Tlhahisoleseling ea Tataiso ho Lenvatinib Bakeng sa Kankere - AASraw
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Lenvatinib

 

  1. Nalane ea Lenvatinib
  2. Lenvatinib ke eng?
  3. Mokhoa oa ts'ebetso oa Lenvatinib
  4. Lenvatinib e Sebelisetsoa'ng?
  5. Ke Litlamorao Life Tseo Nka li Elelloang Ha U Sebelisa Lenvatinib?
  6. Liphetho tsa bongaka tsa Lenvatinib (Kamohelo ea FDA)
  7. Ke lokela ho boloka Lenvatinib kae?
  8. Lithethefatsi tse amanang: Lenvatinib Mesylate (CAS: 857890-39-2)
  9. Re ka reka Lenvatinib inthaneteng hokae?

 

Nalane ea Lenvatinib

Teko ea bongaka ea mokhahlelo oa I oa bakuli ba mofetše e entsoe ka 2006. [8] Teko ea karolo ea III e alafang bakuli ba mofets'e ba qoqotho e qalile ka Hlakubele 2011.

Lenvatinib o fuoe boemo ba khutsana bakeng sa kalafo ea mefuta e fapaneng ea mofets'e oa qoqotho o sa arabeleng radioiodine ho la US le Japane ka 2012 le Europe ka 2013.

Ka Pherekhong 2015, US FDA e ile ea amohela lenvatinib bakeng sa kalafo ea mofets'e oa "cancer" o tsoelang pele, oa radioiodine. Ka Mots'eanong 2015, Setsi sa Meriana sa Europe (EMA) se amohetse setlhare bakeng sa sesupo se tšoanang.

Ka May 2016, FDA e ile ea e amohela (hammoho le everolimus) bakeng sa kalafo ea renal cell carcinoma kamora 'kalafo e le' ngoe ea anti-angiogenic.

Ka Phato 2018, FDA e amohetse lenvatinib bakeng sa kalafo ea mohala oa pele oa batho ba nang le lefu la hepatocellular carcinoma (HCC) le sa bonahaleng.

 

Ke eng Lenvatinib?

Lenvatinib (CAS:417716-92-8) ke receptor tyrosine kinase (RTK) inhibitor e thibelang mesebetsi ea kinase ea li-vascular endothelial grow factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), le VEGFR3 (FLT4). Lenvatinib e boetse e thibela li-RTK tse ling tse bileng le ts'oaetso ho pathogenic angiogenesis, kholo ea hlahala, le tsoelo-pele ea mofets'e ho kenyelletsa mesebetsi ea bona e tloaelehileng ea lisele, ho kenyeletsoa li-receptor tsa fibroblast factor (FGF) FGFR1, 2, 3, le 4; platelet e tsoang ho factor factor alpha (PDGFRcy), KIT le RET. Li-receptor tyrosine kinases (RTKs) tse liseleng tsa sele li bapala karolo ea mantlha ts'ebetsong ea litsela tsa phetisetso ea matšoao tse amehang taolong e tloaelehileng ea lits'ebetso tsa lisele, joalo ka ho ata ha sele, ho falla, apoptosis le phapang, le ho angiogenesis ea pathogenic, lymphogenesis, kholo ea hlahala le kholo ea mofets'e. Haholo-holo, VEGF e fumanoe e le molaoli oa bohlokoa oa li-angiogenesis tsa physiologic le pathologic mme polelo e eketsehang ea VEGF e amahanngoa le seoa se seng sa mefuta e mengata ea mofetše.

Lenvatinib e bonts'oa kalafo ea bakuli ba nang le kankere ea qoqotho e khethollang kankere ea qoqotho e iphetang kapa metastatic, progressive, radioactive iodine (RAI). Bakuli ba bangata ba nang le mofetše oa qoqotho ba na le tšoaetso e ntle haholo ka kalafo (sekhahla sa ho pholoha sa lilemo tse 98%) se amang ho buuoa le kalafo ea lihomone. Leha ho le joalo, bakeng sa bakuli ba nang le mofetše oa qoqotho oa RAI-refractory, likhetho tsa kalafo li na le moeli mme ponelopele e mpe, e lebisang ho sutumetsong ea nts'etsopele ea liphekolo tse shebiloeng joalo ka lenvatinib

 

Lenvatinib Mokhoa oa ketso

Lenvatinib ke receptor tyrosine kinase (RTK) sesitisa e thibelang mesebetsi ea kinase ea li-vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), le VEGFR3 (FLT4). Lenvatinib e boetse e thibela li-RTK tse ling tse bileng le ts'oaetso ho pathogenic angiogenesis, kholo ea hlahala, le tsoelo-pele ea mofets'e ho kenyelletsa mesebetsi ea bona e tloaelehileng ea lisele, ho kenyeletsoa li-receptor tsa fibroblast factor (FGF) FGFR1, 2, 3, le 4; platelet e tsoang ho factor factor alpha (PDGFRcy), KIT le RET.

AASraw ke moetsi ea hloahloa oa Lenvatinib.

Ka kopo tlanya mona bakeng sa tlhaiso-leseling e qotsitsoeng: Lethathamo la rona

 

Ke eng Lenvatinib Sebelisetsoa? 

❶ Lenvatinib e sebelisetsoa ho alafa mofuta o itseng oa thyroid Kankere e khutlileng kapa e nametseng likarolong tse ling tsa 'mele' me e ke ke ea phekoloa ka iodine e nang le mahlaseli a kotsi.

Lenvatinib e boetse e sebelisoa hammoho le everolimus (Afinitor, Zortress) ho phekola renal cell carcinoma (RCC, mofuta oa mofets'e o qalang liphio) ho batho ba neng ba kile ba fumana kalafo ka moriana o mong oa chemotherapy.

Lenvatinib le eona e sebelisetsoa ho alafa hepatocellular carcinoma (HCC; mofuta oa mofetše oa sebete) o ke keng oa phekoloa ka ho buuoa.

Lenvatinib e boetse e sebelisoa hammoho le pembrolizumab (Keytruda) ho phekola mofuta o itseng oa tsoaroa ke kankere ea endometrium (lesela la popelo) le hasaneng likarolong tse ling tsa 'mele kapa le mpefetse nakong ea kalafo kapa kamora' kalafo ka meriana ea chemotherapy kapa e ke keng ea phekoloa ka ho buuoa kapa kalafo ea radiation.

Lenvatinib o sehlopheng sa meriana e bitsoang kinase inhibitors. E sebetsa ka ho thibela ts'ebetso ea protheine e sa tloaelehang e bonts'ang lisele tsa mofetše ho ngatafala. Sena se thusa ho emisa ho ata ha lisele tsa mofetše.

 

Eng Sho joalo Emafu Mke nna Notice When U Sebelisa Lenvatinib?

Litla-morao tseo u lokelang ho li tlalehela ngaka kapa setsebi sa tlhokomelo ea bophelo kapele kamoo ho ka khonehang:

▪ Ho itšoara hampe joalo ka lekhopho la letlalo, ho hlohlona kapa ho qhoma, ho ruruha ha sefahleho, molomo kapa leleme

▪ mathata a ho hema

▪ Ho opeloa ke sefuba kapa ho opa

▪ ho tsekela

▪ ho ikutloa eka u akhehile kapa u le hlooho e bobebe, oa oa

▪ ho tšoaroa ke hlooho

▪ khatello e phahameng ea mali

▪ ho oa

▪ matšoao a ho tsoa mali joalo ka mali a mali kapa a batsho, litulo; moroto o mokgubedu kapa o sootho ka botsho; ho hlatsa mali kapa ntho e sootho e shebahalang joalo ka mabala a kofi; matheba a khubelu letlalong; ho longoa kapa ho tsoa mali ho sa tloaelehang ka leihlong, mareneneng kapa linkong

▪ matšoao a phetoho e kotsi ea ho otla ha pelo kapa morethetho oa pelo joalo ka bohloko ba sefuba; ho tsekela; ho otla ha pelo kapele kapa ka tsela e sa tloaelehang; palpitations; ho ikutloa ke akhehile kapa ke hlooho e bobebe, oa wa; mathata a ho hema

▪ matšoao a kotsi ea liphio joalo ka bothata ba ho feta moroto kapa ho fetoha ha bongata ba moroto

▪ matšoao a ho lemala ha sebete joaloka moroto o mosehla o mosehla kapa o sootho; ho kula ka kakaretso kapa matšoao a kang a sefuba; litulo tse khanyang; ho hloka takatso ea lijo; ho nyekeloa ke pelo; bohloko bo ka holimo ba mpa; fokola kapa ho khathala ka tsela e sa tloaelehang; bosehla ba mahlo kapa ba letlalo

▪ matšoao a potasiamo e tlase joalo ka mesifa ea mesifa kapa bohloko ba mesifa; bohloko ba sefuba; ho tsekela; ho ikutloa ke akhehile kapa ke hlooho e bobebe, oa wa; palpitations; mathata a ho hema; kapa ho otla ha pelo ka lebelo le sa tloaelehang

▪ lipontšo tsa seterouku joaloka liphetoho ponong; pherekano; bothata ba ho bua kapa kutloisiso; hlooho e bohloko; ho thatafala ka tšohanyetso kapa ho fokola ha sefahleho, letsoho kapa leoto; ho tsamaea ka thata; ho tsekela; tahlehelo ya tekano kapa kgokahano

▪ bohloko ba mpeng

▪ ho ruruha ha maoto kapa maqaqailana

▪ A fokola ka tsela e sa tloaelehang kapa a khathetse

 

Litla-morao tseo hangata li sa hlokeng tlhokomelo ea bongaka (tlaleha ngaka ea hau kapa setsebi sa tlhokomelo ea bophelo haeba li tsoela pele kapa li khathatsa):

▪ letšollo

▪ bohloko bo kopantsoeng

▪ ho felloa ke takatso ea lijo

▪ liso tsa molomo

▪ bohloko ba mesifa

▪ ho nyekeloa ke pelo, ho hlatsa

▪ ho theola boima ba 'mele

Lethathamo lena le kanna la se hlalose litlamorao tsohle tse ka bang teng. Bitsa ngaka ea hau bakeng sa likeletso tsa bongaka ka litla-morao. U ka tlaleha litla-morao ho FDA ho 1-800-FDA-1088.

 

Lenvatinib

 

Lenvatinib Liphello tsa Bongaka(Kamohelo ea FDA)

The Tumello ea FDA ea Lenvatinib e ne e ipapisitse le teko e laoloang ea "placebo" e nang le li-multicenter, tse sa sebetseng, tse foufetseng habeli, tse laoloang ka "placebo" lithutong tse 392 tse nang le iodine-refractory e hlahisang methapo ea radio ea lehae. thyroid mofets'e le bopaki ba radiographic ba tsoelo-pele ea mafu nakong ea likhoeli tse 12 pele ho tatellano, e netefalitsoeng ke tlhahlobo e ikemetseng ea radiologic. Lihlooho li ile tsa amohela Lenvatinib 24 mg hang ka letsatsi (n = 261) kapa placebo (n = 131) ho fihlela lefu le ntse le eketseha. Liphetho tsa boithuto li bonts'itse bafo ba phekoloang ke Lenvatinib ba phetse nako e telele ea likhoeli tse 18.3 ntle le lefu la bona le ntse le tsoela pele (ho phela ntle le tsoelo-pele), ha ho bapisoa le likhoeli tse 3.6 bakeng sa bafo ba fumaneng placebo. Ntle le moo, 65% ea lithuto tse alafiloeng le Lenvatinib li bone phokotso ea boholo ba hlahala, ha e bapisoa le 2% ea lithuto tse fumaneng placebo.

AASraw ke moetsi ea hloahloa oa Lenvatinib.

Ka kopo tlanya mona bakeng sa tlhaiso-leseling e qotsitsoeng: Lethathamo la rona

 

Ke lokela ho boloka Lenvatinib kae?

Tlohela bana ho hang.

Boloka lipakeng tsa 20 le 25 degrees C (68 le 77 degrees F). Lahla moriana ofe kapa ofe o neng o sa sebelisoe kamora nako ea ho felloa ke nako.

TLHOKOMELISO: Leqephe lena ke kakaretso. E kanna ea se koahele tlhaiso-leseling eohle e ka bang teng. Haeba u na le lipotso ka meriana ena, buisana le ngaka ea hau, setsebi sa meriana kapa mofani oa tlhokomelo ea bophelo.

 

Lithethefatsi tse amanang: Lenvatinib Mesylate (CAS: 857890-39-2)

Lenvatinib mesylate (CAS: 857890-39-2) ke synthetic, e fumanehang ka molomo inhibitor ea vascular endothelial grow factor receptor 2 (VEGFR2, e tsejoang hape e le KDR / FLK-1) tyrosine kinase e nang le tšebetso ea antineoplastic. E7080 e thibela VEGFR2 ts'ebetso ea VEGF, e hlahisang tšitiso ea tsela ea phetisetso ea li-receptor tsa VEGF, e fokotsitse phallo ea lisele tsa methapo ea methapo le ho ata, le vasot endothelial cell apoptosis.

Lenvatinib mesylate ke letsoai la methanesulfonate le fumanoang ka karabelo ea lenvatinib e nang le molar e lekanang le methanesulfonic acid. Sesebelisoa sa li-kinase inhibitor le khutsana se sebelisitsoeng (joalo ka letsoai la mesylate) bakeng sa kalafo ea mefuta e fapaneng ea mofets'e oa qoqotho o sa arabeleng radioiodine. E na le karolo joalo ka EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, fibroblast growth factor receptor antagonist, lithethefatsi tsa khutsana, vascular endothelial growth factor receptor antagonist le antineoplastic agent. E na le lenvatinib (1+).

 

Lenvatinib mesylate e lumelloa ho sebelisoa e le mong kapa le lithethefatsi tse ling ho alafa:

♦ Endometrial carcinoma e tsoetseng pele le ho mpefala kamora mekhoa e meng ea kalafo. E sebelisoa le pembrolizumab ho bakuli bao kankere ea bona e seng microsatellite ho se tsitse-hodimo (MSI-H) kapa ho se lokisoe hantle ha ho lokisoa (dMMR) mme e ke ke ea alafshoa ka kalafo ea bongaka kapa kalafo ea radiation.

♦ Hepatocellular carcinoma (mofuta oa mofetše oa sebete). E sebelisoa e le kalafo ea mohala oa pele ho bakuli bao mafu a bona a ke keng a tlosoa ka ho buuoa.

Al Renal cell carcinoma (mofuta oa mofetše oa liphio) o tsoetseng pele. E sebelisoa le everolimus ho bakuli ba seng ba ntse ba fumane kalafo ea angiogenesis inhibitor.

Kankere ea qoqotho ho bakuli ba bang ba nang le lefu le tsoelang pele, le iphetang kapa metastatic le sa arabeleng kalafo ka iodine ea radioactive.

Ts'ebeliso ena e amoheloa tlasa Lenaneo la Kamohelo e Potlakileng ea FDA. E le boemo ba tumello, liteko tse netefatsang li tlameha ho bonts'a hore lenvatinib mesylate e fana ka molemo oa bongaka ho bakuli bana. Lenvatinib mesylate le eona e ntse e ithutoa kalafong ea mefuta e meng ea mofets'e.

 

Re Ka Reka Hokae Lenvatinib Inthaneteng?

Ho na le barekisi / bahlahisi ba bangata ba phofo ea lenvatinib 'marakeng, ho e fumana e le' nete ho bohlokoa haholo ho batho bohle ba hlokang sehlahisoa sena ka potlako. Ha re nka qeto ea ho reka phofo ea lenvatinib 'marakeng, re hloka ho ithuta leseli le eketsehileng ka eona, re tsebe ho e sebelisa le mokhoa oa ts'ebetso, likotsi life kapa life ha re nka lenvatinib phofo…. Ntle le moo, theko le boleng e tlameha ho ba lipelaelo tsa rona pele re e reka.

Kamora hore re hlahlobe li-database tse tsoang 'marakeng, ha re bapisa barekisi ba bangata, AASraw e sheba likhetho tse ntle bakeng sa batho ba batlang ho reka tse ngata lenvatinib phofo, tlhahiso ea bona e ne e laoloa ka thata tlasa boemo ba cGMP, boleng bo ka fumanoa nako efe kapa efe mme ba ka fana ka litlaleho tsohle tsa liteko ha o li odara. Ha e le litšenyehelo tsa phofo ea lenvatinib / theko, e lokela ho ba le kahlolo e molemo mahlong a ka. Hobane ke na le litheko tse ngata ho tsoa ho barekisi ba fapaneng, ha li bapisoa le boleng, ke nahana hore aasraw e ke ke ea e-ba khetho e mpe.
Bakeng sa lintlha tse ling, amohela ho bua le AASraw!

 

Reference

[1] H. Erdem, C. Gündogdu, le S. Üipal, "Correlation of E-cadherin, VEGF, COX-2 expression to prognostic parameters in papillary thyroid carcinoma," Experimental and Molecular Pathology, moq. 90, che. 3, maq. 312–317, 2011.

[2] M. Yagi, S. Kato, Y. Kobayashi et al., "Selection inhibition of platelet-derived growth factor (PDGF) receptor autophosphorylation le PDGF-mediated liketsahalo tsa cellular ka se tsoang ho quinoline," Experimental Cell Research, vol. 234, che. 2, maq. 285–292, 1997.

[3] P. Soares, J. Lima, A. Preto et al., "Liphetoho tsa lefutso likarolong tse sa arohaneng hantle le tse sa khetholloeng ke li-carcinoma tsa qoqotho," Hona joale. Genomics, moq. 12, che. 8, maq. 609-617, 2011.

[4] MM Moura, BM Cavaco, V. Leite. RAS proto-oncogene ho medullary thyroid carcinoma. Kankere ea Endocr Relat, 22 (5) (2015), maq. R235-R252.

[5] BR Haugen, SI Sherman Ho fetoha mekhoa ea bakuli ba nang le mofets'e o tsoetseng pele oa mofets'e oa qoqotho. Endocr Rev, 34 (3) (2013), maq. 439-455.

[6] M. Xing, D. Clark, H. Guan, le al. Liteko tsa BRAF tsa phetoho ea `` thyroid '' ea `` nale '' ea `` aspiration biopsy '' ea li-biopsy bakeng sa ts'oaetso ea "preoperative" ea "cancer cancer" ea papillary. J Clin Oncol, 27 (18) (2009), maq. 2977-2982.

[7] SR Wedge, DJ Ogilvie, M. Dukes, et al. ZD6474 e thibela ho tšoaetsoa ha methapo ea methapo ea methapo, angiogenesis, le kholo ea hlahala kamora tsamaiso ea molomo. Cancer Res, 62 (16) (2002), maq. 4645-4655.

[8] SI Sherman, EEW Cohen, P. Schoffski, le al. Ts'ebetso ea cabozantinib (Cabo) ho bakuli ba mofets'e oa kankere ea methapo (MTC) ba nang le phetoho ea RAS kapa RET: Liphetho tsa thuto ea mokhahlelo oa boraro [abstract]. J Clin Oncol, 31 (15 Suppl.) (2013) abstr 6000.

[9] SI Sherman, LJ Wirth, JP Droz, le al. Motesanib diphosphate ka mofets'e o khethollang mofets'e oa qoqotho. N Engl J Med, 359 (1) (2008), maq. 31-42.

[10] K. Okamoto, K. Kodama, K. Takase, le al. Mesebetsi ea Antitumor ea mefuta e mengata ea tyrosine kinase inhibitor lenvatinib (E7080) e khahlano le mefuta ea hlahala e tsamaeang le RET. Kankere Lett, 340 (1) (2013), maq. 97-103.

[11] E. Cabanillas, M. Schlumberger, B. Jarzab, et al. Teko ea karolo ea 2 ea lenvatinib (E7080) ho mofets'e oa qoqotho o tsoetseng pele, o tsoelang pele, oa radioiodine, o khethollang kankere ea qoqotho: litlamorao tsa bongaka le tlhahlobo ea tlhahlobo ea biomarker Cancer, 121 (16) ( 2015), maq. 2749-2756.

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