Ruxolitinib

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Ruxolitinib Myelofibrosis Novartis La 6 Phupu 2024


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TLHOKOMELO SEHLAHISO

Ruxolitinib ke molek'hule e nyenyane Janus kinase inhibitor e sebelisoang ho phekola myelofibrosis e ka hare kapa e kotsing e kholo le mefuta e hanyetsanang ea polycythemia vera le lefu la graft-vs-host. Ruxolitinib e amahanngoa le maemo a phahameng a nakoana 'me hangata a le bobebe ho serum aminotransferase nakong ea kalafo le maemong a sa tloaelehang a kotsi ea sebete e sa bonahaleng, e bonahalang e le teng ka har'a sebete hammoho le linyeoe tsa ho tsosolosa lefu la sebete la mofuta oa B ho batho ba hlaselehang habonolo.

Ruxolitinib ke inhibitor ea molomo ea bioavailable Janus-associated kinase (JAK) e nang le mesebetsi e ka bang teng ea antineoplastic le immunomodulating. Ruxolitinib ka ho khetheha e tlama le ho thibela protheinetyrosinekinases JAK 1 le 2, e ka lebisang ho fokotsa ho ruruha le ho thibela ho ata ha lisele. Tsela ea JAK-STAT (signal transducer le activator of transcription) e phetha karolo ea bohlokoa ho bonts'a li-cytokine tse ngata le lintlha tsa ho hōla 'me e ameha ho ata ha lisele, khōlo, hematopoiesis, le karabelo ea 'mele ea ho itšireletsa mafung; JAK kinases e ka 'na ea laoloa ke mafu a ho ruruha, mafu a myeloproliferative, le mafu a sa tšoaneng.

Ruxolitinib ke apyrazolee nkeloe sebaka sebakeng sa 1 ke sehlopha sa 2-cyano-1-cyclopentylethyl le boemong ba 3 ke sehlopha sa pyrrolo [2,3-d] pyrimidin-4-yl. E sebelisoa e le letsoai la phosphate bakeng sa phekolo ea bakuli ba nang le myelofibrosis e bohareng kapa e kotsing e kholo, ho akarelletsa le myelofibrosis ea mantlha, post-polycythemia vera myelofibrosis le post-essential thrombocythemia myelofibrosis. E na le karolo e le moemeli oa antineoplastic le EC 2.7.10.2 (protheine e seng e khethehileng-tyrosinekinase) inhibitor. Ke nitrile, apyrrolopyrimidinele setho sa pyrazoles.

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