Lack of Pharmacokinetic Interaction Between RitonavirBoosted GS9137 Elvitegravir and Tipranavirr

1
Lack of Pharmacokinetic Interaction Between
Ritonavir-Boosted GS-9137 (Elvitegravir) and
Tipranavir/r

• Anita A. Mathias1, John Hinkle1, Jeff Enejosa1,
• Peter J. Piliero2, and Brian P. Kearney1

1 Gilead Sciences, Foster City, CA 2 Boehringer
Ingelheim Pharmaceuticals, Inc, Ridgefield, CT
4th International AIDS Conference (IAS) July
22-25, 2007 Sydney, Australia
2
Results

• Open-label, multiple dose, three treatment, six
  sequence crossover study

• TPV Ctau of 6050 ng/mL 5-fold greater than
  protein-binding adjusted IC90 for multiple PI
  resistant HIV-1 (King JR and Acosta EP, Clin.
  Pharmacokinet 2006 45(7)665-682)
• Ctau consistent with historical controls (US
  Prescribing Information)

• Safety
• No deaths, or SAE were reported in this study
• No subject discontinued for an AE during
  treatment of EVG/r alone 4 subjects
• discontinued for AE (G1/2 LFT elevations or
  rash) while receiving TPV/r

3
Conclusions

• The steady-state pharmacokinetics of EVG or TPV
  were not altered following coadministration of
  EVG with ritonavir-boosted TPV including
  maintenance of trough concentrations
• EVG can be coadministered with TPV/r without any
  dose adjustment
• Treatment with EVG/r alone was generally well
  tolerated. Treatment with TPV/r alone or in
  combination with EVG was associated with an
  increased incidence of treatment-emergent and
  -related adverse events