Pharmacokinetics, safety and efficacy of darunavir/ritonavir in treatment-experienced children and adolescents

Objective: To assess pharmacokinetics, safety and efficacy of darunavir/ritonavir (DRV/r) and optimized background regimen in treatment-experienced patients (6-17 years). Design: Forty-eight-week, open-label, two-part, phase II study. Methods: In part I, 44 patients were randomized (1 : 1 ratio) to...

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Detalles Bibliográficos
Autores: Blanche, Stephane, Bologna, Rosa, Cahn, Pedro, Rugina, Sorin, Flynn, Patricia, Fortuny, Claudia, Vis, Peter, Sekar, Vanitha, van Baelen, Ben, Dierynck, Inge, Spinosa-Guzman, Sabrina
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2009
País:España
Institución:Fundació Sant Joan de Déu
Repositorio:r-FSJD. Repositorio Institucional de Producción Científica de la Fundació Sant Joan de Déu
OAI Identifier:oai:fsjd.fundanetsuite.com:p6029
Acceso en línea:https://fsjd.fundanetsuite.com/Publicaciones/ProdCientif/PublicacionFrw.aspx?id=6029
Access Level:acceso abierto
Palabra clave:children
darunavir
HIV
safety
treatment-experienced
Descripción
Sumario:Objective: To assess pharmacokinetics, safety and efficacy of darunavir/ritonavir (DRV/r) and optimized background regimen in treatment-experienced patients (6-17 years). Design: Forty-eight-week, open-label, two-part, phase II study. Methods: In part I, 44 patients were randomized (1 : 1 ratio) to receive a body weight-adjusted, adult-equivalent dose (group A) or a 20-33% higher DRV/r twice daily (b.i.d.) dose (group B). Pharmacokinetics, safety and efficacy were assessed following 2-week dosing (part I), which determined dosing for part II (evaluated 48-week safety and efficacy). Results: In part I, both groups met the protocol-specified criteria for pharmacokinetics and showed favorable tolerability and efficacy. The following body-weight doses were selected: DRV/r 375/50 mg b.i.d. (20-<30 kg), 450/60 mg b.i.d. (30-<40 kg) and 600/100 mg b.i.d. (>= 40 kg); these gave an AUC(24h), C(0h), and C(max) of 102, 114 and 112%, respectively, versus the corresponding mean adult pharmacokinetic parameter. In part II, 80 patients received DRV/r (median age: 14 years, mean baseline HIV-1 RNA: 4.64 log(10)copies/ml). One patient (1%) discontinued (treatment-unrelated grade 3 anxiety). An abnormal mean baseline triglyceride level was normalized at 48 weeks (P<0.01). At week 48, 65% had at least 1.0 log(10)HIV-1 RNA reduction; 59 and 48% achieved HIV-1 RNA less than 400 and less than 50 copies/ml, respectively (time-to-loss-of-virologic response). Mean age-adjusted weight z-score increased by 0.2 (P=0.003). Conclusion: In treatment-experienced children and adolescents, DRV/r showed comparable exposure to adults with appropriate dose selection, favorable safety and tolerability, improved body weight and significant virologic response. DRV/r is a valuable therapeutic option for this population. (C) 2009 Wolters Kluwer Health vertical bar Lippincott Williams & Wilkins