Venetoclax: Bcl-2 inhibition for the treatment of chronic lymphocytic leukemia

G. Del Poeta, M. Postorino, L. Pupo, M. I. Del Principe, Tamara Bittolo, M. Dal Bo, F. Buccisano, B. Mariotti, E. Iannella, L. Maurillo, A. Venditti, V. Gattei, P. de Fabritiis, M. Cantonetti, S. Amadori

Research output: Contribution to journalArticlepeer-review

Abstract

Venetoclax (ABT-199) is a small-molecule selective oral inhibitor of the antiapoptotic protein Bcl-2 that promotes programmed cell death of chronic lymphocytic leukemia (CLL) cells regulating the release of proapoptotic factors, such as Smac/Diablo, apoptosis-inducing factor (AIF) and cytochrome c. In April 2016, the U.S. Food and Drug Administration (FDA) granted accelerated approval to venetoclax for patients diagnosed with CLL with 17p deletion, as detected by an FDA-approved test, who have received at least one prior therapy. This review will focus on the mechanism of action, preclinical studies and clinical development of venetoclax both as a monotherapy and in combination with other drugs for CLL in the current milieu of therapy dominated by novel tyrosine kinase inhibitors such as ibrutinib and idelalisib.

Original languageEnglish
Pages (from-to)249-260
Number of pages12
JournalDrugs of Today
Volume52
Issue number4
DOIs
Publication statusPublished - Apr 1 2016

Keywords

  • 17p deletion/TP53 mutation
  • ABT-199
  • Bcl-2
  • Chronic lymphocytic leukemia
  • Novel tyrosine kinase inhibitors
  • Venetoclax

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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