Selexipag is a novel, oral, selective prostacyclin (PGI2) receptor agonist in clinical development for the treatment of pulmonary arterial hypertension. Film-coated tablets with strength between 200 and 1,600 μg were used. Bioequivalence between 8 x 200 μg and a new 1,600 μg tablet was evaluated at steady state in healthy male subjects. This was an open-label, 2-treatment, 2-period, crossover, up-titration, phase 1 study. The treatments were selexipag at 1,600 μg b.i.d. for 4.5 days either as 8 x 200 μg tablets (reference: A) or 1 x 1,600 μg tablet (test: B), both preceded by an up-titration phase starting from 400 μg b.i.d. doses, in 200-μg steps every 4th day. Subjects were randomized 1 : 1 to the A-B or B-A sequence. The pharmacokinetics and tolerability of selexipag and its active metabolite, ACT-333679, were investigated. 80 subjects were enrolled in the study: 65 subjects completed the study according to protocol, and 15 subjects withdrew from the study. The most frequent adverse events (AEs) were headache (86%), myalgia (73%), and jaw pain (73%). There was no difference in nature and overall frequency of AEs between the two treatments. Steady state was attained within 3 days of the selexipag 1,600 Î¼g b.i.d. The 90% confidence intervals (CIs) of the geometric mean ratio (B/A) at steady state for AUCÏ and Cmax,ss were within (0.80, 1.25) bioequivalence interval: (0.92, 1.06) and (0.95, 1.14), respectively, for selexipag and (0.95, 1.06) and (0.94, 1.07), respectively, for the active metabolite, ACT-333679. Bioequivalence was demonstrated between 8 x 200 μg and 1 x 1,600 μg selexipag at steady state.
Selexipag is a novel , oral , selective prostacyclin ( PGI2 ) receptor agonist in clinical development for the treatment of pulmonary arterial hypertension . Film - coated tablets with strength between 200 and 1,600 μg were used . Bioequivalence between 8 x 200 μg and a new 1,600 μg tablet was evaluated at steady state in healthy male subjects . This was an open - label , 2-treatment , 2-period , crossover , up - titration , phase 1 study . The treatments were selexipag at 1,600 μg b.i.d . for 4.5 days either as 8 x 200 μg tablets ( reference : A ) or 1 x 1,600 μg tablet ( test : B ) , both preceded by an up - titration phase starting from 400 μg b.i.d . doses , in 200-μg steps every 4th day . Subjects were randomized 1 : 1 to the A - B or B - A sequence . The pharmacokinetics and tolerability of selexipag and its active metabolite , ACT-333679 , were investigated . 80 subjects were enrolled in the study : 65 subjects completed the study according to protocol , and 15 subjects withdrew from the study . The most frequent adverse events ( AEs ) were headache ( 86 % ) , myalgia ( 73 % ) , and jaw pain ( 73 % ) . There was no difference in nature and overall frequency of AEs between the two treatments . Steady state was attained within 3 days of the selexipag 1,600 Î¼g b.i.d . The 90 % confidence intervals ( CIs ) of the geometric mean ratio ( B / A ) at steady state for AUCÏ and Cmax , ss were within ( 0.80 , 1.25 ) bioequivalence interval : ( 0.92 , 1.06 ) and ( 0.95 , 1.14 ) , respectively , for selexipag and ( 0.95 , 1.06 ) and ( 0.94 , 1.07 ) , respectively , for the active metabolite , ACT-333679 . Bioequivalence was demonstrated between 8 x 200 μg and 1 x 1,600 μg selexipag at steady state .
Selexipag is used for which disease?
Selexipag is used for which disease ?
pulmonary arterial hypertension
pulmonary arterial hypertension