DDInter1628 DDInter905
Ruxolitinib, formerly known as INCB018424 or INC424, is an anticancer drug and a Janus kinase (JAK) inhibitor. It is a potent and selective inhibitor of JAK1 and JAK2, which are tyrosine kinases involved in cytokine signalling and hematopoiesis. Myeloproliferative neoplasms, such as myelofibrosis and polycythemia vera, are often characterized by aberrant activation of the JAK-STAT pathway, leading to abnormal blood cell counts and thrombotic complications. By inhibiting JAK1 and JAK2, ruxolitinib works to block the dysregulated cell signalling pathways and prevents abnormal blood cell proliferation. Due to a large number of patients with myeloproliferative neoplasms who have JAK2 mutations, ruxolitinib was the first ATP-competitive inhibitor of JAK1 and JAK2 ever developed. Rux
Idelalisib is a phosphoinositide 3-kinase inhibitor indicated in the treatment of chronic lymphocytic leukemia (CLL), relapsed follicular B-cell non-Hodgkin lymphoma (FL), and relapsed small lymphocytic lymphoma (SLL). For the treatment of relapsed CLL, it is currently indicated as a second-line agent in combination with rituximab in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities, while in the treatment of FL and SLL it is intended to be used in patients who have received at least two prior systemic therapies. More specifically, idelalisib targets P110δ, the delta isoform of the enzyme phosphatidylinositol-4,5-bisphosphate 3-kinase, also known as PI-3K. The PI-3Ks are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. In contrast to the other class IA PI3Ks p110α and p110β, p110δ is principally expressed in leukocytes (white blood cells) and is important for the function of T cells, B cell, mast cells and neutrophils. By inhibiting this enzyme, idelalisib induces apoptosis of malignant cells and inhibits several cell signaling pathways, including B-cell receptor (BCR) signaling and C-X-C chemokine receptors type 5 and type 4 signalling, which are involved in trafficking and homing of B-cells to the lymph nodes and bone marrow. Treatment of lymphoma cells with idelalisib has been shown to result in inhibition of chemotaxis and adhesion, and reduced cell viability.
Ruxolitinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Nilotinib
Nilotinib {u} may lead to a major life threatening interaction when taken with {v} Idelalisib
Ruxolitinib {u} (Compound) binds {v} (Gene) PLK3
PLK3 {u} (Gene) is upregulated by {v} (Compound) Irinotecan
Irinotecan {u} may lead to a major life threatening interaction when taken with {v} Idelalisib
Ruxolitinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Mercaptopurine
Mercaptopurine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Idelalisib
Ruxolitinib {u} (Compound) binds {v} (Gene) BMP2K
BMP2K {u} (Gene) is bound by {v} (Compound) Sunitinib
Sunitinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Idelalisib
Ruxolitinib {u} (Compound) binds {v} (Gene) PLK3
PLK3 {u} (Gene) is upregulated by {v} (Compound) Teniposide
Teniposide {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Idelalisib
Ruxolitinib {u} (Compound) binds {v} (Gene) BMP2K
BMP2K {u} (Gene) is bound by {v} (Compound) Bosutinib
Bosutinib {u} may lead to a major life threatening interaction when taken with {v} Idelalisib
Ruxolitinib {u} (Compound) binds {v} (Gene) IRAK1
IRAK1 {u} (Gene) is downregulated by {v} (Compound) Omacetaxine mepesuccinate
Omacetaxine mepesuccinate {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Idelalisib
Ruxolitinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is palliated by {v} (Compound) Methylprednisolone
Methylprednisolone {u} may lead to a major life threatening interaction when taken with {v} Idelalisib
Ruxolitinib {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Sibutramine
Sibutramine {u} may cause a minor interaction that can limit clinical effects when taken with {v} Idelalisib
Ruxolitinib {u} (Compound) binds {v} (Gene) ROCK1
ROCK1 {u} (Gene) is downregulated by {v} (Compound) Irinotecan
Irinotecan {u} may lead to a major life threatening interaction when taken with {v} Idelalisib
Ruxolitinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Nilotinib (Compound) and Nilotinib may lead to a major life threatening interaction when taken with Idelalisib
Ruxolitinib (Compound) binds PLK3 (Gene) and PLK3 (Gene) is upregulated by Irinotecan (Compound) and Irinotecan may lead to a major life threatening interaction when taken with Idelalisib
Ruxolitinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Mercaptopurine (Compound) and Mercaptopurine may cause a moderate interaction that could exacerbate diseases when taken with Idelalisib
Ruxolitinib (Compound) binds BMP2K (Gene) and BMP2K (Gene) is bound by Sunitinib (Compound) and Sunitinib may cause a moderate interaction that could exacerbate diseases when taken with Idelalisib
Ruxolitinib (Compound) binds PLK3 (Gene) and PLK3 (Gene) is upregulated by Teniposide (Compound) and Teniposide may cause a moderate interaction that could exacerbate diseases when taken with Idelalisib
Ruxolitinib (Compound) binds BMP2K (Gene) and BMP2K (Gene) is bound by Bosutinib (Compound) and Bosutinib may lead to a major life threatening interaction when taken with Idelalisib
Ruxolitinib (Compound) binds IRAK1 (Gene) and IRAK1 (Gene) is downregulated by Omacetaxine mepesuccinate (Compound) and Omacetaxine mepesuccinate may cause a moderate interaction that could exacerbate diseases when taken with Idelalisib
Ruxolitinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is palliated by Methylprednisolone (Compound) and Methylprednisolone may lead to a major life threatening interaction when taken with Idelalisib
Ruxolitinib (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Sibutramine (Compound) and Sibutramine may cause a minor interaction that can limit clinical effects when taken with Idelalisib
Ruxolitinib (Compound) binds ROCK1 (Gene) and ROCK1 (Gene) is downregulated by Irinotecan (Compound) and Irinotecan may lead to a major life threatening interaction when taken with Idelalisib