Tezacitabine is a cytidine derivative patented by Merrell Dow Pharmaceuticals, Inc. as an antineoplastic and antiviral agent. Tezacitabine acts as irreversible ribonucleotide reductase inhibitor and DNA chain terminator. Tezacitabine shows as potent activity in a broad spectrum of tumor cell lines and in vivo tumor models, including human colon, prostate, and breast tumor xenografts, In clinical trials combination of Tezacitabine and 5-Fluorouracil exerts favor influences in patients with advanced solid tumors particularly in patients with esophageal and other gastrointestinal carcinomas.

Zonampanel (also known as YM872) was developed as selective, potent and highly water-soluble competitive alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor antagonist. Zonampanel possesses the neuroprotective effect against focal cerebral ischemia and participated in phase II clinical trials in acute stroke patients. However, because of the severe effects, including hallucinations, agitation, and catatonia the further studied were terminated.

Steffimycin is a potent inhibitor of DNA dependent-RNA synthesis patented by Upjohn Co. as an antibiotic. Steffimycin interferes with amino acid incorporation mediated by synthetic polyribonucleotides in cell-free bacterial systems. This inhibition is a secondary activity of the antibiotic, which acts primarily as a suppressor of RNA synthesis in bacteria and bacterial cell-free systems. Inhibition of peptide biosynthesis is apparent only at a drug concentration higher than that necessary for inhibition of RNA synthesis in cell-free systems. In addition to antibiotic activity vs certain gram-positive organisms, Steffimycin inhibits the growth of KB cells and several fungi and shows antiviral activity against herpes simplex in mice

Taclamine is an isoquinoline derivative patented by Ayerst, McKenna and Harrison Ltd. as central nervous system depressant and anti-inflammatory agent. In preclinical models, Taclamine antagonizes the turnover of noradrenaline and dopamine in the rat brain during immobilization stress without effects on brain serotonin turnover

Nexeridine, a pethidine derivative, is an opioid analgesic.

Giripladib (PLA 695) is a Cytosolic phospholipase A2 (cPLA2) inhibitor. cPLA2 is associated with tumor progression and radioresistance in mouse tumor models. In these models, treatment with giripladib attenuates radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells. Combined with irradiation, giripladib reduces migration and proliferation in endothelial cells (HUVEC & bEND3) and induces cell death and attenuated invasion by tumor cells (LLC &A549). The combination treatment of giripladib and irradiation also delayes growth in both LLC and A549 tumors and results in reduced tumor vasculature. Phase I studies have been conducted to test the gastrointestinal safety of giripladib, and potential pharmacokinetic interaction with other compounds. A phase II study was terminated.

Mexrenoate potassium is an aldosterone antagonist, which was developed as an antihypertensive agent. However, this drug has never been marketed.

LACTALFATE is an antiulcer agent.

Elocalcitol (also known as BXL-628), a vitamin D3 analog. This compound regulates cell proliferation and apoptosis via its binding to the vitamin D receptor (VDR) having anti-proliferative and anti-inflammatory properties in benign prostatic hyperplasia (BPH) treatment. In a phase, IIb trial in patients with BPH, treatment with elocalcitol resulted in a significantly reduced prostate volume compared with placebo; irritative urinary symptoms (frequency, urgency, and nocturia) and urodynamic parameters were comparable to the alpha1-adrenoceptor antagonist tamsulosin. In a phase IIa trial in patients with prostatitis, elocalcitol significantly reduced levels of IL-8 in semen, suggesting improved quality and forward motility of sperm. However, phase IIb trial data from patients with overactive bladder (OAB) were less promising: elocalcitol failed to meet the primary endpoint despite demonstrating good efficacy in a phase IIa trial. Based largely on these disappointing data, BioXell decided to terminate all further clinical development of elocalcitol, including an uncompleted phase IIa trial in patients with male infertility. Recently was shown, that VDR agonists as elocalcitol could be therapeutic tools for skeletal muscle integrity/function maintenance, an indispensable condition for health homeostasis.