AASraw tsim NMN thiab NRC hmoov hauv qhov ntau!

Erlotinib

Erlotinib, muag nyob hauv cov lag luam muaj npe Tarceva ntawm lwm tus, yog cov tshuaj siv los kho mob tsis yog mob ntsws hauv hlwb tsawg (NSCLC) thiab mob qog nqaij hlav cancer. Tshwj xeeb nws yog siv rau NSCLC nrog kev hloov pauv nyob hauv kev sib kis ntawm cov kabmob loj (EGFR) - ib qho exon 19 deletion (del19) lossis exon 21 (L858R) hloov pauv - uas tau kis mus rau lwm qhov ntawm lub cev.

Hauj lwm yam khoom

Cov yam ntxwv yooj yim

khoom npe Erlotinib
CAS Number 183321-74-6
molecular Formula C22H23N3O4
Mis Lub Cev 393.443
Synonyms CP-358774;

OSI774;

Erlotinib dawb puag;

183321-74-6.

tsos Dawb rau dawb-dawb crystalline 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).

 

Erlotinib Hauj lwm

Erlotinib, muag nyob hauv cov lag luam muaj npe Tarceva ntawm lwm tus, yog cov tshuaj siv los kho mob tsis yog mob ntsws hauv hlwb tsawg (NSCLC) thiab mob qog nqaij hlav cancer. Tshwj xeeb nws yog siv rau NSCLC nrog kev hloov pauv nyob hauv kev sib kis ntawm cov kabmob loj (EGFR) - ib qho exon 19 deletion (del19) lossis exon 21 (L858R) hloov pauv - uas tau kis mus rau lwm qhov ntawm lub cev. Nws yog noj ntawm qhov ncauj.

Erlotinib yog quinazoline derivative nrog antineoplastic cov yam ntxwv. Kev sib tw nrog adenosine triphosphate, erlotinib thim rov qab khi rau qhov tsis txaus ntshai catalytic domain ntawm epidermal kev loj hlob qhov teeb meem receptor (EGFR) tyrosine kinase, yog li thim rov qab los tiv thaiv EGFR phosphorylation thiab thaiv cov teeb liab kis xwm txheej thiab cov teebmeem ntawm cov kabmob uas cuam tshuam nrog EGFR kev ua haujlwm.

Erlotinib tau pom zoo rau kev siv tshuaj kho mob hauv Tebchaws Asmeskas thaum xyoo 2004. Nws nyob rau hauv Lub Tsev Noj Qab Haus Huv Lub Koomhaum cov npe ntawm Cov Tshuaj Tseem Ceeb, uas teev cov tshuaj muaj kev nyab xeeb thiab zoo tshaj plaws uas yuav tsum tau muaj hauv kev noj qab haus huv.

 

Erlotinib Kev Siv Tes Ua ntawm Kev Ua

Erlotinib yog ib qho kev sib kis ntawm daim tawv nqaij receptor inhibitor (EGFR inhibitor). Cov tshuaj ua raws Iressa (gefitinib), uas yog thawj qhov tshuaj ntawm hom no.

Erlotinib tshwj xeeb tshwj xeeb tshaj yog cov kabmob sib kis ntawm cov kabmob loj (EGFR) tyrosine kinase, uas tau hais tawm thiab qee lub sijhawm hloov kho rau ntau hom mob qog nqaij hlav. Nws khi rau hauv kev thim rov qab rau adenosine triphosphate (ATP) khi qhov chaw ntawm lub receptor. Rau cov teeb liab kis tau, ob EGFR lwg me me xav tau los ua ke los ua homodimer.

Cov no tom qab siv cov molecule ntawm ATP rau trans-phosphorylate txhua lwm yam ntawm tyrosine seem, uas ua kom cov phosphotyrosine seem, nrhiav cov phosphotyrosine-khi cov protein rau EGFR kom sib sau ua ke protein ntau uas xa cov teeb liab cascades mus rau lub nucleus lossis qhib lwm cov txheej txheem ntawm biochemical cellular. Thaum erlotinib khi rau EGFR, kev tsim cov phosphotyrosine seem hauv EGFR tsis tau thiab lub teeb liab cascades tsis yog pib.

Erlotinib kuj yog tyrosine kinase receptor inhibitor uas tau siv rau hauv kev kho mob ntawm kev kho mob siab lossis metastatic pancreatic lossis tsis mob qog nqaij hlav hauv hlwb. Erlotinib txoj kev kho yog txuam nrog kev hloov chaw ntau ntxiv hauv cov ntshav aminotransferase ntau ntau thaum lub sij hawm kho thiab qhov tsis tshua pom muaj los ntawm kev raug mob rau daim siab.

 

Daim Ntawv Thov Erlotinib 

Erlotinib yog qhov thim rov qab thawj tiam receptor tyrosine kinase inhibitor (nrog rau Gefitinib) ua yeeb yam feem ntau ntawm tus kabmob epidermal kev loj hlob tau (EGFR), tus tswv cuab ntawm ErbB receptor tsev neeg. Cov tshuaj cuam tshuam nrog ob hom tsiaj qus thiab hloov pauv EGFR. Tsev neeg ErbB tuaj yeem tsim homodimers lossis heterodimers, uas feem ntau cuam tshuam txog cov kev cuam tshuam hauv qab thiab cov kab mob ntawm ntau hom carcinomas tau kawm hauv tib neeg. Receptor tyrosine kinase inhibitors (TKI) tiv thaiv cov phosphorylation ntawm lawv cov ntsaws qis hauv lub xovtooj ntawm tes taw qhia. EGFR ib txwm ua lub luag haujlwm hauv ntau lub xovtooj ntawm tes, suav nrog kev sib txawv, nthuav dav, thiab angiogenesis, txhua qhov ntawm cov yam ntxwv ntawm kev mob qog nqaij hlav.

Kev Hloov Sib Hloov EGFR hauv NSCLC feem ntau yog kev hloov mus rau lwm tus. Qee tus yam ntxwv ntawm tus neeg mob uas ua rau muaj qhov hloov ntawm EGFR ntau dua yuav tsis muaj keeb kwm ntawm kev haus luam yeeb paub tseeb adenocarcinoma los ntawm kev txheeb xyuas histologic, Asian haiv neeg, thiab poj niam txiv neej pw. Kev hloov pauv thib ob hauv EGFR feem ntau tshwm sim, uas cov kab lus no piav qhia hauv qab no.

 

Erlotinib Sab Sijhawm & Ceeb Toom

Cov kev mob tshwm sim nram qab no tshwm sim rau cov neeg mob noj Erlotinib:

Pob Ntxau

. Mob plab zawv

Appetite Tsis qab los noj mov

Igue Qaug zog

Breath Ua tsis taus pa txog pa

Hnoos

Xeev siab thiab ntuav

 

Cov kev mob tshwm sim no tsis tshua pom tshwm sim tshwm sim los ntawm cov neeg mob uas tau txais Erlotinib:

Kab mob

Outh qhov ncauj tawm

Khaus

Skin Qhuav ntawm daim tawv nqaij

Ation Qhov muag khaus

▪ Mob plab

 

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% ntawm cov neeg mob) tsis muaj npe nyob ntawm no. Txawm li cas los xij, koj yuav tsum tau qhia koj tus kws saib xyuas kev noj qab haus huv yog tias koj muaj cov tsos mob txawv txawv.

 

reference

[1] Gao JW, Zhan P, Qiu XY, Jin JJ, Lv TF, Nkauj Y. Erlotinib-based doublet tsom kev kho mob piv rau erlotinib ib leeg hauv kev kho mob ua ntej tsis yog-me me ntawm lub ntsws mob ntsws: kev tsom xam los ntawm 24 qhov kev soj kev sim siab. Oncotarget. 2017 Tsib Hlis 31; 8 (42): 73258-73270. doi: 10.18632 / oncotarget.18319. eCollection 2017 Sep 22. Rov Los Saib. PubMed PMID: 29069867; PubMed Central PMCID: PMC5641210.

[2] Lee CK, Davies L, Wu YL, Mitsudomi T, Inoue A, Rosell R, Zhou C, Nakagawa K, Thongprasert S, Fukuoka M, Tswv S, Marschner I, Tu YK, Gralla RJ, Gebski V, Mok T , Yang JC. Gefitinib lossis Erlotinib vs Kev Siv Tshuaj Kho Mob rau EGFR Kev Sib Hloov-Lub Cev Mob Cancer Zoo: Tus Neeg Mob Cov Ntaub Ntawv Meta-Kev Ntsuam Xyuas Ntawm Tag Nrho Cov Ciaj sia. J Natl Cancer Inst. 2017 Jun 1; 109 (6). doi: 10.1093 / jnci / djw279. Ntsuam Xyuas. PubMed PMID: 28376144.

[3] Yang Z, Hackshaw A, Feng Q, Fu X, Zhang Y, Mao C, Tang J. Kev sib piv ntawm gefitinib, erlotinib thiab afatinib hauv kev mob ntsws tsis muaj mob rau cov cell mos mos: Kev tsom xam meta. Int J Cancer. 2017 Lub Xya Hli 15; 140 (12): 2805-2819. doi: 10.1002 / ijc.30691. Epub 2017 Mar 27. Saib. PubMed PMID: 28295308.

[4] “Erlotinib (Tarceva) Siv Thaum Cev Xeeb Tub”. Drugs.com. 1 Lub Kaum Ib Hlis 2019. Rov Nrhiav Dua 23 Hlis Ntuj nqeg 2019.

[5] "Erlotinib Monograph rau Cov Kws Tshaj Lij". Drugs.com. Txais 12 Lub Kaum Ib Hlis 2019.

[6] “Cov ntsiav tshuaj Tarceva- erlotinib hydrochloride”. Txhua Hnub. 12 Hlis ntuj nqeg 2018. Tshawb Fawb 23 Lub Kaum Ob Hlis 2019.

[7] “Pob Ntawv Pom Zoo Tshuaj: Tarceva (Erlotinib) NDA # 021743”. Meskas cov Khoom Noj thiab Tshuaj (FDA). 28 Lub Peb Hlis 2005. Tshawb Dua 23 Hlis ntuj nqeg 2019.

[8] Raymond E, Faivre S, Armand JP (2000). "Kev loj hlob cuam tshuam kis receptor tyrosine kinase ua lub hom phiaj rau kev kho tshuaj anticancer". Tshuaj. 60 Cov Khoom Siv 1: 15-23, kev sib tham 41–2. doi: 10.2165 / 00003495-200060001-00002. PMID 11129168. S2CID 10555942.