Ispinesib (SB-715992) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP). KSP, also known as HsEg5, is a kinesin that plays an essential role in the formation of a bipolar mitotic spindle and is required for cell cycle progression through mitosis. Ispinesib is the highly specific small-molecule inhibitor of KSP tested for the treatment of human disease. It causes mitotic arrest and growth inhibition in several human tumor cell lines and is currently being tested in multiple phase II clinical trials for treatment of the breast cancer and renal cell cancer.

Darglitazone is a member of the thiazolidinedione class of drugs and an agonist of peroxisome proliferator-activated receptor-γ (PPAR-γ), an orphan member of the nuclear receptor superfamily of transcription factors. It has a variety of insulin-sensitizing effects, such as improving glycemic and lipidemic control, and is used in the treatment of metabolic disorders such as type II diabetes. Darglitazone sodium had been in phase I clinical trials by Pfizer for the treatment of type 2 diabetes. However, this study has been discontinued.

Thiorphan is the first potent synthetic inhibitor of enkephalinase. Thiorphan displays antinociceptive activity after systemic administration. Thiorphan also inhibits to a lesser extent the widely distributed angiotensin-converting enzyme, a carboxydipeptidase implicated in blood pressure regulation. Thiorphan failed to potentiate allergen-induced airway responses in asthma. Thiorphan significantly reduced the castor oil-induced diarrhea in rats when administered intravenously but not when administered intracerebroventricularly. Racecadotril, via its active metabolite thiorphan, was consistently effective in animal models and patients with various forms of acute diarrhea by inhibiting pathologic (but not basal) secretion from the gut without changing gastro-intestinal transit time or motility.

Cizolirtine is a potent analgesic in mice and rats, with an efficacy superior to that of aspirin and other nonsteroid anti-inflammatory drugs. Recent studies have shown that the analgesic effect of cizolirtine could be related, at least partially, to an inhibition of spinal substance P and calcitonin gene-related peptide release. Cizolirtine has been in clinical trials for the treatment of pain and overactive bladder. Reported adverse events are: dry mouth, dizziness, nausea, vomiting, blurred vision.

Icopezil (previously known as CP-118,954) was developed as a selective acetylcholinesterase inhibitor for the treatment of cognitive disorders. Phase II trials of icopezil were underway in Japan and in the USA for the treatment of patients with Alzheimer's disease. However, Pfizer has discontinued these studies.

Bensuldazic acid was used in veterinary as an antifungal agent.

Edonentan (BMS 207940) is a highly selective biphenylsulfonamide endothelin A receptor antagonist. (11)C- and (18)F-labeled analogs of edonentan were evaluated of novel PET radioligands for imaging the endothelin-A receptor. Edonentan was in clinical trials for the treatment of heart failure however its development has been discontinued.

Benzindopyrine belongs to anticholinergic agents. It was studied as an antipsychotic drug.

Remogliflozin is the active component of the pro-drug remogliflozin etabonate, which is used the treatment of non-alcoholic steatohepatitis ("NASH") and type 2 diabetes. Remogliflozin inhibits the sodium-glucose transport proteins (SGLT), is selective for SGLT2, which is responsible for glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine.

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.