Osaterone acetate (previously known as TZP-4238), a synthetic steroidal anti-androgen agent. Osaterone acetate is used in veterinary in Europe in the treatment of benign prostatic hyperplasia (BPH) in male dogs. Osaterone acetate inhibits the effects of an excess of male hormone (testosterone) through various mechanisms. It competitively prevents the binding of androgens to their prostatic receptors and blocks the transport of testosterone into the prostate. Osaterone acetate was also investigated in Japan in the treatment of prostate cancer and BPH and, in addition, was studied in postmenopausal osteoporosis in humans. However, these studies were discontinued.

Nexeridine, a pethidine derivative, is an opioid analgesic.

Spiroxasone is a synthetic, steroidal antimineralocorticoid of the spirolactone group patented by Merck & Co., Inc. as a diuretic and antihypertensive agent. Spiroxasone acts as potent aldosterone antagonists in animals and humans.

Josamycin propionate, a tasteless josamycin derivative suitable for the preparation of pediatric oral suspension. After oral administration Josamycin propionate underwent metabolic transformation to Josamycin, semi-synthetic 16-membered ring macrolide, that acts via protein synthesis inhibition.

Johnson and Johnson was developing usistapide, a microsomal triglyceride transfer protein (MTTP) inhibitor, for the treatment of obesity and type 2 diabetes. Usistapide, also known as JNJ-16269110 and R256918, has been used in trials studying the treatment of obesity, overweight, metabolic diseases, nutrition disorders, and nutritional and metabolic diseases. Usistapide was removed from the company pipeline and appears to have been discontinued.

Triclopyr-butotyl is an ester form of selective systemic herbicide triclopyr. Prolonged or frequently repeated skin contact with triclopyr-butotyl may cause allergic skin reactions in some individuals. Animal and in-vitro genetic studies were negative for triclopyr-butotyl. Triclopyr-butotyl did not cause cancer in laboratory animals.

Cu-64 is a radioisotope of copper with T1/2 12.7 hours. It decays by emission of beta+ particles with energies 0.653 (17.8%) MeV, which makes it suitable for positron emission tomography. The most widely used Cu chelators are DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) and TETA (1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetraacetic acid). Cu-64 acetate is used as a model compound to study metabolism and distribution of Cu-64.

Asperlin (also known as U-13,933), a fungal natural product that was isolated from marine-derived fungus Aspergillus sp. SF-5044 and exhibits antifungal and anti-inflammatory properties in vitro. Experiments in vivo have shown that this compound can prevent atherosclerosis through suppressing inflammation rather than ameliorating dyslipidemia. In addition, asperlin can be developed as a potential anti-cancer therapeutics. It shows anti-cancer properties through ROS generation and ATM pathway in human cervical carcinoma cells.