momelotinib

Momelotinib (brand names Omjjara, Ojjaara) is an orally bioavailable small molecule inhibitor of Janus kinases (JAK1 and JAK2) and activin A receptor type 1 (ACVR1/ALK2). Developed by GSK following its acquisition of Sierra Oncology, it is primarily indicated for the treatment of myelofibrosis, particularly in patients with anemia. Unlike other JAK inhibitors, momelotinib's inhibition of ACVR1 leads to a reduction in hepcidin levels, which helps alleviate anemia of chronic disease by improving iron availability for erythropoiesis. Beyond its primary hematologic indications, momelotinib has been identified as an inhibitor of TANK-binding kinase 1 (TBK1). This secondary mechanism is currently being explored in clinical trials to overcome resistance to immune checkpoint inhibitors in solid tumors, such as cutaneous melanoma, by modulating the tumor microenvironment and enhancing anti-tumor immune responses.

Brand names

OmjjaraOjjaara

Other names

momelotinib dihydrochloride