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.

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.

1α-HYDROXYVITAMIN D5 (CARD-024) is non-hypercalcemic, selective vitamin D receptor agonist under development for the treatment of cardiovascular disease, secondary hyperparathyroidism in chronic kidney disease and intestinal bowel disease fibrosis. CARD-024 attenuated the pro-fibrotic response of colonic myofibroblasts to high matrix stiffness, suggesting that it may ameliorate intestinal fibrosis.

KRN-7000, a compound with an alpha-galactosylceramide structure, shows potent anti-tumor activity in animal models. It also has strong immunostimulating effect being a high-affinity CD1d antigen.

16alpha-Bromoepiandrosterone (HE2000) is a synthetic steroid that limits non-productive inflammation, enhances protective immunity and improves survival in clinical studies of patients with human immunodeficiency virus (HIV), malaria and tuberculosis infections. HE 2000 had also shown activity in vitro against cytomegalovirus, polio, hepatitis B and C and influenza virus. 16alpha-Bromoepiandrosterone inhibits glucose-6-phosphate dehydrogenase (G6PD) and cell proliferation. HE 2000 was in phase II development for the Hepatitis B in Malaysia and Singapore, but it was suspended.

Phorbol 12-myristate 13-acetate (PMA) also commonly known as 12-O-Tetradecanoylphorbol-13-acetate (TPA) is a phorbol ester that is commonly used to activate phospholipid-dependent protein kinase (protein kinase C). PMA/ TPA possesses potential antineoplastic effects and was studied in phase II clinical trials together with dexamethasone in patients with relapsed or refractory acute myeloid leukemia. In addition, PMA/ TPA participated in phase I trial for treating patients with hematologic cancer or bone marrow disorder that has not responded to previous treatment. Nevertheless, both clinical trials were terminated. Besides, PMA/ TPA was studied in patients with solid tumors, which had depressed white blood cell and neutrophil counts because of prior treatment with cytotoxic cancer chemotherapeutic drugs. It was shown, that the drug increased the low white blood cell and neutrophil counts toward the normal range.

Phenylacetate is the ester of a phenol and acetic acid. It is a metabolite of anticancer drug phenylbutyrate (PB), natural neurotransmitter phenylethylamine. Naturally, it is an odorant found in strawberries, passion fruit, and black tea. Phenylacetate level in urine was used as a marker for the diagnosis of some forms of unipolar major depressive disorders. Phenylacetate is used as a tool substrate to study esterase activity in the blood of patients in clinical studies of the effect of nutritional supplements on paraoxonase-1 levels.