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Title: Idelalisib  
Author: World Heritage Encyclopedia
Language: English
Subject: Phosphoinositide 3-kinase inhibitor, Syk, Chemotherapy, Cell-cycle nonspecific antineoplastic agents, Hazardous drugs
Publisher: World Heritage Encyclopedia


Systematic (IUPAC) name
Clinical data
Trade names Zydelig
  • US: D (Evidence of risk)
Legal status
Routes of
CAS Registry Number
ATC code L01
PubChem CID:
Synonyms GS-1101, CAL-101
Chemical data
Formula C22H18FN7O
Molecular mass 415.42 g/mol

Idelalisib (trade name Zydelig, codenamed GS-1101 or CAL-101) is a drug used for the treatment of chronic lymphocytic leukemia. The substance acts as a phosphoinositide 3-kinase inhibitor; more specifically, it blocks P110δ, the delta isoform of the enzyme phosphoinositide 3-kinase.[1][2]

Medical uses

Idelalisib is a second line drug for patients whose chronic lymphocytic leukemia (CLL) has relapsed. Used in combination with rituximab,[3] idelalisib is to be used in patients for whom rituximab alone would be considered appropriate therapy due to other existing medical conditions.[3] It appears to be very effective drug and leads to rapid resolution of lymphadenopathy and splenomegaly. However, the lymphocyte counts takes longer to decrease to normal levels with idelalisib. Idelalisib is effective in patients who have a p53 mutation, which otherwise tends to impart a poor prognosis in CLL patients. This is important as even the first line chemotherapy regimens, such as those incorporating fludarabine are ineffective in patients with p53 mutation. It is also being studied in clinical trials for first line treatment in high risk CLL patients, who are otherwise unable to tolerate aggressive chemotherapy due to their medical history or age.

Adverse effects

Clinical symptoms include diarrhea, fever (pyrexia), fatigue, nausea, cough, pneumonia, abdominal pain, chills and rash. Laboratory abnormalities may include: neutropenia, hypertriglyceridemia, hyperglycemia and elevated levels of liver enzymes. Idelalisib's safety and effectiveness to treat relapsed FL and relapsed SLL were established in a clinical trial with 123 participants with slow-growing (indolent) non-Hodgkin lymphomas. All participants were treated with idelalisib and were evaluated for complete or partial disappearance of their cancer after treatment (objective response rate, or ORR). Results showed 54 percent of participants with relapsed FL and 58 percent of participants with SLL experienced ORR.[4]

Mechanism of action

It is a PI3Kinase delta inhibitor.



In July 2014, the FDA and EMA granted idelalisib approval to treat different types of leukemia.[4][5] The FDA is also granted approval for idelalisib to treat patients with relapsed follicular B-cell non-Hodgkin lymphoma (FL) and relapsed small lymphocytic lymphoma (SLL). Idelalisib is intended to be used in patients who have received at least two prior systemic therapies.


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