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.

Loprodiol is tranquillizer and muscle relaxant.

Fluspiperone, a butyrophenone derivative that was invented as an antipsychotic agent. However, information about the further development of this drug is not available.

Mabuprofen (aminoprofen, AU 7801) is an amide prodrug of ibuprofen, a non-steroidal anti-inflammatory drug with analgesic, antipyretic and anti-inflammatory properties. It is used for topical treatment of various painful processes that occur with inflammation (tendonitis, synovitis, torticollis, lumbago, contusions, sprains, etc).

Flindokalner (BMS 204352; MaxiPost™) is a neuroprotective agent with potential in the treatment of stroke developed by Bristol-Myers Squibb. Flindokalner is a potent and effective opener of two important subtypes of neuronal potassium channels, the calcium-activated, big-conductance potassium channels (K(Ca) channels) and voltage-dependent, non-inactivating potassium channels known as KCNQ channels. Flindokalner significantly reduced cortical infarct volume in a animal models of stroke. Flindokalner failed to show superior efficacy in acute stroke patients compared to placebo in a Phase III study.

Tizabrin is the antithrombotic, fibrinolytic agent. Tizabrin (CP-2129) stimulates fibrinolysis after intravenous administration in human volunteers due to an increase in tissue plasminogen activator (t-PA) activity. Tizabrin has no intrinsic fibrinolytic activity in vitro.