Fluprofylline, a central stimulant, was a very selective though not very potent alpha 1-adrenoceptor antagonist. However, information about the further development of this compound is not available.

Fluperamide was developed as an antiperistaltic agent for the treatment of diarrhea. However, information about the current use of the drug is not available.

MK-0767 is a potent hypoglycaemic insulin sensitizer being evaluated by Kyorin with potential as an antidiabetic agent. MK-0767 acts as a dual agonist of the peroxisome proliferator-activated receptors alpha and gamma, induced high-affinity interactions of PPARα and PPARγ with the transcriptional coactivator CBP in vitro. In ob/ob mice, MK-0767 normalized hyperglycemia and hyperinsulinemia with equal or greater potency and efficacy than pioglitazone. Treatment of hamsters with MK-0767 produced substantial reductions in blood cholesterol and triglycerides. In dogs, MK-0767 reduced serum cholesterol levels with a potency more than 10-fold greater than simvastatin. The efficacies of MK-0767 and simvastatin were additive when given together.

Darinaparsin is a novel mitochondrial-targeted agent being developed for the treatment of various hematologic and solid cancers. In a Phase II study in the US, intravenous darinaparsin demonstrated evidence of clinical activity in malignant lymphoma, and in particular peripheral T-cell lymphoma (PTCL). Darinaparsin was granted Orphan Drug Designation in the US and Europe as a treatment of PTCL. The oral formulation is also being tested in Phase I for the treatment of solid tumors. Darinaparsin induces G2/M cell cycle arrest and apoptosis in tumor cells, primarily through disruption of mitochondrial functions, increased reactive oxygen species (ROS) production and modulation of signal transduction pathways.

CI 1040 is an inhibitor of the mitogen-activated protein (MAP) kinase signal transduction pathway and has been shown to specifically inhibit MAP kinase kinase (MEK). CI 1040 was being developed by Parke-Davis (formerly a division of WarnerLambert, Now Pfizer) as an anticancer agent. It was the initial MEK inhibitor to undergo clinical evaluation based on promising preclinical activity. However, its development has been discontinued.

PERFLUBRODEC is a component of an artificial perfluorochemical-based oxygen carrier OXYGENT. Using solely 3.6%w/v egg yolk phospholipid, Alliance Pharmaceutical Corporation (San Diego, California, USA) developed a concentrated (60% w/v) and stable perfluorocarbon emulsion, OXYGENT, which is composed of 58% w/v perfluorooctyl bromide and 2% w/v perfluorodecyl bromide, with an average particle size of 0.16-0.18 μm diameter. As a blood substitute OXYGENT has been administered to patients undergoing surgeries in clinical trials, however development was discontinued.

CX 516, a compound synthesized by Cortex Pharmaceuticals using Ampakine® technology licensed from the University of California, was in clinical investigations for the treatment of Alzheimer's disease, schizophrenia, fragile X syndrome and autism, and sleep disorders, however, development of this drug candidate has been discontinued. CX 516 had an extremely short halflife in humans, very low potency and failed to show any benefits in phase II studies. The compound did have a good safety profile, reducing concerns about the toxicity of excess glutamate. Cortex subsequently terminated clinical development of CX 516.

Tipifarnib is an oral farnesyltransferase (FTase) inhibitor which was developed by Janssen (J&J). Upon administration, tipifarnib inhibits FTase and thus suppresses the activity of downstream effectors. The drug reached phase III of clinical trials for such diseases as pancreatic cancer (terminated), colorectal cancer (terminated) and acute myeloid leukemia (in elderly patients).