Cocaethylene is the ethyl ester of benzoylecgonine. Cocaethylene is formed in the liver after concurrent use of cocaine and alcohol. Cocaethylene works by blocking the dopamine transporter on dopaminergic presynaptic nerve terminals in the brain. It increases dopamine synaptic content, provoking enhanced postsynaptic receptor stimulation, resulting in euphoria, reinforcement, and self-administration. Compared to cocaine, which is a methyl ether of benzoylecgonine, cocaethylene has three to five times larger half-life in plasma. Cocaethylene is associated with seizures, liver damage and compromised the functioning of the immune system. It carries an 18-25 fold increase in risk for immediate death compared to cocaine alone.

Oxodipine is a dihydropyridine calcium channel blocker that has been developed by IQB as an antihypertensive agent. Experiments on dogs have shown that oxodipine exerted a relatively specific action on blood vessels without significant intrinsic negative chronotropic properties. in addition, in Europe, the drug was involved in phase III clinical trials in and in phase II for the treatment of Hypertension. Besides, oxodipine was studied for the treatment of ischaemic heart disorders. However, these studied were discontinued.

Atiprosin (AY-28,228), an octahydro-pyrazino-pyrido-indole drug, possesses the alpha-adrenoceptor antagonist activity and exerts antihypertensive effects. Atiprosin has never been marketed

Ataquimast, previously known as L0066, inhibits leukotriene release, TNFa and GM-CSF release but have no effect on IL-8 release. This drug participated in clinical trials to treat asthma, but these studies were discontinued.

FEXICAINE, a phenoxyacetic acid derivative, is a vasodilator and local anesthetic.

Rostaporfin (SnET2, Purlytin, REM-001), a second generation photosensitizer drug, that was developed as part of Miravant's PhotoPoint photodynamic therapy (PDT) program, for the potential treatment of wet age-related macular degeneration (AMD). It was found a red light with a wavelength of 664 nm activated the drug. It is injected into the patient, where it distributed and selectively bound to plasma lipoproteins, which were produced in high concentrations by hyperproliferating cells such as cancer cells. In January 2002, results of phase III trials indicated that rostaporfin had not met the primary efficacy endpoint for the wet form of AMD. In addition, rostaporfin has been studied in phase 2 and/or Phase 3 clinical trials in cutaneous metastatic breast cancer (CMBC). It was shown that the drug was able to reduce or eliminate a substantial number of treated CMBC tumors. On March 1, 2018, Adgero Biopharmaceuticals Holdings, Inc. announced that the U.S. Food and Drug Administration (“FDA”) has granted Orphan Drug Designation to REM-001 (rostaporfin), for the treatment of Basal Cell Carcinoma Nevus Syndrome (“BCCNS”). BCCNS is a rare but serious condition with few available therapies and many patients lack treatment options.

IZONSTERIDE, a benzoquinolinone, is a selective inhibitor of the 5-alpha reductase, with antagonistic effect on both the type I (liver, skin, hair follicles) and type II (prostate) isoforms of the enzyme. It is a competitive inhibitor of type I 5-alpha reductase and a non-competitive inhibitor of type II 5-alpha reductase. It was under development for the treatment of prostatic cancer.

Tariquidar, a non-competitive, specific P-glycoprotein (Pgp) inhibitor, is an anthranilamide derivative with multidrug resistance properties. Tariquidar binds to the ATP-binding cassette (ABC) transport protein Pgp, thereby inhibiting transmembrane transport of anticancer drugs resulting in their increased intracellular concentrations augmenting cytotoxicity of an anticancer drug. Tariquidar was discovered by Xenova Group and was developed for the treatment of multidrug resistance in cancer. In October 2002 the US Food and Drug Administration (FDA) has granted fast track review status to tariquidar for the treatment of multi-drug resistance in first-line treatment of non-small cell lung cancer (NSCLC) patients. Tariquidar is still undergoing research as an adjuvant against multidrug resistance in cancer.

FLUALAMIDE is an antiemetic agent.

CPG-52852 (PF-04878691) is a toll-like receptor 7 (TRL7) agonist. The drug was developed by 3M Pharmaceuticals and the Coley Pharmaceutical Group and was investigated in a number of clinical trials in patients with advanced cancer. Sustained tolerability and modest clinical benefit were demonstrated in heavily pretreated recurrent breast, ovarian, and cervix cancers. After Coley was acquired by Pfizer in 2007, the drug was repurposed for the treatment of hepatitis C. A phase 1 clinical trial was conducted. The development of the compound was discontinued because the compound was believed to unlikely to achieve the proof-of-concept criteria as a result of pharmacodynamic modeling.