6 Mibvunzo Nezve Afatinib paAnti-Caners (NSCLC) - AASraw
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Afatinib

 

  1. Chii chinonzi Afatinib?
  2. Patinoda Afatinib?
  3. Afatinib Inoshanda Sei?
  4. Aive Afatinib Yakagamuchirwa neDFA? Chokwadi
  5. Ndeipi Njodzi / mhedzisiro Inounzwa neAfatinib?
  6. Ndezvipi Zvimwe Zvekutsvaga Nezve Afatinib?

 

chii Is Afatinib?

Afatinib (CAS: 439081-18-2) inotarisirwa kurapwa mishonga iyo inozivikanwawo seGiotrif. Iyo inoshandiswa kurapa isiri-diki kenza yemapapu kenza (NSCLC) iyo yatanga kupararira kunze kwepapu kana kune zvimwe zvikamu zvemuviri. Inogona zvakare kushandiswa kurapa mamwe makenza sechikamu chekiriniki kuyedzwa.

Zvakanakisisa kuverenga ruzivo urwu neruzivo rwedu ruzhinji nezve kenza yemapapu kana mhando yekenza yauinayo. Chiremba wako achataura newe nezve kurapwa uku pamwe nemhedzisiro yazvo usati wabvuma (kubvuma) kurapwa. Panguva yekurapwa, iwe uchaona chiremba wekenza kana mukoti. Uyu ndiye watinoreva patinotaura chiremba kana mukoti mune iri ruzivo.

 

Patinenge Tichida Afatinib

Afatinib inogona kushandiswa kurapa isiri-diki kenza yemapapu kenza (NSCLC) iyo ine:

Read Pararira kumatunhu akakomberedza (enzvimbo yepamusoro)

Read Pararira kune zvimwe zvikamu zvemuviri (zvemberi kana metastatic).

Afatinib inoshanda chete kumagomarara ane fomu isina kujairika yeprotein inonzi epidermal kukura factor receptor (Egfr). Kuyedza kunoitwa pane maseru ekenza kubva kubiopsy kana kuvhiyiwa kwakapfuura kutarisa mwero weEGFR. Izvi zvinotaurira chiremba wako kana afatinib angangokubatira iwe.

 

Zvinoita Sei Afatinib Basa?

Afatinib ine simba uye inosarudza, isingadzoreke ErbB yemhuri blocker. Afatinib inosunga kwazvo uye isingadzokere shure kuvharira kusaina kubva kune vese homo nemaheterodimers akaumbwa nenhengo dzemhuri yeErbB EGFR (ErbB1), HER2 (ErbB2), ErbB3 uye ErbB4.

Kunyanya, afatinib inosunga zvakasunga kune iyo kinase domains yeEGFR (ErbB1), HER2 (ErbB2), uye HER4 (ErbB4) uye isingadzokere shure inodzivisa tyrosine kinase autophosphorylation, zvichikonzera kudzikiswa kwechiratidzo cheErbB. Dzimwe shanduko muEGFR, kusanganisira dzisiri-dzinochinja mutserendende mukinase domain, dzinogona kukonzeresa kuwedzera autophosphorylation yeiyo receptor, zvichitungamira kugashira activation, dzimwe nguva mukushayikwa kwegigand inosunga, uye inogona kutsigira kuwanda kwesero muNSCLC. Shanduko dzisingapikisi dzinotsanangurwa seidzo dzinoitika mumakoni anoita kinase domain yeEGFR inotungamira mukuwedzera receptor receptor uye iko kushanda kunofungidzirwa ne1) kuchipatara zvine mutsigo tumarara shrinkage nedhivhosi yakakurudzirwa yeafatinib uye / kana 2) kuvharidzira kwema cell kuwanda. kana EGFR tyrosine kinase phosphorylation pazvikamu zveafatinib yakagadzikana pamutero wakakurudzirwa zvichienderana nenzira dzakabvumidzwa. Dzinonyanya kuwanikwa dzekuchinja uku ndidzo exon 21 L858R inotsiva uye exon 19 kubviswa.

Zvakare, afatinib yakaratidza kuvharirwa kwe autophosphorylation uye / kana in vitro kuwanda kwemasero mitsara inoratidzira yemusango-EGFR uye mune avo vanoratidzira vakasarudzwa EGFR exon 19 deletion mutations, exon 21 L858R shanduko, kana zvimwe zvishoma zvakajairika zvisingapikise shanduko, pane afatinib kuwanda kwakakwenenzverwa. mune varwere. Uye zvakare, afatinib inhibited in vitro kuwanda kwemasero mitsara kunyanyisa HER2.

AASraw ndiye nyanzvi yekugadzira yeAfatinib.

Ndokumbirawo ubaye pano kuti uwane ruzivo Cont Cont us

 

aiva Afatinib Yakagamuchirwa neDFA? Chokwadi

Kubvumidzwa kunopa mutsva wechipiri-mutsara wekurapa sarudzo yevarwere vane yechipiri yakakura-diki-rudzi rweasiri-madiki masero kenza yemapapu (NSCLC), inomiririra ingangoita 20-30% yematambudziko eNSCLC

Kubvumidzwa kwakavakirwa pamhedzisiro yeLUX-Lung 8 kudzidza, iyo yakaratidza zvakanyanya kuvandudzwa kwehupenyu hwese uye kufambira mberi-kwemahara kuenzaniswa naTarceva (erlotinib) mune varwere vane squamous cell carcinoma yemapapu.

Afatinib yakatobvumidzwa munyika dzinopfuura makumi matanhatu kurapa varwere vane mhando dzakasiyana dzeEGFR mutation-positive NSCLC

Afatinib

Ndeipi Njodzi/ Mhedzisiro Izvozvo Afatinib Uyai? 

Zvinhu zvakakosha zvekurangarira nezve mhedzisiro yeafatinib:

▪ Vanhu vazhinji havazowani zvese afatinib mhedzisiro yakanyorwa.

▪ Afatinib mhedzisiro inowanzo fungidzirwa maererano nekutanga kwavo, nguva, uye kuomarara.

▪ Afatinib mhedzisiro inowanzo kuve inodzoserwa uye inozopera mushure mekurapwa kwapera.

▪ Afatinib mhedzisiro inogona kunge ichikwanisika. Pane zvakawanda zvingasarudzwa zvekudzora kana kudzivirira mhedzisiro yeafatinib.

 

Iyi inotevera mhedzisiro yakajairika (inoitika mune yakakura kupfuura 30%) yevarwere vanotora afatinib:

▪ Manyoka

▪ Kuputika kweacneiform (boka remamiriro eganda akafanana neacne)

▪ Maronda emumuromo

▪ Paronychia (kubatwa nezvipikiri)

▪ Mukanwa makaoma

 

Aya mashoma mashoma mhedzisiro (anoitika mu10-29%) yevarwere vanogashira afatinib:

▪ Kuderedza kudya

▪ Kuvava

▪ Kuonda

▪ Mhuno inobuda ropa

▪ Cystitis (chirwere chedundira)

▪ Cheilitis (kuzvimba kwemiromo)

▪ Fivha

▪ Hypokalemia (yakaderera potasium)

▪ Conjunctivitis (ziso repingi)

▪ Rhinorrhea (kubuda mvura)

▪ Ma enzymes eropa akakwirira

Haasi ese mhedzisiro akanyorwa pamusoro. Zvimwe zvisingawanzoitika (zvinoitika mune isingasviki gumi muzana yevarwere) hazvina kunyorwa pano. Gara uchizivisa mupi wako wezvehutano kana iwe uchinge wawana chero zviratidzo zvisina kujairika.

 

Ndezvipi Zvimwe Zvekutsvaga Nezve Afatinib?

 Afatinib (BIBW 2992) kukura mune isiri-diki-sero gomarara kenza

Afatinib (BIBW 2992), inoveli aniline-quinazoline yakabva, isingadzoreke uye zvine simba inongedzera mukati meinase chiitiko chese anoshanda ErbB receptor mitezo yemhuri. Preclinical mhedzisiro inoratidza kuti afatinib inoshanda mumhando dzemukenza yemapapu, kusanganisira avo vane EGF receptor (EGFR) shanduko inopesana neyekutanga-chizvarwa EGFR inhibitors. Afatinib iri kuferefetwa muchirongwa cheLUX-Lung, chinozoongorora afatinib sechirapa chekutanga mune varwere vane EGFR-inogadzirisa shanduko (LUX-Lung 2, 3 na6) uye seyechipiri- kana wechitatu-mutsara kurapwa mune varwere iyo yawana kuramba kwegefitinib uye / kana erlotinib (LUX-Lung 1, 4 ne5). LUX-Lung 1 uye 2 vakaratidza, mukati memapoka avo akatarisana, kuwedzera kwakanyanya muchirwere chekudzivirira huwandu hwe58 uye 86%, zvichiteerana, uye nekuwedzera kuwedzerwa kwekuenderera-kusununguka kwekupona. Kupfuurirazve Phase III kiriniki miedzo irikuenderera mberi kuongorora afatinib mukubatana ne paclitaxel (LUX-Lung 5), uye ichienzaniswa necisplatin / pemetrexed (LUX-Lung 3) kana cisplatin / gemcitabine (LUX-Lung 6).

AASraw ndiye nyanzvi yekugadzira yeAfatinib.

Ndokumbirawo ubaye pano kuti uwane ruzivo Cont Cont us

 

 Afatinib mune yemuno yepamusoro uye metastatic chordoma

Iyi ndiyo Phase 2 kuyedza uchidzidza kushanda kwe yakanangwa cancer cancer inonzi afatinib. Afatinib inhibits iyo EGFR protein, iyo inofungidzirwa kuve inobatanidzwa mukutyaira kukura kwecordoma tumors. Ichi chidzidzo chakagadzirirwa zvakanangana nevarwere vechordoma makore gumi nemasere kana kupfuura vane tumarara twemazuva ese. Parizvino yakavhurika kuLeiden University Medical Center (LUMC) uye University College London Hospital (UCLH) uye ichavhura kuIstituto dei Nazionale Tumori (INT) muMilan mumwedzi inotevera. Vanoongorora zvakanyanya pachidzidzo ichi ndiDr.Hans Gelderblom kuLUMC, Dr. Silvia Stacchiotti kuInt, naDr.Sandra Strauss kuUCLH.

Epidermal Growth Factor Receptor (EGFR) ipuroteni inowanikwa pamusoro pemamwe maseru mumuviri wese. Kazhinji, EGFR inobatsira kudzora kukura kwesero uye inoita basa mukupora kwemaronda. Mune mamwe kanzira, kusanganisira mazhinji chordomas, EGFR inova yakanyanyisa kushanda, zvichitungamira maseru ekenza kuti awedzere kunze kwekudzora.

Mishonga inovhara EGFR inonzi "EGFR inhibitors" inobvumidzwa kurapa akasiyana marudzi ekenza. Afatinib iri EGFR inhibitor iyo parizvino inogamuchirwa kurapa isiri-diki-sero kenza yemapapu uye iri kuongororwa mune mamwe mamota marudzi.

Akawanda EGFR inhibitors akaratidzirwa kunonoka kana kumisa kukura kwechordoma maseru uye chordoma tumors mumakonzo. Pane ese EGFR inhibitors akaedzwa, afatinib ndiyo yainyanyo shanda mumakonzo mamodheru echordoma. Mune mamwe mamodheru modhi, zvakadzora kukura kwemamota, nepo kune mamwe zvakakonzeresa kuti mamota aderere zvakanyanya. Uyu muedzo wakanangana nekuona kana afatinib inogona kudzika kana kumisa kukura kwechordoma tumors mune varwere vane zvinowanzoitika kana metastatic chirwere.

 

Reference

[1] Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel Frühjahr 2013. (muchiGerman)

[2] Spreitzer H (13 Chivabvu 2008). "Neue Wirkstoffe - Tovok". Österreichische Apothekerzeitung (muchiGerman) (10/2008): 498.

[3] Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, et al. (Nyamavhuvhu 2008). "BIBW2992, isingachinjiki EGFR / HER2 inhibitor inoshanda zvakanyanya mumhando dzepenza dzemapapu". Oncogene. 27 (34): 4702–11. doi: 10.1038 / onc.2008.109. PMC 2748240. PMID 18408761.

[4] "Giotrif: EPAR -Product Ruzivo" (PDF). European Medicines Agency. Boehringer Ingelheim International GmbH. 16 Gumiguru 2013. Yakadzorerwa 28 Ndira 2014.

[5] Kobayashi Y, Togashi Y, Yatabe Y, Mizuuchi H, Jangchul P, Kondo C, et al. (Zvita 2015). "EGFR Exon 18 Shanduko muCancer Lung: Molecular Predictors yeAugmented Sensitivity kune Afatinib kana Neratinib zvichienzaniswa neyekutanga- kana chechitatu-chizvarwa TKIs". Kliniki yeKenza Ongororo. 21 (23): 5305–13. doi: 10.1158 / 1078-0432.CCR-15-1046. PMID 26206867.

[6] Lin NU, anokunda EP, Wheatley D, Carey LA, Houston S, Mendelson D, et al. (Chikumi 2012). "Chikamu chepiri chechipiri cheafatinib (BIBW 2992), isingachinjiki ErbB yemhuri blocker, mune varwere vane HER2-positive metastatic kenza yemazamu ichifambira mberi kwe trastuzumab". Kenza Yezamu uye Ongororo. 133 (3): 1057-65. doi: 10.1007 / s10549-012-2003-y. PMC 3387495. PMID 22418700.

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