Edivoxetine (LY-2216684) is a highly selective norepinephrine reuptake inhibitor. It is under development as adjunctive or monotherapy of disorders believed to be associated with alterations in norepinephrine transmission within the central nervous system. Currently, edivoxetine is being studied in the treatment of attention-deficit hyperactivity disorder. Edivoxetine development in the treatment of major depressive disorder has been discontinued.

Pamicogrel is a cyclooxygenase inhibitor with platelet anti-aggregatory properties which is under development by Kanebo for chronic arterial occlusion. It also has potential in both prophylaxis and treatment of ischemic brain injury. An NDA was submitted in Japan in April 1997. The effects of the drug on platelet aggregation were originally disclosed in EP-00159677, while the later European patent, EP-00560136, claims its use in brain dysfunction induced by hypoxia arising from disturbance of cerebral circulation, such as cerebral hemorrhage or cerebral infarction.

As a narcotic antagonist similar in action to naloxone, DIPRENORPHINE is used to remobilize animals after analgesia by super-potent opioid analgesics such as etorphine and carfentanil. It is not used in humans. Diprenorphine binds approximately equally to the three subtypes of opioid receptors (mu, delta, and kappa) and antagonizes them. This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene. The therapeutic efficacy of many other compounds can be decreased when used in combination with Diprenorphine (54 compounds mentioned on www.drugbank.ca).

Glysobuzole (stabinol) is a sulfonamide derivative with antihyperglycemic activity. Like sulfonylureas, glysobuzole is able to lower blood glucose levels by increasing the release of insulin from pancreatic beta cells.

Diamfenetide (aka diamphenethide) is a fasiolicide used in sheep. It is effective against immature flukes but with diminishing activity as the fluke ages. It has proven an effective compound for use in prophylactic programs against Fasciola hepatica. Diamphenethide is deacetylated in the host liver to an active monoamine and diamine. The amine of diamfenetide has an action which produces an elevation of malate concentration in Fasciola. Malate is an intermediary product of glucose in this parasite. It is known that dopamine, a putative neurotransmitter in Fasciola has a protective effect against diamfenetide but the mode of action of a diamfenetide has yet to be defined in greater detail.

CYT997 (Lexibulin) is a wholly synthetic compound that possesses highly potent cytotoxic activity in vitro through inhibition of microtubule polymerization. CYT997 (Lexibulin) is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. CYT997 (Lexibulin) blocks the cell cycle at the G(2)-M boundary, and Western blot analysis indicates an increase in phosphorylated Bcl-2, along with increased expression of cyclin B1. Caspase-3 activation is also observed in cells treated with CYT997 (Lexibulin) along with the generation of poly(ADP-ribose) polymerase. The compound possesses favorable pharmacokinetic properties, is orally bioavailable, and is efficacious per os in a range of in vivo cancer models, including some refractory to paclitaxel treatment. CYT997 (Lexibulin) exhibits vascular disrupting activity as measured in vitro by effects on the permeability of human umbilical vein endothelial cell monolayers, and in vivo by effects on tumor blood flow. CYT997 (Lexibulin) possesses a useful combination of pharmacologic and pharmacokinetic properties having considerable potential as a novel anticancer agent. Lexibulin was being developed by YM BioSciences as a vascular-disrupting agent (VDA) for the potential treatment of cancer, it was in phase II development on YM BioSciences ' pipeline. It appears that the development of lexibulin has been discontinued.

Terbogrel, an agent having two pharmacodynamic actions, namely inhibition of thromboxane A2 synthase and antagonism of the thromboxane A2 receptor. The antithrombotic effect of terbogrel was dose-dependent and was associated with enhanced prostacyclin production. The drug was studied for the treatment of peripheral vascular disorders, pulmonary hypertension, and thrombosis. Terbogrel participated in phase II clinical trial to investigate its safety and efficacy in patients with primary pulmonary hypertension, however, this study was discontinued due to terbogrel’s induction of leg pain.

Mespiperone C-11 (3-N-[11C] methylspiperone) is a radiolabeled 3-N-methylspiperone. 3-N-methylspiperone is high-affinity D2/3 dopamine and 5-HT2A serotonin receptor antagonist. It has been studied as a positron emission tomography (PET) tracer for imaging D2/3 and 5HT2A receptor densities.

Etoxeridine (Carbetidine or Wy2039), a piperidine derivative, is a narcotic analgetic.

Glyprothiazol (VK 57 or RP 2254) is a sulfonamide derivative. This compound lowers blood glucose levels by increasing the release of insulin from the pancreas. It stimulates insulin secretion through a direct action on pancreatic islets. Glyprothiazol was the first of oral hypoglycemic sulfonamides used in the treatment of type 2 diabetes mellitus.