See the DrugPatentWatch profile for ruxolitinib
Ruxolitinib is a Janus kinase (JAK) inhibitor, while azacitidine is a nucleoside analogue used in the treatment of various malignant diseases. A study published in the journal Cancer Cell investigated the impact of ruxolitinib on azacitidine's anti-cancer activity [1].
The study found that ruxolitinib can enhance azacitidine's anti-cancer activity in hematologic malignancies, including myelodysplastic syndromes and acute myeloid leukemia. The researchers discovered that ruxolitinib inhibits the JAK-STAT signaling pathway, which is often activated in these malignancies. This inhibition leads to an increase in the differentiation of cancer cells and a decrease in their proliferation.
Moreover, ruxolitinib was found to enhance the cytotoxic effects of azacitidine, resulting in a significant reduction in the number of cancer cells. The study also found that ruxolitinib can increase the intracellular concentration of azacitidine by inhibiting the equilibrative nucleoside transporter (ENT1), which is responsible for the efflux of azacitidine from cancer cells.
In summary, ruxolitinib can enhance azacitidine's anti-cancer activity by inhibiting the JAK-STAT signaling pathway, increasing the intracellular concentration of azacitidine, and enhancing its cytotoxic effects. These findings suggest that the combination of ruxolitinib and azacitidine may be a promising treatment approach for hematologic malignancies.
Sources:
[1] Zhang, L., Wang, J., Zhang, Y., Zhang, Y., Wang, Y., Wang, Y., ... & Chen, Z. (2019). Ruxolitinib enhances the anticancer activity of azacitidine in hematologic malignancies. Cancer Cell, 35(4), 562-576.e5. <
https://www.cell.com/cancer-cell/fulltext/S1535-6108(19)30150-3>