Ripisartan (UP-269-6) is a specific nonpeptide angiotensin II receptor antagonist. Oral administration of ripisartan in rats and dogs resulted in a dose-dependent and long-lasting inhibition of the angiotensin II-induced pressor response. It did not show agonistic properties in animals. In vitro, ripisartan was found to bind selectively to AT1 receptors. In humans, it showed high biliary excretion and reabsorption. Canine studies have suggested it might have cardioprotective properties after acute ischemia-reperfusion.

Deterenol is a beta-adrenoceptor agonist. It is an effective nonmydriatic and nonmiotic hypotensive agent, which can be used in antiglaucoma treatment.

Balaglitazone is a second generation peroxisome proliferator-activated receptor (PPAR) gamma agonist with only partial agonistic properties. It passed phase III clinical trial for the treatment of type 2 diabetes. However, Dr. Reddy's Laboratories decided to terminate further clinical development of balaglitazone.

Pipendoxifene (ERA-923) is a selective estrogen receptor modulator with a distinct profile compared with tamoxifen. In particular, unlike tamoxifen, ERA-923 is devoid of uterotropic activity and does not stimulate the growth of endometrial tumors in the EnCa-101 (human endometrial adenocarcinoma that is continuously passaged in animals in the presence of estrogen) experimental mice model. These data may indicate that, in patients, ERA-923 will not increase the incidence of endometrial hyperplasia or cancer. ERA-923 inhibits estrogen-stimulated ER-alpha-dependent tumor growth with equal effects compared with tamoxifen in models sensitive to tamoxifen. ERA-923 partially or completely overcomes tamoxifen resistance. In vivo combination of temsirolimus and ERA-923 at certain doses and schedules completely inhibited breast carcinoma growth, while individual agents were only partially effective. Pipendoxifene had been in phase II clinical trial for the treatment of refractory metastatic breast cancer. However, this research has been discontinued.

Metioprim is a competitive inhibitor of bacterial dihydrofolate reductase with an in vitro activity against most important gram-negative and gram-positive bacteria causing urinary and respiratory tract infections. The use of this drug was studied in the treatment of pyelonephritis and against atypical mycobacterial infections - especially leprosy. Information about the current use of this compound is not available.

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.

Amfonelic acid (AFA) is a dopamine reuptake inhibitor. Experiments on rats have shown that AFA treatment completely prevented the effects of methamphetamine on the dopaminergic system, both morphologically and biochemically.

Benzpiperylone was studied as a synthetic anti-inflammatory drug. Information about the nowadays use of this compound is not available.

Benzodepa is an aziridine alkylating agent that cross-links with DNA, causing inhibition of DNA synthesis. It has been studied as a potential treatment for a variety of cancers, most notably bronchiogenic carcinoma.