I-Rusotinib amaphilisi (ruxolitinib / Jakafi) ekwelapheni umongo we-bone fibrosis onobungozi obulinganiselayo noma obuphezulu, kufaka phakathi umnkantsha oyinhloko wamathambo, i-myelofibrosis ngemuva kwe-polycythemia vera, ne-myelofibrosis ngemuva kwesiguli se-idiopathic thrombocytosis. Iziguli ezinomnkantsha wamathambo omaphakathi noma onobungozi obuphakathi zibhekisa ezigulini ezingaphezulu kweminyaka engama-65 noma zibe nalezi zimo ezilandelayo: i-anemia, izimpawu zomzimba, ukwehla kwesibalo samaseli amhlophe egazi, kwehle isibalo se-embryonic cell, noma ukunciphisa ukubalwa kweplatelet. Ama-80% kuya kuma-90% wamacala.
Amaphilisi e-Rusotinib (i-ruxolitinib / Jakafi) okwamanje adayiswa e-United States, eYurophu nakwezinye izindawo, kodwa namanje awakathengiswa ezweni laseChina. I-Rusolitinib iyi-inhibitor yokuqala ehlotshaniswa ne-Janus kinase (JAK) evunyelwe emhlabeni kuze kube manje, kanye nomuthi othile wokuqala wokwelapha we-myelofibrosis ogunyazwe yi-FDA kanye nomhlaba. I-Rusotinib itholakala ngemithamo emi-5 ye-5, 10, 15, 20, kanye ne-25 mg / ithebhulethi, futhi ilawulwa njengomuthi womlomo kabili ngosuku. I-Bone marrow fibrosis yisifo esiqhubekayo futhi esingase sibeke engozini impilo yesistimu yegazi, okuyi-myeloproliferative tumor futhi kulinganiselwa ukuthi sithinta abantu abayizigidi ezingu-1.60-18.5 e-United States. Iziguli ze-bone marrow fibrosis kancane kancane zithathelwa indawo yizicubu ezibomvu, ukuze ukukhiqizwa kwamangqamuzana egazi kwenziwe ezithweni ezifana nesibindi nobende. I-anemia, i-leukopenia, ne-thrombocytopenia kwenzeka. Iziguli ezine-bone marrow fibrosis zibonakala ngokuhluleka komnkantsha kanye ne-splenomegaly, kanye nokukhathala, ubuhlungu be-musculoskeletal, ukungakhululeki kwesisu, ukulunywa okukhulu, ukujuluka ebusuku, nokusutha, okuphazamisa kakhulu izinga lokuphila. Izimpawu ze-Splenomegaly ne-systemic ezigulini ezine-myelofibrosis zihlotshaniswa nokungasebenzi kahle kokubonisa indlela ye-JAK. I-Rusotinib iyi-oral JAK1 kanye ne-JAK2 inhibitor, futhi i-JAK1 ne-JAK2 ihileleke ekulawuleni igazi nokusebenza komzimba.
FDA Isinqumo sokugunyaza okungenhla lusotinib sasisekelwe ikakhulukazi kudatha evela kusigaba sesi-III esingahleliwe, esingaboni kabili, nokuhlolwa komtholampilo okulawulwayo okunamagama ekhodi amabili, i-COMFORT-I kanye ne-COMPORT-Ⅱ. Ucwaningo lwe-COMFORT-I lwaluhlanganisa ingqikithi yeziguli ze-309 ezine-allogeneic bone marrow transplantation engakhululekile noma ephikisanayo, noma i-relapsed primary bone marrow fibrosis, i-myelofibrosis ngemva kwe-polycythemia kanye ne-idiopathic thrombocythemia, futhi imiphumela yabonisa Ingxenye yeziguli ezifinyelele iphuzu lokugcina eliyinhloko ngemva kwe-24 amasonto okwelashwa nge lusotinib noma i-placebo, ngisho noma umthamo we-spleen wehle ngo-≥35%, wawungu-41.9% kanye no-O. ngokulandelana. 7% (P <0.000 1). Ukwengeza, ingxenye yeziguli ezithuthuke ngo-≥50% kuFomu Lokuhlola Izimpawu Zesifo Se-Myelofibrosis Ethuthukisiwe (i-MFSAF TSS) emaqenjini amabili e-lusotinib noma i-placebo yayingu-45.9% kanye no-5.3% (P <0.001), kanye ne- isikhathi esimaphakathi sokuphendula sasingaphansi kwamaviki angu-4. Ucwaningo lwe-C0MPORT-11 lwaluhlanganisa iziguli ze-219 ezine-bone marrow transplantation ezingakhululekile noma ze-allogeneic, noma i-relapsed primary bone marrow fibrosis, i-myelofibrosis ngemva kwe-polycythemia kanye ne-idiopathic thrombocytosis, futhi imiphumela yabonisa ukuthi Ingxenye yeziguli ezine-sotinib noma i-hydroxyurea engcono kakhulu yokwelapha (i-hydroxyurea) noma i-hydroxyurea) i-glucocorticoid ngemva kwamasonto angu-48 wokwelashwa ukunciphisa umthamo we-spleen ≥35% yayingu-28.5% no-0 (P <0.001). Imiphumela emibi kakhulu ye-hematological yokwelashwa kwe-lusotinib ebonwe ku-C0MPORT-mina ne-COMPORT-11 kwakuyi-thrombocytopenia ne-anemia ehlobene nomthamo, kepha le miphumela emibi emibili kulula ukuyilawula futhi ayivamisile ukudala iziguli ukuthi ziyeke ukwelashwa; imiphumela emibi kakhulu ejwayelekile engeyona yegazi uhudo, isiyezi, ikhanda elibuhlungu, ukukhathala kanye nesicanucanu.
