Adaprolol is a beta-adrenergic antagonist that is being developed as a topical agent to treat glaucoma. Adaprolol demonstrated a safer cardiovascular profile, especially in the population over 70 years old. It was in Phase II clinical trials for the treatment of glaucoma. This research has been discontinued.

Acevaltrate is an iridoid found in variable amounts in Valerianaceae and might be among the bioactive compounds which confer anxiolytic properties to the Valeriana species. Acevaltrate inhibited total H⁺/K⁺-ATPase activity (60.7 ± 7.3 %) from rat gastric epithelium. Acevaltrate inhibited Na⁺/K⁺-ATPase with IC₅₀ value of 22.8 uM. Na⁺/K⁺-ATPase might be one of their molecular targets of Acevaltrate in vivo.

Rifalazil (also known as KRM-1648) is a derivative of the antibiotic rifamycin. This orally administered ansamycin is under evaluation for treatment of various bacterial infections. Rifalazil kills bacterial cells by blocking off the β-subunit in RNA polymerase. This drug was originally developed as a therapeutic agent to replace rifampin in the treatment of tuberculosis. It also showed potential to treat indications caused by chlamydia trachomatis and chlamydia pneumoniae. Furthermore, it has been suggested as a potential drug in the treatment of gastric ulcer disease (which is caused by Helicobacter pylori) and antibiotic-associated colitis. Phase II studies evaluated the efficacy and safety of this drug in patients with chlamydia trachomatis and chlamydia seropositive patients. A phase 3 study was initiated including chlamydia seropositive patients. However, the development of rifalazil was terminated in 2013 due to severe side effects.

Cinoxolone is a derivative of glycyrrhetinic acid. Is is claimed to possess antiulcer properties.

Resiniferatoxin (RTX or RTX-107) is a vanilloid derived from a cactus-like plant (Euphoria resiniferous) and has anti-inflammatory activity. This compound is an agonist of the transient receptor potential vanilloid 1 (TRPV1). Resiniferatoxin produces analgesia by desensitizing the TRPV1 receptor. Findings of several studies have suggested a potential therapeutic use of the anti-inflammatory effect of resiniferatoxin. Phase I and II clinical trials have been completed or are underway, evaluating the safety and efficacy of resiniferatoxin in pain-related disorders such as osteoarthritis and cancers.