idelalisib (Zydelig)
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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
Adverse effects
- common
- boxed warning
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]
More general terms
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: https://www.ncbi.nlm.nih.gov/pubmed/24450857
- ↑ 2.0 2.1 2.2 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: https://www.ncbi.nlm.nih.gov/pubmed/24919154
Hirsch E and Novelli F. Natural-born killers unleashed. Nature 2014 Jun 19; 510:342 PMID: https://www.ncbi.nlm.nih.gov/pubmed/24919150 - ↑ 3.0 3.1 3.2 FDA News Release. July 23, 2014 FDA approves Zydelig for three types of blood cancers. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm406387.htm
- ↑ 4.0 4.1 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: https://www.ncbi.nlm.nih.gov/pubmed/24450858