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idelalisib (Zydelig)
Indications:
- chronic lymphocytic leukemia (CLL) in combination with Rituximab
- follicular B-cell non-Hodgkin lymphoma*
- small lymphocytic lymphoma* [3]
* intended for use in patients with at least t2 prior systemic therapies [3]
Dosage:
- 150 mg PO twice daily [4]
Adverse effects:
- common
- diarrhea,
- pyrexia (fever), chills
- fatigue
- nausea
- cough, pneumonia
- abdominal pain
- rash
- neutropenia
- hypertriglyceridemia
- hyperglycemia
- elevated serum transaminases
- boxed warning
- diarrhea
- colitis
- intestinal perforation
- hepatotoxicity
- pneumonitis
Laboratory:
- complete blood count: neutropenia
- serum triglycerides: hypertriglyceridemia
- serum glucose: hyperglycemia
- liver function tests: elevated serum transaminases
Mechanism of action:
- inhibits PI-3-kinase p100 subunit
- PI-3-kinase p100 inhibition in regulatory T cells activates CD8+ cytotoxic T cells & induces tumour regression [2]
Comparative biology:
- active against solid tumors in mice [2]
General
small inhibitory antineoplastic agent (ib drug)
Database Correlations
PUBCHEM cid=11625818
References
- Furman RR et al.
Idelalisib and rituximab in relapsed chronic lymphocytic
leukemia.
N Engl J Med. 2014 Mar 13;370(11):997-1007.
PMID: 24450857
- Ali K, Soond DR, Pineiro R et al
Inactivation of PI(3)K p110 breaks regulatory T-cell-mediated
immune tolerance to cancer.
Nature. 2014 Jun 19;510(7505):407-11
PMID: 24919154
- Hirsch E and Novelli F.
Natural-born killers unleashed.
Nature 2014 Jun 19; 510:342
PMID: 24919150
- FDA News Release. July 23, 2014
FDA approves Zydelig for three types of blood cancers.
http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm406387.htm
- Gopal AK et al
PI3K inhibition by idelalisib in patients with relapsed indolent
lymphoma.
N Engl J Med. 2014 Mar 13;370(11):1008-18
PMID: 24450858