Phase I pharmacokinetic and pharmacodynamic study of the prenyl transferase inhibitor AZD3409 in patients with advanced cancer
2008

Study of AZD3409 in Advanced Cancer Patients

Sample size: 29 publication Evidence: moderate

Author Information

Author(s): Appels N M G M, Bolijn M J, Chan K, Stephens T C, Hoctin-Boes G, Middleton M, Beijnen J H, de Bono J S, Harris A L, Schellens J H M

Primary Institution: The Netherlands Cancer Institute

Hypothesis

The aim of this phase I study was to determine the maximum tolerated dose, toxicities, pharmacokinetics and pharmacodynamics of AZD3409.

Conclusion

Chronic oral dosing with AZD3409 is feasible and results in significant inhibition of FTase activity.

Supporting Evidence

  • AZD3409 was administered orally to patients with advanced solid malignancies using an interpatient dose-escalation scheme starting at 500 mg.
  • The MTD of part A was defined as 750 mg b.i.d. in the fasted state.
  • Adverse events were mainly gastrointestinal and the severity was on average mild to moderate and reversible.
  • Pharmacodynamic studies showed that farnesyltransferase (FTase) was inhibited at all dose levels.
  • The maximal FTase inhibition was estimated at 49±11%.

Takeaway

This study tested a new cancer drug called AZD3409 to see how much can be safely given and how it works in the body. It found that the drug can effectively block a specific enzyme related to cancer.

Methodology

This was a multicenter, dose-escalating phase I study where AZD3409 was administered orally to patients with advanced solid malignancies.

Limitations

The study was limited by the small sample size and the lack of objective tumor responses.

Participant Demographics

{"median_age":59,"age_range":"38-77","sex_distribution":{"male":13,"female":16},"tumor_types":{"colorectal":9,"breast":6,"oesophagus":3,"skin_soft_tissue":3,"pancreas":1,"kidney":1,"liver":1,"other":3}}

Statistical Information

P-Value

0.006

Statistical Significance

p=0.006

Digital Object Identifier (DOI)

10.1038/sj.bjc.6604402

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