Indibulin is a novel synthetic compound that was identified in a cell-based screening assay to discover cytotoxic drugs. Indibulin destabilizes microtubules and blocks cell cycle transition specifically at the G2-M phase. Indibulin effectively induces apoptosis through Bcl-2 phosphorylation and Bax translocation in human malignant glioma cells in a p53-independent manner. This agent has been shown to be active against multidrug-resistant (MDR) and taxane-resistant tumour cell lines. Indibulin was used in phase I/II clinical trials of patients with advanced solid tumours (metastatic breast cancer). Pharmacokinetic analysis showed a better tolerability underfeeding condition. Dose-limiting toxicities were nausea and vomiting, which seemed to be related to solvent lactic acid.

Cimaterol is a chemically stable nonselective agonist β1-, β2-, and β3-adrenoceptors. Cimaterol is used in sport as a stimulant and a fat burner that assists bodybuilders and strength athletes to get rid of body fats. Aside from shedding off fats, another benefit for using cimaterol for athletes is a boost in strength as well as an increase in muscle size or lean body mass. The increase in muscle size has been seen in previous animal studies when cimaterol is used. However, the reason behind the muscle gain is not identified yet, but the body has a very different response compared from taking in anabolic steroids. Experts in the field are saying that the increased nitrogen retention, that is known to cause by cimaterol, maybe the reason behind the muscle gain. Another great thing about Cimaterol is that, it can improve blood flow.

Cilutazoline is phenoxymethyl-imidazoline derivative useful as cardiotonics and vasoconstrictors

Cilostamide (also known as OPC 3689) is a selective inhibitor of type III phosphodiesterases: PDE3A and PDE3B, which inhibits thrombin-induced platelet aggregation. Elevating intracellular cAMP has been shown to inhibit platelet function. cAMP interferes with platelet-activating signals, which leads to aggregation inhibition, but the precise mechanism is unclear. It is known, that inhibition of Akt phosphorylation leads to inhibition of phosphorylation of glycogen synthase kinase 3-beta (GSK-3beta), which is an effector of Akt. However, cAMP-elevating agents’ stimulated GSK-3beta phosphorylation at Ser9. The cAMP-elevating agent cilostamide did not directly affect the enzyme activity of PI3-kinase, and thus it has two effects on PI3K signaling: inhibition of Akt phosphorylation independent of PKA. And stimulation of GSK-3beta phosphorylation dependent on PKA.

Ciheptolane is spirodibenzocycloalkanedioxalane derivative with analgesic, sedative, antihistaminic, antiserotonic, antiinflammatory, anticonvulsant, and antidepressant activity.

Perzinfotel (EAA-090) is a novel squaric acid amide derivative that has been identified as a potential treatment for ischemic brain damage resulting from stroke. EAA-090 is a competitive inhibitor at the NMDA-selective subtype of the glutamate receptor. The compound demonstrates potent inhibitory activity in both in vitro and in vivo models of NMDA-induced excitotoxicity and provides neuroprotective efficacy in several animal models of stroke. EAA-090 is unique among competitive NMDA antagonists in displaying a clear separation between predicted efficacious dose and doses that induce PCP-like psychotomimetic side effects in both animals and humans. This unique profile makes EAA-090 an exciting candidate for assessing the neuroprotective potential of the competitive NMDA mechanism.

Rilapladib (SB659032) is a potent and selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Inhibition of Lp-PLA2 can reduce peripheral measures of inflammation. Rilapladib has been evaluated for treatment in Alzheimer’s disease and atherosclerosis. Initial results from clinical trials in Alzheimer patients suggests that oral administration of rilapladib may slow down the progression of Alzheimer’s disease. Initial evidence has also been found that inhibition of Lp-PLA2 may attenuate intimal macrophage accumulation and consequently stabilize atherosclerotic plaque.

Dacuronium is an aminosteroid, acting as a competitive antagonist of nicotinic acetylcholine receptors. In animals, dacuronium worked as a short-acting muscle relaxant with a rapid onset of action. In a clinical trial, dacuronium was markedly less potent than tubocurarine and did not show a rapid recovery from its action.

Rotraxate (also known as TEI 5103 or TG 51) is an anti-ulcerative agent. Experiments on rodents have shown that only the oral and gastric route of administration lead to the anti-ulcer effect. This drug increased gastric mucosal blood flow and possibly promoted the healing process of peptic ulcers. However, the further development of this drug was discontinued.

Roxibolone, an androstane derivative, possesses the anti-glucocorticoid activity and devoid of any affinity for the androgenic prostate and muscle receptors. This anabolic drug has never been marketed.