Sunitinib Malate phofo - Mofani oa Lihlahisoa tsa Baetsi
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Sunitinib Malate

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Sunitinib e thibela lets'oao la lisele ka ho lebisa tlhokomelo ho li-receptor tse ngata tsa tyrosine kinases (RTKs) tse kenyeletsang li-receptor tsohle tse tsoang ho li-platelet-derived growth factor (PDGF-Rs) le li-vascular endothelial growth factor receptors (VEGFRs), tse phethang karolo ea hlahala angiogenesis le tumor cell ho ata.

Tlhaloso ea Sehlahisoa

Litšobotsi tsa mantlhacs

Name Product Sunitinib Malate phofo
Nomoro ea CAS 341031-54-7
Molecular Formula C22H27FN4O2
Boima ba Molar 398.474
Li-synonyms 557795-19-4;

Sutent;

Sunitinib malate phofo;

SU11248.

Ponahalo Pula e tšoeu
Ho Boloka le ho Sebetsana E boloke ka mocheso oa kamore 'me u se ke ua chesa haholo.

 

Tlhaloso ea phofo ea Sunitinib Malate

Sunitinib (e rekisoang e le Sutent ke Pfizer, eo pele e neng e tsejoa e le SU11248) ke molomo, molek'hule e nyane, receptor tyrosine kinase (RTK) inhibitor e amohetsoeng ke FDA bakeng sa kalafo ea renal cell carcinoma (RCC) le imatinib -thestist gastrointestinal stromal tumor (GIST) ka la 26 Pherekhong 2006. Sunitinib e ne e le sethethefatsi sa pele sa mofets'e se amoheloang ka nako e le ngoe bakeng sa matšoao a mabeli a fapaneng.

 

Mokhoa oa ts'ebetso oa Sunitinib Malate

Sunitinib e thibela lets'oao la lisele ka ho lebisa tlhokomelo ho li-receptor tse ngata tsa li-receptor tyrosine (RTKs).

Tsena li kenyelletsa li-receptor tsohle tsa kholo e tsoang ho platelet (PDGF-Rs) le li-vascular endothelial grow factor receptors (VEGFRs), tse phethang karolo ho hlahala ea angiogenesis le ho ata ha lisele tsa tumor. Thibelo ea nako e le ngoe ea lipheo tsena ka hona e fokotsa hlahala vascularization mme e baka mofets'e oa cell apoptosis mme ka hona e fella ka ho fokotseha ha hlahala.

Sunitinib e boetse e thibela CD117 (c-KIT), [2] receptor tyrosine kinase eo (ha e sebelisoa ka nepo ke phetoho) e tsamaisang boholo ba lihlahala tsa lisele tsa mala. E khothalletsoa e le kalafo ea mohala oa bobeli bakeng sa bakuli bao lihlahala tsa bona li hlahisang liphetoho. ho c-KIT e ba etsang hore ba hanele imatinib, kapa bao ba ke keng ba mamella sethethefatsi.

 

Sunitinib Malate powder Kopo

 Boko ba ka mpeng ba stromal

Joalo ka RCC, GIST ha e arabe ka mokhoa o tloaelehileng ho chemotherapy kapa radiation. Imatinib e ne e le moemeli oa pele oa mofets'e ea netefalitsoeng a sebetsa bakeng sa metastatic GIST mme a emetse nts'etsopele e kholo ho phekoleng lefu lena le sa tloaelehang empa le le thata.

 

 Meningiomas

Sunitinib e ntse e ithutoa bakeng sa kalafo ea meningioma e amanang le neurofibromatosis.

 

 Lihlahala tsa Pancreatic neuroendocrine

Ka Pherekhong 2010, Sutent o ile a fumana tumello ho Khomishene ea Europe bakeng sa kalafo ea lihlahala tsa 'pancreic neuroendocrine' tse ke keng tsa qojoa kapa tse nang le tšoaetso e nang le ts'oaetso ea mafu ho batho ba baholo.

 

 Renal cell carcinoma

Sunitinib e amoheloa bakeng sa kalafo ea metastatic RCC. Likhetho tse ling tsa kalafo maemong ana ke pazopanib (Votrient), sorafenib (Nexavar), temsirolimus (Torisel), interleukin-2 (Proleukin), everolimus (Afinitor), bevacizumab (Avastin), le aldesleukin.

 

Sunitinib Malate phofo Litla-morao & Tlhokomeliso

Liketsahalo tse mpe tsa Sunitinib li nkuoa li le bonolo ho laoleha mme ketsahalo ea liketsahalo tse mpe tse tebileng e tlase.

Liketsahalo tse bohloko ka ho fetisisa tse amanang le kalafo ea sunitinib ke mokhathala, letšollo, ho nyekeloa ke pelo, anorexia, khatello ea kelello, 'mala o mosehla oa letlalo, ho itšoara ka letlalo la maoto le letsoho le stomatitis. Thutong ea Phase III ea GIST e laoloang ke "placebo", liketsahalo tse mpe tse etsahalang khafetsa ka sunitinib ho feta placebo li ne li kenyelletsa letšollo, anorexia, ho soeufala ha letlalo, mucositis / stomatitis, asthenia, tatso e fetotsoeng le popelo.

Ho ne ho hlokahala phokotso ea litekanyetso ho 50% ea bakuli ba ithutileng RCC molemong oa ho sebetsana le chefo e kholo ea moemeli enoa.

Liketsahalo tse mpe (tsa 3 kapa 4) tse mpe li etsahala ho ≤10% ea bakuli mme li kenyelletsa khatello ea mali, mokhathala, asthenia, letshollo le chemotherapy e bakoang ke acral erythema. Lintho tse sa tloaelehang tsa Lab tse amanang le phekolo ea sunitinib li kenyelletsa lipase, amylase, neutrophils, lymphocyte le liplatelete. Hypothyroidism le erythrocytosis e khutliselitsoeng le tsona li amahanngoa le sunitinib.

 

Reference

[1] Tsamaiso ea Lijo le Lithethefatsi ea US (2006). "FDA e amohela kalafo e ncha bakeng sa mofetše oa mala le liphio".

[2] Hartmann JT, Kanz L (Pulungoana 2008). "Sunitinib le ho hlatsuoa ha moriri nako le nako ka lebaka la thibelo ea nakoana ea c-KIT". Arch Dermatol. 144 (11): 1525-6. doi: 10.1001 / archderm.144.11.1525. PMID 19015436. E bolokiloe ho tsoa ho ea mantlha ka 2011-07-25.

[3] Quek R, George S (Hlakola 2009). "Hlahala ea ka mpeng ea stromal: kakaretso ea bongaka". Hematol. Oncol. Tleliniki. North Am. 23 (1): 69-78, viii. doi: 10.1016 / j.hoc.2008.11.006. PMID 19248971.

[4] Blay JY, Reichardt P (Phuptjane 2009). "Sehlahala se tsoetseng pele sa mala a tsoang Europe: tlhahlobo ea likhothaletso tse ntlafalitsoeng tsa kalafo". Setsebi Rev Anticancer Ther. 9 (6): 831-8. doi: 10.1586 / era.09.34. PMID 19496720. S2CID 23601578.

[5] Gan HK, Seruga B, Knox JJ (Phuptjane 2009). "Sunitinib ka lihlahala tse tiileng". Setsebi Opin Investig Lithethefatsi. 18 (6): 821-34. doi: 10.1517 / 13543780902980171. PMID 19453268. S2CID 25353839.

[6] "Ho fana ka tlhaiso-leseling bakeng sa Sutent (sunitinib malate powder)". Pfizer, Inc, New York NY.