Dacopafant (R-enantiomer RP 55778, racemate RP 48740) is an antagonist fo a platelet-activating factor and an inhibitor of TNH-alpha synthesis. It was developed by Rhone-Poulenc Rorer (France, now Aventis). In vitro, treatment of HIV-1 infected monocyte-derived macrophages with dacopafant resulted in a significant decrease in TNF-alpha levels and viral production. RP 48740 inhibited [3H]PAF platelet binding with IC50 of 2.3 uM and antagonized PAF-induced platelet activation with IC50 of 16 uM. In a clinical trial on human volunteers, RP 48740 was well tolerated and inhibited ex vivo platelet aggregation by as much as 79% 6 hr after administration.

Pinolcaine is 10-methyl-2-substituted piperidine. Pinolcaine is a local anesthetic.

Picoplatin is a sterically hindered platinum (II) complex with antineoplastic properties developed for the treatment of cis-platin-resistant cancer. Picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and transcription, and the induction of apoptosis. However, in Phase III trials, picoplatin failed to meet its primary endpoint for advanced cell lung cancer. It remains in development for other cancers.

Alozafone is an anticonvulsant (CNS depressant).

Benolizime is a sedative and hypnotic drug but was never marketed.

Glysobuzole (stabinol) is a sulfonamide derivative with antihyperglycemic activity. Like sulfonylureas, glysobuzole is able to lower blood glucose levels by increasing the release of insulin from pancreatic beta cells.

Foretinib is an orally available multikinase inhibitor that targets c-MET and VEGFR2 with high affinity, which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib is an experimental drug candidate for the treatment of cancer. It was in Phase II trials for the treatment breast cancer, non-small cell lung cancer, gastric cancer, head and neck cancer and papillary renal-cell carcinoma. The most frequent adverse events of any grade associated with foretinib were fatigue, hypertension, gastrointestinal toxicities, and nonfatal pulmonary emboli.

Tesofensine (also known as NS-2330) is a novel triple monoamine reuptake inhibitor with intrinsic inhibitory activity on norepinephrine (NE), serotonin (5-HT), and dopamine (DA) transporter function. It was development by NeuroSearch as a potential therapy for Alzheimer's disease (AD) and Parkinson's diseases, but these efforts have been discontinued. In phase II clinical trials with tesofensine in obese individuals, dose-related reductions in body weight, body fat and waist circumference, as well as improvements in other obesity-related endocrine factors were observed and the FDA recently endorsed the phase III trial program for this agent.

Mivobulin is a synthetic water-soluble colchicine analog with the broad antitumor activity that competitively binds tubulin at the colchicine-binding site and inhibits tubulin polymerization. Cancer cells exposed to Mivobulin isethionate accumulate in the M phase of the cell cycle and subsequently die. Preclinical studies have demonstrated that Mivobulin isethionate is able to cross the blood-brain barrier. Importantly, Mivobulin isethionate demonstrated significant antitumor activity in a broad spectrum of murine and human tumor models that were cross-resistant to vincristine, cisplatin, vinblastine, navelbine, and doxorubicin and in tumor cell lines exhibiting multidrug resistance owing to P-glycoprotein overexpression. In animal studies, the activity of Mivobulin isethionate was largely independent of the route of drug administration but favored a prolonged treatment schedule. Unfortunately, in clinical trials, Mivobulin fail to demonstrate the significant activity

Metrazifone was developed as an analgesic agent. However, this drug has never been marketed.