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Dacomitinib

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Dacomitinib efuefu o le tyrosine kinase taofiofia. O le kinase o se enzyme e faʻamalosia ai le tuputupu aʻe o sela. E tele ituaiga o kinases, e faʻatonutonu ai vaega eseese o le tupuola o sela…

Faamatalaga oloa

Tulaga Autu

Igoa oloa Dacomitinib paula
Numera CAS 1110813-31-4
Faiga Faʻavae Molecular C24H25ClFN5O2
Fua Faatatau o le Umi 469.9
Synonyms Efuefu Dacomitinib;

1110813-31-4;

PF299804;

Dacomitinib paula (PF299804, PF299);

PF-00299804;

(2E)-N-(4-((3-chloro-4-fluorophenyl)Amino)-7-methoxyquinazolin-6-yl)-4-piperidin-1-ylbut-2-enamide.

Faʻaaliga Paʻepaʻe pe ituaiga paʻepaʻe
Teuina ma Taulimaina Faleoloa i le potu vevela i se nofoaga matutu.

 

Dacomitinib Powder Faʻamatalaga

Dacomitinib efuefu o le tyrosine kinase taofiofia. O le kinase o se enzyme e faʻamalosia ai le tuputupu aʻe o sela. E tele ituaiga o kinase, e faʻatonutonu ai vaega eseʻese o le tuputupu aʻe o sela. O lenei vailaʻau faʻatutuina epidermal tuputupu ae vaega receptor (EGFR) tyrosine kinase ma exon 19 soloia po o exon 21 L858R suia suiga. I le poloka o le EGFR, o lenei vailaʻau mafai ona faʻatelegese le tuputupu ae o sela kanesa. O lau kulupu oncology o le a tofotofoina lou patu mo lenei faaletonu, lea e tatau ona i ai ina ia maua ai vailaʻau.

 

Dacomitinib Powder Faiga o Gaioiga

Dacomitinib efuefu o se le mafai ona toe suia laʻititi mole poloka poloka o le gaioiga o le tagata epidermal tuputupu ae mea faʻaola (EGFR) aiga (EGFR / HER1, HER2, ma HER4) tyrosine kinases. E maua ai le taofiofia le mafai ona toe suia e ala i le fusia faʻatasi i totoe o le cysteine ​​i vaega o catalytic o le HER taliaina. O le vavalalata o le dacomitinib paula ua faʻaalia e iai le IC50 o le 6 nmol / L.

O le ErbB poʻo le epidermal tuputupu aʻe tulaga (EGF) aiga faia se matafaioi i tuputupu tuputupu, metastasis, ma togafitiga tetee e ala i le faʻagaoioiina o lalo auala faailoilo auala e pei o Ras-Raf-MAPK, PLCgamma-PKC-NFkB ma PI3K / AKT ala i le tyrosine kinase-driven phosphorylation i le carboxy-terminus. I le 40% o mataupu o loʻo faʻaalia ai le faʻateleina o le EGFR gene ma le 50% o mataupu o loʻo iai le suiga o le EGFRvIII e fai ma sui o le tapeina e maua ai le faʻaauau pea o le tyrosine kinase domain o le receptor.

 

Dacomitinib Powder Talosaga

Dacomitinib paula e faʻaaogaina e togafitia ai se ituaiga ituaiga o kanesa kanesa (e le o se tamai sela kanesa kanesa) E galue e ala i le telegese pe taofi le tuputupu aʻe o kanesa sela.

Dacomitinib paula na faʻamaonia mo le faʻaogaina o fomaʻi i le Iunaite Setete ia Setema 2018, i Iapani i le 2019, ma i le Iuni a Europa i le 2019, mo le togafitia o le leai-laʻau sela mama kanesa ma epidermal tuputupu ae vaega receptor (EGFR) gene mutation.

 

Dacomitinib Powder Itu Aafiaga & Lapataiga

E ui lava e seasea maua, o nisi tagata atonu e matua leaga ma o nisi taimi e leaga ai aʻafiaga a o tagofia fualaʻau. Taʻu i lau fomaʻi pe maua loa se fesoasoani faʻafomaʻi pe a fai e iai se tasi o faʻailoga poʻo faʻailoga nei e ono fesoʻotaʻi ma se leaga aʻafiaga itu:

▪ Faʻailoga o se faʻaletonu o le tino, pei o le mageso; hives; mageso; mumu, fulafula, paʻu, poʻo le paʻuʻu paʻu e i ai pe leai se fiva; paʻu; fufusi i le fatafata poʻo le faʻaʻi; faʻafitauli tau manava, folo, pe tautala; masani le pupula; poʻo le fula o le gutu, foliga, laugutu, laulaufaiva, poʻo le faʻaʻi.

▪ Faailoga o le suka toto maualuga pei o le le mautonu, lagona fia moe, sili atu fia inu, sili atu fiaaai, pasi masani masimasi, flushing, anapogi manava, po o le manava e manogi pei o fualaʻau.

▪ Faʻailoga o faʻafitauli tau eletise e pei o suiga o lagona, le mautonu, tiga o musele poʻo vaivaiga, o le tata o le fatu e le o lagona e masani ai, maʻi o le tino, le fia 'ai, poʻo le leaga tele o le manava poʻo le tiaʻi.

▪ Soʻo se tali a le paʻu.

▪ Mumu poʻo le osooso o alofilima poʻo alofivae.

▪ Tiga o le fatafata.

▪ Fiva.

▪ Ogaoga leaga ma o nisi taimi e oti ai faʻafitauli o le mama na tupu i le pauta dacomitinib. Valaau vave lau fomaʻi pe a iai ni ou māmā poʻo ni manava manava e fou pe sili atu le leaga e pei o le tale poʻo le manava puʻupuʻu.

E leʻo uma uma ni aʻafiaga e ono tutupu. A iai ni au fesili e uiga i aʻafiaga, valaʻau lau fomaʻi. Valaʻau lau fomaʻi mo fautuaga faʻafomaʻi e uiga i aʻafiaga E mafai ona e lipotia ni aʻafiaga i le FDA ile 1-800-332-1088.

 

Tusitaiala

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[2] Janne PA, Boss DS, Camidge DR, Britten CD, Engelman JA, Garon EB, Guo F, Wong S, Liang J, Letrent S, Millham R, Taylor I, Eckhardt SG, Schellens JH: Vaega I fualaʻau faʻateleina Suesueina o le pan-HER inhibitor, PF299804, i tagata mamaʻi ua maua i ni gasegase tuma le alualu i luma. Clin Kanesa Res. 2011 Mati 1; 17 (5): 1131-9. faia: 10.1158 / 1078-0432.CCR-10-1220. Epub 2011 Ian 10.

[3] Smith M (6 Iuni 2017). "Dacomitinib paʻu E seti PFS Faʻamaumauga i le Vaega III NSCLC Tofotofoga". MedPage Aso Nei

[4] Taylor P (28 Ianuari 2014). "Feula ia Pfizer pei o le dacomitinib paʻu ua le manuia i le kanesa o le kanesa tofotofoga". pmlive.com.

[5] Sepulveda JM, Sanchez-Gomez P, Vaz Salgado MA, Gargini R, Balana C: Dacomitinib paula: o se vailaʻau suʻesuʻe mo le togafitia o glioblastoma. Tomai Faʻapitoa Opin Investig. 2018 Oketopa; 27 (10): 823-829. faia: 10.1080 / 13543784.2018.1528225. Epub 2018 Oketopa 5.

[6] Bethune G, Bethune D, Ridgway N, Xu Z: Epidermal tuputupu aʻe suʻega (EGFR) i kanesa kanesa: o se aotelega ma faʻafouina. J Thorac Dis. 2010 Mati; 2 (1): 48-51.

[7] Petesa (2006). Fualaʻau ma Lactation Database. Faletusi a le Atunuʻu.

[8] Fry DW, Bridges AJ, Denny WA, Doherty A, Greis KD, Hicks JL, Hook KE, Keller PR, Leopold WR, Loo JA, McNamara DJ, Nelson JM, Sherwood V, Smaill JB, Trumpp-Kallmeyer S, Dobrusin EM: Faʻapitoa, le mafai ona toe faʻagaoioia o le epidermal tuputupu ae mea taliaina ma le erbB2, e se vasega fou o le tyrosine kinase taofiofia. Proc Natl Acad Sci US A. 1998 Sep 29; 95 (20): 12022-7.