AG3340 Exhibits Marked Anti-Tumor Activity in Preclinical Models

Strategic Insights -

Researchers at Agouron Pharmaceuticals released encouraging results from phase I studies and a preclinical study of their oral anti-angiogenesis drug, AG3340. The data were presented at the 10th European Organization for Research and Treatment of Cancer (EORTC) meeting in Amsterdam, the Netherlands. AG3340 demonstrated promising anti-tumor activity, with over 25% of patients experiencing stabilized disease for periods of 16 to 40 weeks.

Key Takeaways:

  • AG3340 showed marked anti-tumor activity in phase I studies, with more than 25% of 47 evaluable patients experiencing stabilized disease for 16 to 40 weeks.
  • In a separate phase I study, AG3340 in combination with chemotherapy was generally well tolerated among patients with advanced prostate cancer who were resistant to hormonal therapies.
  • AG3340 inhibited tumor growth in a preclinical study by 77%, reducing the formation of new tumor-associated blood vessels.
  • AG3340 selectively inhibits matrix metalloproteases (MMPs) believed to be involved in tumor progression.
  • Agouron Pharmaceuticals has initiated pivotal phase II/III clinical trials using AG3340 in combination with standard chemotherapy for patients with advanced non-small cell lung cancer or advanced hormone-refractory prostate cancer.
  • The safety and tolerability data from the phase I studies led to the initiation of clinical trials with AG3340 at 5mg, 10mg, and 15mg doses given BID.
  • AG3340's mechanism of action involves inactivating MMPs, which are enzymes involved in tumor growth, invasion, and metastasis.
  • Agouron is also conducting preclinical evaluations of third-generation MMP inhibitors with distinct selectivity profiles from AG3340.

Statistics:

  • 25% of 47 evaluable patients experienced stabilized disease for 16 to 40 weeks.
  • 3 patients achieved minor reductions in tumor volume.
  • 9 evaluable patients in two additional dosing groups had not yet received 16 weeks of treatment and are still under evaluation.
  • 5mg, 10mg, and 15mg doses of AG3340 were used in the phase II/III clinical trials.

Sources:

  • Agouron Pharmaceuticals' press release, June 17, 1998.
  • European Organization for Research and Treatment of Cancer (EORTC) meeting in Amsterdam, Netherlands.
  • Agouron Pharmaceuticals' web site at http://www.agouron.com.
  • Agouron Pharmaceuticals, Inc.'s Form 10-K for the fiscal year ended June 30, 1997.