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Afatinib (IBHAYIBHILE2992)

Akukho kalo Udidi:

I-Afatinib powder, ithengiswa phantsi kwegama legama elithi Gilotrif phakathi kwabanye, iyeza elisetyenziselwa ukunyanga i-cell carcinoma (NSCLC) engeyiyo encinci. Yeyosapho lwe-tyrosine kinase inhibitor yamayeza. Ithathwa ngomlomo.

Ingcaciso yeMveliso

Iimpawu ezisisiseko

Igama lemveliso I-Afatinib powder (BIBW2992)
Inani leCAS 850140-73-7
I-Molecular Formula Ikhowudi yemali ye-C32H33ClFN5O11
Ubukhulu beFormula 718.09
Iintetho ezifanayo 850140-73-7;

IBHAYIBHILE-2992;

IBIBW 2992;

IBHAYIBHILE2992. I-Afatinib powder dimaleate;

Kubonakala Uphuzi ophuzi ophuzi
Ukugcina nokuPhatha Okomileyo, omnyama kunye no-0 ukuya ku-4 C okwexesha elifutshane (iintsuku ukuya kwiiveki) okanye -20 C ixesha elide (iinyanga ukuya kwiminyaka).

 

Inkcazo yePowderib Powder

I-Afatinib powder, ethengiswa phantsi kwegama legama elithi Gilotrif phakathi kwabanye, iyeza elisetyenziselwa ukunyanga i-cell carcinoma (NSCLC) engeyiyo encinci. Yeyosapho lwe-tyrosine kinase inhibitor yamayeza, ethathwa ngomlomo, isetyenziselwa ukunyanga iimeko ze-NSCLC ezigcina utshintsho kwi-gene epidermal growth factor receptor (EGFR).

I-Afatinib powder (i-BIBW2992), isithintelo esingenakuphinda senziwe kusapho lakwa-ErbB lwe-tyrosine kinases, yaboniswa icinezela i-EGF-indased phosphorylation ye-EGFR kunye nokwanda kweseli kwiindidi ezahlukeneyo ze-EGFR-overexpressing kunye ne-HER2-echaza imigca yeseli efana ne-A431, NIH-3T3 -HER2, NCI-N87 kunye neBT-474.

Icandelo liye lasetyenziswa kakhulu kwiimodeli ezahlukeneyo zezilwanyana ukufunda indima ye-EGFR / HER2. Ukulawulwa ngomlomo kwe-afatinib powder kuthintele ukukhula komhlaza weseli kunye nokusinda kunye nokucinezela ukubuyela kwesisu kwi-xenograft kunye neemodeli zomhlaza wemiphunga ye-transgenic. Ukongeza, i-afatinib powder ichongiwe njenge-EGFR blocker evunyiweyo kunyango lwezigulana ezinomhlaza wemiphunga yeseli ye-EGFR.

 

Indlela ye-Afatinib Powder yokuSebenza

Njenge-lapatinib kunye ne-neratinib, i-afatinib powder yiprotein kinase inhibitor ekwagcina kungathinteleki ukuthintela ukukhula kwe-epidermal factor receptor 2 (Her2) kunye ne-epidermal growth factor receptor (EGFR) kinases.

I-Afatinib powder ayisebenzi kuphela ngokuchasene notshintsho lwe-EGFR olujolise kwisizukulwane sokuqala se-tyrosine-kinase inhibitors (TKIs) njenge-erlotinib okanye i-gefitinib, kodwa kunye nxamnye notshintsho olungaqhelekanga oluchasene nala machiza.

Nangona kunjalo, ayisebenzi ngokuchasene notshintsho lwe-T790M olufuna ngokubanzi iziyobisi zesithathu ezifana ne-osimertinib. Ngenxa yomsebenzi wayo owongezelelweyo ngokuchasene no-Her2, kuphandwa ngomhlaza wamabele kunye nezinye i-EGFR kunye ne-Her2 yomhlaza oqhutywa..

 

Isicelo sePowderib Powder

I-Afatinib powder yinto efumaneka ngomlomo kwi-anilino-quinazoline derivative kunye ne-inhibitor ye-receptor tyrosine kinase (RTK) ye-epidermal factor factor receptor (ErbB; EGFR) yosapho, enomsebenzi we-antineoplastic.

I-Afatinib powder nayo iyinto engena ngomlomo kwi-receptor receptor tyrosine kinase (RTK) inhibitor enokubakho kwimisebenzi ye-antineoplastic. I-EGFR / HER2 tyrosine kinase inhibitor I-BIBW 2992 ibophelela ngokungenakuphikiswa ibuye ithintele ukukhula kwamanqanaba okukhula kwesidima somntu 1 kunye no-2 (EGFR-1; HER2), enokuthi ikhokelele kuthintelo lokukhula kwethumba kunye ne-angiogenesis. I-EGFR / HER2 zii-RTKs zezosapho lwe-EGFR; Zombini zidlala indima enkulu ekwandeni kweseli kunye ne-tumor vascularization kwaye zixinaniswe kakhulu kwiindidi zesifo somhlaza.

I-Afatinib powder ivunyiwe kwiindawo ezininzi zehlabathi (kubandakanya i-United States, Canada, i-United Kingdom ne-Australia) kunyango lwe-metastatic non-small cell lung carcinoma (NSCLC), ephuhliswe ngu-Boehringer Ingelheim. Isebenza njenge-angiokinase inhibitor.

 

Iziphumo zePowderib zePowder kunye nesilumkiso

Iziphumo ebezingalindelekanga zixhaphakile (zenzeka ngaphezulu kwe-30%) kwizigulana ezithatha i-afatinib powder:

▪ Urhudo

▪ Ukuqhuma kwamabala (iqela leemeko zolusu ezifana namabala)

Izilonda zomlomo

▪ IParonychia (usulelo lweenzipho)

▪ Umlomo owomileyo

 

Ezi ziziphumo ebezingalindelekanga eziqhelekileyo (ezenzeka nge-10-29%) kwizigulana ezifumana umgubo we-afatinib:

▪ Ukunciphisa ukutya

▪ Ukurhawuzelela

▪ Ukwehla kobunzima

▪ Impumlo iyopha

▪ ICystitis (usulelo lwesinyi)

▪ I-Cheilitis (ukudumba kwemilebe)

▪ Umkhuhlane

▪ IHypokalemia (potassium ephantsi)

▪ Isidumbu (iso elipinki)

▪ Irhinorrhea (ukuphuma kwempumlo)

▪ Ii-enzymes zesibindi eziphakamileyo

Ayizizo zonke iziphumo ebezingalindelekanga ezidweliswe apha ngasentla. Ezinye ezinqabileyo (ezenzeka ngaphantsi kweepesenti ezili-10 zezigulane) azibhalwanga apha. Soloko wazisa umboneleli wakho wezempilo ukuba ufumana naziphi na iimpawu ezingaqhelekanga.

 

Izinto ezibalulekileyo ekufuneka uzikhumbule malunga neziphumo ebezingalindelekanga ze-afatinib powder:

▪ Uninzi lwabantu alunakufumana zonke iziphumo ebezingalindelekanga zomgubo ezidwelisiweyo.

▪ Iimpembelelo ze-Afatinib ezichaphazelekayo zihlala ziqikelelwa ngokuqala kwazo, ubude bexesha kunye nobunzima.

▪ Iziphumo ebezingalindelekanga ze-Afatinib zihlala zibuyela umva kwaye ziya kumka emva kokuba unyango lugqityiwe.

▪ Iimpembelelo ze-Afatinib ezichaphazelekayo zinokulawulwa. Kukho iindlela ezininzi zokunciphisa okanye ukukhusela imiphumo emibi ye-afatinib powder.

 

isingqiniso

[1] Prim N, Fore M, Mennecier B. [Afatinib umgubo (BIBW 2992).]. UMfu Pneumol Clin. 2014 ngoMeyi 27. pii: S0761-8417 (14) 00047-9. ikhonkco: 10.1016 / j.pneumo.2014.03.002. [Epub phambi kokuprinta] Uphengululo. IsiFrentshi. Ipapashwe kwi-PMID: 24878189.

[2] D'Arcangelo M, Hirsch FR. Ukusetyenziswa kweklinikhi kunye nokuthelekisa i-afatinib powder kumhlaza womhlaza wamaphaphu ongekho mncinci. Ibhayoloji. Ngo-2014 uMatshi 23; 8: 183-92. ikhonkco: 10.2147 / BTT.S40567. eCollection 2014. Uphengululo. Ipapashwe kwi-PMID: 24790411; Ipapashwe kwi-PMCID eseMbindini: PMC4003149.

[3] I-Bowles DW, i-Weickhardt A, i-Jimeno A. i-Afatinib powder kunyango lwezigulana ezine-EGFR-positive non-small cell cell cancer. Iziyobisi Namhlanje (Barc). Ngo-2013 Sep; 49 (9): 523-35. ikhonkco: 10.1358 / dot.2013.49.9.2016610. Uphononongo. Ipapashwe kwi-PMID: 24086949.

[4] Köhler J, Schuler M. Afatinib powder, erlotinib kunye negefitinib kunyango lokuqala lwe-EGFR mutation-positive lung adenocarcinoma: uphononongo. Onkologie. Ngo-2013; 36 (9): 510-8. ikhonkco: 10.1159 / 000354627. Epub 2013 Aug 19. Uphengululo. Ipapashwe kwi-PMID: 24051929.

[5] I-Yap TA, i-Popat S. Indima ye-afatinib powder ekulawuleni i-cell carcinoma engeyiyo encinci. Ingcali yeOtin yeziyobisi iMetab. NgoNovemba ka-2013; 9 (11): 1529-39. ikhonkco: 10.1517 / 17425255.2013.832755. Epub 2013 Aug 28. Uphengululo. I-PMID epapashiweyo: 23985030.

[6] I-Dungo RT, Ukutsala iMG. I-Afatinib powder: ukuvunywa kokuqala kwehlabathi. Iziyobisi. Ngo-2013 Sep; 73 (13): 1503-15. ikhonkco: 10.1007 / s40265-013-0111-6. Uphononongo. Ipapashwe kwi-PMID: 23982599.

[7] UMinkovsky N, uBerezov A (uDisemba 2008). “IBIBW-2992, i-receptor ezimbini tyrosine kinase inhibitor kunyango lwamathumba aqinileyo”. Uluvo lwangoku lweziyobisi. 9 (12): 1336-46. IINKCUKACHA:

[8] Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, et al. [2008] (Agasti 2992). "I-BIBW2, i-EGFR / HER27 inhibitor engenakuphinda isebenze kwiimodeli zomhlaza wemiphunga". Oncogene. 34 (4702): 11–10.1038. ikhonkco: 2008.109 / onc.2748240. I-PMC 18408761. PMID XNUMX.