Exisulind (tentative trade name Aptosyn) is an antineoplastic agent, which was originally developed by Cell Pathways. This drug is an inhibitor of phosphodiesterase (PDE) isozymes: PDE5 and PDE4. Inhibition of PDE5 appears to be pharmacologically relevant, which leads to increase cGMP and activate protein kinase G at doses that induce apoptosis, whereas cyclic AMP levels were not changed. Exisulind has been in phase III clinical trials for the treatment of Non-Small Cell Lung Cancer and for the treatment of polyps in patients who have familial adenomatous polyposis (Colorectal Cancer and Small Intestine Cancer). In addition, this drug was in phase II/III for the treatment of Prostate Cancer, however, there studies have been discontinued.

Dibupyrone is an analgesic agent.

Davasaicin is a synthetic derivative of capsaicin, developed at the Korea Research Institute of Chemical Technology. Davasaicin possesses very potent analgesic activity, demonstrated in several animal models, such as phenylbenzoquinone-induced writhing test, tail-flick test in mice and adjuvant arthritic flexion test in rats. When administered topically, davasaicin has an antipruritic effect in the mouse model.

Tianafac (also known as L8109) is a thienylacetic acid derivative patented by Labaz group as antipyretics and anti-inflammatory agent useful for the treatment of arthritis. In preclinical models, Tianafac inhibits prostaglandin formation by seminal vesicle microsomes and exerts antipyretic, analgetic, and moderate gastric ulcerogenic activity and had a wide safety margin between toxic and pharmacologically active doses.

Talmetacin is a cyclo-oxygenase inhibitor that was studied as an analgesic and antipyretic agent. This drug was studied in Argentina in patients with rheumatic disorders. However, further development of talmetacin is not available.

Pifenate is an analgesic agent.

Axomadol is a centrally active analgesic agent with opioid agonistic properties and with inhibitory effects on the reuptake of the monoamines noradrenaline and, to serotonin [5‐hydroxytrypyamine (5‐HT)]. The drug participated in phase II clinical trials in the treatment of patients with moderate to severe chronic low back pain. As a result, the axomadol didn’t meet predetermined study endpoint, and studies were discontinued.

Etoprindole is an antiinflammatory agent.

Brifentanii, a potent narcotic analgesic structurally similar to alfentanil, that was studied in clinical trials in the early 1990s. The effects of brifentanil are very similar to those of alfentanil, with strong but short lasting analgesia and sedation, and particularly notable itching and respiratory depression. Side effects of Brifentanii are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening.

Furcloprofen was developed as an analgesic agent with anti-inflammatory properties. Information about the current use of this compound is not available.