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Afatinib (BIBW2992)

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Budada Afatinib, oo lagu iibiyo magaca magaca Gilotrif iyo kuwa kale, waa daawo loo isticmaalo in lagu daaweeyo kansarka yar yar ee kansarka sanbabada (NSCLC). Waxay ka tirsan tahay qoyska daawada tyrosine kinase inhibitor, afka ayaa laga qaadaa.

Product Description

Astaamaha Aasaasiga ah

Product Name Budada Afatinib (BIBW2992)
CAS Number 850140-73-7
Formula kelli C32H33ClFN5O11
Miisaanka Nooca 718.09
Isku mid ahaanshaha 850140-73-7;

BIBW-2992;

BIBW 2992;

BIBW2992. Afatinib budada dimaleate;

Imaanshaha budo huruud Light
Kaydinta iyo Isticmaalka Qalalan, madow iyo 0 - 4 C muddo gaaban (maalmo illaa toddobaadyo) ama -20 C muddo dheer (bilo illaa sannado).

 

Tilmaanta budada Afatinib

Budada Afatinib, oo lagu iibiyo magaca caanka ah ee Gilotrif iyo kuwa kale, waa daawo loo isticmaalo in lagu daaweeyo kansarka unugyada yar-yar ee kansarka (NSCLC). Waxay ka tirsan tahay qoyska daawada tyrosine kinase inhibitor, afka ayaa laga qaadaa, badanaa waxaa loo isticmaalaa in lagu daaweeyo kiisaska NSCLC ee keena isbadal ku dhaca hiddo-wadaha cuncunka cuncunka cuncunka (EGFR).

Budada Afatinib (BIBW2992), oo ah kahortagayaasha aan ka noqoshada lahayn ee qoyska ErbB ee tyrosine kinases, ayaa la muujiyey si loo xakameeyo fosforyaalka EGF ee EGFR iyo kororka unugyada ee noocyada kala duwan ee EGFR-xad-dhaafka ah iyo HER2-muujinta khadadka unugyada sida A431, NIH-3T3 -HER2, NCI-N87 iyo BT-474.

Qaybta ayaa sidoo kale si ballaadhan loogu isticmaalay noocyo kala duwan oo xayawaan ah si loo barto doorka EGFR / HER2. Maamulka afka ee budada afatinib wuxuu joojiyay koritaanka unugyada kansarka iyo noolaanshaha wuxuuna xakameynayaa dib u soo celinta burooyinka ee xenograft iyo moodooyinka kansarka sanbabada transgenic. Intaa waxaa dheer, budada afatinib waxaa loo aqoonsaday inay tahay xannibaadaha EGFR kaas oo loo oggolaaday daaweynta bukaanada qaba kansarka sanbabada ee unugyada unugyada aan caadiga ahayn ee 'EGFR-mutated'.

 

Afatinib Powder Mechanism of Action

Sida lapatinib iyo neratinib, budada afatinib waa borotiin kinase inhibitor ah oo sidoo kale si aan macquul aheyn u xakameynaya cunsur ahaaneedka kobaca cuncunka bini'aadamka 2 (Her2) iyo qanjidhada koritaanka cuncunka epidermal (EGFR) kinases

Budada Afatinib kaliya maahan firfircoonida ka soo horjeedka isbeddelka EGFR ee lagu bartilmaameedsaday jiilka koowaad ee tyrosine-kinase inhibitors (TKIs) sida erlotinib ama gefitinib, laakiin sidoo kale ka soo horjeedka isbeddelada aan caadiga ahayn ee u adkaysta daawooyinkan

Si kastaba ha noqotee, maaha mid firfircoon oo ka dhan ah isbeddelka T790M oo guud ahaan u baahan daawooyinka jiilka saddexaad sida osimertinib. Sababtoo ah waxqabadkeeda dheeriga ah ee ka dhanka ah Her2, waxaa lagu baarayaa kansarka naasaha iyo sidoo kale kansarrada kale ee EGFR iyo Her2.

 

Codsiga Budada Afatinib

Budada Afatinib waa mid ka soobaxda anilino-quinazoline oo bioavailable ah iyo ka-hortagayaasha soo-qaadaha tyrosine kinase (RTK) ee soo-dhoweynta epidermal factor receptor (ErbB; EGFR) qoyska, oo leh waxqabadka antineoplastic.

Budada Afatinib sidoo kale waa afka laga qaato bioavailable dual receptor tyrosine kinase (RTK) inhibitor leh firfircoonida antineoplastic-ka. EGFR / HER2 tyrosine kinase inhibitor BIBW 2992 si aan macquul aheyn ayaa loogu xiraa oo loo xakameeyaa qaboojiyeyaasha kobaca epidermal ee bini'aadamka 1 iyo 2 (EGFR-1; HER2), taas oo sababi karta joojinta koritaanka burooyinka iyo angiogenesis. EGFR / HER2 waa RTKs ka tirsan EGFR superfamily; labaduba waxay door muhiim ah ka ciyaaraan kordhinta unugyada burooyinka iyo vascularization burooyinka waxaana si xad dhaaf ah loogu muujiyay noocyo badan oo unugyada kansarka ah.

Budada Afatinib waxaa laga ansixiyaa adduunka intiisa badan (oo ay kujiraan Mareykanka, Kanada, Boqortooyada Midowday iyo Australia) si loogu daaweeyo metastatic non-small cell carcinoma (NSCLC), oo ay soo saartay Boehringer Ingelheim. Waxay u shaqeysaa sidii loo xakameynayo angiokinase.

 

Afatinib Powder Side Raadka & Digniinta

Dhibaatooyinka soo socda ayaa caadi ah (oo ka dhaca in ka badan 30%) bukaanada qaata budada afatinib:

Arrhea Shuban

Ne Qarxinta finanka (koox ka mid ah xaaladaha maqaarka oo u eg finanka)

So Af xanuun

Ron Paronychia (infekshinka ciddiyaha)

Mouth Af qallalan

 

Kuwani waa waxyeellooyin aan caadi ahayn (oo ku dhaca 10-29%) bukaannada qaata budada afatinib:

Ite Rabitaanka cuntada oo yaraada

Ching Cuncun

Ight Miisaan lumis

▪ Sanka oo dhiig baxa

▪ Cystitis (infekshinka kaadiheysta)

▪ Cheilitis (barar faruuryaha)

Ever Qandho

Po Hypokalemia (potassium yar)

Jun Cudurka 'conjunctivitis'

Rhinorrhea (sanka oo dareera)

Z Enzymyada beerka oo sareeya

Dhibaatooyinka oo dhan kuma qorna kor. Qaar ka mid ah dhif (oo ku dhaca in ka yar 10 boqolkiiba bukaannada) halkan kuma qorna. Had iyo jeer ogeysii bixiyahaaga daryeelka caafimaadka haddii aad isku aragto astaamo aan caadi ahayn.

 

Waxyaabaha muhiimka ah ee laga xasuusto dhibaatooyinka soo raaca budada afatinib:

Dadka badankood ma la kulmi doonaan dhammaan dhibaatooyinka soo raaca budada afatinib ee ku taxan.

Effects Dhibaatooyinka soo raaca budada Afatinib badanaa waa la saadaalin karaa marka loo eego bilowgooda, muddadooda, iyo darnaantooda.

Effects Dhibaatooyinka soo raaca budada Afatinib badanaa had iyo jeer waa la beddeli karaa waana la tagi doonaa ka dib marka daaweynta la dhammeeyo.

Effects Dhibaatooyinka soo raaca budada Afatinib waxay noqon karaan kuwo si wanaagsan loo maareyn karo. Waxaa jira fursado badan oo lagu yareeyo ama looga hortago dhibaatooyinka soo raaca budada afatinib.

 

Tixraaca

[1] Prim N, Fore M, Mennecier B. [Budada Afatinib (BIBW 2992).]. Rev Pneumol Clin. 2014 Meey 27. pii: S0761-8417 (14) 00047-9. doi: 10.1016 / j.pneumo.2014.03.002. [Epub ka hor daabacaadda] Dib u eegid. Faransiis. Caawinaad PMID: 24878189.

[2] D'Arcangelo M, Hirsch FR. Qalabka daaweynta iyo isbarbardhiga ee budada afatinib ee kansarka sanbabada ee unugyada yar. Bayoolaji. 2014 Abriil 23; 8: 183-92. doi: 10.2147 / BTT.S40567. eCollection 2014. Dib u eegis. PubMed PMID: 24790411; PubMed Bartamaha PMCID: PMC4003149.

[3] Bowles DW, Weickhardt A, Jimeno A. Afatinib budada loogu talagalay daaweynta bukaanada qaba kansarka sanbabada ee unugyada yar-yar ee EGFR-positive. Dawooyinka Maanta (Barc). 2013 Sep; 49 (9): 523-35. doi: 10.1358 / dot.2013.49.9.2016610. Dib u eegid. Caawinaad PMID: 24086949.

[4] Köhler J, Schuler M. Afatinib budada, erlotinib iyo gefitinib ee daaweynta-safka koowaad ee EGFR mutation-positive sambabada adenocarcinoma: dib u eegis. Onkologie. 2013; 36 (9): 510-8. doi: 10.1159 / 000354627. Epub 2013 Aug 19. Dib u eegis. Caawinaad PMID: 24051929.

[5] Yap TA, Popat S. Doorka budada afatinib ee maaraynta kansarka sanbabada ee unugyada yar. Khabiirka Opin Drug Metab Toxicol. 2013 Nofeembar; 9 (11): 1529-39. doi: 10.1517 / 17425255.2013.832755. Epub 2013 Aug 28. Dib u eegis. Caawinaad PMID: 23985030.

[6] Dungo RT, Keating GM. Budada Afatinib: oggolaanshaha koowaad ee adduunka. Daroogada. 2013 Sep; 73 (13): 1503-15. doi: 10.1007 / s40265-013-0111-6. Dib u eegid. Caawinaad PMID: 23982599.

[7] Minkovsky N, Berezov A (Diseembar 2008). "BIBW-2992, oo ah laba-qaate-yaqaan tyrosine kinase inhibitor ah oo loogu talagalay daaweynta burooyinka adag". Aragtida Hada laga qabo Daawooyinka Baarista. 9 (12): 1336–46. PMID 19037840

[8] Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, iyo al. (Ogosto 2008). "BIBW2992, oo ah" EGFR / HER2 inhibitor "aan la soo celin karin oo si aad ah waxtar ugu leh moodooyinka kansarka sanbabada ee khaaska ah". Oncogene. 27 (34): 4702–11. doi: 10.1038 / onc.2008.109. PMC 2748240. PMID 18408761.