Effects of a selective glucocorticoid receptor modulator (AZD9567) versus prednisolone in healthy volunteers: two phase 1, single-blind, randomised controlled trials.

Background: Glucocorticoids are highly effective and widely used anti-inflammatory drugs, but their use is limited by serious side-effects, including glucocorticoid-induced hyperglycaemia and diabetes. AZD9567 is a non-steroidal, selective glucocorticoid receptor modulator that aims to reduce side-effects. We aimed to assess the safety, tolerability, and pharmacokinetics of AZD9567 in healthy volunteers.

The new oral immunomodulating drug DiNAC induces brachial artery vasodilatation at rest and during hyperemia in hypercholesterolemic subjects, likely by a nitric oxide-dependent mechanism.

Objectives: To investigate if the immunomodulator drug DINAC (1) affects arterial dimensions in asymptomatic patients with hypercholesterolemia, (2) has effects on leucocyte markers of inflammation and (3) has in vitro effects on nitric oxide synthase (NOS) in human umbilical vein endothelial cells (HUVEC).

Methods And Results: One hundred and fifty-three patients with asymptomatic hypercholesterolemia were randomized to either 100 or 500 mg of DINAC or placebo in a double-blind, parallel-group fashion for 24 weeks. Treatment at the highest dose induced a significant increase in resting brachial artery diameter measured by ultrasound and also induced a significant increase in vessel diameter during hyperemia.