Neratinib (698387-09-6) efuefu - Gaosi oloa Tuuina atu
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Neratinib

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Neratinib o se malosi, le mafai ona toe faʻafouina tyrosine kinase inhibitor (TKI) o HER1, HER2, ma HER4, ma o loʻo galueina nei. Neratinib e le mafai ona toe fusia i le faʻailoga o laina o le HER1, HER2, HER3, ma le epithelial tuputupu ae vaega, ma taofia ai le phosphorylation ma le tele o HER auala faʻailo i lalo. O le iʻuga ua faʻaititia le faʻaolaola ma ua atili tele ai le oti o sela. O suʻesuʻega faʻafomaʻi na faʻaalia ai o le taofiofia o le HER i luga ole faʻailo e ala i le neratinib o se auala sili atu ona aoga e taofi ai le tuputupu aʻe o le HER-faʻafesoʻotaʻi ma le faʻafetaiaia o le sosola ese o le tuma i auala ua masani ai ma togafitiga o loʻo faʻatautaia nei e le HER2 ma sui o le chemotherapeutic.

Faamatalaga oloa

Tulaga Autu

Igoa oloa Efuefu Neratinib
Numera CAS 698387-09-6
Faiga Faʻavae Molecular C30H29ClN6O3
Fua Faatatau o le Umi 557.04
Synonyms HKI-272;

PB272;

Efuefu Neratinib;

Nerlynx;

698387-09-6.

Faʻaaliga Paʻepaʻe-paʻepaʻe i le samasama samasama pauta
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).

 

Neratinib efuefu Faʻamatalaga

Neratinib paula, e taʻua foi o le HKI-272 poʻo le PB272, o se avanoa tuʻu fofoga, e le mafai ona toe faʻafitia le HER-2 receptor tyrosine kinase ma le ono antineoplastic gaioiga.

Neratinib efuefu e fusifusia i le HER-2 talimalo e le mafai ona toe suia, ma faʻaititia ai le autophosporylasi i sela, e foliga mai o le faʻatutuina o se totoe o le cysteine ​​i le ATP-fusifusia taga o le receptor.

Togafitiga o sela ma lenei sooupu e mafua ai le taofiofia o gaioiga o gaioiga faʻasolosolo o gaioiga faʻasolosolo ma sela taʻamilosaga faʻatonutonu auala; pueina i le G1-S (Gap 1 / DNA synthesis) -faʻasologa suiga o le sela vaevaega taʻamilosaga; ma iʻu ai ina faʻaititia le faʻaolaolaina o sela.

Neratinib lūlū foi taofia le epidermal tuputupu ae mea taliaina (EGFR) kinase ma le faʻateleina o EGFR-faʻalagolago sela.

 

Neratinib Powder Auala o Gaioiga

Neratinib efuefu o se malosi, le mafai ona toe faʻafouina tyrosine kinase (TKI) o HER1, HER2, ma HER4, ma o loʻo galueina nei. Neratinib efuefu e le mafai ona toe fusia i le faʻavaʻa o le faʻailo igoa o HER1, HER2, HER3, ma le epithelial tuputupu aʻe o loʻo taliaina, ma taofia ai le phosphorylation ma le tele o lalo auala o faʻailo. O le iʻuga ua faʻaititia le faʻateleina ma faʻateleina le oti sela. O suʻesuʻega faʻapitoa sa faʻailoa mai ai, o le taofiofia o le HER ile faʻailoaina e le neratinib pauta, ose auala sili lea ona aoga e faʻatamaia ai le tuputupu aʻe ole HER ma faʻafetaiaia ai le sosola ese ole tumo ile auala na faʻaaoga ai nei togafitiga faʻasolosolo ma HER2.

Neratinib efuefu ua faʻamaonia foi ona aoga i le laina muamua togafitiga o HER2-lelei, metastatic susu kanesa (MBC). A faʻaaoga faʻatasi ma paclitaxel, o le neratinib paula na faʻaalia se ORR e 73%. A tuʻufaʻatasia ma capecitabine, o leisi chemotherapeutic agents, o le ORR e 63%. I se faʻaopopoga i le HER2-positive MBC, o le neratinib paula sa aoga tele foi i tagata mamaʻi na maua i le kanesa o le susu o le HER2-mutated. I le vaega 2 SUMMIT faʻataʻitaʻiga, o tagata mamaʻi na maua i le kanesa o le susu ua HER2-mutated na maua le 33% ORR i le 8 vaiaso.

Neratinib pauta o le muamua TKI faʻamaonia e faʻaititia le lamatiaga mo faʻamaʻi toe tupu i tagata mamaʻi i le amataga-HER2-lelei kanesa o le susu. Faʻavae i luga o le aoga o le neratinib paʻu i le amataga laʻasaga HER2-lelei kanesa o le susu, MBC, ma HER2-mutant tumors, neratinib paula ua faʻamoemoeina e avea ma fou tulaga o le tausiga i le tele o susu susu togafitiga togafitiga.

 

Neratinib efuefu Talosaga

Neratinib efuefu e fusifusia i le HER-2 talimalo e le mafai ona toe suia, ma faʻaititia ai le autophosporylasi i sela, e foliga mai o le faʻatutuina o se totoe o le cysteine ​​i le ATP-fusifusia taga o le receptor.

HER2-lelei susu kanesa faia tele o le HER2 polotini. O le HER2 protein e nofo i luga o sela o le kanesa ma maua faʻailoga e taʻu ai le kanesa e tupu ma salalau. Neratinib efuefu fusuʻaga HER2-lelei susu kanesa e ala i le poloka o kanesa sela 'mafai ona maua tuputupu aʻe faʻailoga.

Neratinib paula o se faʻatulagaina togafitiga, ae le pei o Herceptin (vailaʻau igoa: trastuzumab), Kadcyla (vailaʻau igoa: T-DM1 poʻo le ado-trastuzumab emtansine), ma le Perjeta (igoa vailaʻau: pertuzumab), e le o se puipuia faʻamoemoeina togafitiga. Ole togafiti faʻapitoa e faʻataʻitaʻia togafitiga o faʻaupuga ia o vailaʻau e masani ona tutupu e pei o meaola niniʻi na faia e le tatou tino puipuia. Neratinib paula o se vailaʻau vailaʻau, ae le o se vailaʻau.

 

Neratinib Powder Itu Itu & Lapataiga

Neratinib paula mafai mafua ai le manaʻomia le manava tata i nisi tagata ma agamalu i feololo manava tatā i le toetoe lava o tagata uma; tagata e aveina o loʻo iai foi i se tulaga lamatia mo faʻafitauli o le manava manava e pei o le dehydration ma electrolyte le paleni.

E faʻapena foi ona iai se aʻafiaga o le leaga o le ate ma le tele o tagata mamaʻi e i ai ni tulaga o ia; faʻailoga o le ate afaina e aofia ai le lelava, niniva, puaʻi, taumatau luga quadrant tiga poʻo le agavaivai, fiva, mageso, ma maualuga tulaga o eosinophils.

I se faʻaopopoga i mea o loʻo taua i luga, e ova atu ma le 10% o tagata o loʻo tago e tiga, tiga o le manava, puaʻi, papala i luga o latou laugutu, tiga le manava, faʻaititia le manaʻo, mageso, ma maso maso.

 

Tusitaiala

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[2] LiverTox: Fomaʻi ma Faʻamatalaga Suesuega e uiga i Vailaʻau-Faʻaosoina Manua o le ate [Initaneti]. Bethesda (MD): National Institute of Diabetes ma Digestive ma Fatugaʻo faʻamaʻi; 2012-. Avanoa mai http://www.ncbi.nlm.nih.gov/books/NBK548937/ PubMed PMID: 31644242.

[3] Booth LA, Roberts JL, Dent P. O le matafaioi a sela faailo i le crosstalk i le va autophagy ma apoptosis i le tulafono faatonutonu o le olaola sela sela i le tali atu i sorafenib ma neratinib. Semin Kanesa Biol. 2019 Oketopa 20. pii: S1044-579X (19) 30024-0. fai: 10.1016 / j.semcancer.2019.10.013. [Epub luma atu o le lolomi] Toe iloiloga. PubMed PMID: 31644944.

[4] Miles J, White Y. Neratinib mo le Togafitiga o le Early-Stage HER2-Positive Breast Cancer. J Adv Faʻapitoa Oncol. 2018 Nov-Tes; 9 (7): 750-754. Epub 2018 Nov 1. Iloilo. PubMed PMID: 31249722; PubMed Central PMCID: PMC6570523.

[5] Collins DM, Conlon NT, Kannan S, Verma CS, Eli LD, Lalani AS, Crown J. Preclinical Characteristics o le Irreversible Pan-HER Kinase Inhibitor Neratinib Faʻatusatusa ma Lapatinib: Aafiaga mo le Togafitiga o HER2-Positive ma HER2- Kanesa o le susu ua suia. Le faʻamaʻa (Basel). 2019 Me 28; 11 (6). pii: E737. faia: 10.3390 / kanesa11060737. Iloiloga PubMed PMID: 31141894; PubMed Central PMCID: PMC6628314.

[6] Deeks ED. Neratinib: Muamua Faʻamaonia i le Lalolagi. Fualaʻau. 2017 Oketopa; 77 (15): 1695-1704. faia: 10.1007 / s40265-017-0811-4. Iloiloga PubMed PMID: 28884417.

[7] Kourie HR, El Rassy E, Clatot F, de Azambuja E, Lambertini M. Faʻalauiloa togafitiga mo HER2-lelei amataga laʻasaga kanesa o le susu: taulaʻi i neratinib. Onco Manulauti Ther. 2017 Jul 10; 10: 3363-3372. faia: 10.2147 / OTT.S122397. eCollection 2017. Iloilo. PubMed PMID: 28744140; PubMed Central PMCID: PMC5513878.

[8] "Faʻauigaina o neratinib - National Cancer Institute Drug Guide". Toe aumai 1 Tesema 2008.

[9] "Neratinib tablets igoa" (PDF). US Food and Drug Administration (FDA). Iulai 2017. Toe aumai ile 6 Fepuari 2018. Mo faʻailoga faʻafouina vaʻai, itulau faasino igoa a le FDA mo NDA 208051 O lenei tusitusiga o loʻo tuʻufaʻatasia ai tusitusiga mai lenei punaoa, o loʻo i totonu o le lautele lautele. Gandhi L, et al. (2017). "MA04.02 Neratinib ± Temsirolimus i HER2-mutant mama kanesa: o se faavaomalo, randomized vaega II suesuega". Tusi o tala o le Thoracic Oncology. 12 (1): S358-9. fai: 10.1016 / j.jtho.2016.11.398.