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Erlotinib

fua faatatau: Category:

Erlotinib, faʻatau atu i lalo o le igoa igoa Tarceva faʻatasi ai ma isi, o se vailaʻau na faʻaaogaina e togafitia ai le laʻititi sela mama kanesa (NSCLC) ma pancreatic kanesa. Faʻapitoa lava faʻaaogaina mo NSCLC ma fesuiaʻiga i le epidermal tuputupu ae mea taliaina (EGFR) - a le o le exon 19 soloia (del19) poʻo le exon 21 (L858R) sui suiga - lea na salalau atu i isi vaega o le tino.

Faamatalaga oloa

Tulaga Autu

Igoa oloa Erlotinib
Numera CAS 183321-74-6
Faiga Faʻavae Molecular C22H23N3O4
Fua Faatatau o le Umi 393.443
Synonyms CP-358774;

OSI774;

Erlotinib fua faʻavae;

183321-74-6.

Faʻaaliga Paʻepaʻe i le paʻu paʻepaʻe paʻepaʻe paʻepaʻe
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).

 

Erlotinib Faʻamatalaga

Erlotinib, faʻatau atu i lalo o le igoa igoa Tarceva faʻatasi ai ma isi, o se vailaʻau na faʻaaogaina e togafitia ai le laʻititi sela mama kanesa (NSCLC) ma pancreatic kanesa. Faʻapitoa lava faʻaaogaina mo NSCLC ma fesuiaʻiga i le epidermal tuputupu ae mea taliaina (EGFR) - a le o le exon 19 soloia (del19) poʻo le exon 21 (L858R) sui suiga - lea na salalau atu i isi vaega o le tino. E ave e le gutu.

Erlotinib o se quinazoline mafuaʻaga ma antineoplastic meatotino. O le tauvaga ma le adenosine triphosphate, o le erlotinib e fesuiaʻi i le vaega o le intracellular catalytic o le epidermal tuputupu aʻe o le receptor (EGFR) tyrosine kinase, o le mea lea e mafai ai ona toe taofiofia le EGFR phosphorylation ma poloka ai faʻailoga o gaioiga o gaioiga ma tumigenic aafiaga e fesoʻotaʻi ma le faʻaolaina EGFR.

Erlotinib na faʻamaonia mo le faʻaogaina o vailaʻau i le Iunaite Setete i le 2004. O loʻo i luga o le Lisi o le Soifua Maloloina Lisi a Lisi o Taua Taua vailaʻau, o loʻo lisi ai le saogalemu ma sili ona aoga vailaʻau e manaʻomia i se soifua maloloina faiga.

 

Erlotinib Faʻatinoina o gaioiga

Erlotinib o se epidermal tuputupu ae mea faʻaola auala (EGFR taofiofia). O le vailaʻau e mulimuli Iressa (gefitinib), o le muamua vailaʻau o lenei ituaiga.

Erlotinib faʻapitoa faʻatutuina le epidermal tuputupu ae mea taliaina (EGFR) tyrosine kinase, lea e sili ona faʻaalia ma faʻasolosolo taimi i ituaiga eseese o kanesa. E fusifusia i se suiga suiga i le adenosine triphosphate (ATP) noataga nofoaga o le receptor. Mo le faʻailoga e tuʻuina atu, lua molimoli EGFR manaʻomia e o mai faʻatasi e fausia ai se homodimer.

O mea ia e faʻaaogaina ai le molemole o le ATP e faʻaliliu ai le tasi i luga o le isi tyrosine, lea e maua mai ai ni vaega o totoe o le phosphotyrosine i le EGFR e faʻapipiʻi ai polotini polotini e faʻasolo le faʻailoga o le cascades i le kulupu poʻo le faʻagaoioia o isi sela. A fusifusia e le erlotinib le EGFR, e le mafai le faʻavaeina o toega o le phosphotyrosine i le EGFR ma e leʻi amataina le faʻailoga o le tino.

O Erlotinib o se tyrosine kinase receptor inhibitor e faʻaaogaina i le togafitiga o le alualu i luma poʻo le metastatic pancreatic poʻo le laʻititi o le kanesa o le kanesa kanesa. Erlotinib togafitiga e fesoʻotaʻi ma siʻitia tulaga maualuga i le serum aminotransferase tulaga i le taimi o togafitiga ma seasea taimi o falemaʻi e manino tiga matuia ate.

 

Talosaga Erlotinib 

Erlotinib o se mafai ona suia muamua-augatupulaga receptor tyrosine kinase iniseti (faʻatasi ai ma Gefitinib) galue muamua i luga o le epidermal tuputupu aʻe resepi (EGFR), o se sui o le ErbB receptor aiga. E faʻafesoʻotaʻi e le vailaʻau le ituaiga vao ma le suiga o le EGFR. E mafai e le aiga o ErbB ona fausia ni homodimers poʻo heterodimers, e masani ona aʻafia i aafiaga o le tafe o le vai ma faʻafitauli o le tele o ituaiga kanesa na suʻesuʻeina i tagata. Receptor tyrosine kinase inisetiute (TKI) puipuia le phosphorylation o latou substrate i le sela faailo auala. EGFR masani ona faia se sao i le tele o sela feʻaveaʻi, aofia ai le vavaeʻesega, faʻateleina, ma angiogenesis, o na mea uma o faʻailoga o le kanesa.

EGFR suiga i le NSCLC e masani lava o se faʻagaoioia suiga. Nisi uiga onosaʻi na mafua ai le iai o suiga EGFR sili ono aofia ai leai talaʻaga o le ulaula faʻamaonia adenocarcinoma e histologic auiliiliga, Asia ituaiga, ma fafine itupa. Maualuga suiga i le EGFR masani ona tupu, o lenei tusitusiga o loʻo faʻamatalaina i lalo.

 

Erlotinib Itu Aafiaga & Lapataiga

O itu nei e masani ona aoga mo tagata mamaʻi e ave Erlotinib:

▪ Faanatinati

▪ Manava

▪ Le lelei le manao

▪ Le lavava

▪ Manava le manava

▪ Maua

▪ Faanoi ma puaʻi

 

O nei itu aʻafiaga e le masani ai aʻafiaga o tagata mamaʻi mauaina Erlotinib:

▪ Siama

▪ Ogaoga o le gutu

▪ O le mageso

▪ Paʻu mago

▪ Faasoesa i mata

▪ Paʻu o le manava

 

E le o aʻafiaga uma e lisi atu i luga. Nisi e seasea (tupu i lalo ifo o le 10% o tagata mamaʻi) e le o lisiina iinei. Peitaʻi, e tatau ona e faʻailoa i taimi uma lau auaunaga faʻasoifua maloloina pe a fai e te maua se faʻailoga e le masani ai.

 

Tusitaiala

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[2] Lee CK, Davies L, Wu YL, Mitsudomi T, Inoue A, Rosell R, Zhou C, Nakagawa K, Thongprasert S, Fukuoka M, Lord S, Marschner I, Tu YK, Gralla RJ, Gebski V, Mok T , Yang JC. Gefitinib poʻo Erlotinib vs Chemotherapy mo le EGFR Mutation-Positive Lung Cancer: Tagata Taʻitoʻatasi Patient Data Meta-Suʻesuʻega o le Aotelega o le Faʻaola. J Natl Kanesa Inst. 2017 Jun 1; 109 (6). faia: 10.1093 / jnci / djw279. Iloiloga PubMed PMID: 28376144.

[3] Yang Z, Hackshaw A, Feng Q, Fu X, Zhang Y, Mao C, Tang J. Faʻatusatusaga o gefitinib, erlotinib ma afatinib i le le laʻititi sela kanesa mama: O se meta-auiliiliga. Int J Kanesa. 2017 Jun 15; 140 (12): 2805-2819. faia: 10.1002 / ijc.30691. Epub 2017 Mati 27. Toe iloiloga. PubMed PMID: 28295308.

[4] "Erlotinib (Tarceva) Faʻaaoga I le taimi o le Maitaga". Drugs.com. 1 Novema 2019. Toe aumai 23 Tesema 2019.

[5] "Erlotinib Monograp mo Tomai Faʻapitoa". Drugs.com. Toe aumai 12 Novema 2019.

[6] "Tarceva- erlotinib hydrochloride laupapa". Aso Taʻitasi 12 Tesema 2018. Toe aumai 23 Tesema 2019.

[7] "Afifi Faʻamaonia Vailaʻau: Tarceva (Erlotinib) NDA # 021743". US Taumafa ma Vailaau Faʻafoeina (FDA). 28 Mati 2005. Toe aumai 23 Tesema 2019.

[8] Raymond E, Faivre S, Armand JP (2000). "Epidermal tuputupu ae vaega taliaina receptor tyrosine kinase o se sini mo anticancer togafitiga". Fualaʻau. 60 Faʻaopopo 1: 15–23, talanoaga 41–2. faia: 10.2165 / 00003495-200060001-00002. PMID 11129168. S2CID 10555942.