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Afatinib (BIBW2992)

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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 taofiofia aiga o vailaʻau. E ave e le gutu.

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.

 

Tusitaiala

[1] Prim N, Fore M, Mennecier B. [Afatinib (BIBW 2992).]. Rev Pneumol Clin. 2014 Me 27. pii: S0761-8417 (14) 00047-9. faia: 10.1016 / j.pneumo.2014.03.002. [Epub luma atu o le lolomi] Toe iloiloga. Falani. PubMed PMID: 24878189.

[2] DʻArcangelo M, Hirsch FR. Togafitiga ma faʻatusatusaga aoga o afatinib i le le-laʻititi sela kanesa kanesa. Biologics. 2014 Ape 23; 8: 183-92. faia: 10.2147 / BTT.S40567. eCollection 2014. Iloilo. PubMed PMID: 24790411; PubMed Central PMCID: PMC4003149.

[3] Bowles DW, Weickhardt A, Jimeno A. Afatinib mo le togafitia o tagata mamaʻi e maua i le EGFR-positive non-cell cell cancer kanesa. Fualaʻau o Aso Nei (Barc). 2013 Sep; 49 (9): 523-35. fai: 10.1358 / togi.2013.49.9.2016610. Iloiloga PubMed PMID: 24086949.

[4] Köhler J, Schuler M. Afatinib, erlotinib ma gefitinib i le laina muamua laina o le EGFR mutation-positive lung adenocarcinoma: o se toe iloiloga. Onkologie. 2013; 36 (9): 510-8. faia: 10.1159 / 000354627. Epub 2013 Aukuso 19. Toe iloiloga. PubMed PMID: 24051929.

[5] Yap TA, Popat S. O le matafaioi a afatinib i le puleaina o le le-laiti sela sela kanesa o le tino. Tomai Faʻapitoa Opin Drug Metab Toxicol. 2013 Nov; 9 (11): 1529-39. faia: 10.1517 / 17425255.2013.832755. Epub 2013 Aukuso 28. Toe iloiloga. PubMed PMID: 23985030.

[6] Dungo RT, Keating GM. Afatinib: muamua faʻamaonia i le lalolagi atoa. Fualaʻau. 2013 Sep; 73 (13): 1503-15. faia: 10.1007 / s40265-013-0111-6. Iloiloga PubMed PMID: 23982599.

[7] Minkovsky N, Berezov A (Tesema 2008). "BIBW-2992, o le lua receptor tyrosine kinase taofiofia mo le togafitia o mautu tuma". Manatu o loʻo iai nei ile Sailiga o Fualaʻau. 9 (12): 1336–46. PMID 19037840

[8] 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 muamua preclinical kanesa kanesa faʻataʻitaʻi". Oncogene 27 (34): 4702–11. faia: 10.1038 / onc.2008.109. PMC 2748240. PMID 18408761.