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Last Updated: 04/25/2012

ABT-888 (NSC 737664)


DNA damaging agents are among the most successful treatments for cancer. The enzyme Poly(ADP-ribose)polymerase (abbreviated PARP) can facilitate repair of DNA damage caused by insult from chemotherapeutic agents and radiation. Increased PARP activity is associated with survival of some cancer cells. ABT-888, an orally bioavailable PARP-inhibitor developed by Abbott Laboratories, significantly enhanced the antitumor activity of DNA-damaging agents and radiation in preclinical models. Further development of this compound is ongoing.

Basic Chemistry

Preclinical Studies

  • in vitro
    • Biochemical Assays
      • Potency was determined in PARP-1 and PARP-2 enzyme assays where the Kis are 5.4 and 2.9 nM, respectively.
      • ABT-888 inhibits the PARP directed formation of its product, PAR, with an EC50 of 2.5 nM in cells.
  • in vivo
    • Efficacy Studies - In vivo efficacy was evaluated in syngeneic and xenograft models in combination with temozolomide, platinums, cyclophosphamide, and ionizing radiation.
    • Pharmacokinetic Studies
      • ABT-888 has good oral bioavailability, and readily crosses the blood-brain barrier.
      • ABT-888 profoundly inhibits the formation of PAR in tumors in xenograft models.

Clinical Studies

  • Investigational New Drug (IND) Information
    • CTEP Exploratory IND
    • Abbott Laboratories IND
  • Active and Closed Clinical Trials
    • ABT-888 has entered a Phase 0 trial for subjects with refractory solid tumors and lymphoid malignancies.
    • Phase I studies are expected to start in 2007.
    • Please see for information on clinical trials with ABT-888.