AASraw tsim NMN thiab NRC hmoov hauv qhov ntau!

Sunitinib Malate

Sunitinib inhibits cellular teeb liab los ntawm kev tsom mus rau ntau lub receptor tyrosine kinases (RTKs) .Qhov no suav tag nrho cov receptors rau platelet-derived growth factor (PDGF-Rs) thiab vascular endothelial growth factor receptors (VEGFRs), uas ua lub luag haujlwm hauv ob lub qog angiogenesis thiab qog cell. loj hlob.

Hauj lwm yam khoom

Cov Qauv Cim Tseem Ceebcs

khoom npe Sunitinib Malate
CAS Number 341031-54-7
molecular Formula C22H27FN4O2
Molar loj 398.474
Synonyms 557795-19-4;

Sutent;

Sunitinib malate;

SU11248.

tsos Dawb hmoov
Cia thiab Ua Haujlwm Khaws nws ntawm chav sov thiab deb ntawm qhov kub thiab noo noo.

 

Sunitinib Malate Cov Lus Qhia

Sunitinib (ua lag luam raws li Sutent los ntawm Pfizer, thiab yav tas los hu ua SU11248) yog qhov ncauj, me-molecule, ntau qhov chaw receptor tyrosine kinase (RTK) inhibitor uas tau pom zoo los ntawm FDA rau kev kho mob ntawm raum cell carcinoma (RCC) thiab imatinib -resistant gastrointestinal stromal hlav (GIST) rau Lub Ib Hlis 26, 2006. Sunitinib yog thawj cov tshuaj tua kabmob kheesxaws ib txhij pom zoo rau ob qhov ntsuas.

 

Sunitinib Malate Cov Haujlwm ntawm Kev Ua

Sunitinib tiv thaiv kev ua haujlwm ntawm tes los ntawm kev siv ntau hom receptor tyrosine kinases (RTKs).

Cov no suav nrog tag nrho cov receptors rau platelet-derived kev loj hlob tau (PDGF-Rs) thiab vascular endothelial growth factor receptors (VEGFRs), uas ua lub luag haujlwm hauv ob lub qog angiogenesis thiab nqaij hlav loj. Ib txhij inhibition ntawm cov hom phiaj yog li txo cov qog vascularization thiab ua rau tus mob cancer cell apoptosis thiab yog li ua rau cov qog ua qog.

Sunitinib tseem inhibits CD117 (c-KIT), [2] receptor tyrosine kinase uas (thaum ua haujlwm tsis zoo los ntawm hloov pauv) ua rau feem ntau ntawm txoj hnyuv plab hnyuv qog nqaij hlav.Nws tau pom zoo raws li txoj kev kho thib ob rau cov neeg mob uas cov qog loj hlob hloov tau. Hauv c-KIT uas ua rau lawv tiv taus imatinib, lossis leej twg tsis tuaj yeem tiv taus cov tshuaj.

 

Daim Ntawv Thov Sunitinib Malate

 Lub plab zom mov qog cov qog

Zoo li RCC, GIST tsis feem ntau teb rau kev kho mob lossis tshuaj tua hluav taws xob. Imatinib yog thawj tus kabmob kheesxaws tau ua pov thawj zoo rau metastatic GIST thiab sawv cev rau kev txhim kho loj hauv kev kho mob tsawg tsawg tab sis tus kabmob nyuaj.

 

 Meningioma

Sunitinib tab tom kawm txog kev kho mob meningioma uas cuam tshuam nrog neurofibromatosis.

 

 Cov hlav hlav neuroendocrine hlav

Thaum Lub Kaum Ib Hlis 2010, Sutent tau txais kev pom zoo los ntawm European Commission rau kev kho mob 'tsis tuaj yeem lossis metastatic, muaj txiaj ntsig zoo ntawm cov leeg leeg mob neuroendocrine hlav nrog cov kab mob kev loj hlob hauv cov neeg laus'.

 

 Carcinoma ntawm tes cell

Sunitinib raug pom zoo rau kev kho mob metastatic RCC. Lwm txoj hauv kev kho mob hauv cov chaw no yog pazopanib (Votrient), sorafenib (Nexavar), temsirolimus (Torisel), interleukin-2 (Proleukin), everolimus (Afinitor), bevacizumab (Avastin), thiab aldesleukin.

 

Sunitinib MalateSab sij huam & Lus Ceeb Toom

Sunitinib qhov xwm txheej tsis zoo yog suav tias yog tus tswj hwm tau me ntsis thiab qhov tshwm sim ntawm qhov tshwm sim tsis zoo.

Cov xwm txheej feem ntau cuam tshuam nrog kev kho mob sunitinib yog nkees, mob plab, xeev siab, mob ntshav qab zib, ua kom tawv nqaij daj, ua kom tawv nqaij daj, ua tes taw ua kom tawv nqaij, thiab mob plab. Hauv cov tshuaj placebo tswj Theem III GIST, cov xwm txheej tsis zoo uas tshwm sim ntau dua nrog sunitinib dua li cov tshuaj placebo suav nrog raws plab, ua kom mob plab, tawv nqaij ua kom tawv nqaij, mucositis / stomatitis, asthenia, hloov pauv, thiab cem quav.

Kev txo tus koob tshuaj yuav tsum nyob hauv 50% ntawm cov neeg mob tau kawm hauv RCC txhawm rau tswj hwm qhov muaj feem ua rau muaj kev phom sij ntawm tus neeg sawv cev no.

Cov mob hnyav (qib 3 lossis 4) muaj qhov tshwm sim tsis zoo tshwm sim hauv ≤10% ntawm cov neeg mob thiab suav nrog kev kub siab, qaug zog, mob asthenia, raws plab, thiab kev kho mob tshuaj lom neeg mob erythema. Kev ua haujlwm hauv lub cev muaj feem nrog kev kho mob sunitinib suav nrog lipase, amylase, neutrophils, lymphocytes, thiab platelets. Hypothyroidism thiab mob erythrocytosis thim rov qab kuj tseem cuam tshuam nrog sunitinib.

 

reference

[1] Asmeskas Chaw Tswj Xyuas Khoom Noj thiab Tshuaj (2006). "FDA pom zoo kho tshiab rau txoj hnyuv thiab lub raum mob cancer".

[2] Hartmann JT, Kanz L (Kaum Ib Hlis 2008). "Sunitinib thiab Periodic plaub hau depigmentation vim yog ib ntus c-K inhibition". Koov Dermatol. 144 (11): 1525–6. doi: 10.1001 / archderm.144.11.1525. PMID 19015436. Tau muab daim qauv ntawm daim qauv qub rau xyoo 2011-07-25.

[3] Quek R, George S (Lub Ob Hlis 2009). “Lub plab zom mov qog: tus saib mob”. Hematol. Oncol. Clin. Qaum Teb Am. 23 (1): 69–78, viii. doi: 10.1016 / j.hoc.2008.11.006. PMID 19248971.

[4] Blay JY, Reichardt P (Lub Rau Hli 2009). “Mob siab rau lub qog stromal nyob hauv cov teb chaws Europe: tshuaj xyuas cov tswv yim kho tshiab”. Cov Kws Muaj Txuj Rev Anticancer Ther. 9 (6): 831–8. doi: 10.1586 / era.09.34. PMID 19496720. S2CID 23601578.

[5] Gan HK, Seruga B, Knox JJ (Lub Rau Hli 2009). "Sunitinib nyob rau hauv cov hlav". Tus Kws Tshawb Fawb Txog Opin Tshuaj. 18 (6): 821–34. doi: 10.1517 / 13543780902980171. PMID 19453268. S2CID 25353839.

[6] “Tshaj tawm cov ntaub ntawv rau Sutent (sunitinib malate)”. Pfizer, Inc, New York NY.