Neratinib (698387-09-6) poda - Mugadziri Fekitori Mutengesi
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Neratinib

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Neratinib ine simba, isingachinjiki tyrosine kinase inhibitor (TKI) yeHER1, HER2, uye HER4, uye parizvino iri kuvandudzwa. Neratinib isingadzoreke inosunga kune intercellular yekuisa chiratidzo dura reHER1, HER2, HER3, uye epithelial yekukura factor receptor, uye inhibits phosphorylation uye akati wandei HER ezasi ekuratidzira nzira. Mhedzisiro yacho yakadzikira kuwanda uye kuwedzera sero kufa. Zvidzidzo zvekiriniki zvakaratidza kuti intracellular inhibition ye HER chiratidzo ne neratinib ndiyo nzira inoshanda yekudzvinyirira HER-inopindirana bundu kukura uye kukunda bundu kupukunyuka nzira dzakasangana neazvino HER2-yakanangwa ekurapa uye chemotherapeutic vamiririri.

Product Description

Basic Hunhu

Product Name Neratinib upfu
CAS Number 698387-09-6
Molecular Formula C30H29ClN6O3
Formula Weight 557.04
Synonyms HKI-272;

PB272;

Neratinib upfu;

Nerlynx;

698387-09-6.

Kuonekwa Kunze-chena kujekesa poda yero
Kuchengeta uye Kubata Kuoma, kusviba uye pa0 - 4 C kwenguva pfupi (mazuva kusvika kumavhiki) kana -20 C kwenguva refu (mwedzi kusvika makore).

 

Neratinib powder Tsanangudzo

Neratinib powder, inozivikanwawo seHKI-272 kana PB272, inowanikwa mumuromo, isingadzoreke inhibitor yeHER-2 receptor tyrosine kinase ine basa rinogona kuita antineoplastic.

Neratinib poda inosunga kune iyo HER-2 receptor isingadzoreke, nokudaro ichideredza autophosphorylation mumasero, sezviri pachena nekunangisa cysteine ​​masara muhombodo yeATP-inosunga yeanogamuchira.

Kurapa kwemasero ane mumiririri kunoguma nekudzvinyirira kwenzvimbo dzekunze chiratidzo kutapurirana zviitiko uye maseru kutenderera nzira dzekutenderera; Kusungwa paG1-S (Gap 1 / DNA synthesis) -phase shanduko yesero rekuparadzanisa maseru; uye pakupedzisira yakaderera kuwanda kwemaseru.

Neratinib powder zvakare inhibits iyo epidermal yekukura factor receptor (EGFR) kinase uye kuwanda kwemasero anoenderana neEGFR.

 

Neratinib Powder Maitiro Ekuita

Neratinib powder ine simba, isingachinjiki tyrosine kinase inhibitor (TKI) yeHER1, HER2, uye HER4, uye parizvino iri kuvandudzwa. Neratinib powder isingadzoreke inosunga kune intercellular yekuisa chiratidzo dura reHER1, HER2, HER3, uye epithelial yekukura factor receptor, uye inhibits phosphorylation uye akati wandei HER ezasi ekuratidzira nzira. Mhedzisiro yacho yakadzikira kuwanda uye kuwedzera sero kufa. Zvidzidzo zvekiriniki zvakaratidza kuti intracellular inhibition ye HER chiratidzo ne neratinib poda ndiyo nzira inoshanda yekudzvinyirira HER-yakagadziriswa tumarara kukura uye kukunda bundu kupukunyuka nzira dzakasangana neazvino HER2-yakanangwa ekurapa uye chemotherapeutic vamiririri.

Neratinib powder yakaratidzawo kuti inoshanda mumutsara wekutanga kurapwa kweHER2-yakanaka, metastatic cancer cancer (MBC). Kana yakashandiswa pamwechete paclitaxel, neratinib poda yakaratidza ORR ye73%. Kana yakabatanidzwa ne capecitabine, imwe chemotherapeutic mumiririri, iyo ORR yaive 63%. Pamusoro peHER2-yakanaka MBC, neratinib poda yaive zvakare inoshanda kune varwere vane HER2-mutated kenza yemazamu. Muchikamu chechipiri SUMMIT kuyedza, varwere vane HER2-mutated kenza yemazamu vakawana 2% ORR pamasvondo masere.

Neratinib powder ndiyo yekutanga TKI yakaratidza kudzikisa njodzi yekudzokazve kwechirwere muvarwere vane yekutanga-nhanho HER2-yakanaka kenza yemazamu. Kubva pane kushanda kweeratinib poda mukutanga-nhanho HER2-yakanaka kenza yemazamu, MBC, uye HER2-mutant tumors, neratinib poda inotarisirwa kuzove iyo nyowani muyero wekutarisira pane akawanda kenza yemazamu ekurapa marongero.

 

Neratinib powder Kunyorera

Neratinib poda inosunga kune iyo HER-2 receptor isingadzoreke, nokudaro ichideredza autophosphorylation mumasero, sezviri pachena nekunangisa cysteine ​​masara muhombodo yeATP-inosunga yeanogamuchira.

HER2-yakanaka kenza yemazamu inoita yakawandisa yeiyo HER2 protein. Iyo HER2 protein inogara pamusoro pecancer maseru uye inogamuchira zviratidzo zvinotaurira kenza kuti ikure nekupararira. Neratinib powder inorwisa kenza yemazamu yeHER2-nekudzivirira maseru ekenza kugona kugamuchira zviratidzo zvekukura.

Neratinib powder inorapa yakanangwa, asi kusiyana neHerceptin (zita remakemikari: trastuzumab), Kadcyla (zita remakemikari: T-DM1 kana ado-trastuzumab emtansine), uye Perjeta (zita remakemikari: pertuzumab), haisi kurapwa kwakanangana ne immune. Zvirwere zvekuzvidzivirira mumuviri maumbirwo eanowanzoitika masoja ekudzivirira chirwere anoshanda semasoja ekudzivirira muviri akagadzirwa nema immune system edu. Neratinib powder chinhu chemakemikari, kwete antibody.

 

Neratinib Powder Side Mhedzisiro & Yambiro

Neratinib powder inogona kukonzera manyoka anotyisidzira hupenyu mune vamwe vanhu uye manyoro ari pakati nepakati kusvika pakati pevanhu vese; vanhu vanozvitora vari panjodzi yematambudziko emanyoka sekushomeka kwemvura uye kusaenzana kwemagetsi.

Saizvozvowo kune njodzi yekukuvara kwakakomba kwechiropa uye varwere vazhinji vane imwe nhanho yacho; zviratidzo zvekukuvara kwechiropa zvinosanganisira kuneta, kuda kurutsa, kurutsa, kurudyi kwepamusoro quadrant kurwadziwa kana unyoro, fivha, mapundu, uye akakwirira mazinga emaosinophil.

Pamusoro peizvo zvataurwa pamusoro, vanodarika gumi muzana vevanhu vanoitora vane kusvotwa, kurwadziwa mudumbu, kurutsa, maronda pamiromo yavo, mudumbu kugumbuka, kuderera kwechido, mapundu, uye mhasuru.

 

Reference

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[2] LiverTox: Ruzivo rweKiriniki uye Rwekutsvagisa nezveMishonga-Inokonzeresa Chiropa Kukuvadza [Internet]. Bethesda (MD): National Institute of Diabetes uye Digestive uye Kidney Zvirwere; 2012-. Inowanikwa kubva ku http://www.ncbi.nlm.nih.gov/books/NBK548937/ PubMed PMID: 31644242.

[3] Booth LA, Roberts JL, Dent P. Basa rechitokisi rinoratidzira mucrosstalk pakati pe autophagy uye apoptosis mukutonga kwechipfuva sero kupona mukupindura sorafenib uye neratinib. Semin Kenza Kanzuru. 2019 Gumiguru 20. pii: S1044-579X (19) 30024-0. doi: 10.1016 / j.semcancer.2019.10.013. [Epub pamberi pokudhinda] Ongororo. PubMed PMID: 31644944.

[4] Miles J, White Y. Neratinib yekurapa Kwekutanga-Chikamu Chikamu HER2-Yakanaka Kenza Yezamu. J Adv Dzidzira Oncol. 2018 Mbudzi-Zvita; 9 (7): 750-754. Epub 2018 Mbudzi 1. Ongororo. PubMed PMID: 31249722; PubMed Central PMCID: PMC6570523.

[5] Collins DM, Conlon NT, Kannan S, Verma CS, Eli LD, Lalani AS, Crown J. Preclinical Hunhu hweiyo Isingachinjiki Pan-HER Kinase Inhibitor Neratinib Kuenzaniswa neLapatinib: Zvinoreva Kurapwa kweHER2-Positive uye HER2- Kachinja Kenza Yezamu. Gomarara (Basel). 2019 Chivabvu 28; 11 (6). pii: E737. doi: 10.3390 / kanzira11060737. Ongorora. PubMed PMID: 31141894; PubMed Central PMCID: PMC6628314.

[6] Dhiekisi ED. Neratinib: Kutanga Kubvumidzwa Kwenyika. Zvinodhaka. 2017 Oct; 77 (15): 1695-1704. doi: 10.1007 / s40265-017-0811-4. Ongorora. PubMed PMID: 28884417.

[7] Kourie HR, El Rassy E, Clatot F, de Azambuja E, Lambertini M. Kurapa kuri kubuda kweHER2-inovheneka gomarara repazamu rekutanga: tarisa pane neratinib. Onco Anonanga Ther. 2017 Jul 10; 10: 3363-3372. doi: 10.2147 / OTT.S122397. eCollection 2017. Ongororo. PubMed PMID: 28744140; PubMed Central PMCID: PMC5513878.

[8] "Tsanangudzo yeNeratinib - National Cancer Institute Duramazwi Drug". Yakadzorerwa 1 Zvita 2008.

[9] "Mahwendefa eNeratinib akanyorwa" (PDF). US Kudya neDrug Administration (FDA). Chikunguru 2017. Kudzoreredzwa Kukadzi 6, 2018. Zvekutsvagisa chitaridzi ona, peji reDFA renongedzo yeNADA 208051 Chinyorwa ichi chinobatanidza zvinyorwa kubva kuno sosi, iri munharaunda yeruzhinji. Gandhi L, et al. (2017). "MA04.02 Neratinib ± Temsirolimus muHER2-mutant cancer cancer: yedzimwe nyika, yakasarudzika chikamu chechipiri kudzidza". Zvinyorwa zveToracic Oncology. 12 (1): S358-9. doi: 10.1016 / j.jtho.2016.11.398.