Orteronel (TAK-700) is a non-steroidal antiandrogen, discovered by Takeda Pharmaceutical Company Limited, that selectively inhibits the 17,20 lyase enzyme (CYP17A1). This enzyme, which is present in both the testes and adrenal glands, is central to the production of steroidal androgens. Synthesis of androgens outside the testes contributes to disease progression in castration-resistant prostate cancer (CRPC). In phase III of clinical trials for metastatic, hormone-refractory prostate cancer it wasn’t shown overall survival rates, and development was voluntarily terminated as a result.

GM-602 (GM6) is a six-amino-acid active analog peptide of Motoneuronotrophic factor (MNTF). This compound is a small peptide that can cross the blood-brain barrier and has been shown to induce an embryonic-like neuroprotective microenvironment that helps detect and self-correct CNS- and neurodegenerative-related pathophysiology. Phase II clinical trials with GM-602, GM-604 and GM-608 have been completed to examine its potential in respectively stroke, Amyotrophic Lateral Sclerosis (ALS), and Parkinson’s disease.

Bisegliptin (also known as KRP-104) was developed as an orally active dipeptidyl peptidase IV (DPPIV) inhibitor. It is known, that DPPIV inhibition reduces blood glucose through suppression of the degradation of the insulin-releasing hormone. Bisegliptin successfully completed the phase II clinical trials for patients with type 2 diabetes. However, further development of the drug has been discontinued for business reason. The company wasn’t able to find a tie-up partner to co-develop.

Avelestat, also known as AZD9668, is a novel, oral inhibitor of neutrophil elastase (NE), an enzyme implicated in the signs, symptoms, and disease progression in NE-driven respiratory diseases such as bronchiectasis, Cystic Fibrosis and chronic obstructive pulmonary disease via its role in the inflammatory process, mucus overproduction, and lung tissue damage. Its development was discontinued due to unknown reasons. Nevertheless, this drug in the phase II of clinical trial as adjunctive therapy in improving insulin sensitivity of insulin-resistant type 2 diabetic subjects. The drug's clinical profile suggests that it will be well tolerated with few, if any, side effects, and the existence of simple methods that can indirectly measure its activity in vivo.

Elbimilast or ronomilast (previously ELB 353) is a phosphodiesterase IV (PDE4) inhibitor. It has been investigated in the treatment of chronic obstructive pulmonary disease.

Mavoglurant (AFQ056) was developed as a new metabotropic glutamate receptor 5 (mGluR5) antagonist. The efficacy of mavoglurant in humans has been assessed in L-dopa induced dyskinesia in Parkinson's disease and Fragile X syndrome in proof of principle clinical studies. However, Novartis had announced that the company would be discontinuing its development program in Fragile X following negative results in a large international clinical trial in adults, and more recently in a trial in adolescents. In both placebo-controlled trials, patients taking mavoglurant did not show improvement over placebo in any outcome measures. In patients with L-Dopa-induced dyskinesias studies failed to meet the primary objective of demonstrating improvement of dyskinesia. Mavoglurant was also investigated in phase II clinical trials to reduce chorea in Huntington's disease, but the target result was not achieved. Currently Novartis is conducting a phase II clinical trial to demonstrate whether or not this drug can benificially reduce cocaine use in Cocaine Use Disorder.

Aganepag isopropyl, an IOP-lowering agent, is an antiglaucoma agent. It is a selective EP2 receptor agonist.

Suncillin is an antibacteria and antifungal agent produced in Phytera's laboratory from a cell culture of a plant. Suncillin was patented by Bristol-Myers Co. In 1968 for the Pseudomonas bacteria treatment but was never marketed.