Ruxolitinib

Ruxolitinib is a potent ATP mimetic that inhibits both JAK1 and JAK2 with IC₅₀ values of 2.7 and 4.5 nM, respectively and is relatively less selective for JAK3 (IC₅₀ = 322 nM).¹ It can block interleukin-6 (IL-6) signaling (IC₅₀ = 281 nM) and proliferation of JAK2^V617F+ Ba/F3 cells (IC₅₀ = 127 nM).² In primary cultures, ruxolitinib preferentially suppresses erythroid progenitor colony formation from JAK2^V617F+ polycythemia vera patients (IC₅₀ = 67 nM) versus healthy donors (IC₅₀ > 400 nM).² In a mouse model of JAK2^V617F+ MPN, 90 mg/kg ruxolitinib reduced splenomegaly, decreased circulating levels of IL-6 and TNF-α, eliminated neoplastic cells, and prolonged survival of the treated animals.²

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1. Verstovsek, S. Therapeutic potential of JAK2 inhibitors. Hematology Am. Soc. Hematol. Educ. Program 636-642 (2009).

2. Quintás-Cardama, A., Vaddi, K., Liu, P., et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: Therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 115(15), 3109-3117 (2010).

Wang, W., Green, M., Choi, J.E., et al. CD8⁺ T cells regulate tumour ferroptosis during cancer immunotherapy. Nature 569(7755), 270-274 (2019).