasiri a cikin maganin NASH idan aka yi amfani dashi da kansa. Koyaya, saboda rikitarwa na cutar, ana iya amfani dashi tare da wasu magunguna wajen gudanar da cutar sankarar hanta, NASH, da cututtukan da ke tattare dasu.

 

Elafibranor (GFT505) sauran amfani

A cikin cututtukan cutar cholstasis

Cutar ta Cholestasis wani yanayi ne da lalacewar samuwar bile da kwarararsa ta cikin gallbladder da duodenum. Zai iya haifar da mummunar cutar rashin tsari da cutar hanta, gazawar hanta, har ma da buƙatar dashen hanta. Wani binciken asibiti da aka gudanar ya nuna cewa Elafibranor (GFT505) foda yana rage alamomi masu amfani da sinadarai a cikin jini don haka ya tabbatar da cewa zai iya zama mai amfani wajen maganin cutar cholestasis.

ciwon

Cutar sankarau wani yanayi ne da ake haifar dashi ta hanyar yin yawaitar sukari ko glucose a cikin jini. Ana shafar kusan mutane miliyan ɗari huɗu a duniya. Develoaya daga cikin su na haifar da nau'in ciwon sukari irin na 2 da zarar jikinsu ya gaza samarwa da amfani da insulin a koda yaushe.

Bincike da aka yi akan elafibranor ya nuna cewa yana rage ci gaban cutar siga ta 2 ta hanyoyi biyu. Na farko shine ta hanyar inganta haɓakar glucose cikin jiki.

Hakanan yana inganta haɓakar insulin a cikin tsokoki da ƙirar mahaifa.

 

 

Kammalawa

Nazarin Elafibranor ya zo ne a matsayin bushara ga duk wanda ke fama da cutar NASH. Bayan an yi wa baki fiye da ɗari takwas magani ta baka har zuwa yau kuma an nuna yana da amfani, akwai fatan mutane ba za su ƙara yin dashen hanta ba.

Babu wani Hulɗa da magungunan Elafibranor gano tare da sitagliptin, simvastatin, ko warfarin, wanda ke nuna cewa za'a iya amfani dashi tare da wasu magungunan lafiya. Elafibranor yana da haƙuri sosai a cikin jiki kuma baya nuna sakamako mai illa.

References

1. Hanyoyin Bincike Tsarin Fassara a cikin Cutar Cutar Cutar Cutar, Cutar Kiba, da Nonalcoholic Fatty, Andrew J. Krentz, Christian Weyer, Marcus Hompesch, Springer Nature, shafi na 261
2. PPARs a cikin salon salula da - Duk Jikin kuzarin metabolism wanda Walter Wahli, Rahila Tee, 457-470
3. Kiba mai yawa da Cutar Gastroenterology, Batun da aka samu na Clinics of North, Octavia Pickett-Blakely, Linda A. Lee, shafi na 1414-1420

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