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Lenvatinib

 

  1. Imbali yeLenvatinib
  2. Yintoni uLenvatinib?
  3. Inkqubo yeLenvatinib yesenzo
  4. Isebenziselwa ntoni uLenvatinib?
  5. Zeziphi iziphumo ebezingalindelekanga endinokuthi ndiziqaphele xa usebenzisa iLenvatinib?
  6. Iziphumo zeKlinikhi (Ukwamkelwa kwe-FDA)
  7. Ndigcina phi uLenvatinib?
  8. Iziyobisi ezihambelanayo: I-Lenvatinib Mesylate (CAS: 857890-39-2)
  9. Singayithenga phi i-Lenvatinib kwi-Intanethi?

 

Imbali ye Lenvatinib

Isigaba sokuqala solingo lwezonyango kwizigulana ezinomhlaza lwenziwa ngo-2006. [8] Uvavanyo lwenqanaba lesithathu lokunyanga abaguli abanomhlaza we-thyroid luqale ngo-Matshi 2011.

U-Lenvatinib wanikwa inqanaba lokuba yinkedama kunyango lweentlobo ezahlukeneyo zomhlaza we-thyroid ongaphenduliyo kwi-radioiodine e-US nase Japan ngo-2012 nase-Europe ngo-2013.

NgoFebruwari 2015, i-US FDA yamkela i-lenvatinib kunyango lwenkqubela phambili, i-radioiodine refractory eyahlukileyo yomhlaza we-thyroid. Ngo-Meyi ka-2015, i-Arhente yamaYeza yaseYurophu (i-EMA) yavuma ukuba ichiza libonakalise okufanayo.

Ngomhla ka-Meyi ka-2016, i-FDA yayivuma (ngokudibanisa ne-everolimus) kunyango lwe-renal cell carcinoma elandela unyango lwaphambi kokulwa i-angiogenic.

Nge-Agasti ka-2018, i-FDA yamkela i-lenvatinib kunyango lomgca wokuqala wabantu abane-hepatocellular carcinoma (HCC) engabonakaliyo.

 

Yintoni i Lenvatinib?

I-Lenvatinib (i-CAS:417716-92-8Ngaba i-receptor tyrosine kinase (RTK) inhibitor ethintela imisebenzi ye-kinase ye-vascular endothelial factor factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), kunye ne-VEGFR3 (FLT4). I-Lenvatinib ikwathintela ezinye ii-RTK ezichaphazeleke kwi-pathogenic angiogenesis, ukukhula kwethumba, kunye nokuqhubela phambili komhlaza ukongeza kwimisebenzi yabo eqhelekileyo yeselula, kubandakanya ne-fibroblast growth factor (FGF) receptors FGFR1, 2, 3, kunye ne-4; iplatelet eyenzelwe ukukhula kwe-receptor alpha (PDGFRcy), KIT, kunye neRET. Ezi receptor tyrosine kinases (RTKs) ezikwi-membrane yeseli zidlala indima ephambili ekusetyenzisweni kweendlela zokudlulisa umqondiso obandakanyeka kulawulo oluqhelekileyo lweenkqubo zeselfowuni, ezinje ukwanda kweseli, ukufuduka, i-apoptosis kunye nokwahlulahlula, kunye ne-pathogenic angiogenesis, lymphogenesis, ukukhula kwethumba kunye nokuqhubela phambili komhlaza. Ngokukodwa, i-VEGF ichongiwe njengomlawuli obalulekileyo we-physiologic kunye ne-pathologic angiogenesis kunye nokunyusa ukubonakaliswa kwe-VEGF kunxulunyaniswa nesifo esingalunganga kwiintlobo ezininzi zomhlaza.

I-Lenvatinib ibonakalisiwe kunyango lwezigulana ezinokuphindaphindeka okanye imastastatic, inkqubela phambili, iodine enemitha (RAI) -umtsalane owahlukileyo umhlaza wedlala lengqula. Uninzi lwezigulana ezinomhlaza wedlala lengqula zinesifo esichanekileyo sokunyanga (i-98% yeminyaka emi-5 yokuphila) ebandakanya utyando kunye nonyango lwehomoni. Nangona kunjalo, kwizigulana ezinomhlaza we-RAI-refractory cancer, ukhetho lonyango lilinganiselwe kwaye isifo sisengalunganga, esikhokelela kuphembelelo lophuhliso lwezinto ekujolise kuzo ezinjengelenvatinib.

 

Lenvatinib Inkqubo yesenzo

I-Lenvatinib yi-receptor tyrosine kinase (RTK) isithintelo ethintela imisebenzi ye-kinase ye-vascular endothelial factor factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), kunye ne-VEGFR3 (FLT4). I-Lenvatinib ikwathintela ezinye ii-RTK ezichaphazeleke kwi-pathogenic angiogenesis, ukukhula kwethumba, kunye nokuqhubela phambili komhlaza ukongeza kwimisebenzi yabo eqhelekileyo yeselula, kubandakanya ne-fibroblast growth factor (FGF) receptors FGFR1, 2, 3, kunye ne-4; iplatelet eyenzelwe ukukhula kwe-receptor alpha (PDGFRcy), KIT, kunye neRET.

I-AASraw ngumenzi wobugcisa weLenvatinib.

Nceda ucofe apha ngolwazi locaphulo: Unxibelelwano nathi

 

Yintoni i Lenvatinib Isetyenziselwe? 

❶ ILenvatinib isetyenziselwa ukunyanga uhlobo oluthile lwe i-thyroid umhlaza obuyileyo okanye osasazeke kwamanye amalungu omzimba kwaye awunakunyangwa nge-iodine eqhumayo.

I-Lenvatinib ikwasetyenziswa kunye ne-everolimus (Afinitor, Zortress) ukunyanga i-renal cell carcinoma (i-RCC, uhlobo lomhlaza oqala kwizintso) kubantu ababekhe bafumana unyango ngamanye amayeza e-chemotherapy.

❸ ILenvatinib ikwasetyenziselwa ukunyanga i-hepatocellular carcinoma (HCC; uhlobo lomhlaza wesibindi) ongenakunyangwa ngoqhaqho.

❹ ILenvatinib ikwasetyenziswa kunye nepembrolizumab (Keytruda) ukunyanga uhlobo oluthile lwe umhlaza ye-endometrium (ulwelwesi lwesibeleko) ethe yanwenwela kwamanye amalungu omzimba okanye iba mandundu ngexesha okanye emva konyango ngamayeza e-chemotherapy okanye angenakuphathwa ngotyando okanye ngonyango lwemitha.

❺ U-Lenvatinib ukwiklasi yamayeza abizwa ngokuba yi-kinase inhibitors. Isebenza ngokuthintela isenzo seprotein engaqhelekanga ebonisa iiseli zomhlaza ukuba zande. Oku kunceda ukunqanda ukusasazeka kweeseli zomhlaza.

 

Intoni SIDE Eiimpembelelo May mna Notice Winkukhu Usebenzisa Lenvatinib?

Iziphumo ebezingalindelekanga ekufuneka uxele kugqirha wakho okanye kwezonyango ngokukhawuleza okukhulu:

▪ Ukungadibani nezinto ezifana nokudumba kolusu, ukurhawuzelela okanye imihlathi, ukudumba kobuso, imilebe nolwimi

▪ iingxaki zokuphefumla

▪ iintlungu esifubeni okanye ukubetha kwentliziyo

▪ isiyezi

▪ Ukuziva udiniwe okanye unentloko elula, uyawa

▪ intloko ebuhlungu

▪ uxinzelelo lwegazi

▪ ukuxhuzula

▪ Iimpawu neempawu zokopha ezifana nokuba negazi okanye mnyama, ilindle; umchamo obomvu okanye mnyama-mdaka; ukutshiza igazi okanye izinto ezimdaka ezibonakala ngathi zizezekofu; amabala abomvu eluswini; ukugruzuka okungaqhelekanga okanye ukopha kwiliso, kwiintsini, okanye empumlweni

▪ Iimpawu kunye neempawu zotshintsho olunobungozi ekubetheni kwentliziyo okanye kwisingqi senhliziyo njengentlungu yesifuba; isiyezi; ukukhawuleza kwentliziyo okanye okungaqhelekanga; ukubetha kwentliziyo; ukuziva udiniwe okanye unentloko elula, ukuwa; iingxaki zokuphefumla

▪ Iimpawu zokulimala kwezintso njengengxaki yokudlula kumchamo okanye ukutshintsha komchamo

▪ iimpawu zokulimala kwesibindi njengomchamo omnyama otyheli okanye omdaka; ukugula ngokubanzi okanye iimpawu ezifana nomkhuhlane; ilindle elikhanyayo; ukuphelelwa ngumdla wokutya; isicaphucaphu; iintlungu zangaphezulu esiswini; ngokungaqhelekanga buthathaka okanye udiniwe; mthubi wamehlo okanye ulusu

▪ Iimpawu kunye neempawu ze-potassium ephantsi enjengezihlunu zemithambo okanye iintlungu zemisipha; iintlungu zesifuba; isiyezi; ukuziva udiniwe okanye unentloko elula, ukuwa; ukubetha kwentliziyo; iingxaki zokuphefumla; okanye ngokukhawuleza, ukubetha kwentliziyo okungaqhelekanga

▪ Iimpawu neempawu zestroke njengotshintsho kumbono; ukudideka; ukuthetha kakubi okanye ukuqonda; intloko ebuhlungu; ukuphazamiseka ngesiquphe okanye ubuthathaka bobuso, ingalo okanye umlenze; ukuhambahamba nzima; isiyezi; ukulahleka kwemali eseleyo okanye yokulungelelanisa

▪ Ubuhlungu esiswini

▪ ukudumba kwemilenze okanye amaqatha

▪ Babuthathaka okanye badiniwe ngokungaqhelekanga

 

Iziphumo ebezingalindelekanga ezingafuneki qho kwezonyango (xela ugqirha wakho okanye ukhathalelo lwempilo ukuba bayaqhubeka okanye bayakhathaza):

▪ urhudo

▪ iintlungu ezidibeneyo

Ukuphelelwa ngumdla wokutya

Izilonda zomlomo

▪ Intlungu yezihlunu

▪ isicaphucaphu, ukugabha

▪ ukunciphisa umzimba

Olu luhlu alunakuchaza zonke iziphumo ebezingalindelekanga ezinokubakho. Shayela ugqirha wakho malunga neengcebiso. Unokuxela iziphumo ebezingalindelekanga kwi-FDA ngo-1-800-FDA-1088.

 

Lenvatinib

 

Lenvatinib Iziphumo zonyango(Ukuvunywa kwe-FDA)

The Ukuvunywa kwe-FDA yeLenvatinib yayisekwe kwimulticenter, ngokungacwangciswanga, kabini-iimfama, ulingo olulawulwa yi-placebo kwizifundo ezingama-392 ezinendawo ephindaphindayo okanye ye-metastatic radioactive iodine-refractory eyahlukileyo i-thyroid umhlaza kunye nobungqina be-radiographic yokuqhubela phambili kwesifo ngaphakathi kweenyanga ezili-12 ngaphambi kokungahleliwe, kuqinisekiswe luphononongo oluzimeleyo lwe-radiologic. Izifundo zafumana i-Lenvatinib 24 mg kanye yonke imihla (n = 261) okanye i-placebo (n = 131) de isifo sinyuke. Iziphumo zophando zibonise ukuba izifundo eziphathwe ngeLenvatinib zihlala ixesha eliphakathi kwiinyanga ezili-18.3 ngaphandle kwesifo esiqhubela phambili (ukusinda okungahambeli phambili), xa kuthelekiswa nomyinge weenyanga ezi-3.6 zezifundo ezifumene i-placebo. Ukongeza, i-65% yezifundo eziphathwe nge-Lenvatinib yabona ukuncitshiswa kwesayizi yethumba, xa kuthelekiswa ne-2% yezifundo ezifumene indawo ye-placebo.

I-AASraw ngumenzi wobugcisa weLenvatinib.

Nceda ucofe apha ngolwazi locaphulo: Unxibelelwano nathi

 

Ndigcina phi uLenvatinib?

Gcina kude nokufikelela kwabantwana.

Gcina phakathi kwama-20 ukuya kuma-25 degrees C (68 ukuya kuma-77 degrees F). Lahla naliphi na iyeza elingasetyenziswanga emva komhla wokuphelelwa.

QAPHELA: Eli phepha sisishwankathelo. Isenokungagubungeli lonke ulwazi olunokwenzeka. Ukuba unemibuzo malunga neli yeza, thetha nogqirha wakho, usokhemisti, okanye umboneleli wezempilo.

 

Iziyobisi ezihambelanayo: Lenvatinib MI-esylate (i-CAS: 857890-39-2)

I-Lenvatinib mesylate (i-CAS: 857890-39-2) yinto yokwenziwa, efumanekayo ngomlomo ye-vascular endothelial grow factor receptor 2 (VEGFR2, ekwabizwa ngokuba yi-KDR / FLK-1) tyrosine kinase enokubakho kwe-antineoplastic activity. I-E7080 ibhloka i-VEGFR2 isebenze nge-VEGF, ekhokelela kuthintelo lwendlela yokuhambisa isiginali ye-VEGF, yehlise ukufuduka kweseli ye-vasot endothelial kunye nokwanda, kunye ne-vasop endoshelial cell apoptosis.

Lenvatinib mesylate yityuwa ye-methanesulfonate efunyenwe ngokuphendula kwe-lenvatinib ngomlinganiso omnye we-methanesulfonic acid. I-multi-kinase inhibitor kunye neziyobisi eziyinkedama ezisetyenzisiweyo (njengetyuwa ye-mesylate) kunyango lweentlobo ezahlukeneyo zomhlaza we-thyroid ongaphenduliyo kwi-radioiodine. Inendima njenge-EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, i-fibroblast yokukhula kwe-receptor antagonist, ichiza lenkedama, i-vascular endothelial growth factor receptor antagonist kunye ne-antineoplastic agent. Iqulethe i-lenvatinib (1+).

 

I-Lenvatinib mesylate ivunyiwe ukuba isetyenziswe yodwa okanye nezinye iziyobisi ukunyanga:

I-Endometrial carcinoma eqhubekile kwaye yaya isiba mandundu emva kolunye unyango. Isetyenziswa nge-pembrolizumab kwizigulana ezinomhlaza ongekho ukungazinzi okuphezulu (MSI-H) okanye ukungalungisi okungalunganga kokulungiswa (dMMR) kwaye ayinakunyangwa ngoqhaqho okanye ngonyango lwemitha.

♦ I-Hepatocellular carcinoma (uhlobo lomhlaza wesibindi). Isetyenziswa njengonyango lodidi lokuqala kwizigulana esingenakususwa sisifo ngotyando.

♦ I-Renal cell carcinoma (uhlobo lomhlaza wezintso) oqhubele phambili. Isetyenziselwa i-everolimus kwizigulana esele zifumene unyango lwe-angiogenesis inhibitor.

Cancer Umhlaza wedlala lengqula kwizigulana ezithile ezinesifo esiqhubela phambili, esiphindaphindayo, okanye se-metastatic esingaphenduliyo kunyango nge-iodine ene-radioactive.

Olu setyenziso luvunyiwe phantsi kweNkqubo yokuVunywa okuKhawulezileyo ye-FDA. Njengombandela wokwamkelwa, izilingo eziqinisekisayo kufuneka zibonise ukuba i-lenvatinib mesylate ibonelela ngoncedo lweklinikhi kwezi zigulana. I-Lenvatinib mesylate iyafundwa kunyango lwezinye iintlobo zomhlaza.

 

Singathenga phi Lenvatinib Kwi-intanethi?

Baninzi abathengisi / abavelisi be-lenvatinib powder kwimarike, ukufumana eyinyani kubaluleke kakhulu kubo bonke abantu abayifunayo ngokukhawuleza le mveliso. Xa sithatha isigqibo sokuthenga i-lenvatinib powder kwimarike, kufuneka sifunde ulwazi malunga nayo, siyazi ukuba siyisebenzisa njani kunye nendlela yokusebenza kwayo, nayiphi na imingcipheko xa sithatha i-lenvatinib powder…. Ukongeza, ixabiso kunye nomgangatho kufuneka ibe yinkxalabo yethu ngaphambi kokuba uyithenge.

Emva kokuba sihlolisise ii-datas ezivela kwiimarike, xa kuthelekiswa nabanikezeli abaninzi, i-AASraw ibukeka kakuhle kubantu abafuna ukuthenga ezininzi lenvatinib powder, imveliso yabo yayilawulwa ngokungqongqo phantsi kwemeko ye-cGMP, umgangatho unokulandelwa nangaliphi na ixesha kwaye banokubonelela ngazo zonke iingxelo zovavanyo xa uzi-odola. Ngokubhekisele kwi-lenvatinib powder iindleko / ixabiso, kufanelekile, emehlweni am. Ngenxa yokuba ndinamaxabiso amaninzi kubathengisi abohlukeneyo, xa kuthelekiswa nomgangatho, ndicinga ukuba i-aasraw ayizukukhetha kakubi.
Ngolwazi oluthe kratya, wamkelekile ukuba uthethe ne-AASraw!

 

isingqiniso

[1] H. Erdem, C. Gündogdu, kunye no-S. Üipal, "Correlation of E-cadherin, VEGF, COX-2 expression to prognostic parameters in papillary thyroid carcinoma," Uvavanyo kunye neMolekyuli yePathology, vol. 90, hayi. 3, iphepha 312-317, 2011.

[2] M. Yagi, S. Kato, Y. Kobayashi et al., "Ukukhetha inhibition yeplatelet-derived factor factor (PDGF) receptor autophosphorylation kunye ne-PDGF-Mediated iminyhadala yeselula sisiphumo sequinoline," Uvavanyo lweSeli yovavanyo, ivol. 234, hayi. 2, iphepha 285–292, 1997.

[3] P. Soares, J. Lima, A. Preto et al., "Utshintsho lwemfuzo kwizinto ezingafani kakuhle nezingafaniyo ze-carcinomas ye-thyroid," ngoku. IGenomics, ivol. 12, hayi. 8, iphepha 609-617, 2011.

[4] MM Moura, BM Cavaco, V. Leite. I-RAS proto-oncogene kwi-medullary thyroid carcinoma. Umhlaza we-Endocr Relat Cancer, 22 (5) (2015), iphe. R235-R252.

[5] I-BR Haugen, i-SI Sherman eguqukayo isondela kwizigulana ezinomhlaza ophambili owahlukileyo we-thyroid. U-Endocr Rev, 34 (3) (2013), iphe. 439-455.

[6] M. Xing, D. Clark, H. Guan, okqhubekayo. Uvavanyo lokutshintsha kwe-BRAF ye-thyroid-inaliti yokufuna inaliti ye-biopsy yesampulu yokufumana umngcipheko kumngcipheko we-papillary cancer yomhlaza. J Clin Oncol, 27 (18) (2009), iphe. 2977-2982.

[7] I-SR Wedge, u-DJ Ogilvie, M. Dukes, okqhubekayo. I-ZD6474 inqanda ukukhula kwe-vascular endothelial factor signaling, angiogenesis, kunye nokukhula kwetyumpa emva kolawulo lomlomo. ICancer Res, 62 (16) (2002), iphe. 4645-4655.

[8] SI Sherman, EEW Cohen, P. Schoffski, okqhubekayo. Ukusebenza kwe-cabozantinib (Cabo) kwizigulana ezinesifo somhlaza we-thyroid (MTC) ezine-RAS okanye i-RET mutations: Iziphumo ezivela kufundo lwesigaba III [abstract]. J Clin Oncol, 31 (15 Suppl.) (2013) abstr 6000.

[9] SI uSherman, uLJ Wirth, uJP Droz, et al. I-Motesanib diphosphate ekuqhubekeni kokwahlulahlula umhlaza wedlala lengqula. N Engl J Med, 359 (1) (2008), iphepha 31-42.

[10] K. Okamoto, K. Kodama, K. Takase, okqhubekayo. Imisebenzi ye-Antitumor ye-multi-tyrosine kinase inhibitor lenvatinib (E7080) ejolise kwimodeli ye-RET ye-gene eqhutywa yimfu. Umhlaza Lett, 340 (1) (2013), iphe. 97-103.

[11] E. Cabanillas, M. Schlumberger, B. Jarzab, et al. Isigaba sesi-2 sokuvavanywa kwe-lenvatinib (i-E7080) kwi-advanced, progressive, radioiodine-refractory, eyahlukileyo yomhlaza we-thyroid: iziphumo zeklinikhi kunye novavanyo lwe-biomarker Cancer, 121 (16) ( 2015), iphepha 2749-2756.

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