Viprostol (also known as CL115,347), a prostaglandin E2 congener that was studied as an antihypertensive agent. Viprostol has a potent and prolonged blood pressure lowering effect in many models of hypertension. In clinical studies, viprostol has been demonstrated to lower arterial blood pressure significantly in man following transdermal and/or intravenous administration. The antihypertensive action of viprostol has been suggested to be the result of peripheral vasodilatation. In addition, the drug participated in a clinical trial in normal subjects and in patients with Raynaud's phenomenon. It was found the optimal dosage was 1000 ug; the effect could last for 84 hours; higher dosage may be associated with a "steal" phenomenon.

Emopamil is a phenylalkylamine calcium antagonist. Emopamil has optically active stereoisomers. Emopamil enhanced the postischemic restoration of high-energy phosphate levels. The racemic mixture and the (-)-enantiomer of emopamil caused similar metabolic changes while (+)-enantiomer of emopamil proved to be ineffective. Emopamil is able to reverse multi-drug resistance in human KB cell lines. No differences in reversing potency were observed between emopamil (R)-isomers, (L)-isomers and the racemic form. There is a pharmacological relationship between sigma1-binding site and the mammalian sterol C8-C7 isomerase which is identical with the emopamil binding protein.

Retaspimycin (IPI-504) was previously under development by manufacturer Infinity Pharmaceuticals in conjunction with MedImmune, a part of AstraZeneca. Retaspimycin is a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis. Orphan drug designation was assigned to the compound by the FDA for the treatment of gastrointestinal stromal cancer (GIST). Infinity Pharmaceuticals has discontinued the development of retaspimycin (IPI-504) an inhibitor of the HSP-90) complex, for the treatment of cancer due to lack of efficacy in 1913.

Myrophine is an opiate analog and long-acting prodrug for morphine with a slow onset of effects. It is weaker than morphine as an analgesic but longer-lasting in effects and was thought to have a more local anesthetic effect than morphine, though with a somewhat greater tendency to cause histamine reactions like itching and rash. In addiction studies conducted in human subjects in the 1950s, myrophine did not substitute for morphine in withdrawal, did not produce notable morphine-like effects, and did not produce addiction or dependence regardless of dose or how it was administered.

Capravirine (S-1153, AG1549) is a 1,2,4,5-tetrasubstituted imidazole derivative patented by pharmaceutical company Shionogi as specific inhibitors of HIV-​1 reverse transcriptase. However, safety and efficacy studies showed that Capravirine had no specific advantages over currently used NNRTIs. Consequently, clinical trials were discontinued after phase IIb.

Desomorphine is the common name for 4,5--epoxy-17- methylmorphinan-3-ol or dihydrodesoxymorphine-D. It is an opioid analogue and morphine derivative in which the 6-hydroxyl group and the double bond at carbons 7 and 8 of morphine are reduced. Desomorphine can cross the blood–brain barrier, binding to opioid receptors, similar to the pharmacokinetic distribution of all phenanthrene-structured alkaloids. Taking Desomorphine causes euphoria as well as sedative and analgesic relief. In addition to its faster onset than other powerful painkillers drugs such as morphine, desomorphine also initiates less sedative effects and seems to have favorable postoperative results, such as reduced need for catheterization, less dizziness, and decreased vomiting incidence. In comparison with Morphine, Desomorphine is faster reduced. It follows that it has to be taken it more frequently to get the same effects. Furthermore, it causes side effects such as respiratory and gastrointestinal problems and increased blood pressure. In addition, Desomorphine’s withdrawal symptoms are up to three times longer than Morphine’s. This leads to the conclusion that Desomorphine is more addictive. At present, desomorphine is classified as a narcotic drug (DEA code number 9055) in Schedule I of the U.S. Controlled Substances Act and is listed as a controlled substance under the international Single Convention on Narcotic Drugs of 1961.

Rivoglitazone hydrochloride (CS-011) is a thiazolidinedione-derivative peroxisome proliferator–activated receptor (PPAR)-γ agonist. It has been developed as potential treatment in type 2 diabetes mellitus and was shown to decrease plasma glucose and triglyceride levels in a dose-dependent manner in animals. Phase II and III clinical studies have assessed the efficacy and safety of rivoglitazone hydrochloride in patients with type 2 diabetes mellitus.

Bedoradrine (also known as KUR-1246 or MN-221), an ultra selective beta 2-adrenoceptor agonist, that participated in phase II clinical trials as an adjunct to standard therapy in the management of patients with acute exacerbation of asthma who did not respond to standard therapy. In addition, the drug was involved in trials for the treatment of preterm labor in obstetrical practice. Bedoradrine is also was studied in phase I of clinical trials for its use for treating chronic obstructive pulmonary disease, however, the efficacy for this disease was uncertain.

Apratastat (Tmi 005) was developed by Wyeth Research as a dual TNF-alpha-converting enzyme and matrix metalloprotease-13 inhibitor for the treatment of rheumatoid arthritis. Apratastat was in phase II clinical trials, but because of the lack of efficacy, this trial was terminated.

Vestipitant, also known as GW597599, is a neurokinin1 receptor antagonist that was being developed by GlaxoSmithKline for the treatment of postoperative nausea and vomiting. Vestipitant is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It was under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitus and insomnia. Vestipitant was shown to improve sleep maintenance in patients with primary insomnia, with no associated next-day cognitive impairment. The effects on wake after sleep onset and total sleep time were maintained following repeated dosing. Vestipitant has anxiolytic properties and a good safety profile. Vestipitant was investigated for potential effect against chronic tinnitus as a stand-alone treatment and in conjunction with a selective serotonin reuptake inhibitor, paroxetine. Although well-tolerated vestipitant, alone or in combination with paroxetine, was not effective in ameliorating tinnitus in this patient group.