Idoxifene (also known as CB 7432), a novel selective estrogen receptor modulator, is originally discovered at the CRC Centre for Cancer Therapeutics, Institute. This drug participated in clinical trials phase II in patients with locally advanced/metastatic breast cancer resistant to tamoxifen. In addition, in phase III in postmenopausal women after one year of idoxifene treatment. However, both studies were discontinued because of insufficient effectiveness.

Mibolerone is a synthetic anabolic steroid. It binds both androgen and progesterone receptors and exerts both androgenic and progestagenic actions. Mibolerone (CHEQUE® Drops) was used in veterinary for estrous (heat) prevention in adult female dogs not intended primarily for breeding purposes. No prescription preparation, human or veterinary, is currently known to contain mibolerone worldwide.

Amicycline is an anti-bacterial agent, an antibiotic of tetracycline class.

Reparixin is a CXC chemokine receptor type 1 (CXCR1) and type 2 (CXCR2) inhibitor. This compound has potential antineoplastic activity. It can be administered orally, binds to CXCR1 (overexpressed on cancer stem cells) and prevents its activation by its ligand interleukin 8. This might result in the death of cancer cells and inhibition of cell progression and metastasis. Reparixin also inhibits CXCR2 activation, possibly reducing both neutrophil recruitment and vascular permeability during inflammation or injury. A phase II clinical trial evaluating the effects of orally administered reparixin on cancer stem cells in the primary tumor and the tumoral microenvironment in an early breast cancer population was terminated. Reparixin has also been suggested as a novel potential therapeutic strategy for aggressive forms of thyroid cancer, based on results of a xenotransplantation study in mice.

AZD-3293 camsylate wider known as Lanabecestat camsylate, a salt of Lanabecestat, a drug that was invented for the treatment of Alzheimer's disease. Lanabecestat inhibits beta-secretase 1 cleaving enzyme (BACE1) thus preventing the buildup of beta-amyloid and help stop the progression of Alzheimer's disease. The drug was in phase III clinical trials, but studies were discontinued because of recommendations by an independent data monitoring committee (IDMC). IDMC concluded that all trials, in early Alzheimer’s disease, and in mild Alzheimer’s disease dementia, were not likely to meet their primary endpoints upon completion and therefore should be stopped for futility.

Lombazole is an antimicrobial agent of the imidazole class. It induced profound ultrastructural changes in Staphylococcus epidermidis and Candida albicans. Like other members of the imidazole series, such as clotrimazole, miconazole, and bifonazole, the compound has a broad spectrum of activity. It is active against several budding and filamentous fungi as well as gram-positive bacteria. Lombazole most probably interferes with fungal lipid synthesis by inhibiting sterol C-14 demethylation. Lipid biosynthesis is the primary site of action of lombazole in the bacterium Staphylococcus epidermidis. Lombazole was recommended against akne.

Coumermycin is from the aminocoumarin class of antibiotic compounds which acts by inhibiting DNA gyrase. Coumermycin is effective against gram-positive bacteria, but not gram-negative bacteria. Coumermycin its derivatives have been studied since the 1950's as potential antibiotic. However, it has seen little to no clinical development because of its low water solubility, toxicity profile, and ineffectiveness against gram-negative bacteria.

Firategrast (SB683699) is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS), that had been studied in phase II trials at GlaxoSmithKline under a license from Mitsubishi Tanabe Pharma for the oral treatment of multiple sclerosis (MS) in Europe. GlaxoSmithKline and Tanabe Seiyaku (now Mitsubishi Tanabe Pharma) had been studying the drug candidate for the treatment of asthma, rheumatoid arthritis (RA) and Crohn’s disease, but these studies had being discontinued. Firategrast is a drug for the treatment of multiple sclerosis (MS) which is found to be caused by the migration of leucocytes (such as monocytes, T cells, B cells and dendritic cells) into CNS. And the integrin α4β1 is found to take participate in the migration through activating the leucocytes. Firategrast has a much shorter half-life than natalizumab with about 2.5 hours to 4.5 hours. It is found to inhibit the binding of the integrins to the associated ligands, including vascular cell adhesion protein 1 and mucosal addressin cell adhesion molecule 1. In CNS, firategrast treatment caused moderate decreases of total lymphocyte count, lymphocyte subset count and the ratio of CD4 to CD8. In peripheral blood, firategrast treatment resulted in the increases of total lymphocyte count, all lymphocyte subset count as well as the peripheral CD34+ early haematopoietic progenitor cell count. Firategrast was well tolerated at the maximum doses of 1200 mg for men and 900 mg for women. Firategrast showed no side effects, such as PML or JC-virus reactivation, at these doses. In Phase I clinical trials, the administration of firategrast significantly reduced the cumulative number of new gadolinium-enhancing lesions in patients with relapsing remitting MS.

Pipratecol is substituted thienoimidazole. It is the H+/K(+)-ATPase inhibitor. In a high concentration of 10(-4) g/ml, pipratecol increased the amplitude of isolated guinea-pig atrial contractions while decreased the rate. But, in a low concentration of 10(-8) g/ml, the drug decrease the amplitude and increased the rate slightly. The effects of adrenaline and noradrenaline were suppressed by the preceding addition of pipratecol, while that of isoproterenol was scarcely. The effect of pipratecol on atrial contractions was hardly influenced by reserpine with which the animal had been pretreated 24 hours before the sacrifice of animal. The augmentative effect of nicotine on atrial contractions was slightly suppressed by the preceding addition of pipratecol. From these results, it was assumed that pipratecol has some affinity with the adrenergic receptor of atria. As a peripheral vasodilator it has been used in conjunction with raubasine in the treatment of cerebrovascular disorders. Pipratecol was used as antiulcerative agent also.

Prorenoate Potassium is a water-soluble synthetic aldosterone antagonist patented by Merck and Co., Inc. as an antihypertensive agent. In preclinical studies a significant natriuretic response was obtained at dosages of 1 mg/kg and approximately 1.8 mg/kg in the dog and rat, respectively. Prorenoate is relatively inactive at the renal level in adrenalectomized rats without mineralocorticoid replacement. Prorenoate possesses no more than 2% of the natriuretic activity of hydrochlorothiazide in the intact animal. Clearance studies in dogs indicate a direct renal tubular site of interaction between prorenoate and aldosterone independent of changes in renal hemodynamics. The natriuretic response occurred within 100 minutes after a single oral dose and was sustained for at least 7 hours. In clinical trials Prorenoate reversing the renal effects of the synthetic mineralocorticoid fludrocortisone in healthy individuals. Prorenoate was significantly more potent in retaining K+ than in increasing Na+ excretion.