IRINDALONE is an antihypertensive agent. It is a serotonin receptor antagonist with weak alpha 1-adrenoceptor blocking properties.

Pirinixil is an ethanolamine derivative of Wy-14,643 [4-chloro-6-(2,3-xylidino)-2-pyrimidinythio]acetic acid. It is the hypolipidemic agent of low toxicity. It has been reported to increase high density lipoprotein cholesterol levels in experimental animals. Pirinixil increased plasma cholesterol levels significantly without affecting plasma triglycerides. Pirinixil exerted a powerful antilipolytic activity against epinephrine, ACTH, nicotine and cold exposure. It is a potent inducer of liver peroxisones and of mitochondrial carmitine acetyltransferase. Pirinixil was developed treatment of hyperlipidemias and atherosclerosis. Pirinixil can increase generation of ROS, leading to DNA damage and p53 phosphorylation, which, in turn, induces the activation of Bax, release of cytochrome-c from mitochondria and activation of caspases, culminating in rat hepatoma FaO cell death.

Odiparcil is a novel, orally active beta-d-thioxyloside analog with antithrombotic activity associated with a reduced risk of adverse bleeding events. Its unique mechanism of action is postulated by means of an elevation in circulating endogenous chondroitin sulfate-related glycosaminoglycans (GAGs) levels. Odiparcil has demonstrated good tolerability, safety and efficacy in phase I and phase IIa studies, in approximately 700 healthy volunteers and 1100 patients. The drug has been investigated in several preclinical models and its potential has been proven in MPS. It may be therefore anticipated that Odiparcil could prove beneficial to MPS patients (MPS I, II and VI) as a substrate reduction therapy as a stand-alone treatment on in adjunction to current treatments. U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation to odiparcil (formerly known as IVA336) for the treatment of mucopolysaccharidosis VI (MPS VI), also known as Maroteaux-Lamy syndrome.

Indiplon is a nonbenzodiazepine, hypnotic sedative that was proposed for the treatment of insomnia. It is a high-affinity allosteric potentiator of GABAA responses that demonstrates preference for α1 subunit-containing GABAA receptors. There is minimal potential for adverse effects, residual daytime sedation, tolerance, respiratory depression. The simultaneous administration of indiplon and alcohol did not result in any significant pharmacokinetic changes. There is little risk of pharmacokinetic interaction between indiplon and any co-administered drugs. Developer (Neurocrine) decided to discontinue all clinical and marketing development of Indiplon in the United States.

Senicapoc (ICA-17043) is a blocker of Gardos channel, a calcium-activated potassium channel, in the red blood cell. Preclinical studies and studies in transgenic models of Sickle cell disease (SCD) show that inhibition of potassium efflux through the Gardos channel is associated with an increased haemoglobin level, decreased dense cells and decreased hemolysis. Senicapoc is well tolerated when administered to SCD patients and produces dose-dependent increases in hemoglobin and decreases in markers of hemolysis. Senicapoc exerts anti-fibrotic and anti-inflammatory activities. Senicapoc has previously been in Phase III and Phase II clinical trials for the treatment of SCD and asthma, respectively.

GW-810781 (wider known as S-1360) was initially developed by GlaxoSmithKline as HIV integrase inhibitor. GW-810781 was well-tolerated and showed acceptable pharmacokinetic profiles that is why it was studied in phase II clinical trials as a potential treatment for HIV infection. However, the development of the drug was discontinued in July 2003.

8-Cyclopentyl-1,3-dipropylxanthine (DPCPX) is a selective high-affinity antagonist radioligand for A1 adenosine receptors. DPCPX is a useful tool with which to explore the potential of activation of adenosine A1 receptors as an important mechanism in physiological and pathophysiological processes.

Salnacedin (also known as G 201) was developed as a topical anti-inflammatory agent; Salnacedin participated in phase II clinical trials in the USA for the treatment of dermatitis, acne, and psoriasis. However, all these studies were discontinued.

KRN-5500, a spicamycin derivative, is a nucleoside-like antibiotic with a broad spectrum of antitumor activity against human cancer cell lines. It also may have value in the treatment of neuropathic pain.