In May, the U.S. Food and Drug Administration granted approval to the NNRTI rilpivirine (Edurant) for use in treatment-naive patients with HIV-1 infection.
The recommended dosage is 25 mg once daily. It requires gastric acid for absorption, and therefore should be taken with a meal.
Important points emerged from registrational studies.
In Phase III studies, rilpivirine was compared with efavirenz, in combination with 2 NRTIs (predominantly tenofovir + emtricitabine). The overall rates of treatment failure were not significantly different in the two groups, but several important distinctions emerged:
|Subjects who received rilpivirine had higher rates of virologic failure but lower rates of treatment discontinuation owing to adverse effects.|
|The higher rates of virologic failure in rilpivirine recipients occurred predominantly in those with pretreatment HIV RNA of >100,000 copies/mL.|
|Virologic failure on rilpivirine-containing regimens was commonly associated with resistance mutations to both NNRTI and NRTI agents, and with cross-resistance to other NNRTIs.|
Little information is available on drug-drug interactions involving rilpivirine, but a number of important interactions have been recognized. Of the ARVs, efavirenz may cause a significant and prolonged lowering of rilpivirine concentrations even after it is discontinued, and it is not known whether it is safe to switch directly from efavirenz to rilpivirine (see Sustained Effect of Efavirenz on Rilpivirine Serum Concentrations). Important recognized interactions with other drugs include those with rifamycins (these drugs should be avoided) and acid-blocking medications (proton pump inhibitors should be avoided; other types require time-specific administration).
The package label is available on the FDA website.