Wane Bayani Dole ne Ku sani Kafin Amfani da Erlotinib - AASraw
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Erlotinib

 

  1. Menene Erlotinib?
  2. Ta yaya Erlotinib ke Aiki?
  3. Waɗanne Cututtuka Ne Erlotinib Ya Fi Jiyya?
  4. Yaya Ake Amfani da Erlotinib A halin Yanzu A Cikin Asibiti?
  5. A cikin Wadanne Marasa Lafiya Erlotinib Ya Fi Yin Tasiri?
  6. Menene Matsayin Erlotinib?
  7. Menene Haɗarin haɗarin tare da Erlotinib?
  8. Wanne Magunguna ko plementsarin Magani tare da Erlotinib?
  9. FDA ta Amince da Erlotinib Jiyya
  10. Summary

 

Abin da ke Erlotinib

Erlotinib (CAS:183321-74-6) yana cikin rukunin magungunan da ake kira tyrosine kinase inhibitors. Yana aiki ta hanyar toshe aikin furotin da ake kira mai karɓar haɓakar haɓakar epidermal (EGFR). Ana samo EGFR akan saman ƙwayoyin kansa da yawa da ƙwayoyin halitta na yau da kullun. Yana aiki azaman “eriya,” yana karɓar sigina daga wasu ƙwayoyin halitta da kuma mahalli wanda ke faɗin sel ya girma da rarrabuwa. EGFR yana taka muhimmiyar rawa wajen haɓakawa da haɓakawa a lokacin haihuwa da lokacin ƙuruciya kuma yana taimakawa wajen kiyaye maye gurbin tsofaffin ƙwayoyin da suka lalace a cikin manya. Koyaya, yawancin kwayoyin cutar kanjamau suna da EGFR mai yawa a saman su, ko kuma an canza EGFR ta hanyar maye gurbin DNA wanda ke ɗaukar lambar kwayar halitta don sunadarin. Sakamakon shine alamun da ke zuwa daga EGFR suna da ƙarfi sosai, suna haifar da ci gaban kwayar halitta da yawa da rarrabuwa, alama ce ta cutar kansa.

 

Yaya Yaya Erlotinib Aiki? 

Hanyar maganin antitumor na asibiti na erlotinib ba cikakke cikakke ba. Erlotinib yana hana ƙwayar phosphorylation na intracellular na tyrosine kinase hade da epidermal girma factor mai karɓar (EGFR). Ididdigar hanawa game da sauran masu karɓar maganin tyrosine ba a cika cika su ba. Ana bayyana EGFR akan saman tantanin halitta na ƙwayoyin yau da kullun da ƙwayoyin kansa.

 

Abin da Cututtuka ke Yi Erlotinib Anyi Mahimmanci? 

(1) Ciwon daji na huhu

Erlotinib a unresectable ba kananan cell huhu ciwon daji a lokacin da kara zuwa jiyyar cutar sankara inganta] aukacin rayuwa ta 19%, da kuma inganta ci gaban-free rayuwa (PFS) da 29%, idan aka kwatanta da jiyyar cutar sankara alone.The Amurka Food and Drug Administration (FDA) amince erlotinib domin lura da gida m ko metastatic ba kananan cell huhu ciwon daji cewa ya gaza a kalla daya kafin jiyyar cutar sankara regimen.

A cikin cutar sankarar huhu, erlotinib ya nuna yana da tasiri ga marasa lafiya tare da ko ba tare da maye gurbi na EGFR ba, amma ya zama mafi tasiri ga marasa lafiya tare da maye gurbin EGFR. far (docetaxel ko pemetrexed). Gabaɗaya ƙimar amsawa ta kusan 50% mafi kyau fiye da daidaitaccen layi na chemotherapy. Marasa lafiya waɗanda ba masu shan sigari ba, da tsofaffin masu shan sigari, tare da adenocarcinoma ko ƙananan abubuwa kamar BAC suna iya samun maye gurbin EGFR, amma maye gurbi na iya faruwa a kowane nau'in marasa lafiya. . Genzyme ne ya kirkirar gwaji don maye gurbin EGFR.

 

(2) pancreatic ciwon daji

A watan Nuwamba 2005, FDA ta amince da erlotinib a haɗe tare da gemcitabine don maganin ci gaban cikin gida, wanda ba za a iya magance shi ba, ko kuma ciwon daji na ƙwayar cuta.

AASraw shine ƙwararren masanin Erlotinib.

Da fatan za a danna nan don bayanin zance: Saduwa da mu

 

(3) Juriya ga magani

Erlotinib ya daure zuwa ErbB1 a ƙudurin 2.6A; launi mai launi yana nuna hydrophobicity.Ya kasance tare da sauran ATP masu gasa ƙananan ƙwayoyin tyrosine kinase masu hanawa, kamar imatinib a cikin CML, marasa lafiya cikin sauri haɓaka juriya. Game da erlotinib wannan yakan faru ne watanni 8-12 daga fara magani. Fiye da 50% na juriya yana haifar da maye gurbi a cikin aljihun ATP na EGFR yankin kinase wanda ya haɗa da maye gurbin ƙaramin maganin pola threonine tare da babban ragowar methionine marasa ruwa (T790M) .Kusan 20% na juriya na ƙwayoyi yana haifar da haɓakawa na mai karɓar haɓakar haɓakar hepatocyte, wanda ke motsa ERBB3 dogaro da kunna PI3K.

 

Erlotinib

 

Yaya Is Erlotinib Clokaci-lokaci Used In The Clayi?

Hukumar Abinci da Magunguna ta Amurka (FDA) ce ta fara amincewa da Erlotinib don amfani da marasa lafiya da ke fama da cutar kansar huhu da ba ta da ƙanƙanin ƙwayar cuta wanda ya sake dawowa bayan aƙalla wani nau'in maganin. A shekara ta 2005, an amince da amfani dashi tare da wani magani, gemcitabine, don ci gaba da cutar sankarar bargo. A cikin 2010, an fadada amfani da shi don haɗawa da maganin kulawa ga marasa lafiya da ke fama da ƙananan ƙwayoyin cuta na huhu wanda cutar ta daidaita bayan zagaye huɗu na jiyya tare da magani na platinum, kamar cisplatin ko karboplatin. Marasa lafiya da ke shan erlotinib yawanci suna haƙuri da maganin sosai. Illolin da suka fi yaduwa sune cututtukan fata da gudawa.

 

In Wjayayya Pda kuma Is Erlotinib Most Eamintacce?

A cikin shekaru goma da suka gabata, likitocin sun sami babban gogewa tare da masu hana cin hanci da rashawa, kamar erlotinib, wanda ke toshe EGFR. Ya zama ƙara bayyana cewa waɗannan kwayoyi suna aiki mafi kyau a cikin marasa lafiya wanda kwayar cutar huhu yana ɗaukar wani nau'i na maye gurbi wanda ke haifar da ƙarancin furotin EGFR. Wadannan marasa lafiyar na iya kasancewa daga zuriya Asiya, mata, kuma ba masu shan taba sigari da wani nau'in sankarar huhu da ake kira bronchoalveolar adenocarcinoma. Don haka, a cikin 2013, an yarda erlotinib ya zama magani na farko ga wannan rukuni na marasa lafiya, idan ba za a iya warkar da cutar kansa ba ta hanyar tiyata.

 

Abin da Is Erlotinib Rtaimakon?

Erlotinib yana da matukar tasiri a cikin rukunin marasa lafiya ɗauke da maye gurbin EGFR. Koyaya, har ma da waɗannan marasa lafiya a ƙarshe zasu fara nuna ci gaba da cutar kansa bayan kimanin watanni 12 na maganin erlotinib. Wannan saboda ci gaban juriya da maganin ƙwayoyin cuta a cikin ragowar ƙwayoyin cuta. A lokuta da yawa, juriya yana faruwa ne daga ci gaba da maye gurbi na biyu a cikin furotin EGFR wanda ke hana erlotinib shiga cikin yankin tyrosine kinase. Sabbin hanyoyi don kula da wadannan marasa lafiya sun hada da wani mai ci gaba tyrosine kinase inhibitor afatinib, shi kadai ko a hade tare da cetuximab (Erbitux), wanda ke hana EGFR ta wata hanyar daban.

 

Menene Haɗarin haɗarin tare da Erlotinib?

A cikin karatu, cututtukan da suka fi dacewa tare da Erlotinib lokacin da aka yi amfani da su azaman maganin ciwon daji na huhu sun kasance kurji (wanda ya shafi 75% na marasa lafiya), gudawa (54%), rashin ci da gajiya (52% kowanne). A cikin nazarin Tarceva da aka yi amfani da shi tare da gemcitabine don ciwon daji na pancreatic, cututtukan da aka fi sani sune gajiya (wanda ya shafi 73% na marasa lafiya), kurji (69%) da gudawa (48%). Don cikakken jerin abubuwan illa da ƙuntatawa tare da Erlotinib, duba takaddun kunshin.

 

Wanne Ddarduma ko Sƙari Isharewa With Erlotinib?

CYP3A4 enzyme ne a cikin hanta wanda ya lalace kuma yana taimakawa kawar da erlotinib daga jiki. Magungunan da ke hana CYP3A4 na iya haifar da babban matakin erlotinib a cikin jiki, kuma manyan matakan na iya haifar da guba daga erlotinib. Irin wadannan kwayoyi sun hada da atazanavir (Reyataz), clarithromycin (Biaxin), indinavir (Crixivan), itraconazole (Sporanox), ketoconazole (Nizoral), nefazodone (Serzone), nelfinavir (Viracept), ritonavir (Norvir), savvv; telithromycin (Ketek), da voriconazole (VFEND). A cikin marasa lafiya da ke karɓar waɗannan magungunan, ana iya buƙatar ƙananan ƙwayar erlotinib don hana haɗari.

Wasu kwayoyi suna haɓaka kawar da erlotinib ta hanyar haɓaka ayyukan CYP3A4 enzymes. Wannan yana rage matakan erlotinib a jiki kuma yana iya rage tasirinsa. Misalan irin wadannan kwayoyi sun hada da rifampicin (Rifadin), rifabutin (Mycobutin), rifapentine (Priftin), phenytoin (Dilantin), carbamazepine (Tegretol), phenobarbital da St. John's Wort. Ya kamata a guji waɗannan kwayoyi a cikin marasa lafiyar shan erlotinib, idan zai yiwu. Idan madadin magunguna ba zaɓi bane, ana iya buƙatar ƙwayoyin erlotinib mafi girma. Shan taba sigari yana rage yawan erlotinib a cikin jini. An shawarci marasa lafiya su daina shan sigari.

Magungunan da ke rage samar da acid a ciki zasu rage shayar erlotinib. Sabili da haka, ba za a gudanar da proton pump inhibitors (PPI's, misali, omeprazole [Prilosec, Zegerid]) tare da erlotinib ba, kuma ya kamata a gudanar da erlotinib awanni 10 kafin masu toshe H2-receptor (misali, ranitidine [Zantac]) ko awanni biyu bayan shan mai hana H2-receptor.

Gudanar da antacids ya kamata a raba shi daga gudanarwar erlotinib da awanni da yawa. Erlotinib yana da alaƙa da haɗarin zub da jini, musamman ma a cikin marasa lafiya suma shan warfarin (Coumadin). Ya kamata a kula da marassa lafiyar shan warfarin sosai.

 

FDA ta amince Erlotinib Jiyya

A ranar 18 ga Oktoba, 2016, Hukumar Abinci da Magunguna ta Amurka ta sauya alamar erlotinib (TARCEVA, Astellas Pharm Global Development Inc.) don maganin ƙananan ƙwayoyin cuta na huhu (NSCLC) don iyakance amfani da marasa lafiya wadanda ciwace ciwacen jikin su ke canza maye gurbi (EGFR).

Canjin lakabin ya shafi marasa lafiya tare da NSCLC suna karɓar kulawa ko magani na biyu ko mafi girma. Wadannan alamomin za a iyakance su ne ga marasa lafiyar wadanda ciwowar su na da EGFR ya goge 19 ko kuma sauya 21 L858R maye gurbin maye gurbinsu kamar yadda gwajin da FDA ta amince da shi ya gano. Alamar layin farko a baya an iyakance ta ne ga marasa lafiya tare da sharewar EGFR 19 da yawa ko maye gurbin maye gurbin 21.

Wannan ƙarin lakanin ya dogara ne da sakamakon gwajin IUNO, bazuwar, makafi biyu, sarrafa wuribo, gwajin erlotinib wanda aka gudanar azaman maganin kulawa da marasa lafiya 643 tare da ci gaban NSCLC waɗanda ba su sami ci gaban cutar ba ko kuma cutar da ba za a yarda da ita ba yayin zagaye huɗu na Layin farko na maganin cutar kantin. Marasa lafiya waɗanda ciwace ciwowinsu ke kunna maye gurbi na EGFR (share 19 ko cire 21 L858R maye gurbi) an cire su daga wannan gwaji. An rarraba marasa lafiya 1: 1 don karɓar erlotinib ko placebo a baki sau ɗaya kowace rana (322 erlotinib, 321 placebo) har sai ci gaba da cutar ko cutar da ba a yarda da ita ba. Bayan ci gaba kan farfadowa na farko, marasa lafiya sun cancanci shiga matakin lakabi. Kashi hamsin na marasa lafiya da aka bazu zuwa erlotinib sun shiga cikin lakabin bude-layi kuma sun sami chemotherapy, yayin da 77% na marasa lafiya da bazuwar zuwa placebo suka shiga cikin lokacin buɗe lambar kuma suka karɓi erlotinib.

Matsayin farko na gwajin shine rayuwa gabaɗaya. Sakamako ya nuna cewa rayuwa bayan bin magani tare da erlotinib bai fi placebo da aka gudanar azaman kiyayewa a cikin marasa lafiya tare da ƙananan ƙwayoyin NSCLC ba waɗanda ke ɗaukar maye gurbin EGFR. Babu wani bambanci a cikin rai mara ci gaba tsakanin hannun erlotinib da hannun wuribo.

FDA ba za ta buƙaci sabon buƙatun bayan tallace-tallace ba ko neman alƙawarin bayan tallace-tallace dangane da sakamakon gwajin IUNO.

AASraw shine ƙwararren masanin Erlotinib.

Da fatan za a danna nan don bayanin zance: Saduwa da mu

 

Summary

Erlotinib magani ne na roba da aka tsara don maganin cutar kansa. An yarda da shi don magance ƙananan ƙwayoyin cuta na huhu, cutar kansa mai saurin ƙwayar cuta, da kuma ciwon sankara. Yi bitar illolin, sashi, mu'amalar miyagun ƙwayoyi, gargaɗi da kiyayewa, da kuma bayanin lafiyar mai ciki kafin amfani Erlotinib.

 

reference

[1] Thomas L. Petty, MD (2003). "Masu ƙayyadewa game da Tumor Response da Rayuwa Tare da Erlotinib a cikin Marasa lafiya Tare da Wadanda Ba Su da Canananan Cutar Ciwon Cutar Hanta". Jaridar Clinical Oncology. 1 (17): 3-4.

[2] "FDA ta Amince da Roche Test a matsayin CDx don Tarceva don Kula da wasu Marasa lafiya NSCLC". Sabbin Yanar. An dawo da 10 Janairu 2020.

[3] Dudek AZ, Kmak KL, Koopmeiners J, et al. (2006). "Sashin fata da kuma tarihin jijiyoyin jini yana daidaita da fa'idar asibiti ga marasa lafiya waɗanda aka kula da su tare da gefitinib a matsayin magani don magance cutar ta ci gaba ko metastatic wacce ba ƙaramar kwayar cutar huhu ba." Ciwon huhu. 51 (1): 89-96.

[4] Jones HE, Goddard L, Gee JM, Hiscox S, Rubini M, Barrow D, Knowlden JM, Williams S, Wakeling AE, Nicholson RI: Alamar haɓakar insulin-mai karɓar sigina kuma ya sami juriya ga gefitinib (ZD1839; Iressa) a nonon mutum da kwayoyin cutar kansar mafitsara. Ciwon daji na Endocr Relat. 2004 Dec; 11 (4): 793-814.

[5] Kobayashi K, Hagiwara K (2013). "Kwayar cutar mai saurin karba mai karba (EGFR) maye gurbi da kuma kebantaccen magani a ci gaba da cutar kanjamau mai cike da nonsmall (NSCLC)". Ilimin Oncology. 8 (1): 27–33. Doi: 10.1007 / s11523-013-0258-9. PMC 3591525. PMID 23361373.

[6] Cohen, Martin H.; Johnson, John R.; Chen, Yeh-Fong; Sridhara, Rajeshwari; Pazdur, Richard (Agusta 2005). "FDA taƙaitaccen taƙaitaccen magani: allunan erlotinib (Tarceva)". Masanin ilimin Oncologist. 10 (7): 461–466.

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[8] "Maganin cutar kansa: Kotun Koli ta ba Cipla damar janye daukaka kara game da Roche". Lokacin Tattalin Arziki. 16 Yuni 2017. An ajiye daga asali a ranar 24 Disamba 2019. An dawo da 23 Disamba 2019.

[9] Delbaldo C, Faivre S, Raymond E: [Epidermal girma factor hanawa]. Rev Med Interne. 2003 Jun; 24 (6): 372-83.

[10] Chen X, Ji ZL, Chen YZ: TTD: Database na Target. Magungunan Nucleic Acid Res. 2002 Janairu 1; 30 (1): 412-5.

[11] Filppula AM, Neuvonen PJ, Backman JT: A cikin ƙididdigar in vitro game da tasirin hana lokaci akan CYP2C8 da CYP3A aiki ta masu hana haɓakar furotin goma sha huɗu. Magungunan ƙwayoyi na Metab. 2014 Jul; 42 (7): 1202-9. Doi: 10.1124 / dmd.114.057695. Epub 2014 Apr 8.

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