Encaleret (JTT-305 or MK-5442) is a potent oral short-acting calcium-sensing receptor (CaSR) antagonist and transiently stimulates endogenous parathyroid hormone (PTH) secretion. CaSR antagonists stimulate endogenous PTH secretion through CaSR on the surface of parathyroid cells and thereby may be anabolic agents for osteoporosis. Japan Tobacco and Merck were developing encaleret for the treatment of osteoporosis however development has been discontinued.

Dexsotalol is an isomer of antiarrhythmic drug d,l-sotalol, but in opposite to drug, it increases the incidence of arrhythmias

Chugai Pharmaceutical is developing a parathyroid 1 receptor agonist called as PCO371. It is known that parathyroid hormone (PTH) is essential for calcium homeostasis and its action is mediated by the PTH type 1 receptor. PCO371 can provide a new treatment option for PTH-related disorders, including hypoparathyroidism. This drug participated in phase I clinical trial in healthy volunteers. However, Chugai Pharmaceutical has terminated this study. No recent reports of the development of PCO371are available.

Icopezil (previously known as CP-118,954) was developed as a selective acetylcholinesterase inhibitor for the treatment of cognitive disorders. Phase II trials of icopezil were underway in Japan and in the USA for the treatment of patients with Alzheimer's disease. However, Pfizer has discontinued these studies.

Vintriptol, a tryptophan ester of vinblastine, was developed as an antitumor drug. Vintriptol participated in a phase I clinical trial for the treatment of non-small cell lung cancer. As a result, was found a recommended dose for stage II. However, the further development of vintriptol was discontinued.

Solabegron (GW427353), a beta-3 adrenoceptor agonist, is in development with AltheRx (now Velicept Therapeutics) for the treatment of irritable bowel syndrome (IBS) and overactive bladder (OAB). Solabegron was discovered and first developed by GlaxoSmithKline. It was acquired by AltheRx, which merged with Velicept in 2015 to continue development of the program. Solabegron has been tested in over 800 study subjects in a twice-a-day formulation and demonstrated efficacy in the treatment of OAB as well as IBS. A once daily formulation designed to optimize patient convenience as well as efficacy has been developed and is currently being evaluated in a phase 2b dose ranging clinical trial. A Phase 2b dose ranging study with the twice daily formulation also began enrollment in Q1 2018.

LEDOXANTRONE, a benzothiopyranoindazole, is an intercalating agent. Its mechanism of action is probably due to DNA helicase blockade. It was under development for the treatment of prostate and ovarian cancers.