Razupenem (also known as PZ-601 or PTZ601) is an anti-MRSA carbapenem antibiotic. It is active against Enterobacteriaceae and Gram-positive bacteria including methicillin-resistant staphylococci and enterococci, and was investigated as potential alternative drug (replacing common antibiotics) against resistant bacteria. In healthy male volunteers, razupenem did not cause serious adverse events. The potential effect and safety of razupenem has been evaluated in a phase II clinical trial studying skin infection.

Volinanserin (MDL-100,907) is a highly selective 5-HT2A receptor antagonist. It is widely used in scientific research to investigate the function of the 5-HT2A receptor. Volinanserin is also being trialed as a potential antipsychotic, antidepressant and treatment for insomnia. Volinanserin (M-100907) was in phase III trials for chronic schizophrenia. In August 1999, development was discontinued for acute schizophrenia (schizoaffective disorder) on the basis of poor results. M-100907 is also active in animal models involving blockade of NMDA glutamatergic channel receptors, an effect known to resemble some behavioral symptoms of schizophrenia in man. M-100907 is also claimed in other patents for the treatment of thromboembolic disorders, for the treatment of various developmental neurological disorders such as autism and attention deficit hyperactivity disorder.

Clomifenoxide (clomifene N-oxide) is a metabolite of clomifene, a nonsteroidal ovulatory stimulant, which is used clinically for the treatment of ovulatory dysfunction in women desiring pregnancy. Compared to clomifene, clomifenoxide exhibits weaker binding to estradiol receptors.

Tibeglisene (also known as BM 13907) is a pentynoic acid derivative patented by Boehringer Mannheim G.m.b.H. as insulin sensitizer with hypoglycemic activity. Tibeglisene is also able to reduce serum triglyceride and cholesterol concentrations. Tibeglisene exerts favor influences on glucose-transport activity.

Rosonabant (E-6776) is a CB1-receptor antagonist that has appetite suppressant activity and was under development for the treatment of obesity. This preclinical anti-obesity drug shows activity that is similar to romonabant, a drug that was withdrawn from the European market due to severe side effects such as nausea, depression and suicidal ideations. Drug development of rosonabant has subsequently been halted.

Desocriptine is an ergot alkaloid (alpha-dihydro-beta-ergocryptine) derivative. It is a combined alpha- and beta-adrenoceptor antagonist. Desocriptine is antihypertensive and antianginal agent.

Cerlapirdine is a selective and potent full antagonist of the serotonin 6 (5-HT6) receptor that has been investigated by Wyeth and Pfizer for the treatment of Alzheimer Disease.

SGI-1776 is a PIM-kinase inhibitor, developed by SuperGen Inc. SGI-1176 was tested in clinical trials against relapsed/refractory leukemias, prostate cancer and Non Hodgkin's Lymphoma, but the dose limiting toxicity of cardiac QTc prolongation was identified and clinical development of SGI-1776 was terminated.

MSDC 0602, a first-in-class oral, once-daily, insulin sensitiser that acts by stimulating mitochondrial proteins, is being developed by Metabolic Solutions and Cirius Therapeutics for treatment Type 2 diabetes mellitus and Non-alcoholic steatohepatitis. MSDC-0602 prevented and reversed liver fibrosis and suppressed expression of markers of stellate cell activation in livers of mice fed a diet rich in trans-fatty acids, fructose, and cholesterol. Moreover, mice with liver-specific deletion of MPC2 were protected from development of NASH on this diet. MSDC-0602 directly reduced hepatic stellate cell activation in vitro, and MSDC-0602 treatment or hepatocyte MPC2 deletion also limited stellate cell activation indirectly by affecting secretion of exosomes from hepatocytes. Cirius Therapeutics plans the phase III trial for Type 2 diabetes mellitus and Non-alcoholic steatohepatitis in September 2019