AASraw tsim NMN thiab NRC hmoov hauv qhov ntau!

Lenvatinib

 

  1. Keeb Kwm Ntawm Lenvatinib
  2. Lenvatinib Yog Dab Tsi?
  3. Lenvatinib Mechanism ntawm kev ua
  4. Lenvatinib Siv Rau Dab Tsi?
  5. Kuv Yuav Pom Cov Kev Phiv Dab Tsi Thaum Koj Siv Lenvatinib?
  6. Lenvatinib Soj Ntsuam Kev Tshawb Nrhiav (FDA Pom Zoo)
  7. Kuv yuav khaws Lenvatinib nyob qhov twg?
  8. Cov Tshuaj Tiv Thaiv: Lenvatinib Mesylate (CAS: 857890-39-2)
  9. Peb tuaj yeem Yuav Lenvatinib online qhov twg?

 

Keeb Kwm Ntawm Lenvatinib

Ib ntu kev kuaj mob hauv cov neeg mob cancer ua rau xyoo 2006. [8] Lub sijhawm III kev sim mus kho cov neeg mob qog noj ntshav qog pib thaum lub Peb Hlis 2011.

Lenvatinib tau tso cai rau menyuam ntsuag kev kho mob rau kev kho mob ntawm ntau hom qog nqaij hlav cancer uas tsis teb rau radioiodine hauv Asmeskas thiab Nyij Pooj xyoo 2012 thiab hauv Europe xyoo 2013.

Thaum Lub Ob Hlis 2015, Asmeskas FDA tso cai lenvatinib rau kev kho mob ntawm kev nce qib, radioiodine refractory txawv cov thyroid mob cancer. Thaum lub Tsib Hlis 2015, European Tshuaj Tshuaj (EMA) tau pom zoo cov tshuaj rau tib qho ntsuas.

Thaum lub Tsib Hlis 2016, FDA tau pom zoo nws (hauv kev sib xyaw nrog everolimus) rau kev kho mob ntawm kev mob siab tshiab ntawm cov qog nqaij hlav hauv qab no ua ntej ib qho kev kho mob tawm tsam.

Thaum Lub Yim Hli 2018, FDA tau pom zoo lenvatinib rau kev kho mob thawj cov neeg uas muaj kev tiv thaiv kab mob siab tsis ua haujlwm zoo (HCC).

 

Yog Dab Tsi Lenvatinib?

Lenvatinib (CAS:417716-92-8) yog ib qhov receptor tyrosine kinase (RTK) inhibitor uas tiv thaiv kinase kev ua si ntawm vascular endothelial kev loj hlob tau (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), thiab VEGFR3 (FLT4). Lenvatinib tseem inhibits lwm RTK uas tau cuam tshuam hauv pathogenic angiogenesis, kev loj hlob ntawm qog, thiab mob qog nqaij hlav ntxiv nrog rau lawv cov kev ua haujlwm ntawm tes ua haujlwm, suav nrog fibroblast kev ua tau zoo (FGF) receptors FGFR1, 2, 3, thiab 4; lub platelet tau txais txiaj ntsig kev loj hlob receptor alpha (PDGFRα), KIT, thiab RET. Cov receptor tyrosine kinases (RTKs) nyob hauv lub cell membrane ua lub luag haujlwm tseem ceeb hauv kev ua haujlwm ntawm cov teeb liab sib kis tau koom nrog cov kev cai ntawm cov txheej txheem ntawm tes, xws li kev hloov ntawm tes, tsiv teb tsaws chaw, apoptosis thiab kev sib txawv, thiab nyob rau hauv pathogenic angiogenesis, kab mob qog mob hlav thiab mob qog noj ntshav. Hauv tshwj xeeb, VEGF tau pom tias yog tus tswj hwm tseem ceeb ntawm ob qho tib si physiologic thiab pathologic angiogenesis thiab kev nce ntawm VEGF yog txuam nrog kev tsis pom tseeb hauv ntau hom qog nqaij hlav.

Lenvatinib yog qhia rau kev kho mob ntawm cov neeg mob hauv zos rov qab los yog metastatic, nce zuj zus, radioactive iodine (RAI) -refractory sib txawv cov qog nqaij hlav cancer. Feem ntau ntawm cov neeg mob qog noj qab zib mob qog ntshav tau txais kev ua tau zoo heev nrog kev kho mob (98% 5 xyoo kom muaj sia nyob) nrog kev phais mob thiab kev kho tshuaj hormone. Txawm li cas los xij, rau cov neeg mob RAI-refractory lub qog mob cancer, cov kev kho mob tau txwv thiab qhov tshwm sim tsis zoo, uas ua rau muaj kev thawb rau kev txhim kho ntawm ntau cov hom phiaj kho mob xws li lenvatinib.

 

Lenvatinib Mechanism ntawm kev txiav txim

Lenvatinib yog ib qho receptor tyrosine kinase (RTK) inhibitor uas inhibits kinase kev ua si ntawm vascular endothelial kev loj hlob tau (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), thiab VEGFR3 (FLT4). Lenvatinib tseem inhibits lwm RTK uas tau cuam tshuam hauv pathogenic angiogenesis, kev loj hlob ntawm qog, thiab mob qog nqaij hlav ntxiv nrog rau lawv cov kev ua haujlwm ntawm tes ua haujlwm, suav nrog fibroblast kev ua tau zoo (FGF) receptors FGFR1, 2, 3, thiab 4; lub platelet tau txais txiaj ntsig kev loj hlob receptor alpha (PDGFRα), KIT, thiab RET.

 

Yog Dab Tsi Lenvatinib Siv Rau? 

Vat Lenvatinib yog siv los kho ib hom mob thyroid mob cancer uas tau rov qab los lossis tau kis mus rau lwm qhov ntawm lub cev thiab tsis tuaj yeem siv tshuaj kho hluav taws xob los ntawm iodine.

❷ Lenvatinib kuj tseem siv nrog everolimus (Afinitor, Zortress) los kho mob raum cell carcinoma (RCC, ib hom mob qog nqaij hlav uas pib hauv lub raum) hauv cov neeg uas yav tas los tau txais kev kho mob nrog lwm txoj kev siv tshuaj kho mob.

Vat Lenvatinib kuj tseem siv los kho mob hepatocellular carcinoma (HCC; ib hom mob qog nqaij hlav) uas kho tsis tau yam mob phais mob.

❹ Lenvatinib kuj tseem siv nrog pembrolizumab (Keytruda) txhawm rau kho qee yam mob cancer ntawm endometrium (txheej txheem ntawm lub tsev menyuam) uas tau kis mus rau lwm qhov ntawm lub cev lossis mob hnyav thaum lub sijhawm lossis tom qab siv tshuaj kho mob lossis tsis tuaj yeem kho nrog kev phais mob lossis hluav taws xob.

❺ Lenvatinib yog nyob rau hauv chav kawm ntawm cov tshuaj hu ua kinase inhibitors. Nws ua haujlwm los ntawm kev thaiv qhov kev txiav txim ntawm cov protein tsis txaus uas ua rau muaj hlwb hlav hlav. Qhov no yuav pab kom tsis txhob kis mob hlwb.

 

Yuav ua li cas Skev xav Entxuav kab mob May I Notice Wrau Koj Siv Lenvatinib?

Cov kev mob tshwm sim uas koj yuav tsum qhia rau koj tus kws kho mob lossis kws kho mob kom sai li sai tau:

Reactions ua xua raws li tawv nqaij ua pob khaus, khaus lossis ua pob khaus, o ntawm lub ntsej muag, daim di ncauj lossis tus nplaig

▪ cov teeb meem ua pa

▪ mob hauv siab lossis mob hauv siab

▪ kiv taub hau

Zoo nkaus li tsaus muag los sis taws taub hau, poob

▪ mob taub hau

. Ntshav siab

▪ qaug dab peg

▪ cov cim thiab cov tsos mob los ntshav xws li los ntshav lossis dub, quav ua kua; zis liab lossis tsaus-xim av; nti tawm ntshav lossis xim av uas zoo li kas fes kas fes; cov pob liab liab ntawm daim tawv nqaij; doog ntshav los ntshav tawm ntawm lub qhov muag, pos hniav, lossis qhov ntswg

▪ cov cim thiab cov tsos mob ntawm qhov hloov pauv lub plawv dhia lossis lub plawv dhia xws li mob hauv siab; kiv taub hau; lub plawv dhia nrawm lossis ceev; palpitations; xav tsaus muag lossis pom ntsej muag, ntog; teeb meem ua pa

▪ cov cim thiab cov tsos mob ntawm lub raum zoo li muaj teeb meem tso zis lossis hloov raws li cov zis

Cov cim thiab tsos mob ntawm daim siab raug mob xws li mob tsaus daj lossis daj; cov kev mob tshwm sim ib txwm muaj lossis cov tsos mob zoo li mob khaub thuas; lub teeb xim ua kom pom tseeb; tsis qab los noj mov; xeev siab; txoj cai mob plab sab saud; dog dig tsis muaj zog lossis nkees; daj daj ntawm qhov muag lossis tawv nqaij

Cov cim thiab cov tsos mob ntawm cov poov tshuaj qis xws li mob plab ntswj lossis mob leeg; mob hauv siab; kiv taub hau; xav tsaus muag lossis pom ntsej muag, ntog; palpitations; teeb meem ua pa; los yog lub plawv dhia ceev, lub plawv dhia tsis xwm yeem

Cov cim thiab cov tsos mob ntawm tus mob stroke zoo li hloov lub zeem muag; tsis meej pem; teeb meem hais lus los yog nkag siab; mob taub hau heev; doog ceev lossis tsis muaj zog ntawm lub ntsej muag, caj npab lossis ceg; teeb meem taug kev; kiv taub hau; poob ntawm kev tshuav lossis kev sib koom tes

Mob plab

▪ o ntawm ceg lossis pob taws o

Us ib txwm qaug zog lossis nkees

 

Cov kev mob tshwm sim uas feem ntau tsis xav tau kev kho mob (qhia rau koj tus kws kho mob lossis tus kws saib xyuas kev noj qab haus huv yog tias lawv txuas ntxiv lossis ua xeb):

. Raws plab

▪ Mob sib koom tes

▪ tsis qab los noj mov

▪ qhov ncauj tawm

▪ mob leeg

Xeev siab, ntuav

Loss qhov hnyav poob

Daim ntawv teev npe no yuav tsis piav txog txhua cov kev mob tshwm sim muaj. Hu koj tus kws kho mob rau cov lus qhia kho mob txog cov kev mob tshwm sim. Koj yuav qhia txog tej kev phiv rau FDA ntawm 1-800-FDA-1088.

 

Lenvatinib

 

Lenvatinib Soj ntsuam kev tshwm sim(Kev Pom Zoo FDA)

cov FDA pom zoo ntawm Lenvatinib tau ua raws li tus neeg siv ntau lub zog, sib tw, ob lub qhov muag dig muag, tshuaj xyuas cov teeb meem hauv 392 cov ncauj lus nrog hauv ib cheeb tsam lossis cov pa hluav taws xob hluav taws xob iodine-refractory sib txawv. thyroid mob cancer thiab hluav taws xob radiographic pov thawj ntawm kev mob tshwm sim tsis pub dhau 12 lub hlis ua ntej randomization, paub tseeb los ntawm kev txheeb xyuas radiologic ywj siab. Cov ncauj lus tau txais Lenvatinib 24 mg ib hnub ib zaug (n = 261) lossis placebo (n = 131) txog ntua mob. Cov txiaj ntsig kev tshawb pom pom tias Lenvatinib-kho cov ncauj lus nyob nruab nrab ntawm 18.3 lub hlis yam tsis muaj lawv cov kab mob kev vam meej (tsis muaj kev vam meej-ciaj sia taus), piv rau nruab nrab ntawm 3.6 lub hlis rau cov uas tau txais cov placebo. Tsis tas li ntawd, 65% ntawm cov kev kho mob nrog Lenvatinib pom muaj qhov txo cov qog loj, piv rau 2% ntawm cov neeg uas tau txais cov placebo.

 

Kuv yuav khaws Lenvatinib nyob qhov twg?

Khaws tsis ncav cuag ntawm cov menyuam yaus.

Cia li 20 txog 25 degrees C (68 thiab 77 degrees F). Pov tseg cov tshuaj tsis siv tom qab hnub tas sij hawm.

NCO TSEG: Cov ntawv no yog cov ntsiab lus xaus. Tej zaum nws yuav tsis npog tag nrho cov lus qhia tau. Yog tias koj muaj lus nug txog cov tshuaj no, nrog koj tus kws kho mob, kws muag tshuaj, lossis cov kws saib xyuas kev noj qab haus huv tham.

 

Lwm Yam Tshuaj: Lenvatinib Mesylate (CAS: 857890-39-2)

Lenvatinib mesylate (CAS: 857890-39-2) yog hluavtaws, qhov ncauj muaj cov tshuaj tiv thaiv kab mob vascular endothelial kev loj hlob yam receptor 2 (VEGFR2, tseem hu ua KDR / FLK-1) tyrosine kinase nrog kev muaj peev xwm ua antineoplastic. E7080 thaiv VEGFR2 kev ua haujlwm los ntawm VEGF, ua rau inhibition ntawm VEGF receptor teeb liab kis kab mob, qis vascular endothelial cell tsiv thiab loj hlob, thiab vascular endothelial cell apoptosis.

Lenvatinib mesylate yog cov methanesulfonate ntsev tau los ntawm cov tshuaj tiv thaiv ntawm lenvatinib nrog ib tus hniav puas sib npaug ntawm methanesulfonic acid. Ntau lub kinase inhibitor thiab tshuaj rau me nyuam ntsuag siv (vim nws cov mesylate ntsev) rau kev kho mob ntawm ntau yam mob qog uas tsis teb rau radioiodine. Nws muaj lub luag haujlwm ua haujlwm EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, fibroblast qhov zoo tshaj tawm receptor antagonist, tshuaj pleev ib ce, ib qho vascular endothelial kev loj hlob tau receptor antagonist thiab tus neeg sawv cev antineoplastic. Nws muaj cov lenvatinib (1+).

 

Lenvatinib mesylate raug pom zoo kom siv ib leeg lossis nrog lwm cov tshuaj los kho:

Cin Endometrial carcinoma uas yog nce thiab muaj ntau dua tom qab lwm cov kev kho mob. Nws siv nrog pembrolizumab hauv cov neeg mob uas mob cancer tsis yog microsatellite instability-siab (MSI-H) lossis mismatch kho tsis muaj peev xwm (dMMR) thiab tsis tuaj yeem raug kho nrog kev phais mob lossis hluav taws xob.

Pat Hepatocellular carcinoma (hom mob qog nqaij hlav cancer). Nws raug siv los ua kev kho thawj zaug hauv cov neeg mob uas tsis tuaj yeem raug tshem tawm los ntawm kev phais mob.

Cin Lub raum cell carcinoma (ib hom mob qog mob ntshav raum) uas muaj ntau dua tuaj. Nws yog siv nrog everolimus hauv cov neeg mob uas twb tau txais kev kho mob angiogenesis inhibitor kho.

♦ Mob qog noj ntshav mob qog rau qee tus neeg mob uas muaj mob ntau ntxiv, mob tshwm sim, lossis cov kab mob metastatic uas tsis teb rau kev kho mob nrog radioactive iodine.

Qhov kev siv tshuaj no tau pom zoo nyob rau hauv FDA's Accelerated Pom Zoo Cov Kev Pab. Raws li qhov xwm txheej ntawm kev pom zoo, kev sim lub siab (s) yuav tsum qhia tias lenvatinib mesylate muab kev pab soj ntsuam hauv cov neeg mob no. Lenvatinib mesylate tseem tau kawm txog kev kho mob lwm yam mob qog noj ntshav.

 

Peb Yuav Nyob Qhov Twg Lenvatinib hauv internet?

Muaj ntau tus xa khoom / chaw tsim tshuaj paus ntawm lenvatinib hmoov hauv khw, pom qhov tseeb tseem ceeb heev rau txhua tus neeg uas xav tau cov khoom no sai. Thaum peb txiav txim siab yuav lenvatinib hmoov hauv khw, peb yuav tsum kawm paub ntau ntxiv txog nws, paub siv nws thiab nws yog cov haujlwm ntawm kev coj ua, txhua yam kev pheej hmoo thaum peb noj lenvatinib 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 lenvatinib 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 lub lenvatinib hmoov cov nqi / nqi, nws yuav tsum 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.
Kom paub meej ntxiv, txais tos tham nrog AASraw!

 

reference

[1] H. Erdem, C. Gündogdu, thiab S. Tus thawj coj, "Sib txheeb ntawm E-cadherin, VEGF, COX-2 qhia rau cov kev ntsuas tshwm sim hauv papillary thyroid carcinoma," Kev Sim thiab Molecular Pathology, vol. 90, tsis muaj. 3, pp. 312–317, 2011.

[2] M. Yagi, S. Kato, Y. Kobayashi li al., "Xaiv inhibition ntawm platelet-derived kev loj hlob tau (PDGF) receptor autophosphorylation thiab PDGF-mediated cov xwm txheej ntawm tes los ntawm quinoline derivative," Kev Tshawb Nrhiav Cell, vol. 234, tsis muaj. 2, pp. 285–292, 1997.

[3] P. Soares, J. Lima, A. Preto et al., "Kev hloov caj ces hauv cov nqaij hlav sib txawv tsis zoo thiab tsis muaj qhov tsis txawv txav," Tamsis no. Genomics, vol. 12, tsis muaj. 8, pp. 609–617, 2011.

[4] MM Moura, BM Cavaco, V. Leite. RAS proto-oncogene hauv kev mob qog nqaij hlav cancer. Endocr Relat Cancer, 22 (5) (2015), pp. R235-R252.

[5] BR Haugen, SI Sherman Evolving txuas rau cov neeg mob uas muaj ntau yam mob qog noj ntshav qog ntshav siab. Endocr Rev, 34 (3) (2013), phab 439-455.

[6] M. Xing, D. Clark, H. Guan, li al. Kev soj ntsuam BRAF hloov pauv ntawm cov qog zoo-koob txhaj tshuaj me me rau txoj kev pheej hmoo txhawm rau mob qog nqaij hlav cancer papillary thyroid. J Clin Oncol, 27 (18) (2009), phab 2977-2982.

[7] SR Npoo, DJ Ogilvie, M. Dukes, li al. ZD6474 inhibits vascular endothelial kev loj hlob yam taw qhia, angiogenesis, thiab qog loj hlob raws li kev tswj hwm ntawm qhov ncauj. Cancer Res, 62 (16) (2002), pp. 4645-4655.

[8] SI Sherman, EEW Cohen, P. Schoffski, li al. Kev ua tau zoo ntawm cabozantinib (Cabo) hauv kev mob qog nqaij hlav cancer hauv lub qog nqaij hlav (MTC) nrog cov neeg mob RAS lossis RET hloov: Kev tshwm sim los ntawm kev kawm qib III [paub daws teeb meem]. J Clin Oncol, 31 (15 Cov Khoom Siv.) (2013) abstr 6000.

[9] SI Sherman, LJ Wirth, JP Droz, li al. Motesanib diphosphate nyob rau hauv kev sib txawv ntawm cov qog nqaij hlav ua rau mob qog. N Engl J Med, 359 (1) (2008), p. 31-42.

[10] K. Okamoto, K. Kodama, K. Takase, li al. Antitumor cov haujlwm ntawm cov phiajcim ntau-tyrosine kinase inhibitor lenvatinib (E7080) tawm tsam RET gene fusion-driven qog qauv. Cancer Lett, 340 (1) (2013), pp. 97-103.

[11] E. Cabanillas, M. Schlumberger, B. Jarzab, li al.A theem 2 sim ntawm lenvatinib (E7080) hauv kev nce qib, vam meej, xov tooj cua-refractory, txawv cov qog nqaij hlav thyroid: kev soj ntsuam cov txiaj ntsig thiab kev ntsuas biomarker Cancer, 121 (16) ( 2015), phab 2749-2756.

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