Ndeapi Ruzivo Rwaunofanirwa Kuziva Usati Washandisa Erlotinib - AASraw
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Erlotinib

 

  1. Chii chinonzi Erlotinib?
  2. Erlotinib Anoshanda Sei?
  3. Ndezvipi Zvirwere Zvinotarisirwa naErlotinib?
  4. Erlotinib Parizvino Anoshandiswa Sei Mukiriniki?
  5. Erlotinib Anonyanya Kubudirira Mune Varwere Vapi?
  6. Chii chinonzi Erlotinib Kuramba?
  7. Ndedzipi Ndidzo Njodzi Dzakabatana naErlotinib?
  8. Ndeapi madhiragi kana ekuwedzera anopindirana naErlotinib?
  9. FDA Yakagamuchirwa Erlotinib Kurapa
  10. pfupiso

 

Chii Erlotinib

Erlotinib (CAS:183321-74-6ndeyekirasi yemishonga inozivikanwa se tyrosine kinase inhibitors. Inoshanda nekudzivirira kushanda kweprotein inonzi epidermal kukura factor receptor (EGFR). EGFR inowanikwa pamusoro pemasero mazhinji egomarara pamwe nemasero akajairwa. Inoshanda se "kanyanga," ichigamuchira zviratidzo kubva kune mamwe maseru uye nharaunda inotaurira sero kukura nekukamurana. Iyo EGFR inoita basa rakakosha mukukura uye kukura prenatally uye panguva yehucheche uye inobatsira kuchengetedza zvakajairwa kutsiva kwemaakare uye akakuvara maseru muvakuru. Zvisinei, masero emukenza mazhinji ane huwandu husingaenzanisike hweEGFR pamusoro payo, kana EGFR yavo yakashandurwa nekuchinja kweDNA inotakura iyo genetic kodhi yeproteine. Mhedzisiro yacho ndeyekuti zviratidzo zvinouya kubva kuEGFR zvakanyanyisa kusimba, zvichitungamira mukuwandisa kwemasero kukura uye kupatsanurwa, chiratidzo checancer.

 

Zvinoita Sei Erlotinib Basa? 

Iyo michina yekiriniki antitumor chiito cheerlotinib haina kunyatso kuzivikanwa. Erlotinib inhibits iyo intracellular phosphorylation ye tyrosine kinase inosangana neiyo epidermal growth factor receptor (EGFR). Hakananga yekudzivirira maererano nezvimwe tyrosine kinase receptors haina kunyatso kuzivikanwa. EGFR inoratidzirwa pane sero pamusoro pemasero akajairwa uye maseru ekenza.

 

Zvinoitwa nezvirwere Erlotinib Kunyanya Kubata? 

(1) Kanza yemaperembudzi

Erlotinib mune isingazivikanwe isina-diki kenza yemapapu kenza kana ichiwedzerwa kune chemotherapy inovandudza kurarama kwese ne19%, uye nekuvandudza kufambira mberi-kusununguka kwehupenyu (PFS) ne29%, kana ichienzaniswa nekemotherapy chete. US Food and Drug Administration (FDA) yakabvumidzwa. erlotinib yekurapa yekenza yemuno yepamusoro kana metastatic isiri-diki kenza yemapapu kenza iyo yakundikana chero imwechete yekutanga chemotherapy regimen.

Mune kenza yemapapu, erlotinib yakaratidzirwa kuve inoshanda kune varwere vane kana vasina EGFR shanduko, asi inoita kunge inoshanda zvakanyanya kune varwere vane EGFR shanduko. kurapa (docetaxel kana pemetrexed). Yakazara mhinduro ndeye 50% zvirinani pane yakajairwa yechipiri-mutsara chemotherapy Varwere vasiri vaputi, uye vasina kumbobvira vaputa, vane adenocarcinoma kana subtypes seBAC vanowanzo kuve nekuchinja kweEGFR, asi shanduko dzinogona kuitika mumhando dzese dzevarwere. . Muedzo wekuchinja kweEGFR wakagadzirwa neGenzyme.

 

(2) Kenza yepancreatic

MunaNovember 2005, iyo FDA yakabvumidza erlotinib pamwe chete ne gemcitabine yekurapwa kwekenza yepamberi, isinga gadzirisike, kana metastatic cancer.

AASraw ndiye nyanzvi yekugadzira Erlotinib.

Ndokumbirawo ubaye pano kuti uwane ruzivo Cont Cont us

 

(3) Kuramba kurapwa

Erlotinib akasungirwa ErbB1 pa 2.6A resolution; pamusoro pevara rinoratidza hydrophobicity.Sezvimwe nezvimwe ATP inokwikwidza idiki mamorekuru tyrosine kinase inhibitors, senge imatinib muCML, varwere vanokurumidza kusagadzikana. Muchiitiko che erlotinib izvi zvinowanzoitika mwedzi 8-12 kubva pakutanga kwekurapwa. Kupfuura 50% yekushomeka kunokonzerwa nekuchinja mune iyo ATP inosunga homwe yeEGFR kinase domain inosanganisira kuchinjisa diki polar threonine masara ane hombe nonpolar methionine masara (T790M) .Angangoita 20% yekurwisa zvinodhaka kunokonzerwa nekusimudzira kweiyo hepatocyte grow factor receptor, iyo inotyaira ERBB3 inoenderana nekuitwa kwePI3K.

 

Erlotinib

 

sei Is Erlotinib Ckukurumidza Used In The Clinic?

Erlotinib akatanga kubvumidzwa neUnited States Chikafu neDrug Administration (FDA) kuti ishandiswe mune varwere vane epamberi isiri-diki kenza yemapapu yemapapu avo vakadzokazve mushure meimwe imwe mhando yerapi. Muna 2005, yakagamuchirwa kuti ishandiswe pamwe chete nemumwe mushonga, gemcitabine, yekenza yepancreatic yepamberi. Muna 2010, kushandiswa kwayo kwakawedzerwa kusanganisira kurapa kurapwa kwevarwere vane epamberi isiri-diki kenza yemapapu kenza iyo chirwere ichi chakadzikama mushure memakona mana ekurapwa neplatinum-based drug, senge cisplatin kana carboplatin. Varwere vanotora erlotinib vanowanzo shivirira mushonga uyu zvakanaka. Mhedzisiro inowanzoitika ndeyekuputika kweganda uye manyoka.

 

In Which Patients Is Erlotinib Mmabvazuva Effective?

Mumakore gumi apfuura, varapi vakawana ruzivo rwakakura ne tyrosine kinase inhibitors, sa erlotinib, inovhara iyo EGFR. Zvave kuwedzera pachena kuti mishonga iyi inoshanda zvakanyanya muvarwere vane kenza yemapapu inotakura imwe mhando yekuchinja iyo inoguma neisina kujairika EGFR protein. Varwere ava vanogona kunge vari verudzi rweAsia, vakadzi, uye vasingatomboputa vane fomu yekenza yemapapu inozivikanwa se bronchoalveolar adenocarcinoma. Nekudaro, muna2013, erlotinib yakabvumidzwa kuve yekutanga kurapwa kweiyi subgroup yevarwere, kana gomarara ravo risingakwanise kurapwa kurapwa.

 

chii Is Erlotinib Rrubatsiro?

Erlotinib inoshanda zvakanyanya mune subset yevarwere vakatakura EGFR shanduko. Zvisinei, kunyangwe varwere ava vanozopedzisira vatanga kuratidza kufambira mberi kwekenza yavo mushure memwedzi gumi nemiviri yeerlotinib therapy. Izvi zvinokonzerwa nekusimudzira kwekushomeka kwemushonga mumasero egomarara akasara. Muzviitiko zvakawanda, kuramba kunoguma kubva mukuvandudzwa kweshanduko yechipiri mupuroteni yeEGFR iyo inodzivirira erlotinib kubva mukubatanidza kune dombo re tyrosine kinase. Maitiro matsva ekurapa varwere aya anosanganisira tyrosine kinase inhibitor afatinib, iri yoga kana yakabatana necetuximab (Erbitux), iyo inotadzisa iyo EGFR neimwe nzira.

 

Ndedzipi Ndidzo Njodzi Dzakabatana naErlotinib?

Mune zvidzidzo, zvinowanzoitika mhedzisiro neErlotinib painoshandiswa semonotherapy yekenza yemapapu yaive yekumhanyisa (yaibata 75% yevarwere), manyoka (54%), kurasikirwa nechido uye kuneta (52% imwe neimwe). Mune ongororo yaTarceva inoshandiswa pamwe chete ne gemcitabine yekenza yepancreatic, mhedzisiro yakajairika yaive kuneta (kubata 73% yevarwere), mapundu (69%) uye manyoka (48%). Kuti uwane izere rondedzero yemhedzisiro uye zvinorambidzwa neErlotinib, ona iyo pepa pepa.

 

izvo Dmagumbezi kana Supplements Interact With Erlotinib?

CYP3A4 i enzyme iri muchiropa inoputsika-pasi uye inobatsira kubvisa erlotinib kubva mumuviri. Mishonga inodzivisa CYP3A4 inogona kukonzeresa mazinga erlotinib mumuviri, uye iwo mazinga epamusoro anogona kukonzera huturu kubva kuerlotinib. Mishonga yakadaro inosanganisira atazanavir (Reyataz), clarithromycin (Biaxin), indinavir (Crixivan), itraconazole (Sporanox), ketoconazole (Nizoral), nefazodone (Serzone), nelfinavir (Viracept), ritonavir (Norvir), saquasevir (Invvase) telithromycin (Ketek), uye voriconazole (VFEND). Mune varwere vanogamuchira iyi mishonga, yakaderera dosi yeerlotinib inogona kudikanwa kudzivirira huturu.

Mimwe mishonga inowedzera kubviswa kweerlotinib nekuwedzera chiitiko cheCYP3A4 enzymes. Izvi zvinoderedza nhanho dzeerlotinib mumuviri uye zvinogona kudzikisira maitiro acho. Mienzaniso yemishonga yakadaro inosanganisira rifampicin (Rifadin), rifabutin (Mycobutin), rifapentine (Priftin), phenytoin (Dilantin), carbamazepine (Tegretol), phenobarbital neSt. John's Wort. Iyi mishonga inofanirwa kudzivirirwa mune varwere vanotora erlotinib, kana zvichibvira. Kana mamwe madhiragi asiri iwo sarudzo, mizinga yepamusoro yeerlotinib inogona kudiwa. Kusvuta fodya zvakare kunoderedza kuwanda kweerlotinib muropa. Varwere vanorayirwa kuti varege kusvuta.

Mishonga inoderedza kugadzirwa kweacid mudumbu inoderedza kunwa kweerlotinib. Naizvozvo, proton pump inhibitors (semuenzaniso, maPI, semuenzaniso, omeprazole [Prilosec, Zegerid]) haifanire kupihwa neerlotinib, uye erlotinib inofanira kupihwa maawa gumi H10-receptor blockers (semuenzaniso, ranitidine [Zantac]) kana maawa maviri mushure kutora H2-receptor blocker.

Kutungamirwa kwemaantacids kunofanira kupatsanurwa kubva mukutungamira kweerlotinib nemaawa akati wandei. Erlotinib yave ichibatanidzwa neyakawedzera njodzi yekubuda ropa, kunyanya kune varwere vanotorawo warfarin (Coumadin). Varwere vanotora warfarin vanofanirwa kuongororwa zvakanyanya.

 

FDA Yakagamuchirwa Erlotinib mabatiro

Musi waGumiguru 18, 2016, iyo US Kudya neDrug Administration yakashandura chiratidzo che erlotinib (TARCEVA, Astellas Pharm Global Development Inc.) yekurapa kenza isiri-diki kenza yemapapu yemapapu (NSCLC) kudzora kushandiswa kune varwere vane mamota ane chaiwo epidermal kukura factor receptor (EGFR) shanduko.

Iko kunyorera shanduko kunoshanda kuvarwere vane NSCLC vanogashira yekuchengetedza kana yechipiri kana yakakura kurapa mutsara. Zviratidzo izvi zvichaganhurirwa kune avo varwere vane mamota ane EGFR exon 19 kubviswa kana exon 21 L858R chinja shanduko sezvinoonekwa nemuedzo unobvumidzwa neDFA. Mutsara wekutanga wairatidza kare waive wakaganhurirwa kune varwere vane EGFR exon 19 kubviswa kana exon 21 chinja shanduko.

Izvi zvinowedzera kuwedzera kunobva pamhedzisiro yeiyedzo yeIUNO, yakasarudzika, yakapofomara-yakapofumadzwa, inodzorwa ne placebo, kuyedzwa kweerlotinib inoitwa senzira yekurapa muvarwere mazana matanhatu nemakumi matanhatu nevemberi NSCLC vasina kumboona kufambira mberi kwechirwere kana huturu husingagamuchirike panguva ina dzekutenderera platinum-based-first-line chemotherapy. Varwere vane mamota avo akachengetedza shanduko yeEGFR (exon 643 kubviswa kana exon 19 L21R shanduko) vakabviswa pamuedzo uyu. Varwere vakasarudzika 858: 1 kuti vagamuchire erlotinib kana placebo nemuromo kamwe chete zuva nezuva (1 erlotinib, 322 placebo) kudzamara hosha ichiwedzera kana hutachiona husingagamuchirwe. Kutevera kufambira mberi pakurapa kwekutanga, varwere vaikodzera kupinda muchikamu chakavhurika. Makumi makumi mashanu muzana evarwere vakasarudzika erlotinib vakapinda muakavhurika-kara chikamu uye vakagamuchira chemotherapy, nepo 321% yevarwere vakasarudzika ku placebo vakapinda muakavhurika-chikamu chikamu uye vakagamuchira erlotinib.

Ekupedzisira kwekutongwa kwekutongwa kwaive kupona kwese. Mhedzisiro yakaratidza kuti kupona mushure mekurapwa neerlotinib kwaive kusiri nani pane placebo yakapihwa sekuchengetedza mune varwere vane metastatic NSCLC mamota asiri kuchengeta EGFR-inomutsa shanduko. Hapana musiyano mukupfuurira mberi-kwemahara kupona pakati peerlotinib ruoko uye ruoko rwe placebo rakaonekwa.

FDA haidi zvinoda zvitsva zvekushambadzira kana kukumbira post-kushambadzira kuzvipira kunoenderana nezvabuda muyedzo yeIUNO

AASraw ndiye nyanzvi yekugadzira Erlotinib.

Ndokumbirawo ubaye pano kuti uwane ruzivo Cont Cont us

 

pfupiso

Erlotinib mushonga unogadzirwa wakatemerwa kurapwa kwekenza. Iyo inobvumidzwa kurapa isiri-diki kenza yemapapu kenza, yakakwira isingadzoreke metastatic kenza yeprostate, uye yekenza yepancreatic. Ongorora mhedzisiro, muyero, kudyidzana kwezvinodhaka, yambiro uye matanho, uye nhumbu kuchengetedza ruzivo pamberi shandisa Erlotinib.

 

Reference

[1] Thomas L. Petty, MD (2003). "Kutsunga kweKumhanyisa Kupindura uye Kupona naErlotinib mune Varwere Vasiri-Mashoma-Maseru Lung Cancer". Zvinyorwa zveKiriniki Oncology. 1 (17): 3-4.

[2] "FDA Inotendera Roche Bvunzo seCDx yeTarceva yekurapa Vamwe Varwere veNSCLC". GenomeWeb. Yakadzorerwa 10 Ndira 2020.

[3] Dudek AZ, Kmak KL, Koopmeiners J, uye al. (2006). "Kuputika kweganda uye bronchoalveolar histology inoenderana nekiriniki kubatsirwa mune varwere vanorapwa negefitinib senzira yekurapa yakamborapwa yepamusoro kana metastatic isiri-diki kenza yemapapu yemukenza". Kenza Yemapapu. 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: Insulin-senge chinhu chekukura-ini receptor chiratidzo uye ndawana kuramba gefitinib (ZD1839; Iressa) mu zamu revanhu uye gomarara reprostate maseru. Endocr Relat Kenza. 2004 Zvita; 11 (4): 793-814.

[5] Kobayashi K, Hagiwara K (2013). "Epidermal growth factor receptor (EGFR) mutation uye yakasarudzika kurapa mune yepamusoro nonsmall cell lung cancer (NSCLC)". Targeted 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 (Nyamavhuvhu 2005). "FDA mvumo yemvumo yemishonga: erlotinib (Tarceva) mapiritsi". Iyo Oncologist. 10 (7): 461-466.

[7] Blum G, Gazit A, Levitzki A: Substrate yemakwikwi inhibitors eGG-1 receptor kinase. Biochemistry. 2000 Zvita 26; 39 (51): 15705-12.

[8] "Chirwere cheCancer: Dare Repamusorosoro rinobvumidza Cipla kubvisa kukwidza mhosva pamusoro paRoche". Nguva Yehupfumi. 16 June 2017. Yakachengetwa kubva kune yekutanga musi wa24 Zvita 2019. Yakadzorerwa 23 Zvita 2019.

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

[10] Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nyukiliya Acids Res. 2002 Jan 1; 30 (1): 412-5.

[11] Filppula AM, Neuvonen PJ, Backman JT: In vitro kuongororwa kwenguva-inoenderana inhibitory mhedzisiro kuCYP2C8 uye CYP3A chiitiko negumi nemana protein kinase inhibitors. Zvinodhaka Metab Dispos. 2014 Jul; 42 (7): 1202-9. doi: 10.1124 / dmd.114.057695. Epub 2014 Kubvumbi 8.

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