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Updated: Feb 13, 2026

Examining BCL-2 Family Function with Large Unilamellar Vesicles
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Published on: October 5, 2012

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Targeting BCL-2 in Hematologic Malignancies

Nadia Khan1, Brad Kahl2

  • 1Fox Chase Cancer Center, Philadelphia, PA, USA. Nadia.Khan@fccc.edu.

Targeted Oncology
|March 10, 2018
PubMed

Insights

Venetoclax, a B-cell lymphoma 2 (BCL-2) inhibitor, targets cancer

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Resistance to apoptosis is a key feature of cancer.
  • The B-cell lymphoma 2 (BCL-2) protein family regulates apoptosis and is often upregulated in cancers, leading to chemotherapy resistance.
  • BCL-2 proteins are therefore attractive therapeutic targets for cancer treatment.

Purpose of the Study:

  • To describe Venetoclax, a small-molecule inhibitor targeting BCL-2 proteins.
  • To highlight Venetoclax's mechanism of action as a BCL-2 homology domain 3 (BH3) mimetic.
  • To summarize the clinical development and approved indications of Venetoclax.

Main Methods:

  • Venetoclax functions as a BCL-2 homology domain 3 (BH3) mimetic.
  • It is an orally administered small molecule.
  • Clinical trials assess its efficacy in various hematological malignancies.

Main Results:

  • Venetoclax is approved as a monotherapy for certain chronic lymphocytic leukemia (CLL) patients in the USA and EU.
  • The drug is in Phase III clinical development for multiple myeloma (MM).
  • Phase II or I/II trials are ongoing for acute myeloid leukemia and other B-cell malignancies, including diffuse large B-cell lymphoma, Waldenstrom's macroglobulinaemia, follicular lymphoma, and mantle-cell lymphoma.

Conclusions:

  • Venetoclax is an effective apoptosis stimulant targeting BCL-2 proteins.
  • Its approved use in CLL and ongoing trials in other hematological cancers demonstrate its therapeutic potential.
  • Venetoclax represents a significant advancement in targeting BCL-2-driven cancers.

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