WS-12 is a cooling agent and potent TRPM8 agonist. It activates TRPM8 but not related TRP channels like TRPM3 and TRPV6. WS-12 seems to activate TRPM8 mediated cation currents by shifting the voltage dependence of the activation curves to the left toward more physiological membrane potentials. Highly selective TRPM8 activators may be useful for prostate cancer imaging and/or therapy and for therapy in chronic neuropathic pain states.

Pexiganan is a 22-amino-acid synthetic cationic peptide. It is an analog of magainin 2, which is a host defense peptide isolated from frog skin. The drug is thought to act by disturbing the permeability of the cell membrane or cell wall. Pexiganan exhibited in vitro broad-spectrum antibacterial activity when it was tested against 3,109 clinical isolates of gram-positive and gram-negative, anaerobic and aerobic bacteria. It is currently in phase 3 clinical trials as a topical antimicrobial agent for the treatment of mild infections associated with diabetic foot ulcers. In vitro data for pexiganan acetate suggest that the drug does have hemolytic activity at concentrations relevant for antibacterial activity. In association with tigecycline, pexiganan administration could overcome antibiotic resistance and increase the effectiveness of treatment against P. aeruginosa sepsis.

Surotomycin is a benzenebutanoic acid derivative patented by Cubist Pharmaceuticals, Inc. as antibacterial agents for the treatment of Gram-positive infections. Surotomycin has a fourfold greater in vitro potency than vancomycin against C. Difficile and other Gram-positive bacteria with minimal impact on the Gram-negative organisms of the intestinal microbiota. Surotomycin, given orally, has been shown to be highly effective against both initial and relapsing hamster Clostridium difficile-associated diarrhea, with a potency similar to vancomycin. Surotomycin is non-inferior to vancomycin and offers a promising alternative for the treatment and prevention of C. diff infection.

Ticalopride is an isomer of the active metabolite of cisapride, which is marketed by Janssen for the treatment of nocturnal heartburn due to gastroesophageal reflux disease. Ticalopride acts through the stimulation of the serotonin 5-HT4 receptors which increases acetylcholine release in the enteric nervous system (specifically the myenteric plexus). This results in increased tone and amplitude of gastric contractions, relaxation of the pyloric sphincter and the duodenal bulb, and increased peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. Phase II clinical trials of the Ticalopride are being suspended while investigators study reports of adverse events in patients with gastroesophageal reflux disease and diabetes.

Lotilibcin (WAP-8294A2) is an antibiotic originally isolated from Lysobacter sp. It is active against methicillin-resistant gram-positive bacteria. Lotilibcin antimicrobial activity is due to lysis of the bacterial membrane, and its membrane-disrupting effect depends on the presence of menaquinone, an essential factor for the bacterial respiratory chain. It was developing for the treatment of susceptible bacterial infections