Zoniporide hydrochloride is a novel, potent and selective NHE-1 inhibitor (IC50 = 14 nM). Reduces infarct size in the isolated heart (EC50 = 0.25 nM). Attenuates post-ischemic cardiac contractile dysfunction and ischemia-reperfusion-induced ventricular fibrillation in vivo. Zoniporide hydrochloride represents a novel class of potent and selective human NHE-1 inhibitors with potential utility for providing cardioprotection in a clinical setting.

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.

Chlorphenoctium is amsonic acid salt with potent long-lasting antimicrobial activity

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.

Topilutamide is a non-steroidal anti-androgen. Topilutamide downregulated androgen receptor expression by 40% at 3 uM and up to 95% at 10 uM in LNCaP Cells After 48-h drug incubation. While highly hydrophobic and hydrolytically degradable, it is systemically nonresorbable. In animals, fluridil demonstrated high local and general tolerance. After 3 months of topical application of topilutamide, the average anagen percentage did not change in placebo subjects but increased in topilutamide subjects (male with androgenetic alopecia) from 76% to 85%, and at 9 months to 87%. In former placebo subjects, topilutamide increased the anagen percentage after 6 months from 76% to 85%. Sexual functions, libido, hematology, and blood chemistry values were normal.

LADIRUBICIN is an idarubicin derivative with potential antineoplastic activity. Its primary effect is a DNA alkylation with sequence specificity similar to that of conventional nitrogen mustards. It possesses a wide spectrum antitumor activity against rapidly proliferating murine leukemias and on slowly growing transplantable human tumor xenografts.

Posatirelin is a synthetic peptide that, in animal models, has been shown to improve cognitive and motor disturbances associated with aging or induced by central neurotransmission disruption. Modulation of various neurotransmission systems and activation of excitatory amino acid receptors have been suggested as possible mechanisms of action, since posatirelin increases the turnover and release of catecholamines in several brain areas as well as choline acetyltransferase activity in the cerebral cortex. In neuronal cultures, posatirelin has been shown to have trophic effects, accelerating the maturation of cerebellar granule cells and stimulating neurite growth. The benefits of posatirelin therapy in patients with late-onset Alzheimer's disease have potential clinical relevance. Significant improvements in motor, intellectual and emotional impairments were seen in posatirelin recipients. The difference in these parameters with respect to the reference and inactive drugs was significant. Posatirelin can improve cognitive and functional abilities of patients suffering from degenerative or vascular dementia. Posatirelin had been in phase III clinical trial for the treatment of cognition disorders. However, this development was discontinued.

Prazepine is a tricyclic antidepressant (TCA). Propazepine is sometimes confused with imipramine, which has the central ring nitrogen in a different location. Propazepine appears to never have actually been used as a tricyclic antidepressant outside of initial medical tests. Prazepine showed potent antihistaminic properties.

Prisotinol is aminoalkyl-5-pyridinol patented by Ciba-Geigy A.-G. for treatment of angina pectoris. Prisotinol was studied in phase II clinical trials as a cardioprotective agent.

Prideperone is 5-Cyano-2-methoxy-benzamide derivative patented by Ciba-Geigy A.-G. as antipsychotic.