Sufosfamide is an oxazaphosphorine derivative patented by Asta-Werke A.-G as immunosuppressives agent. Sufosfamide is a mixed-function oxazaphosphorine differing from ifosfamide in that the extracyclic 2-chloroethyl function has been replaced by a mesyl-oxyethyl group. It is characterized by an extraordinary intensifi¬cation of the immunosuppressive component of action compared to the carcinotoxic component. Sufosfamide activates of a specific immune tolerance in models of humoral end cell-bound antibodies.

Adibendan [BM 14478] is a phosphodiesterase inhibitor that increases the calcium sensitivity of the myocardium. Adibendan selectively inhibited phosphodiesterase III (PDE III) activity concentration-dependently (IC50 = 2.0 umol/l). The IC50 values for the inhibition of PDE I or II were more than 60-fold higher. Adibendan has both vasodilator and positive inotropic properties. Adibendan was investigated as the potential treatment of heart failure and ischaemic heart disorders. However, research has been discontinued at phase II of development.

Examorelin (Hexarelin) is a hexapeptide (His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2) that stimulates the release of growth hormone lease through binding to the growth hormone secretagogue receptor (GHSR). Hexarelin might have direct cardiovascular actions beyond growth hormone release and neuroendocrine effects. Europeptides and Mediolanum Farmaceutici were developing examorelin for the treatment of somatotropin deficiency.

Zimidoben was developed as an antiinfective drug. Information about the current use of this compound is not available.

Temarotene (also known as Ro 15-0778), the arotinoid with immunosuppressive and immunostimulatory activities. Temarotene was also studied as a chemopreventive agent. Information about the current development of this compound is not available.

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.

Almestrone (7 alpha-methylestrone) is a synthetic steroidal estrogen. It is a precursor of several highly active steroidal hormones.

Sonolisib (PX-866) is a small-molecule inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. Sonolisib inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Inhibition of the PI3K pathway with Sonolisib leads to inhibition of cell growth and decreased activation of downstream targets in GBM, both in vitro and in vivo, using U87–tumor-bearing mice, including Akt, S6, and mTOR. Sonolisib was in phase II clinical trials by Oncothyreon for the treatment of glioblastoma multiforme and castration-resistant prostate cancer (CRPC). It was in phase I/II clinical trials for the treatment of malignant melanoma, non-small cell lung cancer and Head and neck cancer. In clinical trials, Sonolisib was well tolerated, with common side effects being diarrhea, nausea, vomiting, and elevated liver enzymes. However, no recent development has been reported.

Prenoverine is diphenylmethanol derivative patented by Andreu, Dr. S. A. as a muscle relaxant. Prenoverine shows good multidrug resistance-reversal activity.

Namitecan (ST1968) is a camptothecin analogue being developed by sigma-tau (a subsidiary of Alfasigma) in Switzerland for the treatment of cancer. Namitecan, a novel hydrophilic camptothecin analog of the 7-oxyiminomethyl series, was selected for clinical development on the basis of its promising preclinical efficacy. Namitecan is a topoisomerase I inhibitor. Namitecan exhibited an acceptable toxicity profile, with neutropenia being the dose-limiting toxic effect, and clinical benefit was appreciable in patients with different tumor types, particularly bladder and endometrium carcinomas.