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The Body Covers: The 39th Annual Meeting of the Interscience Conference on Antimicrobial Agents and Chemotherapy
Slide Session 66.A: Drug Interactions in HIV Therapy

September 27, 1999

Tipranavir, formerly PNU-140690 is a nonpeptidic HIV protease inhibitor that is active in vitro against highly resistant viruses. It was tested in 23 healthy volunteers in theses studies.

Tipranavir is a potent inducer of CYP 3A and a P glycoprotein substrate. It induces a significant increase in ritonavir metabolism, with an 80-88% reduction in AUC and a decrease in half-life and peak levels. There is a 20-fold decrease in trough levels (Cmin).

On the other hand, ritonavir causes a marked rise in all PK parameters of tipranavir, with an increase in AUC of 12 fold and an increase of Cmin of 45 fold.

The second study reported here showed that even a low dose of ritonavir could produce this effect with tipranavir.

It appears that Pharmacia & Upjohn, the manufacturer of tipranavir, is already talking to Abbott about producing a combination pill to improve the pharmakokinetics of tipranavir.

Abstract: Pharmacokinetic (PK) Interaction between the HIV Protease Inhibitors Tipranavir and Ritonavir (Paper 657)
Authored by: J. R. Baldwin, et al.

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