Furterene is a diuretic of the aminopteridine series, with aldosterone antagonist activity. Furterene is able to antagonize aldosterone at the mineralocorticoid receptor in the kidneys. It thereby increases sodium excretion while inhibiting potassium excretion.

Pirmagrel is the selective thromboxane synthetase inhibitor. The compound was well tolerated by all subjects without evidence of any adverse reactions. Serum thromboxane B2 levels (the stable metabolic product of thromboxane A2) were significantly reduced after administration of the compound, with the maximal effect of a 99 per cent reduction occurring at 0.5 and 1 hour after administration. Bleeding times showed a slight increase 2 hours after administration of the compound. Pirmagrel was able to completely prevent the increase in serum thromboxane B2 following allergen challenge in asthmatic patients; while it caused a very small reduction in the early response to allergen, there was no effect on the late response or on airway hyperresponsiveness. Pirmagrel was developed for the treatment of ischemic heart disorders and thrombosis. However, this development was discontinued.

Tecarfarin (also known as ATI-5923), an anticoagulant, is a vitamin K reductase antagonist. Tecarfarin is participating in phase III clinical trials for the treatment of thromboembolism and thrombosis. On March 11, 2019, Espero BioPharma Inc. announced that the U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation (ODD) for tecarfarin for the prevention of systemic thromboembolism of cardiac origin. Tecarfarin is metabolized by esterases, escaping metabolism by the cytochrome P450 system and thereby avoiding cytochrome P450-mediated drug-drug or drug-food interactions as well as genetic variations found in the cytochrome P450 system.

Dazmegrel [UK 38485] is a thromboxane synthetase inhibitor which was undergoing development in the treatment of thrombosis, ischaemic heart disease, arrhythmias and asthma. Pfizer were conducting phase II studies in Denmark and the UK, phase I studies in Germany and Italy, and preclinical studies in France. Later this research was discontinued.

Triflocin is a nicotinic acid derivative. Triflocin is a diuretic agent. It is structurally dissimilar from ethacrynic acid and furosemide although their natriuretic potency and site of action in the kidney appear similar. Triflocin inhibits sodium-stimulated, ouabain-insensitive ATPase. In vivo, a natriuretic effect of Triflocin has been reported in both the proximal convoluted tubule and the thick ascending limb of Henle's loop. Upon acute isohydric hypercapnia, Triflocin depolarizes the basolateral membrane potential. Triflocin inhibits the basolateral electrogenic Na-(HCO3)n > 1 cotransport in proximal tubules.

Indacrinone is an orally active, indanone-based loop diuretic patented by American pharmaceutical company Merck and Co as mixture of two enantiomers. In healthy volunteers, the racernic mixture of indacrinone exhibited greater natriuretic potency than furosemide, with a slower onset and longer duration of action. Furthermore, single doses of indacrinone decreased serum uric acid concentrations and increased uric acid clearance, while similar doses of furosemide generally had the opposite effects. Differences in the pharmacologic effects of the resolved enantiomers of indacrinone were initially studied in animals and confirmed in a series of studies we conducted in healthy human volunteer. The S( + ) form is a potent uricosuric agent that produces mild natriuresis only at higher doses, while the R( - ) form is a potent loop diuretic with only transient uricosuric effects. The (-) enantiomer and its active metabolite appear to be primarily responsible for the natriuretic effects of the racemic mixture; the ( + ) enantiomer is 20-40 times less potent a natriuretic agent.

Alipamide is an antihypertensive and diuretic agent. It is a hydrazide derivative of m-sulfamoylbenzoic acid with diuretic activity. Alipamide primarily causes a saluretic effect and is able to inhibit carbonic anhydrase at higher doses which may also contribute to this agent's diuretic effect.

RU 28318 also known as OXPRENOATE is a mineralocorticoid receptor (MR) antagonist, inhibiting aldosterone production and secretion. RU 28318 has been studied in normal and diabetic rats. It was revealed, that in combination with angiotensin converting enzyme inhibitors, RU 28318 was the most effective at improving -dP/dt (a measure of diastolic function) and attenuated cardiac dysfunction in diabetes.

GBT440 (previously GTx011) is a potent and direct drug for sickle cell treatment. In sickle cell anemia, abnormal hemoglobin molecules are formed, which causes problems for the flow of blood and oxygen through the body. GBT440 can selectively bind to hemoglobin, thereby increasing its affinity for oxygen. By inhibiting hemoglobin polymerization, it also prevents deformation of the red blood cells. GBT440, renamed Voxelotor, is thought to help prevent sickle cells blocking blood vessels, and therefore reduces pain (sickle cell crisis) experienced by patients. GBT440 is well absorbed following intravenous and oral administration, and quickly partitions into the red blood cell with a small part re‐distributed into the plasma. GBT440 was well tolerated in a randomized, placebo‐controlled, double blind, parallel group phase I/II study in healthy volunteers and sickle cell disease patients. Headache is the most reported adverse event related to the use of this drug, and no serious adverse events are known. A phase 3 clinical trial examining the efficacy and safety of the drug (compared to placebo) is planned to be completed in 2019. Voxelotor was also studied as a potential therapy for treatment of low oxygen levels in the blood of idiopathic pulmonary fibrosis patients, but this program was discontinued because of a lack of clinical benefits.