Lexacalcitol (KH1060) is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 and is of potential interest in the treatment of psoriasis and other diseases characterized by accelerated cell growth and T lymphocyte activation, which was studied in the clinical trial. KH1060 also prevents type I diabetes in the preclinical investigation without significant effects on calcium or bone metabolism. In addition also was shown that neuroblastoma (NB) cell lines were more susceptible to growth inhibition by KH1060, suggesting its possible use in NB to potentiate the action of retinoids, which are in clinical use for this disease. The underlying biochemical reasons for the increased biological activity of KH1060 are unknown, but it can include 1) metabolic considerations in addition to explanations based upon 2) enhanced stability of KH1060-liganded transcriptional complexes.

Carfentanil is a synthetic fentanyl analog. It is a mu-opioid receptor agonist with an estimated analgesic potency approximately 10,000 times that of morphine and 20-30 times that of fentanyl, based on animal studies. Receptor binding studies have shown that carfentanil binds selectively and competitively to the μ subtype of opioid receptors relative to δ and κ opioid receptors. Preclinical studies have demonstrated that the pharmacodynamic effects, such as analgesia and constipation, produced by carfentanil are similar to other μ opioid agonists. Its extreme potency and propensity to produce rapid and profound respiratory depression has prompted recommendations that an opioid antagonist, such as naloxone or naltrexone, be available whenever carfentanil is used or suspected to be present. Carfentanil (Wildnil) has been used in veterinary as a prescription-only general anesthetic for intramuscular injection in large animals. Carfentanil is no longer FDA-approved for use in animals after Wildlife Laboratories withdrew the application for Wildnil. Carfentanyl is increasingly involved in opioid overdose deaths among illicit opioid users.

Atocalcitol is a vitamin D analogue. A hallmark of vitamin D3 analogues in psoriasis amelioration is the ability to inhibit the proliferation of keratinocytes. Atocalcitol had been in phase II clinical trials for the treatment of psoriasis. However, this research has been discontinued.

Pfizer developed AG-013958, also known as AG-13958 for treatment of age-related macular degeneration (AMD). As a VEGFR tyrosine kinase inhibitor, AG13958 was targeted to FLT/TYK receptor inhibition.

Dehydroascorbic acid (DHA) is an oxidized form of ascorbic acid. Ascorbic acid is transported in its oxidized form via GLUT1 across the blood-brain barrier. Dehydroascorbic acid delay low-density lipoprotein (LDL) oxidation when added before the initiation of the process, they accelerate the process if added to minimally oxidized LDL. Dehydroascorbic acid is used as biochemical markers of oxidative stress in clinical investigations. Dehydroascorbic acid has been used as a vitamin C dietary supplement.

Seocalcitol (EB 1089) is a vitamin D analog, and agonist of the vitamin D receptor. Antineoplastic activity of seocalcitol was tested in clinical trials against hepatocellular carcinoma, pancreatic, breast and colorectal cancer. Due to inconsistent results of clinical trials, development of seocalcitol was discontinued by Leo Pharma.

Sumarotene (also known as Ro 14-9706) is a third-generation retinoid developed by Hoffmann-La Roche, F., und Co. A.-G., as a topical dermatologic agent for the repair of photodamage, antikeratinization, and antiproliferation. Sumarotene shows activity in standard preclinical and pharmacologic models of repair of photodamage, antikeratinization, and antiproliferation. In clinical trials, Sumarotene effectively decreases the number of actinic keratoses. Sumarotene is well-tolerated and most patients have only slight or absent local inflammation.

Tiapirinol is a thiazine derivative patented by Tanabe Seiyaku Co., Ltd. as a low toxic compound useful to prevent hypohepatia. In acute toxicity tests on mice, the toxicity of Tiapirinol is lower than that of pyridoxal phosphate and other vitamin B6 derivative. Tiapirinol showed vitamin B6 activity approximately equivalent to that of pyridoxal phosphate or pyridoxine for the growth of vitamin B6 deficient rats and also for the convulsions caused by antivitamin B6 agents.

Fluoromisonidazole F-18 ([F-18] FMISO) is used as a positron emission tomography (PET) radiotracer for imaging. It is generated by labeling fluoromisonidazole with fluorine-18. It is the most widely used nitroimidazole imaging agent for use as a non-invasive way to localize and quantify hypoxia. [18F] decays by positron emission. FMISO binds covalently to cellular molecules at rates that are inversely proportional to intracellular oxygen concentration. In hypoxic cells, FMISO is trapped, which is the basis for the use of this tracer to measure hypoxia.