Tulaga Autu

Igoa oloa	Afatinib paula (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 efuefu ua faʻaletonu;
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).

 

Afatinib Powder Faʻamatalaga

Afatinib paula, faʻatau atu i lalo o le igoa igoa Gilotrif faʻatasi ai ma isi, o se vailaʻau na faʻaaogaina e togafitia ai le laʻititi sela mama kanesa (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 paula (BIBW2992), o le le mafai ona toe faʻafitia le aiga ErbB o tyrosine kinases, na faʻaalia e taofi le EGF-faʻaosofia phosphorylation o EGFR ma sela faʻateleina i le tele o EGFR-overexpressing ma HER2-faʻaali laina laina pei o A431, NIH-3T3 -HER2, NCI-N87 ma 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 le afatinib efuefu taofiofia kanesa sela tuputupu ae ma ola ma taofi le tuma faʻafitauli i xenograft ma transgenic mama kanesa faʻataʻitaʻiga. I se faʻaopopoga, afatinib pauta ua faʻailoa o le EGFR poloka na faʻamaonia mo le togafitia o tagata mamaʻi ma EGFR-mutated sela le mama nonsmall sela.

 

Afatinib Powder Faiga o Gaioiga

E pei o le lapatinib ma le neratinib, o le afatinib pauta o le polotini kinase taofi e faʻafuaseʻi foi ona taofia le faʻatupuina o le toto o tagata i luga o le tino (2) ma le faʻaolaola o mea tutupu (EGFR).

Afatinib efuefu e le gata faʻagaoioia faasaga i EGFR fesuiaʻiga fuafuaina e le augatupulaga muamua tyrosine-kinase iniseti (TKI) pei erlotinib po gefitinib, ae faʻapea foi faasaga i laʻititi masani suiga e teteʻe atu 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 Powder Application

Afatinib efuefu o se gaioiga bioavailable anilino-quinazoline mafuaʻaga ma taofia o le receptor tyrosine kinase (RTK) epidermal tuputupu ae mea taliaina (ErbB; EGFR) aiga, ma antineoplastic gaioiga.

Afatinib efuefu o se tuʻufaʻatasia bioavailable lua receptor tyrosine kinase (RTK) taofia ma ono 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 faʻamaʻi vascularization ma ua soona faʻaalia i le tele o ituaiga kanesa sela.

Afatinib efuefu ua faʻamaonia i le tele o le lalolagi (aofia ai le Iunaite Setete, Kanata, le Malo Tele ma Ausetalia) mo le togafitiga o metastatic lē-laiti sela sela kanesa (NSCLC), atiina ae e Boehringer Ingelheim. E avea o se angiokinase taofia.

 

Afatinib Powder Itu Aafiaga & Lapataiga

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

▪ 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 paula:

▪ 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 le afatinib paula:

▪ Tele o tagata o le a le mauaina uma aafiaga afatinib paula itu afaina lisiina.

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

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

▪ Afatinib efuefu itu aʻafiaga ono mafai ona foʻia. E tele filifiliga e faʻaititia pe puipuia ai aʻafiaga o le afatinib paula.

 

Tusitaiala

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[2] DʻArcangelo M, Hirsch FR. Fomaʻi ma faʻatusatusa aoga o afatinib paʻu i 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 paʻu 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 paula, erlotinib ma gefitinib i le laina muamua togafitiga 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 le afatinib paula 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 paula: muamua faʻamaonia ile lalolagi. 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.

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