Pyrazoloacridine is a pyrazolo[3,4,5-kl]acridine derivative patented by Warner-Lambert Co. as an anticancer agent. Pyrazoloacridine acts as topoisomerase I and II inhibitor that decrease the formation of topoisomerase-DNA adducts. In vitro experiments, Pyrazoloacridine shows efficacy against multidrug-resistant neuroblastoma doxorubicin-resistant human colon carcinoma and breast cancer cell lines. In clinical trials, Pyrazoloacridine demonstrates moderate efficacy in metastatic breast cancer and a high level of adverse events. The dose-limiting toxicity was grade 4 neutropenia. Other grade 3 and 4 toxicities include vomiting, nausea, neurotoxicity, fatigue, and anemia.

Locicortolone is an anti-inflammatory and antiallergic synthetic glucocorticoid. It has high glucocorticoid cytoplasmic receptor binding affinity in vitro (more than four times higher than dexamethasone) but comparable to dexamethasone relative TAT (tyrosine aminotransferase induction) activity. It has six times lower binding affinity to mineralocorticoid receptor in comparison to dexamethasone.

Tedatioxetine (previously known as Lu AA24530) is a multimodal antidepressant that was developed for the treatment of depression and anxiety disorders (generalized anxiety disorder mainly). Tedatioxetine is a monoamine enhancer with reuptake inhibition at monoamine transporters and possesses an antagonist activity at 5-HT3 and 5-HT2c receptors. In 2009, the drug was studied in phase II clinical trials where it showed positive results in major depressive disorder. However, it remains unclear as to whether tedatioxetine development has been postponed and/or abandoned.

Galactitol (dulcitol) is a sugar alcohol, the reduction product of galactose. Galactitol is known to be the major toxic metabolites of galactose. Deficiency of any one of three possible enzymes involved in the metabolism of galactose: galactokinase, transferase or epimerase results in galactosemia. Any single deficient enzyme can result in cataract through the accumulation of galactitol in the lens. Accumulation of galactose and galactitol within the lens cells leads to an increase in intracellular osmotic pressure and an influx of fluid in the lens. Kinoshita was the first to demonstrate the hyperosmotic effects of intracellular sorbitol or galactitol accumulation and to postulate that the resulting cellular swelling can lead to increased membrane permeability and a series of complex biochemical changes associated with sugar cataract formation. The excretion of abnormal quantities of galactitol in the urine of galactosemia patients is characteristic of this disorder. A patent claims galactitol as carrier for the therapeutic agent since galactitol enhances the chemical and physical stability of the drug and allows faster reconstitution of the formulation in water than mannitol.

Chlorothalonil (2,4,5,6-tetrachloroisophthalonitrile) is an organic compound mainly used as a broad spectrum, nonsystemic fungicide, with other uses as a wood protectant, pesticide, acaricide, and to control mold, mildew, bacteria, algae. Chlorothalonil reduces fungal intracellular glutathione molecules to alternate forms which cannot participate in essential enzymatic reactions, ultimately leading to cell death. Chlorothalonil is slightly toxic to mammals, but it can cause severe eye and skin irritation in certain formulations. Very high doses may cause a loss of muscle coordination, rapid breathing, nose bleeding, vomiting, and hyperactivity. Dermatitis, vaginal bleeding, bright yellow and/or bloody urine, and kidney tumors may also occur, followed by death. In a number of tests of varying lengths of time, rats which were fed a range of doses of chlorothalonil generally showed no effects on physical appearance, behavior, or survival. Kidney changes such as kidney enlargement were common. In the US, chlorothalonil is used predominantly on peanuts (about 34% of usage), potatoes (about 12%), and tomatoes (about 7%), though the EPA recognizes its use on many other crops. It is also used on golf courses and lawns (about 10%) and as a preservative additive in some paints (about 13%), resins, emulsions, and coatings. Chlorothalonil is commercially available in many different formulations and delivery methods. It is applied as a dust, dry or water-soluble grains, a wettable powder, a liquid spray, a fog, and a dip. It may be applied by hand, by ground sprayer, or by aircraft

ABC-294640 is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 uM. ABC-294640 inhibits SK2, a lipid kinase that catalyzes formation of the lipid signaling molecule sphingosine 1-phosphate (S1P). S1P promotes cancer growth, and proliferation and pathological inflammation, including TNFα signaling and other inflammatory cytokine production. Specifically, by inhibiting the SK2 enzyme, ABC-294640 blocks the synthesis of S1P which regulates fundamental biological processes such as cell proliferation, migration, immune cell trafficking and angiogenesis, and are also involved in immune-modulation and suppression of innate immune responses from T cells. Preliminary evidence suggests that because of its specificity for targeting SK2, rather than SK1, ABC-294640 may have a better therapeutic ratio than nonspecific sphingosine kinase inhibitors or those targeting only SK1. Oral administration of ABC-294640 to mice bearing mammary adenocarcinoma xenografts results in dose-dependent antitumor activity associated with depletion of S1P levels in the tumors and progressive tumor cell apoptosis. Therefore, this newly developed SK2 inhibitor provides an orally available drug candidate for the treatment of cancer and other diseases. ABC-294640 has completed multiple successful pre-clinical studies in inflammatory, GI, radioprotection and oncology models, as well as a Phase I clinical study in cancer patients with advanced solid tumors.

Glyceryl trierucate (trierucin) is a trierucic acid triglyceride that has been investigated for the treatment of adrenoleukodystrophy, a rare genetic disorder characterized by the breakdown or loss of myelin in the brain. To investigate treatment options for adrenoleukodystrophy, most studies have used “Lorenzo's oil" (LO), a 4:1 mixture of glyceryl trioleate and glyceryltrierucate. Lorenzo’s oil was found to reduce the levels of saturated very long chain fatty acids (ELOVL) in the plasma, adipose tissue and liver, but to a lesser extent in the brain. Inhibition of ELOVL 1 may be an underlying mechanism by which Lorenzo's oil exerts its action. Several clinical trials have been conducted to study the potential of glyceryl trierucate in treatment of adrenoleukodystrophy.

Secoisolaricircsinol is one of the most abundant dietary lignans in various foods, such as plant seeds, whole grains, legumes, vegetables, and fruits. Secoisolariciresinol is the major lignin found in flaxseed and is present in a polymer that contains Secoisolariciresinol diglucoside. Secoisolariciresinol and Secoisolariciresinol diglucoside are known to have a number of health benefits, including reduction of the serum cholesterol levels, delaying of the onset of type 2 diabetes, and reduction of the formation of hormone-sensitive cancers such as breast, prostate, and colon cancers. Following the consumption of Secoisolariciresinol diglucoside, it is further converted by the bacteria in the colon of humans and other animals into aglycone Secoisolariciresinol and the mammalian lignans, enterodiol and enterolactone. The structures of enterodiol and enterolactone are similar to that of estradiol, an endogenous estrogen. This structural similarity accounts for the ability of these compounds to bind to estrogen receptors and to exert weak estrogenic or anti-estrogenic effects, depending on the presence of stronger estrogen. It is well known that Secoisolariciresinol has an estrogen-like activity and stimulates the cell growth of human breast cancer MCF-7 cells.