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Sunitinib Malate

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Sunitinib inhibits masero ekuratidzira nekutarisa akawanda receptor tyrosine kinases (RTKs) - izvi zvinosanganisira zvese zvinogamuchirwa zveplatelet-yakatorwa kukura chinhu (PDGF-Rs) uye vascular endothelial grow factor receptors (VEGFRs), iyo inoita chinzvimbo mune zvese tumor angiogenesis uye tumarara sero. kuwanda.

Product Description

Hunhu Hwekutangacs

Product Name Sunitinib Malate upfu
CAS Number 341031-54-7
Molecular Formula C22H27FN4O2
Molar uremu 398.474
Synonyms 557795-19-4;

Sutent;

Sunitinib malate powder;

SU11248.

Kuonekwa White powder
Kuchengeta uye Kubata Zvichengetedze pamhepo tembiricha uye kure nekupisa kwakanyanya uye hunyoro.

 

Sunitinib Malate powder Tsanangudzo

Sunitinib (inotengeswa seSutent naPfizer, uye yaimbozivikanwa seSU11248) inotaurwa, diki-mamorekuru, yakawanda-yakanangwa receptor tyrosine kinase (RTK) inhibitor iyo yakabvumidzwa neDFA yekurapa renal cell carcinoma (RCC) uye imatinib -kuramba mudumbu stromal bundu (GIST) musi waNdira 26, 2006. Sunitinib ndiyo yaive kenza yekutanga mushonga panguva imwe chete yakatenderwa zviratidzo zviviri zvakasiyana.

 

Sunitinib Malate powder Mechanism yeAction

Sunitinib inhibits maseru ekuratidzira nekutarisa akawanda receptor tyrosine kinases (RTKs).

Izvi zvinosanganisira zvese zvinogamuchirwa zveplatelet-yakatorwa kukura chinhu (PDGF-Rs) uye vascular endothelial grow factor receptors (VEGFRs), iyo inoita chinzvimbo mune zvese bundu angiogenesis uye tumarara sero kuwanda. Iko kuvhiringidza panguva imwe chete kwezvinangwa izvi nekudaro kunoderedza bundu vascularization uye kunokonzeresa cancer cancer apoptosis uye nekudaro kunoguma nechuma shrinkage.

Sunitinib inodzivisawo CD117 (c-KIT), [2] iyo receptor tyrosine kinase iyo (kana ikamisikidzwa zvisirizvo) inofambisa ruzhinji rwematumbu maseru ezviremera.Iyo yakakurudzirwa seyechipiri-mutsara kurapa kwevarwere vane mamota anovandudza shanduko. mu c-KIT izvo zvinoita kuti zvidzivirire kune imatinib, kana ndiani asingakwanise kushivirira mushonga.

 

Sunitinib Malate powder Kunyorera

 Dumbu remudumbu stromal bundu

SaRCC, GIST haiwanzo pindura kune yakajairwa chemotherapy kana radiation. Imatinib yaive yekutanga kenza mumiririri yakaratidzirwa inoshanda kune metastatic GIST uye yakamiririra hukuru hukuru pakurapa kwechirwere chisingawanzo asi chinonetsa.

 

 Meningioma

Sunitinib iri kuongororwa kurapwa kwe meningioma iyo inosangana neurofibromatosis.

 

 Pancreatic neuroendocrine mamota

MunaNovember 2010, Sutent akawana mvumo kubva kuEuropean Commission yekurapa 'isingagadzirisike kana metastatic, yakanyatso kusiyaniswa pancreatic neuroendocrine tumarara nekuwedzera kwechirwere muvakuru'.

 

 Renal cell carcinoma

Sunitinib inogamuchirwa kurapwa kwemasastatic RCC. Dzimwe nzira dzokurapa mune ino mamiriro ipazopanib (Votrient), sorafenib (Nexavar), temsirolimus (Torisel), interleukin-2 (Proleukin), everolimus (Afinitor), bevacizumab (Avastin), uye aldesleukin.

 

Sunitinib Malate upfu Side Migumisiro & Yambiro

Sunitinib zviitiko zvakashata zvinoonekwa sezvisingakwanisike uye zviitiko zvezviitiko zvakakomba zvakashata zvakaderera.

Zviitiko zvinowanzoitika zvakasangana ne sunitinib kurapa ndiko kuneta, manyoka, kuda kurutsa, anorexia, hypertension, yero ganda kupunduka, ruoko-rutsoka ganda kuita, uye stomatitis. Muchidzidzo che placebo-chinodzorwa Phase III GIST kudzidza, zviitiko zvakashata zvinoitika kazhinji ne sunitinib pane placebo yaisanganisira manyoka, anorexia, kugadzikana kweganda, mucositis / stomatitis, asthenia, yakachinja kuravira, uye kupatira.

Kuderedzwa kwemadhiza kwaidikanwa mu50% yevarwere vakadzidza muRCC kuitira kuti vagadzirise huturu hwakakosha hwemumiriri uyu.

Zvakakomba (giredhi 3 kana 4) zviitiko zvakashata zvinoitika mu10% yevarwere uye zvinosanganisira hypertension, kuneta, asthenia, manyoka, uye chemotherapy-inosimudzira acral erythema. Lab isina kujairika inosangana ne sunitinib therapy inosanganisira lipase, amylase, neutrophils, lymphocytes, uye maplatelet. Hypothyroidism uye erythrocytosis inodzoserwa zvakare yakabatana ne sunitinib.

 

Reference

[1] US Kudya neDrug Administration (2006). "FDA inobvumidza kurapwa kutsva kwegomarara remudumbu uye itsvo".

[2] Hartmann JT, Kanz L (Mbudzi 2008). "Sunitinib uye periodic bvudzi depigmentation nekuda kwekanguva c-KIT inhibition". Arch Dermatol. 144 (11): 1525-6. doi: 10.1001 / archderm.144.11.1525. PMID 19015436. Yakachengetedzwa kubva pane yekutanga pane 2011-07-25.

[3] Quek R, George S (Kukadzi 2009). "Gastrointestinal stromal bundu: kuongororwa kwechipatara". Hematol. Oncol. Clin. Maodzanyemba Am. 23 (1): 69-78, viii. doi: 10.1016 / j.hoc.2008.11.006. PMID 19248971.

[4] Blay JY, Reichardt P (Chikumi 2009). "Yepamberi dumbu stromal bundu muEurope: wongororo yakagadziridzwa yekurapa kurudziro". Nyanzvi Rev Anticancer Ther. 9 (6): 831-8. doi: 10.1586 / era.09.34. PMID 19496720. S2CID 23601578.

[5] Gan HK, Seruga B, Knox JJ (Chikumi 2009). "Sunitinib mune yakasimba mamota". Nyanzvi Opin Investig Zvinodhaka. 18 (6): 821-34. doi: 10.1517 / 13543780902980171. PMID 19453268. S2CID 25353839.

[6] "Kunyora ruzivo rweSutent (sunitinib malate powder)". Pfizer, Inc, New York NY.