IndraLab

"28 Finally, momelotinib (also known as CYT-387) inhibits both JAK1 (IC 50 11 nm) and JAK2 (IC 50 18 nm), rather than JAK3 (IC 50 0.16 muM), although off-target effects (serine/threonine kinase IKBKE) have been described."

"In recent years, several independently developed Chinese JAK inhibitors (e.g., including jaktinib, golidocitinib, ivarmactinib, and itacitinib) under different phases of clinical trials are being considered to have great clinical potential. xref – xref In October 2022, Jaktinib, a deuterated compound of momelotinib that widely inhibits JAK1, JAK2, JAK3, TYK2 and ACVR1, became the first approved domestic JAK inhibitor for the treatment of moderate-to-severe myelofibrosis. xref , xref A published phase 2 trial has shown that jaktinib reduced the spleen size and alleviated the clinical symptoms of patients with moderate-to-severe myelofibrosis. xref It was evident that jaktinib was well-tolerated and that anemia and thrombocytopenia were the most common adverse events."

"Notably, both ruxolitinib and momelotinib inhibit JAK1 as well as JAK2, while pacritinib and fedratinib are relatively more specific for JAK2."

"Momelotinib inhibited JAK1 and JAK2 at nanomolar concentrations in in vitro assays , and reduced ex vivo formation of erythroid colonies from JAK2V617F-positive PV patients [ 22 ] ."

"Momelotinib is a potent inhibitor of JAK1 and JAK2 that demonstrated efficacy in patients with primary and secondary myelofibrosis."

"Momelotinib is a potent inhibitor of JAK1 and JAK2."

"In October 2022, Jaktinib, a deuterated compound of momelotinib that widely inhibits JAK1, JAK2, JAK3, TYK2 and ACVR1, became the first approved domestic JAK inhibitor for the treatment of moderate-to-severe myelofibrosis."

"Momelotinib inhibited JAK1 and JAK2 at nanomolar concentrations in in vitro assays, and reduced ex vivo formation of erythroid colonies fromJAK2 V617F -positive PV patients [ xref ]."

"Momelotinib inhibited JAK1 and JAK2 at nanomolar concentrations in in vitro assays, and reduced ex vivo formation of erythroid colonies from JAK2 -positive PV patients [22]."

"Momelotinib (MMB) is a small-molecule inhibitor of activin receptor type 1 (ACVR1), Janus kinase 1 (JAK1), and JAK2, with clinical activity against anemia, constitutional symptoms, and splenomegaly."