Pharmacokinetics, Safety, Tolerability and Antiviral Activity of Switching to Oral Rilpivirine in Combination With Other Antiretroviral Therapy in Virologically Suppressed Children Living With HIV-1 Infection: Forty-eight-week Results From the Phase 2, Open-label, Single-arm, PICTURE Study

Background: – PICTURE (NCT04012931) was a phase 2, open-label, single-arm, multicenter study evaluating pharmacokinetics (PK), safety, tolerability and antiviral activity of oral rilpivirine in combination with other antiretroviral therapy (ART) in children living with HIV-1 with virologic suppression. Methods: – Children (≥2 to <12 years, ≥10 kg) living with HIV-1, virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable ART were enrolled. Weight-based rilpivirine [25 mg once-daily (qd) for ≥25 kg, 15 mg (6 × 2.5 mg) qd for 20 kg to <25 kg and 12.5 mg (5 × 2.5 mg) qd for 10 to <20 kg in film-coated or investigational dispersible tablet formulations] was administered orally in combination with background ART for 48 weeks. The primary objectives were evaluation of rilpivirine steady-state PK, determination of an appropriate weight-based dose, and safety and tolerability when combined with other ARTs. Results of the primary (week 24) and final (week 48) analyses are presented. Results: – Of 40 participants screened, 26 (65%) were enrolled and treated with rilpivirine. All participants completed the week 48 visit and were included in the final analysis. PK parameters were observed to be in the target range for all rilpivirine weight-based doses. Through week 48, 19/26 (73.1%) participants had ≥1 adverse event; all grade 1–2 and none were treatment related. All 26 participants (100%) receiving rilpivirine in combination with ART remained virologically suppressed at both weeks 24 and 48. Adherence to treatment was 98.99%. Conclusion: – Rilpivirine in combination with background ART was well-tolerated and maintained virologic suppression from baseline through week 48 in the studied population of children living with HIV-1. Rilpivirine exposure was within the target range for all doses.