Interaction Checker

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Etravirine Interactions.

Wednesday 05 September 2007

Interactions with etravirine are now available on the website.

Etravirine (TMC125) is a next generation NNRTI that shows high intrinsic activity against both wild-type HIV-1 and strains with resistance-inducing mutations. Etravirine is metabolised by CYP3A4, CYP2C19 and UDP-glucuronyl transferase, and has been shown to induce CYP3A and inhibit CYP2C19 in vivo.

A substantial improvement in the oral bioavailability was achieved by means of reformulation, with the licensed phase III formulation (F060) showing a 9-fold increase in AUC when compared to a phase II formulation (TF035). As a result of the reformulation, several phase II formulations (TF002, TF034, TF035) and doses have been used in interaction studies as well as the phase III formulation (F060, 200 mg twice daily). However, interactions are independent of formulation (Kakuda T, et al. 8th International Congress on HIV Therapy, Glasgow, November 2006, abstract PL5.2).

An interaction chart has been produced to summarise the studies performed to date. Interactions between etravirine and the other anti-HIV drugs (i.e. as rows) have been added to the charts. It is envisaged that interactions between etravirine and other drugs (i.e. a column) will be added once etravirine is licensed in Europe and/or the US.

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