Conference: 2010 International PHA Conference and Scientific Sessions
Release Date: 06.24.2010
Presentation Type: Abstracts
White RJ1, Allen R2, Torres F3, Jerjes C4, Pulido T5, Carroll J6, Yehle D7, Laliberte K7, Mottola D7, Galie N8, Simonneau G9, Tapson VF10.
1. University of Rochester, Rochester, NY, USA
2. University of California at Davis, Sacramento, CA, USA
3. University of Texas Southwestern, Dallas, TX, USA
4. Unidad de Investigacion Clinica en Medicina SC, Monterrey, Mexico
5. Instituto Nacional de Cardiologia, Mexico City, Mexico
6. University of Iowa, Iowa City, IA, USA
7. United Therapeutics Corp, Research Triangle Park, NC, USA
8. University of Bologna, Bologna, Italy
9. Hopital Antoine Beclere, Clamart, France
10. Duke University Medical Center, Durham, NC, USA
BACKGROUND: Treprostinil diethanolamine sustained release tablets (UT-15C SR) are currently being evaluated for the treatment of pulmonary arterial hypertension (PAH). UT-15C is a unique salt related to the prostacyclin analog, Remodulin¨ (treprostinil sodium).
METHODS: During the open-label extension phase of the initial trials for UT-15C SR, we studied the pharmacokinetic profile of 74 patients who had received active drug for a minimum of 4 weeks and at a stable dose for at least 5 days. Each patient provided a trough sample, ingested UT-15C SR with a standardized meal, and subsequently provided seven additional blood samples over 12 hours.
RESULTS: Patients were predominantly female (74%) with a mean age of 45 (range, 16-67) years and mean (+/-SD) weight of 80 (+/-20) kg; most patients had an idiopathic PAH diagnosis. Thirty-seven patients were not taking other PAH specific therapy; 37 patients were using approved PAH therapies: an ERA (19), a PDE-5 inhibitor (9), or both an ERA and PDE-5 inhibitor (9). The median morning dose of UT-15C SR was 4 mg (range, 0.5 to 16 mg BID) with 90% of patients on a dose < 7 mg. Correlations (r2) of area under the curve over the 12 hour dosing interval and maximum plasma concentration with dose were 0.7 and 0.71, respectively.
CONCLUSION: We conclude that UT-15C SR tablets provide sustained treprostinil plasma concentrations over approximately 12 hours in patients with PAH and further that the plasma levels achieved are similar to those observed with therapeutic doses of Remodulin.
This study is supported entirely by United Therapeutics, Inc.