Sumarotene (also known as Ro 14-9706) is a third-generation retinoid developed by Hoffmann-La Roche, F., und Co. A.-G., as a topical dermatologic agent for the repair of photodamage, antikeratinization, and antiproliferation. Sumarotene shows activity in standard preclinical and pharmacologic models of repair of photodamage, antikeratinization, and antiproliferation. In clinical trials, Sumarotene effectively decreases the number of actinic keratoses. Sumarotene is well-tolerated and most patients have only slight or absent local inflammation.

Lotifazole (F 1686) - 4-phenyl-2-(2',2',2-trichloroethoxycarboxamido) thiazole is an immunostimulant. It has a range of anti-inflammatory activities in animals that differs from the activities of classic non-steroidal drugs.

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

Sabeluzole (previously known as R 58 735) was developed for the treatment of Alzheimer's disease. It reached phase II clinical trials in Canada and Belgium before its development was discontinued. This drug possibly acts as N-methyl-D-aspartate (NMDA) receptor antagonist. In addition, the effect of sabeluzole on sleep, breathing and daytime symptoms was investigated in 13 patients with obstructive sleep apnea. Besides, no beneficial effect of sabeluzole was shown on peripheral nerve function in patients at an early stage of diabetic polyneuropathy.

Alprenoxime is a prodrug to alprenolol. Alprenoxime is a β-blocker that was in phase II clinical trials with Pharmos in the USA as an antiglaucoma agent. Alprenoxime is a potent ocular antihypertensive agent. Alprenoxime was designed to undergo metabolic activation to the beta-blocker, alprenolol, specifically within the eye using hydrolase and reductase enzymes that reside in the iris-ciliary body. Previous studies in rabbits confirmed that intraocular pressure (IOP) significantly decreased after topically instilling ophthalmic drops of alprenoxime, while heart rates remained essentially unchanged after intravenous dosing. Alprenoxime has no significant cardiac activity at doses much greater than potential therapeutic levels, supporting that alprenoxime could be safely used in treating glaucoma. Alprenoxime was taken to clinical trials and has successfully passed Phase I studies, demonstrating complete lack of cardiovascular side effects, even in humans, including isoprenaline induced tachycardia.

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).

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.

Vintoperol (also known as RGH 2981), a peripheral circulation-enhancing compound that was developed as a moderate serotonin and calcium channel antagonist. Vintoperol was studied for the treatment of arterial occlusive disease and peripheral vascular disorders. It was shown that this compound interfered with platelet aggregation both in vitro and in vivo and possessed potent antithrombotic effects in thrombosis models in which platelet activation was mainly involved. Vintoperol participated in phase II clinical trials in Japan for the treatment patients with arterial occlusive disorders, peripheral vascular disorders, and thrombosis. However, because of its toxic side effects, vintoperol was discontinued from the clinical practice.