Faamatalaga oloa
Tulaga Autu
Igoa oloa | Afatinib (BIBW2992) |
Numera CAS | 850140-73-7 |
Faiga Faʻavae Molecular | C32H33ClFN5O11 |
Fua Faatatau o le Umi | 718.09 |
Synonyms | 850140-73-7;
BIBW-2992; BIBW 2992; BIBW2992. Afatinib dimaleate; |
Faʻaaliga | Malamalama lanu efuefu |
Teuina ma Taulimaina | Faʻamago, pogisa ma i le 0 - 4 C mo se taimi puʻupuʻu (aso i vaiaso) poʻo le -20 C mo se taimi umi (masina i tausaga). |
Faamatalaga Afatinib
Afatinib, faʻatau atu i lalo ole igoa igoa Gilotrif faʻatasi ai ma isi, o se vailaʻau na faʻaaogaina e togafitia ai non-cell cell lung carcinoma (NSCLC). E ona le tyrosine kinase inhibitor aiga o vailaʻau. E ave e le gutu. E masani ona faʻaaoga e togafitia ai mataupu o le NSCLC o loʻo taofia fesuiaʻiga i le epidermal tuputupu aʻe mea maua (EGFR) gene.
Afatinib (BIBW2992), o le le mafai ona toe faʻafitia le aiga ErbB o tyrosine kinases, na faʻaalia e taofi le EGF-faʻasolosolo phosphorylation o EGFR ma sela faʻateleina i le tele o EGFR-overexpressing ma HER2-faʻaalia laina laina e pei o A431, NIH-3T3- HER2, NCI-N87 ma le BT-474.
O le vaega na faʻatele foi ona faʻaaogaina i manu eseʻese e suʻesuʻe ai le sao o le EGFR / HER2. Tautala tuʻuina o afatinib taofiofia kanesa sela tuputupu ae ma ola ma taofi le tuma faʻafitauli i xenograft ma transgenic mama kanesa faʻataʻitaʻiga. I se faʻaopopoga, afatinib ua faʻailoa o le EGFR blocker lea na faʻamaonia mo le togafitia o tagata mamaʻi ma EGFR-mutated nonsmall sela mama kanesa.
Afatinib Faiga o Gaioiga
E pei o le lapatinib ma le neratinib, o le afatinib o le poloka kinase e taofia ai ma e le mafai ai ona toe taofia le faʻatupuina o le tupuola o le tino i luga o le tino (2) ma le faʻaolaola o mea tutupu (EGFR).
Afatinib e le gata o faʻagaoioia ma le EGFR suiga na faʻatulagaina e le augatupulaga muamua tyrosine-kinase inhibitors (TKI) pei o le erlotinib poʻo le gefitinib, ae faʻapea foʻi ma le laʻititi o suiga masani e teteʻe i nei vailaʻau.
Ae ui i lea, e le o faʻagaioia faʻasaga i le T790M suiga e masani ona manaʻomia ai le isi augatupulaga lona tolu vailaʻau pei o le osimertinib. Ona o lona faʻaopopo gaioiga faʻasaga ia Her2, o lea ua suʻesuʻeina mo kanesa o le susu faʻapea foi ma isi EGFR ma Her2 faʻamalosi kanesa.
Afatinib Talosaga
Afatinib o se gaioiga bioavailable anilino-quinazoline derivative ma inhibitor o le receptor tyrosine kinase (RTK) epidermal tuputupu ae receptor (ErbB; EGFR) aiga, ma antineoplastic gaioiga.
Afatinib foi o se tautala tuʻufaʻatasia bioavailable lua receptor tyrosine kinase (RTK) taofia ma ono antineoplastic gaioiga. EGFR / HER2 tyrosine kinase inhibitor BIBW 2992 e le mafai ona toe fusifusia ma taofia le faʻatupulaia e tagata o le epidermal tuputupu aʻe vaega 1 ma le 2 (EGFR-1; HER2), lea e ono mafua ai le taofiofia o le tuputupu ae tuputupu ae ma angiogenesis. EGFR / HER2 o RTKs e ona le aiga EGFR; o loʻo i ai uma matafaioi taua i le faʻatupulaia o sela sela ma fula vascularization ma ua ova ona faʻamatalaina i le tele o ituaiga kanesa sela.
Afatinib ua faʻamaonia i le tele o le lalolagi (aofia ai le Iunaite Setete, Kanata, Peretania ma Ausetalia) mo le togafitiga o metastatic le-laiti sela sela kanesa (NSCLC), atiina ae e Boehringer Ingelheim. E avea o se angiokinase taofia.
Afatinib Itu Aafiaga & Lapataiga
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.
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.