Google updates on Treprostinil

 

A more stable prostacyclin analogue, treprostinil has a half life of four hours and can be 

administered subcutaneously FDA approved in 2002 or intravenously approved in 2004. 

A randomized, placebo controlled study of subcutaneous treprostinil in 470 WHO class 

III or IV patients with IPAH or PAH associated with connective tissue disease, or CHD 

demonstrated a dose related improvement in six minute walk distance of 16 meters in the 

whole treated group and 38 meters in the quartile of patients receiving the highest dose.

Not all patients could be dose increased to a high level because of pain at the infusion site 

in the majority, as well aside effects of headache, diarrhea, rash and nausea.

The potential advantages of intravenous treprostinil are the absence of site pain, as well 

as easier preparation and administration and less rebound compared to epoprostenol. An 

open label study of intravenous treprostinil in 16 symptomatic PAH patients showed an 

82 meter increase in six minute walk distance after 12 weeks, and improved pulmonary 

henodynamics. Most patients originally treated with epoprostenol can be switched over to 

intravenous treprostinil with maintenance of six minute walk distance though at a larger 

dose. Studies of inhaled and oral administration of treprostinil are underway.

The prostacyclin analogue iloprost is an inhaled aerosol approved for use in 2004. 

In a randomized, placebo-controlled 12 week study, iloprost produced a placebo-

corrected improvement in six minute walk distance by 36 meters in two hundred patients 

with symptomatic IPAH, PAH associated with connective tissue disease or appetite 

suppressants, or PH related to inoperable chronic thromboembolic disease. Long term 

maintenance of beneficial effects of exercise capacity and hemodynamics have been 

observed. Iloprost may cause side effects common to prostacyclin analogues including 

headache, flushing, and jaw pain, and also may cause cough.

The objective of treatment with an endothelin receptor antagonist is to minimize the 

impact of excessive endothelin effects in the pulmonary vasculature in patients with 

PAH. Bosentan is a non-selective, or dual, A and B-endothelin receptor antagonist 

available in oral form. Placebo controlled randomized drug trials have shown a relative 

improvement in six minute walk distance ranging from 36 to 76 meters, an improvement 

in pulmonary hemodynamics and delay in clinical worsening.

Facebooktwitterredditpinterestlinkedintumblrmail