Safety, Tolerability, and Pharmacokinetics of Treprostinil Palmitil Inhalation Powder for Pulmonary Hypertension: A Phase 1, Randomized, Double-Blind, Single- and Multiple-Dose Study

Abstract

x the mean (CV%) of C max , C min , and AUC s were 193-228 pg/mL (32.9-46.4%), 17.6-22.8 ng/mL (43.7-64.4%), and 1680-1820 pgÁh/mL (28.7-36.6%), respectively. The elimination t 1/2 was 6.84-8.82 h after repeat dosing. No steadystate accumulation was observed. Plasma concentrations of TP were below the limit of quantification (100 pg/mL) at all time points measured. Conclusion: TPIP was well tolerated at the doses tested, and dose titration improved tolerability. Treprostinil pharmacokinetics were linear and supportive of a QD treatment regimen. These results support further development of TPIP in patients with PAH and PH-ILD.

Future Perspectives of Pulmonary Arterial Hypertension: A Review of Novel Pipeline Treatments and Indications

“…In a phase I study, treprostinil palmitil inhalation powder (TPIP) demonstrated a safety profile and good tolerability. Also, pharmacokinetic studies indicated the potential for once-daily administration [ 79 ].…”

Therapeutic Potential of Treprostinil Inhalation Powder for Patients with Pulmonary Arterial Hypertension: Evidence to Date

“…TPIP was first evaluated in human subjects in a phase Ib study to evaluate safety and tolerability of the drug. 38 Subjects were randomized to single or multiple (7 days) daily doses. Treatment-emergent adverse events largely consisted of cough, headache, and nausea, and upward dose titration appeared to reduce the incidence of adverse events compared to initiation at high dose.…”