Flutafuranol F-18 (also known as NAV4694), a fluorine-18 labeled positron emission tomography (PET) imaging agent that was developed for diagnostic use. Flutafuranol F-18 binds to beta-amyloid deposits in the brain that could then be imaged in PET scans. It is known that amyloid plaque pathology is a required feature of Alzheimer’s disease (AD) and the presence of amyloid pathology is a supportive feature for the diagnosis of probable AD. Patients who are negative for amyloid pathology do not have AD. Thus, flutafuranol F-18 was studied in phase III clinical trial as an aid in the imaging for patients with Alzheimer’s disease and in phase II clinical trial for patients with mild cognitive impairment.

T-900607 is a pentafluorophenylsulphonamide derivative patented by Tularik Inc. as antiproliferative agent. Antitumor mechanism of T900607 is similar to the vinca alkaloids in terms of disruption of microtubule polymerization but uniquely causes a specific covalent modification of β-tubulin. In preclinical studies, T900607 was shown to bind irreversibly and specifically to the β1, β2, and β4 isotypes of β-tubulin is not a substrate for p-glycoprotein drug pump and has activity in the preclinical setting in MDR models. T900607 was evaluated in human tumor xenografts and showed activity in MX-1, MCF-7, and MCF-7/ADR mammary, C13 ovarian, HT 29 colon, and Caki-1 renal carcinoma as well as lymphoblastic leukemia, with equal or more efficacious effects compared to vinblastine, doxorubicin and paclitaxel. In a clinical trial, T-900607 shows significant toxicity, consisting of thrombocytopenia, nausea/vomiting, fatigue, and apparent cardiac toxicity.

Tetramethylhexamethylenediamine (6,3-ionene) is a Hexanediamine derivative patented by Abbott Laboratories. U.S.A. as heparin neutralizer. Heparin is anionic polymer and positively charged Tetramethylhexamethylenediamine, prevents its anticoagulant action. The antagonistic capacity would be due to the PEC formation between the ionene and heparin. Tetramethylhexamethylenediamine can also be used as an antispasmolytic drug.

KW-2478 is a novel and potent non-ansamycin inhibitor of heat shock protein 90 designed to overcome the limitations, including low water solubility and hepatotoxicity, of 17-allylamino-17-demethoxygeldanamycin (17-AAG). KW-2478 exerts a strong antitumor activity against multiple myeloma (MM) cells with various chromosomal translocations. KW-2478 inhibits cell growth and apoptosis associated with Hsp90 client protein degradation. Recent study results have revealed that KW-2478 is able to deplete Hsp90 client Cdk9 and the phosphorylated 4E-BP1, a transcriptional kinase and a transcription inhibitor respectively, leading to reduced expression of FGFR3, c-Maf, and cyclin D1. KW-2478 suppresses tumor growth and induces the degradation of client proteins in tumors in NCI-H929 s.c. inoculated model at doses of 100 mg/kg or more. KW-2478 reduces both serum M protein and MM tumor burden in the bone marrow in OPM-2/GFP i.v. inoculated mouse model at doses of 100 mg/kg.

Troxonium tosylate is a triethylcholine ester which resembles hemicholinium in some of its pharmacological effects. In animal pharmacological studies, it was noted that troxonium tosylate had a marked antitremorine activity with an associated hypotensive effect. This antitremorine activity, which is a common characteristic of antiparkinsonian agents, was found to be combined with an inhibitory function on acetylcholine synthesis and with a reduction of brain catecholamines. Troxonium tosylate was found to be an effective antiparkinsonian medication for drug-induced extrapyramidal manifestations. Troxonium tosylate caused a pronounced fall in the blood pressure in both normotensive and hypertensive animals. It produced this depressor effect mainly by antagonism of both central and peripheral autonomic ganglia. Troxonium did not possess atropine-like properties and was not active as an adrenergic blocker. Despite the potent effect upon the blood pressure, it did not significantly inhibit renal function and cardiac output. Because of its unique properties, it was postulated that troxonium might be of value in the management of hypertension of various etiologies.

Piromelatine is an investigational therapy being developed by Neurim Pharmaceuticals to manage sleeping difficulties. The compound is now being studied for its potential to improve cognitive function and slow the progression of Alzheimer’s disease by promoting better sleep. It acts primarily as an agonist of MT1/MT2/MT3 melatonin receptors and serotonin 5-HT1A and 5-HT1D receptors, but reportedly also is a low-affinity antagonist of 5-HT2B, P2X3, and TRPV1 receptors. Piromelatine may benefit control of circadian rhythm, metabolism, cognition and mood. Preclinical studies have reported cognitive improvement in rats that received hippocampal Aβ42 injections to simulate Alzheimer’s disease. There are also reports on painkilling and hypnotic effects in a mouse model of neuropathic pain, as well as blood pressure lowering in rats. Piromelatine is in phase II clinical trial for the treatment of Alzheimer's disease, Insomnia, Ocular hypertension and Open-angle glaucoma.

Chlorogenic acid is the ester of caffeic acid and (-)-quinic acid. Chlorogenic acid is a naturally occurring plant metabolite and can be found with the related compounds cryptochlorgenic acid and neochlorogenic acid in the leaves of Hibiscus sabdariffa, coffee, potato, eggplant, peaches, and prunes. Chlorogenic acid has been investigated as a dietary supplement to improve glucose intolerant hypoglycemia and non-alcoholic fatty liver disease. It has also been identified as a potential anticancer agent by reducing the expression of HIF-1a and Sphingosine Kinase-1. Chlorogenic acid was also identified as a neuraminidase blocker effective against influenza A virus (H1N1 and H3N2).

Fedovapagon, also known as VA106483 and VT483, is a potent, nonpeptidic vasopressin V2 receptor agonist. Vasopressin (AVP) is a hormone that stimulates an increase in water permeability through activation of V2 receptors in the kidney. Fedovapagon (VA106483) was discovered by Vantia and currently in Phase II trials for the treatment of nocturia, a common condition that causes sufferers to wake frequently during the night in order to urinate. Fedovapagon has been extensively studied in clinical trials and data, presented at the American Urological Association meeting in 2010, demonstrated a dose-dependent reduction in nocturnal urine volumes and a reliable pharmacodynamic effect on repeated dosing. More recently, data presented in San Diego at the 2012 American Urological Association meeting, showed that fedovapagon was effective from the first night of dosing and that there was no effect following cessation of dosing. Further presentations are planned for the International Continence Society meeting being held in Barcelona in August 2013. These data suggest that fedovapagon has the potential to be an effective and well tolerated antidiuretic for the treatment of nocturia. Fedovapagon is currently being investigated as a new treatment for nocturia in a Phase-II/III clinical trials in USA (PO)(NCT02637960).

Calcium magnesium carbonate (dolomite), a mineral with the chemical formula CaMg(CO3)2, is made up of 60% calcium carbonate (equivalent to 24% calcium) and 40% magnesium carbonate (equivalent to 12% magnesium). It is recommended by lay periodicals as a desirable source of calcium and magnesium, but found to be also a source of potentially toxic heavy metals. Exposure to high atmospheric concentrations of this compound is likely to be associated with respiratory symptoms.

The three major isoflavones present in kudzu extracts, daidzin, daidzein and puerarin are responsible for the beneficial effects in reduction of alcohol consumption. It has been discovered, that daidzin was a strong, selective and reversible inhibitor of mitochondrial aldehyde dehydrogenase. Daidzin did not inhibit human class I, II, or III alcohol dehydrogenases. However further studies for daidzin’s treatment in alcohol addiction were discontinued.