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.

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

Nalmexone is an opioid partial agonist or mixed agonist-antagonist with both analgesic and narcotic antagonist properties. In preclinical models parenteral nalmexone was a moderately active antagonist and therefore might have low abuse potential. At the same time, early work in man indicated analgesic activity in doses above 20 mg.

Posizolid (AZD2563 or AZD5847) is an oxazolidinone, identified from an antibiotic research programme which aimed to synthesise agents that inhibited all Gram-positive bacteria, including multiresistant strains likely to be encountered clinically. Oxazolidinones bind to the 50S ribosomal subunit and inhibit the initiation phase of translation. Posizolid had been in phase II clinical trials for the treatment of tuberculosis. However, this study was discontinued.

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

Trithiozine is an alkoxythiobenzamide said to have antisecretory and tranquillising properties without anticholinergic, antihistaminic, or ganglion-blocking effects. Trithiozine in animal studies proved to have a marked anti-secretory and anti-ulcer effect, along with a very low acute and chronic toxicity. Clinical trials with trithiozine have been performed in some European countries. The results of these trials, most of which were conducted on a double-blind basis, and including already several hundreds of patients, have shown that oral trithiozine: exerts a very significant action on both basal and stimulated gastric acid secretion, without a rebound hypersecretion; promotes, in most patients, a complete endoscopic healing of peptic ulcer, in addition to an early symptomatic relief; has a mild sedative action; does not affect the pancreatic secretion; is well tolerated even for long-term (up to 10 months) treatments.

Gallium maltolate is an oral agent in development for the potential treatment of chronic bacterial infections, bone disease and cancer. The bioavailable form, composed of a trivalent gallium cation (Ga3+) competes with and replaces Fe3+ in many vital Fe 3+-mediated biological reactions, but cannot mimic Fe3+ functions. High amounts of iron are needed for DNA synthesis in cancer, and the incorporation of Ga3+ inactivates the Fe3+-dependent enzyme ribonucleotide reductase (RR), an enzyme essential for DNA synthesis, leading to an inhibition of DNA synthesis and induction of cell death in rapidly proliferating cells. Gallium similarly reduces bacterial cell growth. Ga3+ is also able to suppress inflammation through the down-regulation of pro-inflammatory cells and the inhibition of pro-inflammatory cytokine secretion. Other effects that have been mentioned are analgesic effects, interference with the activity of certain metalloproteinases and neuropeptides that are implicated in pain, and prevention of the destruction of bone by tumors. Gallium maltolate is being investigated for use/treatment in bladder cancer, lymphoma (unspecified), multiple myeloma, paget's disease, and prostate cancer.

Darinaparsin is a novel mitochondrial-targeted agent being developed for the treatment of various hematologic and solid cancers. In a Phase II study in the US, intravenous darinaparsin demonstrated evidence of clinical activity in malignant lymphoma, and in particular peripheral T-cell lymphoma (PTCL). Darinaparsin was granted Orphan Drug Designation in the US and Europe as a treatment of PTCL. The oral formulation is also being tested in Phase I for the treatment of solid tumors. Darinaparsin induces G2/M cell cycle arrest and apoptosis in tumor cells, primarily through disruption of mitochondrial functions, increased reactive oxygen species (ROS) production and modulation of signal transduction pathways.

Forasartan (also known as SC-52458) was developed as an orally active, competitive angiotensin (Ang) II subtype 1 (AT1)-receptor antagonist for the treatment of hypertension. Forasartan competes with angiotensin II for binding at the AT1 receptor subtype. It is known that angiotensin II is a vasoconstrictor and stimulates the synthesis and release of aldosterone, and blockage of its effects results in a decrease in systemic vascular resistance. Information about the further development of forasartan is not available.

Metamfazone exerts analgesic and antirheumatic activities.