Dovitinib is an orally active small molecule that exhibits potent inhibitory activity against multiple receptor tyrosine kinases (RTK) involved in tumor growth and angiogenesis. Dovitinib strongly binds to fibroblast growth factor receptor 3 (FGFR3) and inhibits its phosphorylation, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell death. In addition, this agent may inhibit other members of the RTK superfamily, including the vascular endothelial growth factor receptor; fibroblast growth factor receptor 1; platelet-derived growth factor receptor type 3; FMS-like tyrosine kinase 3; stem cell factor receptor (c-KIT); and colony-stimulating factor receptor 1; this may result in an additional reduction in cellular proliferation and angiogenesis, and the induction of tumor cell apoptosis. There are several ongoing Phase I/III clinical trials for dovitinib.

Viprostol (also known as CL115,347), a prostaglandin E2 congener that was studied as an antihypertensive agent. Viprostol has a potent and prolonged blood pressure lowering effect in many models of hypertension. In clinical studies, viprostol has been demonstrated to lower arterial blood pressure significantly in man following transdermal and/or intravenous administration. The antihypertensive action of viprostol has been suggested to be the result of peripheral vasodilatation. In addition, the drug participated in a clinical trial in normal subjects and in patients with Raynaud's phenomenon. It was found the optimal dosage was 1000 ug; the effect could last for 84 hours; higher dosage may be associated with a "steal" phenomenon.

alpha-MELANOTROPIN (also known as an alpha-melanocyte-stimulating hormone or alpha MSH) is an endogenous melanocortin 1-receptor agonist, which exclusively expressed in cells of the melanocytic lineage. alpha-MELANOTROPIN possesses anti-inflammatory properties and antagonizes proinflammatory mediators, including TNF-alpha, IL-6 and NO, and induces anti-inflammatory cytokine IL-10. alpha-MELANOTROPIN was studied in phase I clinical trial in patients with acute renal failure. In addition, this compound was assigned of orphan designation for the treatment of chronic beryllium disease.

Castanospermine (1,6,7,8-tetrahydroxyoctahydroindolizine) is an indolizine alkaloid first isolated from the seeds of Australian tree Castanospermum austral. Castanospermine is a potent inhibitor of some glucosidase enzymes and has antiviral, immunosuppressant and anti-inflammatory activity in vitro and in animal models. Castanospermine has been shown to be a potent inhibitor of almond emulsion β-glucosidase, and also to inhibit fungal β-xylosidase. Additionally, castanospermine may have the potential ability to inhibit syncytium formation between HIV-infected and CD4-expressing cells and may also interfere with infectivity. It has also been demonstrated that this agent inhibits inflammation at the level of leukocyte extravasation in rat models of experimental adjuvant-induced arthritis and autoimmune encephalomyelitis. Celgosivir, Castanospermine’s oral prodrug, is currently tested in clinical trials.

KRN-7000, a compound with an alpha-galactosylceramide structure, shows potent anti-tumor activity in animal models. It also has strong immunostimulating effect being a high-affinity CD1d antigen.

Mivazerol is a new and selective alpha 2-adrenoceptor agonist, devoid of hypotensive effects, which has been designed to prevent adverse cardiac outcome in perioperative patients with, or at risk coronary artery disease. This compound, which lacks hypotensive effects, has been demonstrated to prevent hyperadrenergic activity and myocardial ischemia in perioperative patients and tachycardia in rats at emergence from halothane anesthesia. This type of ischemia, frequently encountered in postoperative patients, is considered to be a consequence of stress-induced hyperactivation of the sympathetic system. Anti-ischemic effects of this compound have been demonstrated in different animal models of myocardial ischemia, and Mivazerol has also been shown to improve exercise-induced ischemia in patients with angina pectoris.

Chloralose (alpha-Chloralose, 1,2-O-(2,2,2-Trichloroethylidene)-α-D-glucofuranose) is an avicide, and a rodenticide commonly used for the control of mice and birds. Since its initial description in 1893, alpha-chloralose has undergone extensive pharmacologic evaluation. It has been characterized as a compound possessing potent CNS activity and has been evaluated in humans and animal models for its therapeutic properties. Though the toxicity of the compound prohibits its use as a human therapeutic agent, it has been employed widely as an animal anesthetic in the laboratory setting. α-Chloralose is widely used as an anesthetic in studies of the cerebrovasculature because of its presumed minimal depression of autonomic function. α-Chloralose acts as the positive allosteric modulator of GABA-A receptor and increases the affinity for GABA 5-fold and produced a small increase in the efficacy of GABA. Studies of α-Chloralose interactions with other allosteric modulators determined that α-Chloralose binds to a site on the GABAA receptor complex distinct from the benzodiazepine, neurosteroid and barbiturate sites.