Dacomitinib (1110813-31-4) phofo - Mofani oa thepa ea moetsi
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Dacomitinib

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Dacomitinib phofo ke tyrosine kinase inhibitor. Kinase ke enzyme e khothalletsang kholo ea lisele. Hona le mefuta e mengata ea li-kinase, e laolang mekhahlelo e fapaneng ea kholo ea lisele…

Tlhaloso ea Sehlahisoa

Litšobotsi tsa Motheo

Name Product Dacomitinib phofo
Nomoro ea CAS 1110813-31-4
Molecular Formula EA-KO24-C25
Boima ba 'mele 469.9
Li-synonyms Dacomitinib phofo;

1110813-31-4;

PF299804;

Dacomitinib phofo (PF299804, PF299);

EA-00299804;

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

Ponahalo Tšoeu kapa mofuta oa phofo e tšoeu
Ho Boloka le ho Sebetsana Boloka ka mocheso oa kamore sebakeng se ommeng.

 

Tlhaloso ea Phofo ea Dacomitinib

Dacomitinib phofo ke tyrosine kinase inhibitor. Kinase ke enzyme e khothalletsang kholo ea lisele. Hona le mefuta e mengata ea li-kinase, e laolang mekhahlelo e fapaneng ea kholo ea lisele. Meriana ena e shebile epidermal growth factor receptor (EGFR) tyrosine kinase ka exon 19 e tlositsoeng kapa exon 21 L858R liphetoho tse ling. Ka ho thibela EGFR, meriana ena e ka liehisa kholo ea lisele tsa mofetše. Sehlopha sa hau sa oncology se tla hlahloba hlahala ea hau bakeng sa sena se sa tloaelehang, se lokelang ho ba teng molemong oa ho fumana meriana.

 

Mokhoa oa Ts'ebetso oa Powder oa Dacomitinib

Dacomitinib phofo ke molek'hule e nyane e ke keng ea khutlisoa ea tšebetso ea lelapa la motho la kholo ea li-epidermal factor (EGFR) (EGFR / HER1, HER2, le HER4) tyrosine kinases. E fihlella thibelo e ke keng ea khutlisoa ka tlamahano e kopaneng ea masale a cysteine ​​a libakeng tse nang le matla a li-receptor tsa HER. Kamano ea phofo ea dacomitinib e bontšitsoe e na le IC50 ea 6 nmol / L.

Lelapa la ErbB kapa epidermal growth factor (EGF) le bapala karolo ea kholo ea hlahala, metastasis le kalafo ea kalafo ka ho kenya tšebetsong litsela tsa phetisetso ea lets'oao le tlase joalo ka Ras-Raf-MAPK, PLCgamma-PKC-NFkB le PI3K / AKT ka tyrosine Phase ea phasefase e tsamaeang le kinase ho carboxy-terminus. Hoo e ka bang 40% ea linyeoe li bonts'a kholiso ea lefutso la EGFR le 50% ea linyeoe tse hlahisang phetoho ea EGFRvIII e emelang ho tlosoa ho hlahisang ts'ebetso e tsoelang pele ea domain ea tyrosine kinase ea receptor.

 

Kopo ea Dacomitinib Powder

Phofo ea Dacomitinib e sebelisetsoa ho alafa mofuta o itseng oa mofets'e oa matšoafo (mofetše o seng o monyane oa lisele tsa matšoafo). E sebetsa ka ho fokotsa kapa ho emisa kholo ea lisele tsa mofetše.

Phofo ea Dacomitinib e ile ea amoheloa bakeng sa ts'ebeliso ea bongaka United States ka Loetse 2018, Japane ho 2019, le ho European Union ho 2019, bakeng sa kalafo ea mofets'e o seng o monyane oa lisele tsa lisele tse nang le phetoho ea lefutso ea epidermal factor factor receptor (EGFR).

 

Litla-morao tsa Dacomitinib Powder & Temoso

Le ha e ka ba ka seoelo, batho ba bang ba ka ba le litla-morao tse mpe haholo 'me ka linako tse ling ba bolaea ha ba noa sethethefatsi. Bolella ngaka ea hau kapa u fumane thuso ea bongaka hanghang haeba u na le matšoao kapa matšoao a latelang a ka amanang le litlamorao tse mpe haholo:

▪ Matšoao a tšoaetso, joalo ka lekhopho; hives; ho hlohlona; khubelu, ho ruruha, makhopho kapa letlalo le ebolang ka feberu kapa ntle le eona ho honotha; ho tiea sefubeng kapa 'metso; bothata ba ho hema, ho koenya kapa ho bua; hoarseness e sa tloaelehang; kapa ho ruruha ha molomo, sefahleho, molomo, leleme kapa qoqotho.

▪ Matšoao a tsoekere e phahameng maling joaloka pherekano, ho ikutloa u tšoeroe ke boroko, ho nyoreloa le ho feta, ho lapa ho feta, ho ntša moroto khafetsa, ho fofa, ho hema kapele kapa ho hema ho nkha joaloka litholoana.

Lipontšo tsa mathata a elektrolyte joaloka phetoho ea maikutlo, pherekano, bohloko ba mesifa kapa bofokoli, ho otla ha pelo ho sa utloeng hantle, ho oa, ho sa lape, kapa ho ferekana haholo ka mpeng kapa ho fafatsa.

▪ Boikutlo bofe kapa bofe ba letlalo.

▪ Bofubelu kapa ho teneha liatleng tsa matsoho kapa bohatong ba maoto.

▪ Ho opeloa ke sefuba.

▪ Feberu.

▪ Ho bile le mathata a mabe haholo 'me ka linako tse ling a bolaeang a matšoafo ka phofo ea dacomitinib. Bitsa ngaka hang-hang haeba u e-na le mathata a matšoafo kapa a phefumolohang a macha kapa a mabe joaloka ho khohlela kapa ho hema hanyane.

Tsena ha se litla-morao tsohle tse ka hlahang. Haeba u na le lipotso mabapi le litla-morao, letsetsa ngaka ea hau. Bitsa ngaka ea hau bakeng sa likeletso tsa bongaka mabapi le litla-morao U ka tlaleha litla-morao ho FDA ho 1-800-332-1088.

 

Reference

[1] Brzezniak C, Carter CA, Giaccone G: Dacomitinib phofo, kalafo e ncha ea kalafo ea mofets'e o seng o monyane oa kankere ea matšoafo. Setsebi Opin Pharmacother. 2013 Hlakola; 14 (2): 247-53. doi: 10.1517 / 14656566.2013.758714. Epub 2013 Pherekhong 7.

[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: Mokhahlelo oa I oa ho nyoloha ho ithuta ka pan-HER inhibitor, PF299804, ho bakuli ba nang le lihlahala tse thata tse tsoetseng pele. Kankere ea Kankere ea Kliniki. 2011 Mar 1; 17 (5): 1131-9. 10.1158 / 1078-0432.CCR-10-1220 (Lebitso la Mocha) Epub 2011 Pherekhong 10.

[3] Smith M (6 Phuptjane 2017). "Dacomitinib phofo e beha Record ea PFS Tekong ea Phase III NSCLC". MedPage Kajeno.

[4] Taylor P (28 Pherekhong 2014). "Foka Pfizer ha phofo ea dacomitinib e hloleha litekong tsa mofets'e oa matšoafo". pmlive.com.

[5] Sepulveda JM, Sanchez-Gomez P, Vaz Salgado MA, Gargini R, Balana C: Dacomitinib phofo: setlhare sa lipatlisiso bakeng sa kalafo ea glioblastoma. Setsebi Opin Investig Lithethefatsi. 2018 Mphalane; 27 (10): 823-829. doi: 10.1080 / 13543784.2018.1528225. Epub 2018 Mphalane 5.

[6] Bethune G, Bethune D, Ridgway N, Xu Z: Epidermal growth factor receptor (EGFR) ka mofetše oa matšoafo: kakaretso le ntlafatso. J Thorac Dis. 2010 Mar; 2 (1): 48-51.

[7] Bethesda (2006). Lithethefatsi le Lactation Database. Laeborari ea Naha ea Bongaka.

[8] Fry DW, Marokho AJ, Denny WA, Doherty A, Greis KD, Hicks JL, Hook KE, Keller PR, Leopold WR, Loo JA, DJ McNamara, Nelson JM, Sherwood V, Smaill JB, Trumpp-Kallmeyer S, Dobrusin EM: Ho sebetsa ka mokhoa o ikhethileng, o ke keng oa etsolloa oa li-epidermal growth factor receptor le erbB2, ke sehlopha se secha sa tyrosine kinase inhibitor. Proc Natl Acad Sci US A. 1998 Sep 29; 95 (20): 12022-7.