Important note: Information in this article was accurate in June 2006. The state of the art may have changed since the publication date.
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HIV Treatment Bulletin - Vol. 7, No. 6, June 2006
Ben Cheng, HIV i-Base
TMC-278 is a new non-nucleoside reverse transcriptase inhibitor in early stage clinical development. It had been previously reported that many of the commonly used HIV treatments and drugs used to treat and prevent opportunistic infections might interact with TMC-278.
Two separate studies, involving 16 HIV-negative individuals in each study, evaluated how ketoconazole and rifampin might affect TMC-278 drug levels. Rifampin significantly reduced TMC-278 levels by an average of 80% over a 24 hour period and perhaps more importantly, TMC-278 levels were reduced by 89% at its lowest level (commonly referred to as Cmin), usually found right before taking the next dose. TMC-278 had no effects on rifampin drug levels. This marked reduction in TMC-278 levels has led to the recommendation that the two drugs should not be used together.
The second study found that ketoconazole increased TMC-278 levels by an average of 49% over a 24 hour period and TMC-278 reduced ketoconazole levels by 24%. It is likely that there will have to be a change in the dose of TMC-278 if the drug is used in combination with ketoconazole.
Ref: van Heeswijk R et al. The effects of CYP3A4 modulation on the pharmacokinetics of TMC-278, an investigational non-nucleoside reverse transcriptase inhibitor (NNRTI). 7th International Workshop on Clinical Pharmacology of HIV Therapy, 20-22 April 2006, Lisbon. Abstract 74.
2006-06-10
IB060706-15
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