LY 300502 is now called bexlosteride was developed as an inhibitor of the human-specific type I-selective steroid 5alpha-reductase. This drug was studied for patients with prostate cancer, however, has never been marketed.

Morocromen is an oxobenzopyranyl derivative patented by Troponwerke Dinklage und Co. as the coronary dilating agent.

Gadopenamide is an MRI contrast agent that was introduced in 1991. It has been investigated as a potential clinical contrast medium by Schering AG (Germany), but has never been used as such.

Temelastine (also known as SK&F 93944) is a competitive histamine H1-receptor antagonist, which does not penetrate the central nervous system. This drug was studied as an anti-allergic agent. Experiments on animals have shown that the drug was efficacious vs. pharmacologic and antigen-induced bronchoconstriction.

Piclidenoson (CF101), generically known as IB-MECA (methyl 1-[N6-(3-iodobenzyl)-adenin-9-yl]-b-D-ribofuronamide), is an oral small molecule drug formulated in a tablet. The activity of CF101 as an anti-inflammatory agent has been tested in a number of different experimental models including adjuvant and collagen induced arthritis and inflammatory bowel disease. CF101 is a highly specific agonist at the A3AR known to induce a robust anti-inflammatory effect in different experimental animal models. The CF101 mechanism of action entails down-regulation of the NF-κB-TNF-α signaling pathway, resulting in inhibition of pro-inflammatory cytokine production and apoptosis of inflammatory cells. Piclidenoson is currently being developed for the treatment of autoimmune inflammatory diseases like RA and psoriasis, hoping to replace the current standard of care, methotrexate (MTX). Can-Fite has tested CF101 in a number of Phase II studies in different diseases. A Phase II study in Psoriasis successfully met its primary endpoint showing that CF101 effectively ameliorated disease symptoms. In an interim analysis of the Phase II/III study the data justified full enrollment of the study. Phase II studies in Rheumatoid Arthritis (RA) demonstrated efficacy of CF101 given as a monotherapy. Moreover, a direct correlation between A3AR at baseline and patients’ response to CF101, suggesting its utilization as a predictive biomarker. Piclidenoson is headed into Phase 3 trials for RA and psoriasis.

Etintidine is a potent competitive antagonist of histamine H2-receptors. It has a low level of antiandrogenic activity. Etintidine was being investigated in the treatment of peptic ulcer, however, its development has been discontinued.

Noberastine (NOB), a histamine H1 antagonist, has potent and specific peripheral antihistaminic activity. Noberastine, a furan derivative of nor-astemizole (an astemizole metabolite), has been shown to have a more rapid onset, and shorter duration of action than astemizole with peak antihistaminic activity at 4h following ingestion. Noberastine is rapidly absorbed and the peak plasma levels are obtained within 2 h of oral dosing. In preclinical studies Noberastine has been shown to lack central nervous system effects. After subacute (steady-state) administration of noberastine, there was increasing inhibition of weal and flare formation with higher doses of the drug. The 30 mg daily dose showed maximum antihistaminic effects.

Mixidine is negative chronotropic agent patented by McNeil Laboratories. Mixidine produced a dose-related decrease in heart rate elevated reflexly by aminophylline, by beta-adrenergic stimulation induced by isoproterenol, by sympathetic nerve stimulation and by intravenous infusion of glucagon. Mixidineattenuated the increase in contractile force produced by sympathetic nerve stimulation but not that induced by isoproterenol. The compound antagonized the increase in the rate of isolated guinea-pig atria induced by both isoproterenol and histamine. In the conscious dog, Mixidine caused no decrease in resting heart rate, mean arterial pressure and cardiac output. It reduced atropine-induced sinus tachycardia as well as that induced by treadmill exercise.