Cronidipine (LF 2.0254) is a calcium channel blocker. LF 2.0254 inhibited in a time-dependent fashion K(+)- and Ca2(+)-induced contractions of rabbit aorta with respective IC50 of 2.7 nM and 1.7 nM. Cronidipine had a long-lasting antihypertensive action in spontaneously hypertensive rats and was able to decrease blood pressure and increase heart rate and plasma renin activity in hypertensive dogs.

IRIDIUM IR-192 is a radioactive isotope of iridium. It can be used in brachytherapy to treat tumors by selectively delivering a cytotoxic dose of radiation to the tumor site. IRIDIUM IR-192 implants are also used. They are produced in wire form and are introduced through a catheter to the target area.

Artemisone (also known as BAY-44-9585; BAY-449585) is a 10-amino-artemisinin derivative that is markedly superior in vitro and in vivo to current artemisinins against malaria and also possesses antitumor activity. Nonetheless, its low water solubility and bioavailability has limited its clinical use, that is why was studied the encapsulated artemisone against human melanoma A-375. In addition, artemisone has the potential to be efficacious for the treatment of H. pylori infection, especially in combination with antibiotics.

Propoxate (R7464) is a potent anesthetic agent in cold-blooded vertebrates, which has never been marked and has never been used on humans.

Rezatomidine (AGN 203818) is an alpha adrenergic receptor agonist that was developed for the treatment of chronic pain conditions. Phase II studies have evaluated the safety and effectiveness of rezatomidine in treating the pain in patients with fibromyalgia, irritable bowel syndrome, interstitial cystitis, and diabetic neuropathy. However, three studies were terminated early based on a business decision. Pancreatitis, gastric ulcer, viral infections and dehydration were reported as serious adverse events in patients when administered a 60mg dose.

Abamectin B1b (Avermectin B1b) is a macrocyclic lactone containing an isopropyl reside in the 25-position broad anthelmintic activity. The oral administration of this formulation of avermectin B1 appeared to be highly efficacious against intestinal strongyles and Onchocera microfilaria. Avermectin B1b is a component of marketed and provided commercially Abamectin, which is used to control livestock parasitic nematodes. It is a broad-spectrum acaricide with additional insecticidal action on a limited number of insects. Abamectin acts on insects by increasing the membrane permeability to chloride ions, and it mainly stimulates the release of Ȗ-aminobutyric acid (GABA). The affected arthropod becomes paralysed, stops feeding, and dies after a few days. It exerts contact and stomach action, with limited plant systemic activity, but exhibits translaminar movement into treated leaves. Abamectin is also used as an anthelmintic drug in veterinary medicine.

Fluzinamide (AHR-8559), an anticonvulsant agent that was studied in patients with refractory partial seizures. However, information about the further development of this drug is not available.

Tideglusib (NP031112, NP-12, Nypta, Noscira SA, Madrid, Spain), a drug, which belongs to the thiadiazolidinone family, is a GSK-3β inhibitor. Tideglusib was in phase II clinical trials for the treatment of Alzheimer disease (AD) and progressive supranuclear palsy. Participants showed no benefit on either of the primary outcome measures or exploratory endpoints and further development in the drug was halted for these two disease. However, Tideglusib is on phase II clinical trial to determine whether drug is safe and efficacious in the treatment of adolescents and adults with congenital and juvenile-onset Myotonic Dystrophy.

Volasertib (BI 6727), a dihydropteridinone derivative, is a small-molecule cell cycle inhibitor of polo-like kinase-1 (PLK-1). Volasertib induces G2-M arrest and induction of apoptosis in cancer cells and potently inhibits tumor growth in xenograft models. Boehringer Ingelheim is developing intravenously administered volasertib for the treatment of acute myeloid leukaemia (AML), myelodysplastic syndromes (MDS), chronic myelomonocytic leukaemia (CMML), non-small cell lung cancer, urogenital cancer, ovarian cancer and solid tumours.

Carotegrast is phenylalanine derivative patented by pharmaceutical company Ajinomoto Co. for the treatment or prevention of inflammatory disease states related to the α4 integrin-dependent adhesion process. In preclinical studies, Carotegrast shows pharmacological activity in rheumatoid arthritis and inflammatory bowel disease.