DDInter899 DDInter905
Ibrutinib is a small molecule that acts as an irreversible potent inhibitor of Burton's tyrosine kinase. It is designated as a targeted covalent drug and presented as a promising activity in B-cell malignancies in clinical trials. Ibrutinib was developed by Pharmacyclics Inc and was first approved by the FDA in November 2013 for the treatment of mantle cell lymphoma (MCL) under accelerated approval; however, in April 2023, the drug manufacturer withdrew the accelerated approvals for ibrutinib in the US. Ibrutinib was approved by the EMA in October 2014 and by Health Canada in November 2014. It is currently approved for the treatment of various conditions, such as chronic lymphocytic leukemia (CLL), Waldenström's Macroglobulinemia, and chronic graft versus host disease (cGVHD) in August 2017. Notably, ibrutinib became the first FDA-approved
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.
Idelalisib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Sibutramine
Idelalisib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Cannabidiol
Idelalisib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Eltrombopag
Idelalisib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Satralizumab
Idelalisib {u} may lead to a major life threatening interaction when taken with {v} Baricitinib
Idelalisib {u} may lead to a major life threatening interaction when taken with {v} Vinorelbine
Idelalisib may cause a minor interaction that can limit clinical effects when taken with Sibutramine
Idelalisib may cause a minor interaction that can limit clinical effects when taken with Cannabidiol
Idelalisib may cause a moderate interaction that could exacerbate diseases when taken with Eltrombopag
Idelalisib may cause a moderate interaction that could exacerbate diseases when taken with Satralizumab
Idelalisib may lead to a major life threatening interaction when taken with Baricitinib
Idelalisib may lead to a major life threatening interaction when taken with Vinorelbine