The Sound of Evolution
Idelalisib
Mechanism of action:
Idelalisib is a PI3K-δ inhibitor. Phosphoinositide 3-kinase delta (PI3K-δ) is primarily expressed in various blood cells, especially B lymphocytes, and plays a key role in B cell receptor (BCR) signaling. Idelalisib inhibits PI3K-δ activity, blocking the conversion of PIP2 into PIP3 and thereby reducing the activity of downstream signaling pathways such as AKT and mTOR, leading to suppressed cell proliferation and increased apoptosis.
Reference(s):
1. Jin F et al. (2015). Clinical drug interaction profile of idelalisib in healthy subjects. J Clin Pharmacol.
2. Fiorcari S et al. (2013). The PI3-kinase delta inhibitor idelalisib (GS-1101) targets integrin-mediated adhesion of chronic lymphocytic leukemia (CLL) cell to endothelial and marrow stromal cells. PLoS One.
3. Flinn IW et al. (2014). Idelalisib, a selective inhibitor of phosphatidylinositol 3-kinase-delta, as therapy for previously treated indolent non-Hodgkin lymphoma. Blood.