6 Fesili e uiga i Afatinib i Aneti-Caners (NSCLC) - AASraw
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Afatinib

 

  1. O le a le Afatinib?
  2. Pe a Tatou Manaʻomia Afatinib?
  3. Faʻafefea ona galue Afatinib?
  4. Na faʻatagaina Afatinib e le FDA? Mautinoa
  5. O a ni lamatiaga / Aafiaga e maua mai i Afatinib?
  6. O a isi suʻesuʻega e uiga i Afatinib?

 

ā Is Afatinib?

Afatinib (CAS: 439081-18-2) o se fualaʻau faʻatulagaina togafitiga faʻapitoa e lauiloa foi o le Giotrif. E faʻaaogaina e togafitia ai le kanesa ninii o le sela sela (NSCLC) ua amata ona sosolo i fafo atu o le māmā poʻo isi vaega o le tino. E mafai foʻi ona faʻaaoga e togafitia ai isi kanesa o se vaega o le suʻesuʻega faʻafomaʻi.

E sili le faitau i nei faʻamatalaga ma matou lautele faʻamatalaga e uiga i kanesa kanesa poʻo le ituaiga kanesa o loʻo ia te oe. O le a talanoa atu lau fomaʻi ia te oe e uiga i nei togafitiga ma ona aʻafiaga ono e te leʻi malie ai (malie i ai) e faia ou togafitiga. I taimi o togafitiga, o le a e vaʻai i se fomaʻi kanesa poʻo se teine ​​tausimaʻi. Lenei matou te faʻauiga iai pe a matou taʻua se fomaʻi poʻo se tausi soifua i lenei faʻamatalaga.

 

Pe a Tatou Manaʻomia Afatinib

Afatinib e mafai ona faʻaaogaina e togafitia ai le laʻititi sela kanesa mama (NSCLC) o loʻo i ai:

♦ Faʻasalalau atu i autafa o aano (faʻalautele i totonu)

♦ Faʻasalalau i isi vaega o le tino (advanced pe metastatic).

Afatinib naʻo galue mo kanesa o loʻo iai se tulaga le masani ai o se polotini e taʻua o le epidermal tuputupu aʻe mea taliaina (EGFR). O suʻega e faia i sela o le kanesa mai le biopsy poʻo se taotoga muamua e siaki ai le maualuga o le EGFR. E taʻu atu ai i lau fomaʻi pe ono galue le afatinib mo oe.

 

E faapefea ona Afatinib Galue?

Afatinib o se malosi ma filifili, le mafai ona toe suia ErbB aiga poloka. Afatinib covalently fusifusia i ma le toe suia poloka faailo mai uma homo ma heterodimers fausiaina e le ErbB aiga tagata EGFR (ErbB1), HER2 (ErbB2), ErbB3 ma ErbB4.

Ae maise lava, afatinib covalently fusifusia i le kinase domains o EGFR (ErbB1), HER2 (ErbB2), ma le HER4 (ErbB4) ma le le mafai ona toe taofia le tyrosine kinase autofosforilasi, mafua ai le faʻaleagaina o le ErbB faʻailoga. O nisi suiga i le EGFR, e aofia ai suiga e le teteʻe i lona vaega o le kinase, e mafai ona faʻatupuina ai le faʻateleina o le tali o le talipupuni, e mafua ai le faʻatagaina o le receptor, o isi taimi e leai ai ni fusifusiga, ma mafai ona lagolagoina le faʻateleina o sela i le NSCLC O le fesuiaʻiga o fesuiaʻiga o loʻo faʻamatalaina o mea na tutupu i exons o loʻo avea ma vaega ole kinase o le EGFR e mafua ai le faʻateleina o le receptor activation ma o le aoga o loʻo valoʻia mai e le 1) o le aoga o le tuma e faʻaitiitia ai le tino faʻatasi ai ma le vailaʻau fautuaina o le afatinib ma / poʻo le 2) taofiofi o le faʻaolaola o sela. poʻo le EGFR tyrosine kinase phosphorylation i faʻaputuga o afatinib gafataulimaina i le fualaʻau fautuaina e tusa ai ma faʻamaonia metotia. O le sili ona masani ona maua o nei fesuiaiga o exon 21 L858R suiga ma exon 19 soloia.

E le gata i lea, na faʻaalia e le afatinib le taofiofia o le autophosphorylation ma / poʻo le in vitro faʻateleina o sela laina faʻaalia vao-ituaiga EGFR ma i latou na faʻaalia filifilia EGFR exon 19 faʻamamaina mutations, exon 21 L858R mutations, poʻo isi le masani ai masani le teteʻeina fesuiaʻiga, i afatinib concentrations 'ausia. i tagata mamaʻi. I se faʻaopopoga, afatinib taofiofia in vitro faʻateleina o sela laina overexpressing HER2.

 

sa Afatinib Faamaonia e le FDA? Mautinoa

Faʻamaoniga maua ai se fou lua-laina togafitiga filifiliga mo tagata mamaʻi ma le lona lua sili ona tele sub-ituaiga o le-laiti sela kanesa o le mama (NSCLC), fai ma sui o le 20-30% o NSCLC mataupu

Faʻamaoniga e faʻavae i luga o iʻuga o le suʻesuʻega LUX-Lung 8, lea na faʻaalia ai le faʻaleleia atili o le ola ma le alualu i luma-leai se ola faʻatusatusa ia Tarceva (erlotinib) i tagata mamaʻi ma squamous sela kanesa o le mama

Afatinib ua uma ona faʻamaonia i le sili atu nai lo 60 atunuʻu mo togafitiga o tagata gasegase ma tuʻu eseʻese ituaiga o EGFR mutation-positive NSCLC

Afatinib

O le a se lamatiaga/ Aʻafiaga aʻafiaga Pe Afatinib Aumai? 

Mea taua e manatua e uiga i le itu aʻafiaga o afatinib:

▪ Tele o tagata e le maua uma aafiaga afatinib afaina lisiina.

▪ Afatinib afaina o aʻafiaga e masani ona vaʻaia i tulaga o latou amataga, umi, ma ogaoga.

▪ Afatinib afaina o aʻafiaga e toeititi lava a suia ma o le a mou pe a maeʻa togafitiga.

▪ Afatinib afaina aʻafiaga ono mafai ona foʻia. E tele filifiliga e faʻaititia pe puipuia ai faʻafitauli o le afatinib.

 

O itu ole itu e masani ai (e tupu tele atu ile 30%) mo tagata mamaʻi e ave afatinib:

▪ Manava

▪ Fuafua paʻu (vaega o paʻu tulaga e pei o fuafua)

▪ Ogaoga o le gutu

▪ Paronychia (faʻamaʻi o fao)

▪ Gutu mago

 

Nei e le masani masani aʻafiaga (tupu i le 10-29%) mo tagata mamaʻi mauaina afatinib:

▪ Faʻaitiitia le fiaai

▪ O le mageso

▪ Leiloa o le pauna

▪ Ua tafetoto le isu

▪ Cystitis (faʻamaʻi pipisi)

▪ Cheilitis (mumu o laugutu)

▪ Fiva

▪ Hypokalemia (maualalo potasiuma)

▪ Conjunctivitis (mata piniki)

▪ Rhinorrhea (isu o le isu)

▪ Maualuga gaʻo o le ate

E le o aʻafiaga uma e lisi atu i luga. Nisi e seasea (tupu i lalo ifo o le 10 pasene o tagata mamaʻi) e le o lisiina iinei. Faʻailoa i taimi uma lau tautua faʻafomaʻi pe a fai e te iloa ni faʻailoga iloga.

 

O a Isi Suʻesuʻega Afatinib?

 Afatinib (BIBW 2992) atinaʻe i le le-laiti-sela kanesa kanesa

Afatinib (BIBW 2992), o le tala o le aniline – quinazoline na tupuga mai, le mafai ona toe faʻafouina ma faʻatulagaina gaioiga i totonu o le gaioiga gaioiga gaioiga a tagata toaaga o le ErbB tagata faʻataʻitaʻi o aiga. O faʻaiuga ua aliali mai o le afatinib e aoga tele i le kanesa o le kanesa, e aofia ai ma fesuiaʻiga o le EGF (EGFR) e fesuisuiaʻi i suiga muamua o le augatupulaga EGFR. Afatinib o loʻo suʻesuʻeina i le polokalame LUX-Lung, lea o le a iloiloina afatinib o se muamua-laina togafitiga i tagata mamaʻi ma EGFR-activating mutations (LUX-Lung 2, 3 ma 6) ma o se lona lua po o le lona tolu-laina togafitiga i tagata mamaʻi ua maua le teteʻe atu i gefitinib ma / poʻo le erlotinib (LUX-Lung 1, 4 ma le 5). LUX-Lung 1 ma le 2 ua faʻaalia, i totonu o a latou vaega faʻatulagaina, se taua tele i le faʻatonutonuina o faʻamaʻi o le 58 ma le 86%, i le faʻasologa, ma le faʻaumiumi taua o le alualu i luma-leai se ola. O isi vaega ole falemaʻi ile falemaʻi o loʻo fai pea ile taimi nei e iloilo le afatinib ma le paclitaxel (LUX-Lung 5), ma faʻatusatusa ile cisplatin / pemetrexed (LUX-Lung 3) poʻo le cisplatin / gemcitabine (LUX-Lung 6).

 

 Afatinib i le alualu i luma ma metastatic chordoma

Ole vaega 2 lea e suʻesuʻe ai le aoga ole a fualaʻau faʻatamaʻi kanesa valaʻau afatinib. Afatinib taofia le EGFR porotini, lea e talitonuina e aofia ai i le aveina o le tuputupu ae o chordoma tumors. O lenei suʻesuʻega ua fuafuaina faʻapitoa lava mo tagata mamaʻi chordoma 18 tausaga pe sili atu ma le faʻaauau poʻo le metastatic tumors. O loʻo tatala nei ile Leiden University Medical Center (LUMC) ma le University College London Hospital (UCLH) ma e tatala i le Istituto dei Nazionale Tumori (INT) i Milan i masina a sau. O le au suʻesuʻe autu mo lenei suʻesuʻega o Dr. Hans Gelderblom i LUMC, Dr. Silvia Stacchiotti i INT, ma Dr. Sandra Strauss i UCLH.

Epidermal Growth Factor Receptor (EGFR) o se polotini maua i luga o nisi sela i le tino atoa. Masani ai, EGFR fesoasoani e faʻatonutonu sela tupu ma faia ai se sao i manuʻa faʻamaloloina. I nisi kanesa, e aofia ai ma le tele o chordomas, EGFR avea soona galue, taʻitaʻia le kanesa sela e fanafanau tele i fafo atu o le taofiofia.

O fualaʻau e poloka ai le EGFR e taʻua o le "EGFR inhibitors" ua faʻamaonia e togafitia ai le tele o ituaiga kanesa. Afatinib o se EGFR taofiofia ua faʻamaonia nei e togafitia kanesa laiti-sela-mama kanesa ma o loʻo faʻataʻitaʻia i isi ituaiga tuma.

E tele EGFR inhibitors ua faʻaalia e telegese pe taofi le tuputupu aʻe o sela chordoma ma tuma o le chordoma i isumu. O mea uma na taofia EGFR na faʻataʻitaʻia, o le afatinib o le sili lea ona aoga i faʻataʻimoa o le chordoma. I nisi o isumu faʻataʻitaʻiga, na faʻatelegeseina le tupu aʻe o le tuma, aʻo isi na mafua ai ona faʻavaivaʻa tagata. O lenei faʻamasinoga faʻamoemoe e faʻamautinoa pe afatinib mafai ona tuʻumuli pe taofi le tuputupu aʻe o le chordoma tumors i tagata mamaʻi ua toe tupu poʻo metastatic faʻamaʻi.

 

Tusitaiala

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

[2] Spreitzer H (13 Me 2008). "Neue Wirkstoffe - Tovok". Österreichische Apothekerzeitung (i le Siamani) (10/2008): 498.

[3] Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, et al. (Aukuso 2008). "BIBW2992, o le le mafai ona suia EGFR / HER2 inhibitor aoga tele i preclinical kanesa kanesa faʻataʻitaʻi". Oncogene 27 (34): 4702–11. faia: 10.1038 / onc.2008.109. PMC 2748240. PMID 18408761.

[4] "Giotrif: EPAR -Product Information" (PDF). Ofisa o Vailaau a Europa. Boehringer Ingelheim Faʻavaomalo GmbH. 16 Oketopa 2013. Toe aumai 28 Ianuari 2014.

[5] Kobayashi Y, Togashi Y, Yatabe Y, Mizuuchi H, Jangchul P, Kondo C, et al. (Tesema 2015). "EGFR Exon 18 Mutations in Lung Cancer: Molecular Predictors of Augmented Sensitivity to Afatinib or Neratinib pe a Faʻatusatusa i le Muamua poʻo le Tolu augatupulaga TKI". Suesuega o le Kanesa Togafitiga. 21 (23): 5305–13. faia: 10.1158 / 1078-0432.CCR-15-1046. PMID 26206867.

[6] Lin NU, Winer EP, Wheatley D, Carey LA, Houston S, Mendelson D, et al. (Iuni 2012). "O le vaega II suʻesuʻega o afatinib (BIBW 2992), o se le mafai ona toe suia ErbB aiga poloka, i tagata mamaʻi ma HER2-lelei metastatic kanesa o le susu faʻasolosolo ina ua maeʻa trastuzumab". Suʻesuʻega ma Togafitiga ole Kanesa o le susu. 133 (3): 1057–65. faia: 10.1007 / s10549-012-2003-y PMC 3387495. PMID 22418700.

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