Lobendazole is a metabolite of veterinary drug thiophanate. Lobendazole possesses teratogenic effect.

Pirodavir (R77975) (ethyl 4-[2-(1-[6-methyl-3-pyridazinyl]-4-piperidinyl)ethoxy]benzoate) and its predecessor (R61837) belong to a series of pyridazine analogues developed by the Janssen Research Foundation. Compared to R61837, pirodavir was 500-fold more potent as an antiviral in vitro, inhibiting 80% of 100 rhinovirus serotypes tested at concentration of 0.064 mg/mL or less. Pirodavir acts at an early stage of the viral replication cycle (up to 40 min after infection) and reduces the yield of selected rhinoviruses 1,000- to 100,000-fold in a single round of replication. The mode of action appears to be serotype specific, since pirodavir was able to inhibit the adsorption of human rhinovirus 9 but not that of human rhinovirus 1A. Pirodavir is a novel capsid-binding antipicornavirus agent with potent in vitro activity against both group A and group B rhinovirus serotypes.

Stirimazole is an imidazole derivative patented by Lilly Industries Ltd. as an antiparasitic agent effective against Trypanosoma congolense, T. gambiense, T. rhodesiense, and T. cruzi. Stirimazole inhibited Trichomonas vaginalis in vitro at 0.225 μg/ml and eliminated infected lesions in mice at 20 mg/kg orally. Stirimazole eliminated intestinal amebiasis in rats at 50 mg/kg orally and hepatic amebiasis in hamsters at 100 mg/kg i.p. Stirimazole was curative against Trypanosoma rhodesiense, Trypanosoma cruzi, Trypanosoma gambiense, and Trypanosoma congolense in mice at 25, 100, 12.5, and 25 mg/kg (4 times, i.p.), respectively, and against Trypanosoma vivax in calves at 25 mg/kg i.v.

Phthalylsulfamethizole is the sulfonamide. It was used as an antibacterial agent.

Libenzapril is a long-acting, small polar angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Libenzapril competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Libenzapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. Both libenzapril and water transport was found to be significantly higher (about two- to five-fold) in six of the seven different brain regions in hypertensive rats as compared to the normotensive controls.

PPI-2458 is a synthetic derivative of fumagillin with antineoplastic and cytotoxic properties. PPI-2458 irreversibly inhibits the enzyme methionine aminopeptidase type 2 (MetAP2), thereby preventing abnormal cell growth and angiogenesis. PPI-2458 is reported to have a better toxicity profile compared to other agents of its class. In a phase 1 clinical study, PPI-2458 was administered to patients with non-Hodgkin lymphoma. The data confirm the participation of active metabolites in the in vivo efficacy of PPI-2458. In in vitro studies, osteoclast formation and activity were inhibited by PPI-2458, a mechanism not previously attributed to MetAP-2 inhibition. PPI-2458 treatment reduced synovial and osteochondral angiogenesis, synovial inflammation, joint damage, and pain behavior. PPI-2458 exerts disease-modifying activity in experimental arthritis through its direct inhibition of several pathophysiologic processes of this disease. These results provide a rationale for assessing the potential of PPI-2458 as a novel rheumatoid arthritis therapy.

Piroxicam cinnamate (Cinnoxicam) is the anti-inflammatory agent. It is a cyclooxygenase inhibitor. Cinnoxicam was used in patients with inflammatory-degenerative osteoarticular diseases. The treatment brought about a significant improvement in the clinical variables considered (spontaneous pain at rest and on movement and functional limitation), which was observed within a few days of starting therapy. Tolerance was good, only a few slight side-effects having been reported. Cinnoxicam is a safe and reliable therapeutic option for men with oligoasthenospermia associated with a grade III varicocele, but surgery is better for those with grade II, IV and V. Piroxicam cinnamate as a long-acting prodrug is marketed by SPA in Italy for the treatment of rheumatic disorders.

Belfosdil (or SR-7037) is an antihypertensive calcium channel blocker.

Prazitone (also known as AGN-511) is a barbiturate derivative patented by Aspro-Nicholas Ltd. as a non-sedating anxiolytic and antidepressant