Review Article
JAK2 Inhibition: Reviewing a New Therapeutical Option in Myeloproliferative Neoplasms
Table 1
Current therapies for BCR-ABL1 negative MPN patients to be combined with JAK2 inhibitors.
| Drug | Target | Results | JAK2V617F load | Reference |
| JAK2 inhibitors | | | | | INCB018424 Ruxolitinib | JAK2, JAK1 | >50% reduction in splenomegaly and constitutional symptoms | JAK2V617F load marginally reduced | Verstovsek et al. [29] | TG101348 or SAR302503 | JAK2, FLT3 | Reduction in splenomegaly | JAK2V617F load significantly reduced | Pardanani et al. [34] | CYT387 | JAK2, JAK1, TYK2 | In a murine model, normalized erythrocytes, leukocytes, spleen size, and levels of inflammatory cytokines | JAK2V617F load reduced | Tyner et al. [35] | CEP-701 Lestaurtinib | JAK2, FLT3 | Reduction in splenomegaly | JAK2V617F load no reduced | Hexner et al. [36] Santos et al. [37] |
| Immunomodulators | | | | | Interferon-alpha | Stromal cells | Inhibit cytokine signalling, proliferation and angiogenesis | Unknown | Kiladjian et al. [43] | Thalidomide | Stromal cells | Inhibition of angiogenesis | Unknown | Jabbour et al. [45] | Lenalidomide | Stromal cells | Inhibition of angiogenesis | Unknown | Jabbour et al. [45] | Pomalidomide | Stromal cells | Inhibition of angiogenesis | Unknown | Begna et al. [46] |
| Other | | | | | Hydroxycarbamide | JAK2 mutant burden | Inhibition of proliferation | JAK2V617F load significantly reduced | Besses et al. [47] | Histone post-translationa modificators | JAK2 nuclear | Depletion of JAK2V617F autophosphorylation, apoptosis in vitro | Unknown | Wang et al. [26] |
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