Pharmacokinetic evaluation of oblimersen sodium for the treatment of chronic lymphocytic leukemia

Pooja P. Advani, Aneel Paulus, Ayesha Masood, Taimur Sher, Asher Chanan-Khan

Research output: Contribution to journalArticlepeer-review

26 Scopus citations


Introduction: Chronic lymphocytic leukemia (CLL) is the most common form of leukemia in the western hemisphere. Developing new therapies remains a priority as present treatment options do not offer a cure. BCL-2 overexpression in CLL is associated with aggressive disease features and resists chemotherapy. Oblimersen sodium (G3139) is a phosphorothioate oligonucleotide antisense drug targeting the BCL-2 mRNA and is the first antisense to reach advanced clinical testing in oncology. Preclinical evaluation has demonstrated good antineoplastic effect in B-cell cancers; several clinical trials have confirmed its safety and efficacy both alone and in combination with other therapeutics. Areas covered: This review focuses on the chemistry, pharmacodynamics, pharmacokinetics and clinical evaluation of oblimersen in CLL. PubMed and MEDLINE searches assisted in data collection. Expert opinion: Bcl-2 is an important target in CLL. Antisense therapy is a novel approach to target oncoproteins; this can be beneficial in the clinical setting. Oblimersen sodium demonstrates the clinical safety of the antisense therapeutic approach and, with chemotherapy, shows survival advantage in a subset of CLL patients. However, future approval of oblimersen sodium in CLL remains uncertain. Nevertheless, BCL-2 remains a critical target in drug development and is an area of high-priority research.

Original languageEnglish (US)
Pages (from-to)765-774
Number of pages10
JournalExpert Opinion on Drug Metabolism and Toxicology
Issue number6
StatePublished - Jun 2011


  • Bcl-2
  • antisense oligonucleotide
  • antisense oligonucleotide therapy
  • chronic lymphocytic leukemia
  • oblimersen sodium
  • phosphorothioate oligonucleotide

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology


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