Tilomisole (also known as Wy-18,251) is a benzimidazole derivative patented by American Home Products Corp. as an antineoplastic agent with immunomodulating and antimetastatic activity. Tilomisole significantly enhanced the blastogenic response of cancer patients' lymphocytes in vitro. Tilomisole significantly increases macrophage phagocytosis against 51chromium labeled opsonized chicken red blood cells. In preclinical models, Tilomisole administration significantly increases peripheral blood lymphocytes in rats and demonstrates marked anti-inflammatory activity. The acute anti-inflammatory of Tilomisole.) was similar to aspirin, but in contrast to aspirin, Tilomisole failed to demonstrate antipyretic activity. Tilomisole also inhibited chronic inflammatory responses in the adjuvant- and collagen-induced arthritis models. Unfortunately, in clinical trials, Tilomisole failed to demonstrate significant antitumor responses.

Ameltolide (ADD 75073, LY 201116) is a 4-aminobenzamide anticonvulsant patented by Research Corporation Technologies in the USA. Ameltolide is a sodium channel antagonist, it represents a potential therapy for the treatment of epilepsy. Ameltolide had been in phase I clinical trials by Research Corporation Technologies for the treatment of epilepsy. However, this research has been discontinued.

SQ-109 is a [1,2]-diamine-based ethambutol (EMB) analog developed for the treatment of tuberculosis. SQ109 acts by inhibiting MmpL3, a transporter of trehalose monomyclate, which is an important component of cellular wall. The drug was investigated as a monotherapy or in combination with rifampicin in phase II clinical trials in pulmonary tuberculosis patients. The clinical trials, however, did not demonstrate activity of SQ-109 alone or its ability to enhance the activity of rifampicin.

Tasisulam sodium, previously known as LY573636, were initially recognized by Eli Lilly for their significant antiproliferative activities in solid tumor cell lines, but their mechanism of action was unknown. Subsequent studies have revealed that LY573636 induces apoptosis via a mitochondrial-mediated mechanism that appears unique among other anti-cancer compounds. This drug was in the phase III clinical trial for the treatment of Metastatic Melanoma and in phase II for the treatment Non-Small-Cell Lung Cancer, breast cancer, ovarian cancer, but these studies were discontinued. In vivo pharmacokinetic studies in rats and dogs indicate that tasisulam is metabolized primarily by the liver, and has low total plasma clearance with a relatively long half-life. In addition, there was preclinical evidence of a correlation between the maximum plasma concentration (Cmax) of tasisulam and toxicity.

Raluridine (also know as 935U83) is a nucleoside analog reverse transcriptase inhibitor patented by Wellcome Foundation Ltd. for the treatment of HIV infection. Raluridine has demonstrated selective anti-human immunodeficiency virus (HIV) activity in vitro and favorable safety profiles in monkeys and mice. When tested in phytohemagglutinin-stimulated normal human peripheral blood lymphocytes against fresh clinical isolates of HIV type 1 Raluridine inhibited virus growth with an average 50% inhibitory concentration of 1.8 microM. Importantly, Raluridine retained activity against HIV strains that were resistant to zidovudine, 2',3'-dideoxyinosine, or 2',3'-dideoxycytosine. The anabolic profile of Raluridine was similar to that of zidovudine, and Raluridine triphosphate was a potent inhibitor of HIV-1 reverse transcriptase. In clinical trials systemic exposure to Raluridine at levels exceeding its average in vitro antiretroviral 50%, inhibitory concentration (approximately 1.8 microM) can be achieved after a single oral dose.

Latrunculin A is a naturally occurring toxin that can be purified from the red sea sponge Latrunculia magnifica. It disrupts actin polymerization and prevents mitotic spindle formation; therefore preventing proper cellular replication. It was discovered that latrunculin A has strong anticancer effects, and it was investigated as a treatment candidate for peritoneal dissemination of gastric cancer.

Leukotriene B4 is a pro-inflammatory mediator synthesized in myeloid cells from arachidonic acid. Leukotriene B4 induces recruitment and activation of neutrophils, monocytes and eosinophils. It also stimulates the production of a number of proinflammatory cytokines and mediators indicating an ability to augment and prolong tissue inflammation. Elevated levels of leukotriene B4 have been found in a number of inflammatory diseases and levels are related to disease activity in some of these. Leukotriene B4 has a central role in metabolic dysfunctions. By increasing MyD88 expression, leukotriene B4 enhances macrophage response to TLR/IL1 receptor agonists potentiating the sterile inflammation, a central event in metabolic disease progression. Thus, leukotriene B4 is a potential therapeutic target for the treatment of metabolic disorders. Leukotriene B4 could serve as a biomarker for evaluating bestatin efficacy in colorectal cancer.

Suricainide (also known as AHR 10718) is an aminoalkylurea derivative patented by A. H. Robins Co., Inc. as an antiarrhythmic agent. Suricainide induces a use-dependent decrease in Vmax and significantly decreased Purkinje fiber conduction velocity and action potential duration. Suricainide had no effect on slow response action potentials induced by isoproterenol but ventricular muscle action potentials were significantly prolonged by Suricainide. Suricainide significantly decreased normal automaticity, catecholamine-enhanced automaticity, and abnormal automaticity induced by barium or myocardial infarction. In preclinical modes, Suricainide suppresses the aconitine-induced canine atrial arrhythmia.