FLOVAGATRAN is a potent, reversible, low-molecular-weight, highly selective synthetic direct thrombin inhibitor that has demonstrated promising pharmacokinetic properties and biological activity in preclinical studies. However, its development for thrombosis was discontinued in Phase II.

Cu-64 is a radioisotope of copper with T1/2 12.7 hours. It decays by emission of beta+ particles with energies 0.653 (17.8%) MeV, which makes it suitable for positron emission tomography. The most widely used Cu chelators are DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) and TETA (1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetraacetic acid). Cu-64 acetate is used as a model compound to study metabolism and distribution of Cu-64.

Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda. Alisertib inhibited AAK over ABK with a selectivity of more than 200-fold in cells and produced a dose-dependent decrease in bipolar and aligned chromosomes in the HCT-116 xenograft model, a phenotype consistent with AAK inhibition. Alisertib inhibited proliferation of human tumor cell lines in vitro and produced tumor growth inhibition in solid tumor xenograft models and regressions in in vivo lymphoma models. It is currently in phase II clinical trials for acute myeloid leukaemia; B cell lymphoma; brain cancer; mesothelioma; prostate cancer; small cell lung cancer.

Pirolate is the pyrimidoquinoline. It was developed as an antiasthmatic and antiallergic agent. Pirolate does show high potency in passive cutaneous anaphylaxis in rats, both by intravenous and oral routes. It has some 84 times the potency of disodium cromoglycate. Pirolate is a leukotriene biosynthesis inhibitor.

Quazolast is an orally active mast cell stabilising agent which was in development with Rhône-Poulenc Rorer. In preclinical trials Quazolast was evaluated for efficacy against acid independent (alcohol, HCl), or dependent (aspirin, indomethacin) gastric damage in rats. Quazolasts gastroprotective profile was compared to that of ranitidine. Quazolast, in direct contrast to ranitidine, protected the rat gastric mucosa from acid-independent, but not acid-dependent gastric damage. Quazolast lacked antisecretory activity in rats; however, it did heal acetic acid induced gastric ulcers in this species. In clinical trials Quazolast was superior to placebo in protecting against nasal congestion and nasal itchiness after ragweed nasal challenge.

Benzobarbital (under the brand name Benzona), a barbiturate derivative developed in Russia that is used to treat convulsive forms of epilepsy, newborn hemolytic disease, and insomnia.

Metbufen is a non-steroid anti-inflammatory drug.

Palonidipine (also known as TC 81) a calcium antagonist that was developed by Teijin for the treatment of hypertension and angina pectoris. Palonidipine was involved in phase II clinical trials in Japan. However, these studies were discontinued.

Pranidipine is the calcium channel blocker. Pranidipine did not affect the sensitivity of the contractile proteins to calcium. Pranidipine also did not alter cyclic GMP-induced relaxation in alpha-toxin-skinned vascular preparations. Pranidipine also prolonged glyceryl trinitrate-induced relaxation in the endothelium denuded rat aorta. Pranidipine enhances cyclic GMP-independent NO-induced relaxation of smooth muscle by a mechanism other than through NO-induced hyperpolarization. These effects were in direct contrast to amlodipine, another new 1,4-dihydropyridine calcium antagonist. Pranidipine increased blood velocity and probably blood flow in the optic nerve head, choroid, and retina of rabbits. Pranidipine was not detrimental to global cardiac function in animals with dilated cardiomyopathy. Pranidipine enhances relaxation produced by endothelium-derived relaxing factor in carotid artery. Pranidipine was investigated as pharmacological agent for the treatment of angina pectoris and hypertension.

Nileprost is a prostacyclin analogue stabilized by introduction of the cyano group at its 5-position. Nileprost is a mixed type PGI2/PGE2 agonist. The development of the prostaglandin analogue nileprost [ZK 34798] for use in peptic ulcers has been discontinued at phase II by Schering AG in Germany.