AASraw tsim NMN thiab NRC hmoov hauv qhov ntau!

Dacomitinib

 

  1. FDA pom zoo dacomitinib rau cov kab mob ntsws tsis ua mob ntsws loj hauv hlwb
  2. Kab Mob Ntshav Uas Tsis Yog Cov Me Me Yog Dab Tsi?
  3. Dacomitinib soj ntsuam daim ntawv thov hauv cov kab mob ntsws tsis mob ntsws me me
  4. Dacomitinib Tshuaj Xyuas
  5. Dacomitinib Kev Siv Tes Ua ntawm kev nqis tes ua
  6. Dacomitinib Siv
  7. Dacomitinib Sab Sij Huam
  8. Tsis yog-Lub cev ntsws mob ntsws siv rau Kev Kho Mob: Dacomitinib VS Gefitinib
  9. Yuav Ua Li Cas Dacomitinib Hmoov Hauv online?

 

FDA pom zoo dacomitinib rau metastatic tsis yog cell me kab mob ntsws

Thaum Lub Cuaj Hli 27, 2018, Lub Chaw Tswj Xyuas Khoom Noj thiab Tshuaj Yeeb Tshuaj pom zoo dacomitinib ntsiav tshuaj (VIZIMPRO, Pfizer Pharmaceutical Company) rau thawj qhov kev kho mob ntawm cov neeg mob nrog metastatic cov kab mob ntsws uas tsis yog mob hlwb (NSCLC) nrog cov kabmob loj hlob nthuav dav (EGFR) exon 19 tshem tawm lossis tshem tawm 21 L858R kev hloov pauv uas tau tshawb pom los ntawm FDA pom zoo.

Kev pom zoo yog txiav txim siab los ntawm kev sib tw, ntau yam, qhib-daim ntawv lo, cov tswj kev sim (ARCHER 1050; NCT01774721) sib piv txog kev nyab xeeb thiab kev ua tau zoo ntawm dacomitinib rau gefitinib hauv 452 cov neeg mob uas tsis tuaj yeem tiv thaiv, metastatic NSCLC. Cov neeg mob yuav tsum tsis muaj kev kho ua ntej rau cov mob metastatic lossis kab mob rov qab uas muaj tsawg kawg 12 lub hlis tsis muaj kabmob tomqab ua tiav txoj haujlwm tsis-EGFR TKI-muaj kev kho mob; ib qho Kev Koom Tes Sab Hnub Tuaj Oncology Pab Pawg qhov ua tau zoo ntawm 0 lossis 1; thiab EGFR exon 19 tshem tawm lossis exon 21 L858R kev hloov pauv. Cov neeg mob tau xaiv (1: 1) tau txais dacomitinib 45 mg rau qhov ncauj ib zaug txhua hnub lossis gefitinib 250 mg qhov ncauj ib hnub ib zaug kom txog thaum muaj mob ntxiv lossis lom tsis zoo.

Qhov kev sim ua rau pom tias muaj kev txhim kho tseem ceeb hauv kev muaj sia tsis muaj sia; Tsis muaj kev txhim kho hauv tus lej teb tag nrho lossis tag nrho cov ciaj sia tau pom. Qhov nruab nrab ntawm kev vam meej tsis muaj txoj sia nyob ntev, raws li tau txiav txim los ntawm pawg neeg soj ntsuam kev ywj pheej. yog 14.7 thiab 9.2 lub hlis nyob rau hauv dacomitinib thiab gefitinib caj npab, feem (qhov phom sij txaus ntshai 0.59; 95% CI: 0.47, 0.74; p <0.0001).

Cov ntaub ntawv sau cia muaj cov lus ceeb toom thiab cov kev ceev faj txog cov kab mob ntsws interstitial (ILD), raws plab, thiab dermatologic phiv tshuaj. Ntawm 394 tus neeg mob uas tau txais dacomitinib, muaj qhov tshwm sim tsis zoo tshwm sim rau 27%. Cov kev phiv tshuaj uas nquag muaj uas ua rau tsis dacomitinib yog zawv plab thiab ILD. Feem ntau (> 20%) phiv los ntawm dacomitinib yog zawv plab, tawm pob, paronychia, stomatitis, tsis qab los, daim tawv nqaij qhuav, poob phaus, alopecia, hnoos, thiab mob caj dab).

 

Kab Mob Ntshav Uas Tsis Yog Cov Me Me Yog Dab Tsi?

Kab mob qog nqaij hlav yog feem ntau mob cancer thoob ntiaj teb, nrog ntau dua ob lab tus neeg mob tshiab kuaj thoob ntiaj teb xyoo 2018. Kwv yees li 85 feem pua ​​ntawm tag nrho cov mob qog nqaij hlav hauv lub ntsws yog qhia tias tsis yog cell me, thiab kwv yees li 75 feem pua ​​ntawm cov no yog metastatic, lossis siab tshaj, thaum kuaj pom Cov.

EGFR yog ib cov protein uas pab cov keeb ua thiab tawg. Thaum cov EGFR gene hloov pauv nws tuaj yeem ua rau cov protein tsis txaus ntseeg ua rau cov kabmob kheesxaws tau tsim. EGFR kev sib hloov yuav tshwm sim hauv 10 txog 35 feem pua ​​ntawm NSCLC cov qog thoob plaws lub ntiaj teb, thiab cov kev hloov pauv uas nquag siv tshaj plaws yog tshem tawm hauv exon 19 thiab exon 21 L858R hloov chaw, uas suav nrog ntau dua 80 feem pua ​​ntawm kev paub ua kom hloov EGFR kev hloov pauv. Tus kab mob cuam tshuam nrog kev muaj txoj sia nyob tsawg thiab kev hloov kho tus kab mob tseem yog ib qho nyuaj.

AASraw yog lub chaw tsim khoom ntawm Dacomitinib.

Thov nyem ntawm no rau cov ntaub ntawv hais: dawb paugHu rau peb

 

Dacomitinib soj ntsuam daim ntawv thov hauv cov kab mob ntsws tsis mob ntsws me me

Dacomitinib yog qhov thib ob tiam EGFR tyrosine kinase inhibitor (TKI) uas khi tsis tau thiab khi EGFR / Her1, Her2 thiab Her4 subtypes nrog kev ua tau zoo piv rau lwm yam TKIs. Hauv ARCHER 1050 kev sim, qhov kev vam meej-tsis muaj txoj sia nyob tau zoo dua los ntawm dacomitinib piv nrog gefitinib, txhawb dacomitinib ua thawj txoj kev kho mob rau cov kev mob qias neeg tsis-me-cell nrog mob EGFR hloov tau. Hais txog qhov ua rau muaj kev phom sij ntau dua, kev txo qhov koob tshuaj tsis txo qis kev ua haujlwm ntawm dacomitinib thiab tuaj yeem txo qis qhov tshwm sim thiab qhov tsis zoo ntawm cov xwm txheej tsis zoo. Xav txog qhov hloov pauv ntawm thaj av ntawm EGFR-mutant tsis yog-me me-cell mob ntsws, yav tom ntej lub taub hau rau lub taub hau sib piv ntawm dacomitinib thiab osimertinib tuaj yeem muab cov ntaub ntawv tseem ceeb los txiav txim siab rau TKI kev kho mob lub sijhawm.

 

Dacomitinib

 

Qhov tshwm sim ntau ntawm Cov Tsis Mob Qog Cell Tsis Tau Ua Hluav Taws Xob tau yuam peb txoj kev xav txog kev kho mob, yuav ua li cas thiaj nrhiav tau cov txheej txheem tau zoo? Dacomitinib kev kho mob yuav raug pom zoo rau txhua tus. Tom ntej no, cia wb mus saib Dacomitinib:

 

Dacomitinib Tshuaj Xyuas

Dacomitinib, tsim raws li (2E) -N-16-4- (piperidin-1-yl) tab sis-2-enamide, yog qhov ncauj xaiv tau zoo quinazalone ib feem ntawm tiam thib ob tiam tyrosine kinase inhibitors uas tau pom los ntawm qhov tsis muaj kev cuam tshuam ntawm ATP sau ntawm phaum epidermal kev loj hlob tau receptor tsev neeg kinase puav. Dacomitinib yog ib qho tshuaj rau kev kho mob uas tsis yog-tus me-cov ntsws mob ntsws carcinoma (NSCLC). Nws yog qhov xaiv xaiv thiab tsis hloov pauv ntawm EGFR.

Dacomitinib tau tsim los ntawm Pfizer Inc thiab tau pom zoo los ntawm FDA rau lub Cuaj Hlis 27, 2018. Qee cov pov thawj hauv cov ntawv sau qhia tias muaj peev xwm kho tau dacomitinib hauv kev ua haujlwm ntawm epithelial ovarian mob cancer, txawm hais tias yuav tsum muaj kev tshawb nrhiav ntxiv.

Txog rau tam sim no, Dacomitinib hmoov (CAS:1110813-31-4) tuaj yeem muab los ntawm AASraw los ntawm Tuam Tshoj.

 

Dacomitinib Kev Siv Tes Ua ntawm kev nqis tes ua

Dacomitinib yog ib qho tsis nkag siab me me molecule inhibitor ntawm kev ua si ntawm tib neeg epidermal kev loj hlob yam receptor (EGFR) tsev neeg (EGFR / HER1, HER2, thiab HER4) tyrosine kinases. Nws ua tiav qhov tsis yooj yim ntawm kev txwv tsis pub dhau ntawm covalent tsevneeg mus rau cysteine ​​residues hauv catalytic puav ntawm HER receptors. Qhov sib xws ntawm dacomitinib tau pom tias muaj IC50 ntawm 6 nmol / L.

Tsev neeg ErbB lossis kev loj hlob nthuav dav (EGF) ua lub luag haujlwm hauv kev mob qog, metastasis, thiab kev kho mob los ntawm kev ua kom lub teeb liab xa cov teeb meem sib hloov xws li Ras-Raf-MAPK, PLCgamma-PKC-NFkB thiab PI3K / AKT los ntawm tyrosine Ib puag ncig 1% ntawm cov neeg mob nthuav qhia kev ua kom nrov nrov ntawm EGFR noob thiab 40% ntawm cov teeb meem nthuav tawm EGFRvIII kev hloov pauv uas sawv cev rau ib qho kev tshem tawm uas ua rau muaj kev ua haujlwm txuas ntxiv ntawm tyrosine kinase sau ntawm lub receptor.

 

Dacomitinib Siv

Dacomitinib raug pom zoo rau kev kho mob: Cov kab mob ntsws tsis mob ntsws hauv hlwb (NSCLC) uas muaj metastasized (kis mus rau lwm qhov ntawm lub cev). Nws yog siv ua kev kho mob ua ntej rau cov neeg mob uas lawv cov qog muaj qee cov EGFR hloov pauv.

Dacomitinib tseem tau kawm txog kev kho mob lwm yam mob qog noj ntshav.

 

Dacomitinib Sab Sij Huam

Cov khoom tseem ceeb uas yuav tsum nco ntsoov txog cov kev mob tshwm sim ntawm dacomitinib:

People Cov neeg feem coob yuav tsis pom tag nrho cov kev mob tshwm sim ntawm dacomitinib muaj nyob ntawm no.

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

Effects Dacomitinib phiv yuav zoo dua tom qab kho tiav.

Effects Dacomitinib phiv yuav tswj tau heev. Muaj ntau txoj kev xaiv kom txo qis lossis tiv thaiv kev phiv ntawm dacomitinib.

AASraw yog lub chaw tsim khoom ntawm Dacomitinib.

Thov nyem ntawm no rau cov ntaub ntawv hais: dawb paugHu rau peb

 

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

Rash Cov tawv nqaij ua pob

Nail Cov kab mob los yog pwm nyob ntsia hlau (paronychia)

Skin Qhuav ntawm daim tawv nqaij

▪ Tsawg albumin

Calcium Muaj cov calcium qis

Gluc Cov ntshav ntshav qabzib feem ntau

. Mob plab zawv

Outh Lub qhov ncauj tawm

Tsis qab los noj mov

Emia Kev Mob Ntshav (hemoglobin tsawg)

Count Muaj cov qe ntshav dawb tsawg

Liver Ua rau lub siab nce ntxiv

 

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

▪ Mob hauv siab

Om Ua Txhaum Cai

Plaub hau ploj

Khaus

Liab, liab, thiab mob ntawm lub xib teg ntawm txhais tes thiab / lossis txhais taw ntawm ko taw

Potassium Muaj cov poov tshuaj tsawg, magnesium thiab qib qis

Loss Poob phaus

▪ Xeev

Cem quav

▪ Limb mob

Pain Musculoskeletal mob

Tsis muaj zog / tsis muaj lub zog

Mob lossis mob ntawm lub qhov muag

In Ntau ntxiv cov ntshiab si creatinine

Hnoos, mob ntswg thiab cov tsos mob, ua pa nyuaj thiab ua pa ntawm txoj hlab pa

Tsis yog tag nrho cov kev mob tshwm sim muaj npe saud. Cov kev mob tshwm sim uas tsis tshua pom tshwm sim tshwm sim tsawg dua 10 feem pua ​​ntawm cov neeg mob - tsis muaj npe nyob ntawm no. Tab sis koj yuav tsum tau qhia koj tus kws kho mob txhua lub sij hawm yog koj muaj cov tsos mob txawv txawv.

 

Tsis yog-Lub cev ntsws mob ntsws siv rau Kev Kho Mob: Dacomitinib VS Gefitinib

Ntawm cov neeg mob EGFR-zoo, tsis yog – lub hlwb metastatic tsis – cov kab mob ntsws me me (NSCLC), thawj kab dacomitinib txhim kho kev vam meej-tsis muaj sia nyob (PFS) hla gefitinib, raws li ib qib 3 txoj kev tshawb fawb luam tawm hauv The Lancet Oncology.Dacomitinib

Thawj tiam EGFR – tyrosine kinase inhibitors (TKIs), suav nrog gefitinib, tau siv rau hauv thawj kab rau cov neeg mob EGFR-txoj hauj lwm muaj kab mob, uas muaj li ntawm 10% thiab 44% ntawm tag nrho cov ntsws adenocarcinomas. Cov kev tshawb fawb dhau los tsis tau txiav txim siab seb EGFR-TKIs thib ob tiam yog zoo dua rau cov thawj tiam thawj.

Rau qhov no qhib-daim ntawv lo, kev kawm randomized (ARCHER 1050; ClinicalTrials.gov Tus Cim: NCT01774721), uas cov sau phau ntawv sau tseg yog thawj theem 3 kawm tshawb fawb los piv rau EGFR-TKI tiam thib ob nrog EGFR-TKI hauv qhov kev teeb tsa no. , cov kws tshawb nrhiav cuv npe rau 452 tus neeg mob kom tau txais dacomitinib (227 tus neeg mob) lossis gefitinib (225 tus neeg mob). Cov neeg mob lub hlwb metastases tsis tsim nyog.

Ntawm qhov nruab nrab taug qab ntawm 22.1 lub hlis, theem nrab PFS yog 14.7 lub hlis rau dacomitinib vs 9.2 lub hlis rau gefitinib; pawg tsom xam tseem nyiam qhov dacomitinib. Kaum ob cov lus teb tiav tau muab sau cia hauv dacomitinib pawg vs 4 hauv pawg gefitinib. Lub hom phiaj ntawm cov lus teb tau yog, txawm li cas los xij, zoo sib xws (75% rau dacomitinib thiab 72% rau gefitinib; P = .4234).

Nees nkaum-cov neeg mob tau txais dacomitinib tau muaj kev kho mob hnyav-cuam tshuam rau qhov tshwm sim (AE); qhov no muaj tseeb ntawm 10 tus neeg mob tau txais gefitinib. Kev kho mob ntsig txog kev tuag tau qhia rau 2 tus neeg mob uas tau txais dacomitinib vs 1 rau gefitinib.

Cov sau phau ntawv xaus lus tias "kev kho mob dacomitinib yog qhov zoo dua gefitinib nrog rau kev hwm [PFS] thiab lub sijhawm teb rau cov kab mob kev kho mob thawj zaug ntawm cov neeg mob EGFR-kev hloov pauv-zoo NSCLC thiab yuav tsum raug txiav txim siab ua qhov kev xaiv kho mob tshiab rau cov neeg no. "

 

Yuav Ua Li Cas Dacomitinib Hmoov Hauv online?

Muaj ntau tus xa khoom / chaw tsim tshuaj paus ntawm dacomitinib hmoov hauv khw, nrhiav ib qho tseem ceeb heev rau txhua tus neeg uas xav tau cov khoom no sai. Thaum peb txiav txim siab yuav dacomitinib hmoov hauv kev ua lag luam, peb yuav tsum kawm paub ntau ntxiv txog nws, paub siv nws thiab nws yog cov txheej txheem ntawm kev ua, txhua yam kev pheej hmoo thaum peb noj dacomitinib hmoov…. Ntxiv rau, nqe thiab qhov zoo yuav tsum yog peb qhov kev txhawj xeeb ua ntej yuav nws.

Tom qab peb tau soj ntsuam cov ntaub ntawv los ntawm kev ua lag luam, piv rau ntau tus neeg muab khoom, AASraw zoo li kev xaiv zoo rau cov neeg uas xav yuav ntau dacomitinib hmoov, lawv cov khoom lag luam raug tswj hwm nruj me ntsis raws li cGMP, cov khoom zoo tuaj yeem taug qab txhua lub sijhawm thiab lawv tuaj yeem muab tag nrho cov ntawv xeem thaum koj xaj. Raws li rau dacomitinib hmoov cov nqi / nqi, nws yuav tsum muaj qhov tsim nyog, hauv kuv qhov muag. Vim tias kuv tau txais ntau tus nqi los ntawm cov neeg xa khoom sib txawv, piv nrog zoo, Kuv xav tias aasraw yuav tsis yog qhov kev xaiv tsis zoo.

 

reference

[1] Kobayashi Y, Fujino T, Nishino M, li al. EGFR T790M thiab C797S hloov pauv raws li cov txheej txheem ntawm kev xav tiv taus dacomitinib. J Thorac Oncol. Xyoo 2018; 13 (5): 727–731. doi: 10.1016 / j.jtho.2018.01.009.

[2] Kris MG, Camidge DR, Giaccone G, li al. Cuam tshuam HER2 aberrations raws li cov neeg tsav tsheb hauv cov qog nqaij hlav ntsws: theem II sim ntawm yias-HER tyrosine kinase inhibitor dacomitinib hauv cov neeg mob HER2-mutant lossis cov qog loj. Ann Oncol. 2015; 26 (7): 1421–1427. doi: 10.1093 / annonc / mdv383.

[3] Park K, Tan EH, O'Byrne K, li al. Afatinib piv rau gefitinib yog thawj kab kev kho mob ntawm cov neeg mob EGFR kev hloov pauv-kev mob tsis zoo-cov kab mob ntsws tsis loj-mob ntsws ntsws (LUX-ntsws 7): theem 2B, qhib-daim ntawv lo, sim tswj kev sim. Lancet Oncol. 2016; 17 (5): 577–589. doi: 10.1016 / S1470-2045 (16) 30033-X.

[4] Lacouture ME, Keefe DM, Sonis S, li al. Kev tshawb fawb theem II (ARCHER 1042) txhawm rau soj ntsuam kev kho mob dacomitinib-dermatologic thiab lub plab zom mov tsis zoo hauv cov qib siab uas tsis yog-me me ntawm lub ntsws. Ann Oncol. 2016; 27 (9): 1712–1718. doi: 10.1093 / annonc / mdw227.

[5] Reckamp KL, Giaccone G, Camidge DR, li al. Ib theem 2 kev sim ntawm dacomitinib (PF ‐ 00299804), lub qhov ncauj, qhov tsis tau rov qab pan HER (tib neeg epidermal kev loj hlob tau receptor) inhibitor, hauv cov neeg mob uas tsis yog – me me cell mob ntsws tom qab tsis ua haujlwm ntawm kev kho mob ua ntej thiab kev kho mob erlotinib. Mob Cancer. Xyoo 2014; 120 (8): 1145–1154. doi: 10.1002 / cncr.28561.

[6] Engelman JA, Zejnullahu K, Mitsudomi T, li al. MET amplification ua rau cov kab mob gefitinib tsis kam hauv ntsws mob ntsws los ntawm kev ua kom cov paib ERBB3 taw. Kev Tshawb Fawb. 2007; 316 (5827): 1039–1043. doi: 10.1126 / science.1141478.

[7] Liu X, Wang P, Zhang C, li al. Epidermal growth factor receptor (EGFR): Lub hnub qub nce siab zuj zus nyob rau lub sijhawm muaj cov tshuaj tua kab mob ntsws. Oncotarget. 2017; 8 (30): 50209–50220.

[8] Girard N. Kev ua kom tau zoo hauv EGFR kev hloov pauv-zoo NSCLC: qhov twg tus mob tyrosine kinase inhibitor thiab thaum twg? Yav Tom Ntej Oncol 2018.

[9] Inoue A, Kobayashi K, Maemondo M, li al. Thaum kawg qhov kev ua neej nyob tas li ntawm NEJ002, ib theem III kev sib piv piv cov gefitinib rau carboplatin (CBDCA) ntxiv rau paclitaxel (TXL) ua thawj kab kev kho mob rau cov tsis muaj mob ntsws ua mob ntsws (NSCLC) nrog EGFR kev hloov pauv. J Clin Oncol 2011; 29: 7519.

[10] Sequist LV, Yang JC, Yamamoto N, li al. Kev tshawb fawb nyob qib III ntawm afatinib lossis cisplatin ntxiv pemetrexed hauv cov neeg mob uas mob metastatic ntsws adenocarcinoma nrog rau kev hloov pauv EGFR. J Clin Oncol 2013; 31: 3327-34.

[11] Lin JJ, Cardarella S, Lydon CA, li al. Tsib Xyoo Ciaj sia nyob hauv EGFR-Mutant Metastatic Lub ntsws Adenocarcinoma Kho nrog EGFR-TKIs. J Thorac Oncol 2016; 11: 556-65.

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