LASCUFLOXACIN, a fluoroquinolone derivative, is an antibacterial agent with a broad spectrum of activity against various clinical isolates. It is under development for the treatment of respiratory tract infections and community-acquired pneumonia.

Auriclosene (previously known as NVC-422) is a broad-spectrum, fast-acting topical anti-infective agent against microbial pathogens, including antibiotic-resistant microbes. It has been investigated in phase II clinical trials for the treatment of bacterial conjunctivitis and as a topical gel in children with impetigo. In addition, using a guinea pig model was shown, that auriclosene was effective in the treatment of dermatophytosis, including onychomycosis.

Furegrelate (previously known as U-63557A), a selective orally active thromboxane synthase inhibitor, with potential for the treatment of various diseases including hypertension, thrombosis, and renal disorders, arrhythmias, but these studies were discontinued.

Furofenac (also known as SAS 650), a drug that has antiplatelet-aggregation activity and anti-inflammatory activity combined with low ulcerogenic power. It was shown that the furofenac mechanism of action involved the modulation of the platelet cyclooxygenase pathway.

Furofenac (also known as SAS 650), a drug that has antiplatelet-aggregation activity and anti-inflammatory activity combined with low ulcerogenic power. It was shown that the furofenac mechanism of action involved the modulation of the platelet cyclooxygenase pathway.

Sulfasuccinamide is a sulfonamide antibacterial with properties similar to those of sulfamethoxazole. It has been applied topically in the treatment of local infections of the ear, nose, and throat. It has also been given as the sodium salt. Sulfasuccinamide is a carbonic anhydrase inhibitor.

Pibrozelesin (KW-2189) is a semisynthetic water-soluble derivative of the antineoplastic antibiotic duocarmycin B2. Activated by carboxyl esterase, pibrozelesin alkylates DNA by binding to adenine-thymine (A-T)-rich sequences in the minor groove of DNA, thereby inhibiting DNA replication and inducing apoptosis. KW-2189 induced DNA strand breaks in H69 cells in a concentration-dependent manner. DNA cleavage is one of the major mechanisms of KW-2189-mediated cytotoxicity. KW-2189 showed evidence of anti-tumor activity in hepatocellular carcinoma (HCC). However, because of significant and prolonged hematologic toxicity, when given as a single dose every 6 weeks, further development of this drug in HCC is not possible. Pibrozelesin had been in phase II clinical trial for the treatment of advanced malignant melanoma and advanced renal cell carcinoma. No activity in metastatic renal cell carcinoma was demonstrated and the lack of significant antitumor activity in advanced malignant melanoma treatment was shown.

Esuberaprost (314d) is an active enantiomer of beraprost, a prostacyclin analog. The pharmacologic action of esuberaprost is mediated by specifically binding to PGI2 receptors in smooth muscle cells (the blood vessel’s endothelium) and platelets. Upon binding, the compound widened blood vessels, preventing the formation of blood clots, and lowering blood pressure in the lungs. As a result, it was expected to improve the symptoms of pulmonary arterial hypertension. United Therapeutics announced it has ended its Phase 3 BEAT trial testing esuberaprost as an add-on therapy to its product Tyvaso (inhaled treprostinil) for clinically symptomatic patients with pulmonary arterial hypertension (PAH). According to a company press release, the study failed to reach its main endpoint of delaying the time to first clinical worsening events.

Rose Bengal lactone is a polyhalogenated derivative of Fluorescein. Rose Bengal lactone is a dye compound described to produce cell membrane damage. Rose Bengal lactone and other Fluorescein derivatives are also described to modulate the function of ATP-sensitive K+ channels. Rose bengal lactone reacts readily with bases so treatment with triethylamine immediately yields the Rose Bengal salt.