The prescribing information for Uptravi (selexipag; Actelion) has been updated to include a new contraindication and additional drug interaction information.
Uptravi is a prostacyclin receptor agonist indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression and reduce the risk of hospitalization for PAH. The labeling now states that the use of Uptravi with concomitant strong inhibitors of CYP2C8 (eg, gemfibrozil) is contraindicated. Studies have shown that concomitant administration with gemfibrozil doubled exposure to selexipag and increased exposure to the active metabolite by approximately 11-fold.
While not studied, the use of moderate CYP2C8 inhibitors (eg, teriflunomide, deferasirox) can be expected to increase exposure to the active metabolites as well. For patients on a moderate CYP2C8 inhibitor initiating Uptravi, a less frequent dosing regimen should be considered; Uptravi should be reduced when a moderate CYP2C8 inhibitor is initiated.
When coadministered with an inducer of CYP2C8 and UGT 1A3 and 2B7 enzymes (eg, rifampin), the dose of Uptravi should be doubled as exposure to the active metabolite is halved. The Uptravi dose should be reduced once rifampin is discontinued.
Uptravi is available as a film-coated tablet in 200mcg, 400mcg, 600mcg, 800mcg, 1000mcg, 1200mcg, 1400mcg, and 1600mcg strengths.
For more information visit FDA.gov.