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Home > A. Molecular pathology > Targeted therapy > Small molecules > idelalisib


Wednesday 19 April 2017


Idelalisib (trade name Zydelig, codenamed GS-1101 or CAL-101) is a drug used for the treatment of certain hematological malignancies.

The substance acts as a phosphoinositide 3-kinase inhibitor / PI-3Ks inhibitor; more specifically, it blocks P110δ, the delta isoform of the enzyme phosphoinositide 3-kinase.

PI3K(s)) 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.

PI3Ks are a family of related intracellular signal transducer enzymes capable of phosphorylating the 3 position hydroxyl group of the inositol ring of phosphatidylinositol (PtdIns).

The pathway, with oncogene PIK3CA and tumor suppressor PTEN, is implicated in insensitivity of cancer tumors to insulin and IGF1, and in calorie restriction.


- idelalisib-induced colitis