AstraZeneca (formerly Astra) is developing robalzotan (NAD-299, AZD-7371), a 5-HT1A antagonist, for the potential treatment of depression and anxiety. The compound has entered phase II trials but was discontinued. Then it investigated for the treatment of irritable bowel syndrome, but the study was prematurely terminated. The same final has expected the development of robalzotan in phase II to treat overactive bladder, this investigation was terminated in July 2005.

Zaurategrast (CDP323) is an ethyl ester prodrug of CT7758, a potent carboxylic acid antagonist of integrin alpha4-beta1 (α4β1) or very late antigen 4 (VLA4). CDP323 was under development with UCB and Biogen Idec for the treatment of multiple sclerosis. Its development was discontinued in 2009 based on inadequate interim efficacy data in a phase II clinical trial.

Alovudine (3’ -deoxy-3’ fluorothymidine) is a nucleoside reverse transcriptase inhibitor (NRTI) initially tested in the early 1990s, before the era of combination therapy and before the availability of plasma viral load measurement. Initial toxicity studies showed that the primary target organ of toxicity was the bone marrow. A lack of clear advantages in activity over zidovudine, the only drug approved in the early 1990s, and the potential for bone marrow toxicity caused alovudine development to be stopped [6]. However, later in vitro studies found alovudine to be very effective at suppressing several NRTI-resistant HIV-1 mutants, including isolates with multiple thymidine-associated mutations (TAMs) or multi-NRTI-resistance mutations. Alovudine at a dose of 7.5 mg/day added to a failing antiretroviral combined regimen in patients with isolates resistant to other NRTIs yielded a median viral load decline after a 4-week period in patients not receiving concomitant stavudine. In July 2003, Medivir out-licensed it's HIV antiviral MIV-310 to Boehringer Ingelheim. Under the terms of the agreement, Boehringer Ingelheim will make upfront and milestone payments to Medivir totaling up to 122 million euro in the event that all development and performance milestones are met. In March 2005, Boehringer Ingelheim recently completed a clinical trial of MIV-310 (alovudine) in HIV/AIDS. The efficacy exhibited by MIV-310 at the doses tested showed antiviral activity but did not achieve the target level of efficacy which had previously been defined. Boehringer Ingelheim, therefore, decided to stop the development of this investigational drug.

Ravuconazole is a triazole with antifungal properties that inhibits cytochrome P450 sterol 14a-demethylase, an enzyme involved in sterol synthesis, resulting in lysis of the fungal cell wall and fungal cell death. It was investigated for the treatment of aspergillosis, candidiasis, and onychomycosis, but these studies were discontinued. Ravuconazole is now in phase II clinical trials to investigate efficacy in preventing fungal infections in patients undergoing chemotherapy and stem cell transplantation.

Sulrnazole (the former AR-L 115 BS) is a benzimidazole derivative with positive inotropic, positive chronotropic and vasodilator effects. Sulrnazole also has been shown to improve cardiac index and reduce pulmonary capillary wedge pressure without significant change in heart rate or arterial pressure. Intravenous administration caused a 217 per cent increase in cardiac output with a 25 per cent decrease in pulmonary wedge pressure. Short-term oral administration resulted in a 317 per cent increase in cardiac index and a 317 per cent increase in ejection fraction. Side effects have included visual blurring and transient colour blindness. Sulmazol has been demonstrated to improve regional wall motion in patients with ischemic heart disease and to abolish pacing-induced ischemia. Sulrnazole is an A1 adenosine receptor antagonist. It is also a phosphodiesterase inhibitor.

The natural tetrapeptide acetyl-N-Ser-Asp-Lys-Pro (AcSDKP also known as Goralatide) is generated from the N-terminus of thymosin-β4 through enzymatic cleavage by prolyl oligopeptidase (POP). AcSDKP regulation of proliferation of different cells is implicated in hematopoiesis and angiogenesis. This tetrapeptide present in almost all cells was recently detected at elevated concentrations in neoplastic diseases. However, previously reported in vitro and in vivo studies indicate that AcSDKP does not contribute to the pathogenesis of cancers. AcSDKP was in the phase II clinical trial for development of a new non-radioactive test for measuring glomerular filtration rate in patient with Chronic Kidney Disease. In addition, using mice models was concluded ,that AcSDKP might be an oral antifibrotic peptide drug that would be relevant to combating fibroproliferative kidney diseases such as diabetic nephropathy.

MK-2866 (Gtx-024) is a selective androgen receptor modulator (SARM) for treatment of conditions such as muscle wasting and osteoporosis. It is a non-steroidal agent with anabolic activity designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.

Loxoribine [RWJ 217C7] is an immunostimulant which was developed by Johnson and Johnson. It is a selective agonist for TLR7 (Toll-like receptor 7), which possesses antitumor and antiviral properties and was investigated in a rat model of endometriosis and in addition, in phase I of a clinical trial for patients with advanced cancer.

Taranabant is a highly selective cannabinoid-1 (CB1) receptor inverse agonist developed by Merck & Co for the treatment of obesity. The Phase III taranabant study involved about 2,400 patients and was to be conducted for two years. In March 2008, after completion of 52 weeks of the study, Merck reported positive results of the drug in conjunction with diet and exercise in obese patients. The patients experienced double the amount of weight loss by taking 2mg of taranabant when compared to the patients treated with placebo. However, in October 2008, the company discontinued the Phase III programme and clinical development of taranabant because of its side effects. The drug showed gastrointestinal and psychiatric side effects such as increased anxiety, depression and irritability. Merck had previously planned to file for regulatory approval with the US Food and Drug Administration in 2008, but subsequently withdrew it.

Linifanib (ABT-869) is a structurally novel, receptor tyrosine kinase (RTK) inhibitor that is a potent inhibitor of members of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor families, but has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib (ABT-869) does not have a general antiproliferative effect due to its high dose requirement. However, it may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3). Linifanib (ABT-869) was in phase III clinical trial for the treatment of hepatocellular carcinoma, but the study failed to meet the primary end point.