EDURANT®
(rilpivirine)
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EDURANT® (rilpivirine)
Medical Information
EDURANT - Pharmacokinetic Food Effects
Last Updated: 07/08/2026
Summary
- Administration of EDURANT without food or with a nutritional drink reduced the exposure by approximately 40-50% compared with administration with a standard meal.1
Crauwels et al (2013)1 evaluated the effect of fasting conditions and different meal types on rilpivirine (RPV) exposure.
Study Design/Methods
- This was a phase 1, open-label, randomized, 4-way crossover study in HIV-negative healthy subjects (N=20; 90% male; median age, 34.5 years).
- All subjects were administered 1 single EDURANT 75 mg tablet (75 mg formulation compositionally proportional to commercial 25 mg tablet) in 4 different sessions (random order), each separated by a washout period of ≥13 days. Subjects fasted for 10 hours, overnight, prior to each EDURANT administration.
- Normal-fat breakfast (533 kcal): standard breakfast (4 slices of bread, 1 slice of ham, 1 slice of cheese, butter, jelly and 2 cups of decaffeinated coffee or tea with milk and/or sugar, if desired)
- Fasting conditions (0 kcal): fasted ≥10 hours prior to dosing, until 4 hours after dosing
- High-fat breakfast (928 kcal): high-fat breakfast (2 eggs fried in butter, 2 strips of bacon, 2 slices of white bread with butter, 1 croissant with one slice of cheese and 240 mL of whole milk)
- Protein-rich drink (300 kcal): nutritional drink (240 mL of Ensure®
HP)
- Pharmacokinetic (PK) parameters for RPV including peak concentrations (Cmax), time to Cmax (tmax), half-life (t1/2), area under the plasma concentration-time curve (AUC), safety, and tolerability were evaluated.
- PK parameters for RPV administered after each treatment session are provided in Table: RPV PK Parameters.
- The mean plasma concentration-time profiles for RPV, when administered with a normal-fat and high-fat breakfast, were comparable.
- When EDURANT was administered in a fasted state, RPV AUClast and Cmax were reduced by 43% and 46%, respectively compared with a normal-fat breakfast. Likewise, when administered with a protein-rich drink, RPV AUClast and Cmax were reduced by 50% each.
| Normal-Fat Breakfast (Ref: n=19) | Fasting Conditions (Test: n=19) | High-Fat Breakfast (Test: n=19) | Protein-Rich Drink (Test: n=18) | |
|---|---|---|---|---|
| Mean Cmax, ng/mL (SD) | 296±118 | 170±66 | 280±103 | 156 ± 60 |
| Median tmax, hrs (range) | 5 (2-9) | 4 (2-24) | 5 (3-9) | 5 (4-9) |
| Mean AUClast, ng•h/mL (SD) | 10,340±3894 | 6320±2339 | 9717±3535 | 5437±2421 |
| Mean AUCinf, ng•h/mL (SD) | 11,450±4431 | 7202 ± 3024 | 10,670±4331 | 6094±3047 |
| Mean t1/2,term, hrsa | 48±22 | 55±28 | 43±17 | 47±23 |
| Least-squares means ratio for test to reference (90% confidence interval) | ||||
| Cmax | - | 0.54 (0.43-0.69) | 0.92 (0.81-1.05) | 0.50 (0.40-0.63) |
| AUClast | - | 0.57 (0.46-0.72) | 0.92 (0.80-1.07) | 0.50 (0.41-0.61) |
| AUCinf | - | 0.59 (0.47-0.74) | 0.91 (0.79-1.05) | 0.51 (0.42-0.62) |
| Abbreviations: AUCinf, area under the plasma concentration time curve from time point zero to infinity; AUClast, area under the plasma concentration time curve from administration until the last timepoint with a measurable concentration; Cmax, maximum plasma concentration; PK, pharmacokinetic; Ref, reference; SD, standard deviation; t1/2,term, terminal elimination half-life; tmax, time to Cmax. aAccurate determination of t1/2, term was not possible in all volunteers because t1/2, term was relatively long compared to the sampling of up to 168 hours (applicable to 5 volunteers when EDURANT was administered with a normal-fat breakfast, 9 volunteers when administered under fasting conditions, 3 volunteers when administered with a high-fat breakfast, and 6 volunteers when administered with a protein-rich drink). | ||||
- Five subjects reported 5 separate treatment-emergent adverse events (AEs) all rated DAIDS grade 1 or 2 (mild or moderate) in intensity [DAIDS: Division of Acquired Immunodeficiency Syndrome (grades the severity of adult and pediatric AEs)].
- One case of hot flush, reported when EDURANT was administered with a normal-fat breakfast, was considered possibly related to EDURANT.
- No AEs led to treatment discontinuation.
- Treatment-emergent laboratory abnormalities, primarily grade 1 or 2, were reported in all subjects.
- One grade 4 transient hyponatremia occurred when EDURANT was administered with a high-fat breakfast.
- Fifteen grade 3 abnormalities were reported in 8 subjects.
- An overestimation of these graded laboratory abnormalities may have occurred because local laboratory normal ranges did not always correspond to the DAIDS graded abnormalities defined in the protocol.
References
| 1 | Crauwels HM, van Heeswijk RP, Buelens A, et al. Impact of food and different meal types on the pharmacokinetics of rilpivirine. J Clin Pharmacol. 2013;53(8):834-840. |
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