Turosteride [FCE 26073] is a selective 5α-reductase inhibitor being developed by Pharmacia Corporation. Turosteride inhibits human and rat prostatic 5 alpha-reductases with IC50 values of 55 and 53 nM, respectively. It was in phase II clinical trials in Italy for the treatment of benign prostatic hyperplasia.

Asoprisnil (J867) is a novel selective steroid receptor modulator that shows unique pharmacodynamic effects in animal models and humans. Asoprisnil, its major metabolite J912, and other structurally related compounds represent a new class of progesterone receptor (PR) ligands that exhibit partial agonist and antagonist activities in vivo. Asoprisnil demonstrates a high degree of receptor and tissue selectivity, with a high-binding affinity for PR, moderate affinity for glucocorticoid receptor (GR), low affinity for androgen receptor (AR), and no binding affinity for estrogen or mineralocorticoid receptors. This compound was recently in clinical trials for the treatment of uterine fibroids and endometriosis, but those studies were discontinued.

Formebolone is an orally active anabolic-androgenic steroid that is included in the list of prohibited substances by the World Anti-Doping Agency. Formebolone was used in Italy and Spain for infants with malnutrition.

Sunagrel is a phenylethanolamine derivative patented by Maggioni Farmaceutici S.p.A. as platelet aggregation inhibitor and antilipidaemic agent.

Fialuridine I-124 is an isotope-labeled form of fialuridine, or 1-(2-deoxy-2-fluoro-1-D-arabinofuranosyl)-5-iodouracil (FIAU), a thymidine nucleoside analog with activity against various herpesviruses and hepatitis B virus (HBV) in vitro and in vivo. Bacterial or herpes virus thymidine kinase (TK) considered to be a target of FIAU. Fialuridine I-124 is a positron emission tomography/computed tomography (PET/CT) tracer that was developed for imaging of cells transfected with the herpes simplex virus 1 (HSV1) thymidine kinase reporter gene. This enzyme transfers a γ phosphate group fom ATP to the 5’ hydroxyl group of pyrimidine deoxynucleosides. The lipophilic tracer diffuses into the cell and is trapped in the cell with HSV1-TK activity, because the phosphorylated tracer cannot pass the plasma membrane. TK gene of bacteria was sufficiently similar to that of the viral TK of HSV1 and fialuridine I-124 could also be phosphorylated by the endogenous bacterial TK. Once phosphorylated by TK, fialuridine I-124 becomes trapped within bacteria and can be detected with positron emission tomography/computed tomography (PET/CT).

Tigloidine is a tropane alkaloid and a naturally occurring analog of atropine, found in small quantities in Duboisia myoporoides. Tigloidine has been found to be beneficial in the treatment of Parkinsonism, Huntington’s Chorea and spastic paraplegia. Tigloidine may provide relief in parkinsonian patients by increasing the gamma-efferent activity and reducing alpha motoneurone activity. In preclinical models, Tigloidine failed to reverse sedation and ptosis in rats induced by reserpine and tetrabenazine. In mice, amphetamine response was not significantly affected by Tigloidine or atropine. However, in the cat and dog, it was markedly facilitated by Tigloidine but not by atropine.

Dexamethasone beloxil is anti-inflammatory used in the treatment of uveitis, iritis, keratitis, postsurgical inflammation, vernal keratoconjunctivitis, and giant papillary conjunctivitis.

Rebeccamycin analog (RA, Becatecarin/ BMS 181176, rebeccamycin derivative, NSC 655649) is an antitumor antibiotic with inhibitory activity against both topoisomerase I and II, and DNA-intercalating properties. The mechanism of action of becatecarin is not exactly known, but it is thought that by inhibiting (blocking) the function of topoisomerase enzymes, it will destroy cancer cells and slow down the growth of the tumour. On 25 July 2006, orphan designation (EU/3/06/388) was granted by the European Commission to Helsinn Birex Pharmaceuticals Ltd, Ireland, for becatecarin for the treatment of cancers of the biliary tree.

Lodenosine is the experimental HIV reverse transcriptase inhibitor. It was designed as a chemically and enzymatically stable anti-AIDS drug. A phase II trial of the nucleoside analog lodenosine was suspended after one participant died and others showed signs of liver or kidney damage.