Ruxolitinib
I-Ruxolitinib yi-molecule encinci i-Janus kinase inhibitor esetyenziselwa unyango lwe-myelofibrosis ephakathi okanye ephezulu kunye ne-resistant form of polycythemia vera kunye ne-graft-vs-host disease.I-Ruxolitinib inxulunyaniswa nokuphakama okwethutyana kwaye okuqhelekileyo kwi-serum aminotransferase ngexesha lonyango kunye nezihlandlo ezinqabileyo zokulimala okubonakalayo, okubonakalayo kwekliniki ye-idiosyncratic acute yesibindi kunye neemeko zokuphinda kusebenze i-hepatitis B kubantu abasesichengeni.
I-Ruxolitinib yinto yomlomo ye-bioavailable ye-Janus-associated kinase (JAK) inhibitor ene-antineoplastic kunye nemisebenzi ye-immunomodulating.I-Ruxolitinib ibophelela ngokukodwa kwaye inqanda iprothenityrosinekinases JAK 1 kunye ne-2, enokuthi iholele ekunciphiseni ukuvuvukala kunye nokuthintela ukwanda kwamaselula.I-JAK-STAT (i-transducer yesignali kunye ne-activator ye-transcription) indlela idlala indima ephambili ekubonakalisweni kwee-cytokines ezininzi kunye nezinto ezikhulayo kwaye zibandakanyeka ekwandeni kwamaselula, ukukhula, i-hematopoiesis, kunye ne-immune response;I-JAK kinases inokulawulwa kwizifo ezivuthayo, ukuphazamiseka kwe-myeloproliferative, kunye neentlobo ezahlukeneyo ezimbi.
IRuxolitinib yiipyrazoleifakwe kwindawo ye-1 ngeqela le-2-cyano-1-cyclopentylethyl kunye ne-3 yeqela le-pyrrolo [2,3-d] pyrimidin-4-yl.Isetyenziswe njengetyuwa ye-phosphate kunyango lwezigulane ezine-myelofibrosis ephakathi okanye ephezulu, kuquka i-myelofibrosis ephantsi, i-post-polycythemia vera myelofibrosis kunye ne-post-essential thrombocythemia myelofibrosis.Inendima njenge-antineoplastic agent kunye ne-EC 2.7.10.2 (iprotheyini engeyiyo ngqo-tyrosinekinase) inhibitor.Yinitrile, apyrrolopyrimidinekunye nelungu lepyrazoles.
Isindululo18Iiprojekthi zoVavanyo loBulunga ezivunyiweyo4, kwaye6iiprojekthi ziphantsi kolwamkelo.
Inkqubo yolawulo lomgangatho wehlabathi ephucukileyo ibeke isiseko esiluqilima sokuthengisa.
Ukongamela umgangatho kutyhutyha umjikelo wobomi bemveliso ukuqinisekisa umgangatho kunye nesiphumo sonyango.
Iqela leMicimbi yoLawulo lobuGcisa lixhasa iimfuno zomgangatho ngexesha lesicelo nokubhaliswa.