Resatorvid (TAK-242) is a Toll-like receptor 4 (TLR4) antagonist that was designed for the treatment of severe sepsis because of its inhibitory effect on suppressing cytokine levels. This compound suppresses production of inflammatory mediators by inhibiting signal transduction through TLR4. It has also been shown that topical resatorvid, in a UV-induced skin tumorigenesis model, displays photochemopreventive activity, suppressing tumor area and multiplicity. Resatorvid has furthermore shown neuroprotective effects after traumatic brain injury (in a mouse model). Phase III studies evaluating the effects of resatorvid on sepsis have been completed. One such study was ended after it was determined that there was insufficient cytokine suppression in the first stage of the study.

FLESTOLOL is an ultra-short-acting beta-adrenergic blocking agent without any intrinsic sympathomimetic activity.

Lifarizine is a use- and voltage-dependent antagonist of human voltage sensitive sodium currents. Lifarizine inhibited both the plateau and the spike phases of the Ca2+ increases suggesting that, in addition to its known sodium channel blocking properties, it may also inhibit more than one class of calcium channel in the synaptosomes. Lifarizine reduced both infarct area and volume in the mouse with middle cerebral artery occlusion. Lifarizine was in phase II for the treatment of stroke but this investigation was discontinued.

Rivoglitazone hydrochloride (CS-011) is a thiazolidinedione-derivative peroxisome proliferator–activated receptor (PPAR)-γ agonist. It has been developed as potential treatment in type 2 diabetes mellitus and was shown to decrease plasma glucose and triglyceride levels in a dose-dependent manner in animals. Phase II and III clinical studies have assessed the efficacy and safety of rivoglitazone hydrochloride in patients with type 2 diabetes mellitus.

Cefsumide is an antibiotic of the cephalosporin group patented by Fujisawa Pharmaceutical Co. Cefsumide binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Carzelesin is a cyclopropylpyrroloindole prodrug analogue and DNA minor groove binding agent, with antineoplastic activity. Activation of carzelesin requires hydrolysis of a phenylurethane substituent to form U-76073, followed by ring closure to form the cyclopropyl-containing DNA-reactive U-76074. The formation of the DNA-reactive metabolites from carzelesin was shown to proceed very slowly in phosphate-buffered saline, but to occur rapidly in plasma from mouse, rat, dog, and human and in cell culture medium. Although carzelesin was less potent in terms of in vitro cytotoxicity and in vivo optimal dosage and showed low affinity for binding to DNA, it was therapeutically more efficacious against mouse L1210 leukemia

Cebaracetam is piperazinylpyrrolidinone derivative patented by pharmaceutical company Ciba-Geigy A.-G. for treatment of amnesia and retention defects.

Tepirindole (also known as HR-592), an indole derivative has a high affinity for DA, 5-HT and NE receptors but has little properties to cause catalepsy. Animal experiments have shown that this compound could alleviate the adverse effect of neuroleptics such as haloperidol. Information about the current development of tepirindole is not available.

Tizoprolic acid is an anti-lipolytic drug, a blood ketone lowering agent.