Cov yam ntxwv yooj yim

khoom npe	Afatinib (BIBW2992)
CAS Number	850140-73-7
molecular Formula	C32H33ClFN5O11
Mis Lub Cev	718.09
Synonyms	850140-73-7; BIBW-2992; PHAJ 2992; BIBW2992. Afatinib dimaleate;
tsos	Lub teeb daj hmoov
Cia thiab Ua Haujlwm	Qhuav, tsaus thiab nyob rau hauv 0 - 4 C rau lub sij hawm luv (hnub mus rau lub lis piam) lossis -20 C rau lub sij hawm ntev (hli txog xyoo).

 

Afatinib Hauj lwm

Afatinib, muag nyob rau hauv lub npe lag luam Gilotrif nrog rau lwm tus, yog cov tshuaj siv los kho mob tsis yog-cov me me ntsws ntsws carcinoma (NSCLC). Nws belongs rau tyrosine kinase inhibitor tsev neeg ntawm cov tshuaj noj.Nws noj ntawm qhov ncauj.Nws feem ntau yog siv los kho cov mob ntawm NSCLC uas muaj kev cuam tshuam kev sib kis hauv cov kabmob epidermal kev loj hlob tau receptor (EGFR) noob.

Afatinib (BIBW2992), ib qho tsis cuam tshuam kev tsis haum ntawm ErbB tsev neeg ntawm tyrosine kinases, tau pom tias yuav tua EGF-phosphorylation ntawm EGFR thiab kev nthuav tawm ntawm tes rau ntau yam ntawm EGFR-overexpressing thiab HER2-qhia kab xov tooj ntawm tes xws li A431, NIH-3T3- HER2, NCI-N87 thiab BT-474.

Cov khoom siv kuj tau siv dav siv ntau yam tsiaj qauv los kawm lub luag haujlwm ntawm EGFR / HER2. Qhov ncauj tswj hwm ntawm afatinib inhibited cell cell kev loj hlob thiab kev muaj sia nyob thiab txwv cov qog hlav qog hauv xenograft thiab transgenic ntsws mob qog qauv. Tsis tas li ntawd, afatinib tau pom tias yog EGFR blocker uas tau pom zoo rau kev kho mob rau cov neeg mob EGFR-mutated nonsmall cell mob ntsws.

 

Afatinib Kev Txom Nyem Ntawm Kev Ua

Zoo li lapatinib thiab neratinib, afatinib yog protein kinase inhibitor uas tseem tso tsis taus tib neeg txoj kev loj hlob qhov ua kom haum receptor 2 (Her2) thiab epidermal kev loj hlob yam receptor (EGFR) kinases.

Afatinib tsis yog tsuas yog ua haujlwm tiv thaiv EGFR kev hloov pauv tau tsom los ntawm thawj tiam tyrosine-kinase inhibitors (TKIs) zoo li erlotinib lossis gefitinib, tab sis kuj tawm tsam tsawg dua kev hloov pauv uas tiv taus cov tshuaj no.

Txawm li cas los xij, nws tsis muaj txiaj ntsig tawm tsam T790M hloov uas feem ntau yuav tsum tau cov tshuaj thib peb tiam zoo li osimertinib. Vim tias nws muaj ntau yam haujlwm los tawm tsam Her2, nws tseem raug kuaj mus rau mob qog noj ntshav mis thiab lwm yam mob EGFR thiab Her2 uas tau tsav.

 

Daim Ntawv Thov Afatinib

Afatinib yog qhov ncauj ntawm cov khoom noj khoom haus anilino-quinazoline derivative thiab inhibitor ntawm receptor tyrosine kinase (RTK) epidermal kev loj hlob tau receptor (ErbB; EGFR) tsev neeg, nrog kev ua haujlwm antineoplastic.

Afatinib kuj tseem yog qhov ncauj lom neeg ua kom tau txais dual receptor tyrosine kinase (RTK) inhibitor nrog cov kev muaj peev xwm ua antineoplastic. EGFR / HER2 tyrosine kinase inhibitor BIBW 2992 irreversibly khi rau thiab tiv thaiv tib neeg epidermal kev loj hlob yam receptors 1 thiab 2 (EGFR-1; HER2), uas yuav ua rau muaj kev txwv tsis pub muaj qog thiab angiogenesis. EGFR / HER2 yog RTK uas zwm rau EGFR superfamily; ob leeg ua si lub luag haujlwm loj hauv qog nqaij hlav loj zuj zus thiab nqaij hlav vascularization thiab muaj ntau heev nyob rau ntau hom qog nqaij hlav cancer.

Afatinib tau txais kev pom zoo hauv ntau lub ntiaj teb (suav nrog Asmeskas, Canada, Lub Tebchaws Askiv thiab Australia) rau kev kho mob ntawm cov kab mob ntsws tsis loj, mob ntsws (carcinoma) (NSCLC), tsim los ntawm Boehringer Ingelheim. Nws ua raws li angiokinase inhibitor.

 

Afatinib Sab Sij Huam & Ceeb Toom

Cov kev mob tshwm sim hauv qab no yog tshwm sim (tshwm sim hauv ntau dua 30%) rau cov neeg mob noj afatinib:

. Mob plab zawv

Ne Pob txuv tawv (pawg neeg tawv nqaij zoo li pob txuv)

Outh qhov ncauj tawm

Ony Paronychia (kis mob ntsia hlau)

Mouth Qhov ncauj qhuav

 

Cov no yog cov tshwm sim tsawg dua (tshwm sim hauv 10-29%) rau cov neeg mob tau txais afatinib:

Tsis qab los noj mov

Khaus

Loss Poob phaus

▪ qhov ntswg ntshav

▪ Cystitis (zais zis)

Il Cheilitis (mob rau daim di ncauj)

▪ Ua npaws

Yp Mob Hypokalemia (ntshav qab zib tsawg)

J Mob pob ntseg (qhov muag liab)

In Kabmob Ntshav (los ntswg)

Z Kev nce siab hauv lub siab enzymes

Tsis yog tag nrho cov kev mob tshwm sim muaj npe saum toj no. Qee qhov tsis tshua muaj tshwm sim (tshwm sim hauv tsawg dua 10 feem pua ​​ntawm cov neeg mob) tsis muaj npe nyob ntawm no. Nco ntsoov qhia rau koj tus kws saib xyuas kev noj qab haus huv yog tias koj muaj cov tsos mob txawv txawv.

 

Cov khoom tseem ceeb kom nco qab txog cov kev mob tshwm sim los ntawm afatinib:

People Cov neeg feem coob yuav tsis pom tag nrho ntawm afatinib phiv uas teev tseg.

▪ Afatinib phiv feem ntau tuaj yeem kwv yees hais txog lawv qhov pib, ntev, thiab mob hnyav.

Effects Afatinib phiv yuav luag txhua qhov thim rov qab thiab yuav ploj mus tom qab kev kho tiav.

Effects Afatinib phiv yuav tswj tau heev. Muaj ntau txoj hauv kev los txo qis lossis tiv thaiv qhov tshwm sim ntawm afatinib.

 

reference

[1] Prim N, Fore M, Mennecier B. [Afatinib (BIBW 2992).]. Rev Pneumol Clin. 2014 Lub Tsib Hlis 27. pii: S0761-8417 (14) 00047-9. doi: 10.1016 / j.pneumo.2014.03.002. [Epub ua ntej sau] Tshawb xyuas. Fab Kis. PubMed PMID: 24878189.

[2] D'Arcangelo M, Hirsch FR. Cov chaw khomob siv tau thiab kev sib piv ntawm afatinib hauv cov kabmob uas tsis yog kabmob me me. Cov khoom siv roj ntsha. 2014 Plaub Hlis 23; 8: 183-92. doi: 10.2147 / BTT.S40567. eCollection 2014. Kev Ntsuam Xyuas. PubMed PMID: 24790411; PubMed Central PMCID: PMC4003149.

[3] Bowles DW, Weickhardt A, Jimeno A. Afatinib rau kev kho mob ntawm cov neeg mob uas muaj EGFR-tsis zoo-tsis muaj kev mob ntsws ntawm tes ntsws loj. Cov Tshuaj Niaj Hnub No (Barc). 2013 Sep; 49 (9): 523-35. doi: 10.1358 / dot.2013.49.9.2016610. Ntsuam Xyuas. PubMed PMID: 24086949.

[4] Köhler J, Schuler M. Afatinib, erlotinib thiab gefitinib hauv kev kho thawj zaug ntawm EGFR kev hloov pauv-zoo ntsws adenocarcinoma: tshuaj xyuas. Onkologie. 2013; 36 (9): 510-8. doi: 10.1159 / 000354627. Epub 2013 Lub Yim Hli 19. Rov Ntsuam Xyuas. PubMed PMID: 24051929.

[5] Yap TA, Popat S. Lub luag haujlwm ntawm afatinib hauv kev tswj hwm tsis yog cov kabmob ntsws tsis muaj kabmob me. Tus Kws Paub Txog Opin Yeeb Tshuaj Metab Toxicol. 2013 Nov; 9 (11): 1529-39. doi: 10.1517 / 17425255.2013.832755. Epub 2013 Aug 28. Tshawb Xyuas. PubMed PMID: 23985030.

[6] Dungo RT, Keating GM. Afatinib: thawj qhov kev pom zoo hauv ntiaj teb. Tshuaj. 2013 Sep; 73 (13): 1503-15. doi: 10.1007 / s40265-013-0111-6. Ntsuam Xyuas. PubMed PMID: 23982599.

[7] Minkovsky N, Berezov A (Lub Kaum Ob Hlis 2008). "BIBW-2992, muaj dual receptor tyrosine kinase inhibitor rau kev kho cov qog ua haujlwm". Cov tswvyim Tam Sim No Hauv Kev Tshuaj Yeeb. 9 (12): 1336–46. PMID 19037840

[8] Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, li al. (Lub Yim Hli 2008). "BIBW2992, ib qho tsis paub txog EGFR / HER2 inhibitor ua tau zoo nyob rau hauv kev tiv thaiv kabmob ntsws ua rau mob ntsws" Oncogene. 27 (34): 4702–11. doi: 10.1038 / onc.2008.109. PMC 2748240. PMID 18408761.

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