Systemic Sclerosis Patients Treated With Oral Treprostinil Diethanolamine PDF Print E-mail
Wednesday, 12 June 2013 20:55
Patients with systemic sclerosis effectively absorbed oral treprostinil diethanolamine, which produced a temporal association with improved cutaneous perfusion and temperature, according to study results. In a dual-center, open-label, phase 1 study, researchers evaluated 19 patients with systemic sclerosis (SSc; mean age, 48 years; 84.2% women; 89.5% Caucasian; 53% limited SSc). Eleven patients had an active digital ulcer at baseline. Treprostinil diethanolamine sustained release (SR) was administered to patients with dose titration up to 4 mg twice daily.

Laser Doppler imaging quantified drug concentrations and perfusion, which were measured across 12 hours at 2 mg or 4 mg (or maximally tolerated) doses. Individual plasma concentration vs. time profiles using noncompartmental analysis methods determined pharmacokinetic parameters.

“Digital perfusion and skin temperature were modeled as a function of log-transformed drug concentration and other covariates by performing repeated measures analyses using random effects models,” the researchers wrote.

Sixteen patients completed the 8-week study. Approximately 3.6 hours after administration of treprostinil diethanolamine, peak plasma concentrations reached means of 1,176 pg/mL and 2,107 pg/mL for 2-mg and 4-mg doses, respectively. Overall exposure (AUC from 0 to 12 hours) was linear between doses and observed at 7,187 hr*pg/mL for 2-mg and 12,992 hr*pg/mL for 4-mg doses. Log-transformed plasma at the 4-mg dose had a positive association with perfusion (P=.015) and digital skin temperature (P=.013).

The most common adverse events were headache (89%), diarrhea (47%) and nausea (42%), which were similar to those seen with prostacyclin analogs. No serious adverse events or deaths were reported.

“Currently prostacyclin analogs are administered via intravenous or subcutaneous routes in [systemic sclerosis] patients with vascular complications,” the researchers concluded. “Our data show that oral SR formulation of treprostinil diethanolamine was effectively absorbed in patients with SSc, was associated with improved cutaneous perfusion and temperature with short-term treatment, and may provide a new therapeutic option for Raynaud’s phenomenon and peripheral vascular disease of SSc.”

Source: Helio
 
More articles :

» Calcium Deposits Under the Skin

Numerous health effects or conditions are associated with calcinosis or calcium deposits under the skin. According to the , calcinosis is the medical term for calcium deposits that can form under the skin or in the muscles. Calcium deposits in these...

» UTHealth Scientists Closing In On Genes Tied To Scleroderma

A new study designed to test suspected links between genes and two immune disorders could open the door to better ways to diagnose and treat the conditions that affect a combined total of approximately 2.5 million people in the United States, report...

» What The Science Says About Stress And Relaxation Techniques

In the past 30 years, there has been considerable interest in the relaxation response and how inducing this state may benefit health. Research has focused primarily on illness and conditions in which stress may play a role either as the cause of the...

» Natural Alternatives for Dealing With Scleroderma

In a recent article, it was noted that conventional medicine attempts to treat the symptoms of with immunosuppressant drugs, NSAIDS and , but has no cure and little advice for prevention. It was noted however, that the world of natural healing has...

» Active Biotech Presents Data regarding the 57-57 Project at EULAR

Active Biotech (NASDAQ OMX Nordic: ACTI) has presented data from an exploratory clinical trial in Systemic Lupus Erythematosus (SLE) patients at the Annual European Congress of Rheumatology EULAR 2011, an international event for specialists in the...

» FDA Approves New Lupus Drug

The FDA has approved (Benlysta) for reducing disease activity in (SLE), making it the first new lupus drug in more than 50 years. Belimumab is a monoclonal antibody targeting the B-lymphocyte stimulator protein, called BLyS. It was co-developed by...