| Texto completo | |
| Autor(es): |
Pippa, Leandro Francisco
;
Vieira, Carolina Pinto
;
Caris, Juciene Aparecida
;
Rocha, Adriana
;
Marques, Maria Paula
;
Garcia, Camile Prates
;
Rezende, Rosamar Eulira Fontes
;
Lanchote, Vera Lucia
Número total de Autores: 8
|
| Tipo de documento: | Artigo Científico |
| Fonte: | CLINICAL PHARMACOLOGY & THERAPEUTICS; v. 114, n. 1, p. 9-pg., 2023-05-16. |
| Resumo | |
The activity of the membrane transporters organic anion-transporting polypeptide 1B1 (OATP1B1) & breast cancer resistance protein (BCRP) (rosuvastatin) and P-glycoprotein (P-gp) (fexofenadine) was evaluated in patients with chronic hepatitis C virus (HCV) infection (n = 28), genotypes 1 and 3, investigated before the treatment with direct-acting antiviral agents (Phase 1) and up to 30 days after the assessment of the virologic response (Phase 2). Participants allocated in Groups 1 (n = 15; F0/F1 and F2, mild to moderate liver fibrosis) and 2 (n = 13; F3 and F4, advanced course of liver fibrosis/cirrhosis) received in both phases fexofenadine (10 mg) and rosuvastatin (2 mg). OATP1B1 & BCRP activity (rosuvastatin area under the plasma concentration-time curve of rosuvastatin from time zero to infinity (AUC(0-infinity))) was reduced in Groups 1 and 2, respectively, by 25% (ratio 0.75 (0.53-0.82), P < 0.01) and 31% (ratio 0.69 (0.46-0.85), P < 0.05) in Phase 1 compared with Phase 2. OATP1B1 & BCRP activity was reduced in Phases 1 and 2, respectively, by 49% (median ratio 1.51 (1.17-2.20), P < 0.05) and 61% (ratio 1.39 (1.16-2.02), P < 0.01) in Group 2 compared with Group 1. P-gp activity (fexofenadine AUC(0-8)) was also reduced in Phase 1 compared with Phase 2 (ratio Phase2/Phase1 0.79 (0.66-0.96) in Group 1 and 0.81 (0.69-0.96) in Group 2) as well as in Group 2 compared with Group 1 in both Phases (ratio Group2/Group1 1.47 (1.08-2.01) in Phase 1 and 1.51 (1.10-2.07) in Phase 2). Thus, clinicians administering OATP1B1 & BCRP and P-gp substrates with low therapeutic indexes should consider the evolution of the treatment and the stage of HCV infection. (AU) | |
| Processo FAPESP: | 18/05616-3 - Farmacocinética clínica em doenças infecciosas |
| Beneficiário: | Vera Lúcia Lanchote |
| Modalidade de apoio: | Auxílio à Pesquisa - Temático |