Question
How important is it to take etravirine with food?
12 May 2009. Related: Adherence, All topics, Drug interactions.
The leaflet that comes with etravirine says to take etravirine with a meal. How important is this and was does ‘with a meal’ mean?
Answer
The food advice is very important. If you take etravirine without food you only get half the drug levels and would risk your treatment failing and developing resistance. It is therefore very important that you take etravirine with a meal.
The details of the food interaction study are interesting because it showed than different types of food have a different effect.
For example, most foods were fine, but the study seems to show that some level of fat is important. A standard breakfast, a high fat breakfast or just a croissant with butter and jam were all okay. However, a high fibre meal (fruit, fruit juice, mixed grain bread and jam) did not have the same effect.
So what many people think of as a full ”healthy’ breakfast may not be enough but a lighter breakfast snack with some fat is okay.
When the regulatory agencies (the EMEA in Europe and the FDA in the US) interpreted the results, through various complicated analyses, they decided that any meal would be sufficient, and didn’t break the type of food down any further.
If you are taking a drug, this can be very confusing. More information should be provided whenever there is a food interaction. It should give a guide depending on the mechanism of the effect. If absorption is improved by fat, it should indicate the minimum fat percentage or calorie count. If is it related to stomach acidity, it should probably be either fasted or with a minimum calorie count etc.
Although the EMEA and FDA say that any meal is okay, if you want to optimise the drug levels, then, based on the study, including some fat in the meal may help.
Details of the types of meal in the study are shown below.
Options 1 and 2 produced much lower drug levels.
Options 3, 4, and 5 were judged to be similar.
Options studied:
1) fasted (ie on an empty stomach)
2) a high fibre breakfast: 320g mixed fresh fruit, a banana, orange juice + 2 slices of mixed grain toast + jam.
855g: 685 calories, 4% fat, 89% carbs, 8% protein, 8g fibre
3) a standard breakfast: 4 slices of bread, butter, jam, 2 slices of ham or cheese, 2 cups of coffee with milk/sugar.
213g: 561 calories, 24% fat, 61% carbs, 16% protein, 16g fibre
4) a snack breakfast: one croissant, butter, jam, coffee, milk/sugar
855g: 345 calories, 45% fat, 49% carbs, 6% protein, 1.3g fibre
5) a high fat breakfast: 2 fried eggs, 2 rashers of bacon, 1 croissant, 2 slices of white bread., butter, 30g bar of chocolate, coffee + milk/sugar.
468g: 1,160 calories, 54% fat, 32% carbs, 14% protein, 2.2g fibre
Ref: Scohller-Gyure M et al. Effect of food on the oral bioavailability of the phase III formulation of TMC-125 (etravirine). 7th International PK Workshop, Lisbon, 2006. Abstract 60.
PDF of study poster:
Effect of food on the oral bioavailability of the phase III formulation of TMC125 (etravirine)
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