Bimosiamose, discovered by Encysive Pharmaceutical and presently being developed by Revotar Biopharmaceuticals, is an 863 g/mol molecular weight dimer with minimal carbohydrate content and is, to date, the leading selectin inhibitor in clinical development. It was developed as anti-inflammatory drug fir the treatment of acute chronic inflammatory disorders including COPD. This compound has shown promise in a phase IIa 'proof of concept' trial in patients with asthma, reducing airway recruitment of eosinophils after intravenous administration. In acute lung injury, neutrophils (a type of white blood cells, thus belonging to the group of cells of the body’s defence system-the immune system) are drawn to the small lung bloodvessels and migrate into the air sacs (alveoli). There they release substances, which cause the inflammation leading to further destruction of the lung tissue. Bimosiamose disodium is expected to hinder the migration of these neutrophils into the alveoli.

Betacetylmethadol is a synthetic narcotic analgesic under international control according to the UN Single Convention 1961.

Mapracorat (BAY-865319, BOL-303242-X or ZK-245186) is a selective non-steroid glucocorticoid receptor agonist exerting anti-inflammatory activity. Mapracorat showed partial attenuation of the classical NF-κB pathway, consistent with traditional steroids. However, mapracorat uniquely potentiated a novel anti-inflammatory mechanism through rapid upregulation of RelB, an anti-inflammatory member of the NF-κB alternative pathway. Mapracorat was being studied in the treatment of ocular and skin inflammatory diseases.

Hydroxyflutamide is the major active metabolite of flutamide. Flutamide undergoes extensive first-pass metabolism by CYP1A2 to its metabolite hydroxyflutamide and its hydrolysis product, 3-trifluoromethyl-4-nitroaniline. Hydroxyflutamide is a more powerful antiandrogen in vivo, with higher affinity for the receptor than that of flutamide. Hydroxyflutamide is in phase II clinical trials for the treatment of prostate cancer. However, a drug resistance problem appears after about one year's treatment. Per-residue free energy decomposition analyses indicate that N705, T877, and M895 androgen receptor mutations are vital residues in the agonist/antagonist mechanism of hydroxyflutamide.

Pytamine is a nitrosamine derivative patented by Hercules Powder Co. as antioxidants, stabilizers, rubber additives, insecticides, fungicides, bactericides, and pharmaceutical intermediates. In preclinical trials Pytamine shows potent psychotropic effects associated modulation of GABAA receptors.

Flurocitabine is an anti-metabolite that was developed by Hoffmann-La Roche for the treatment of cancer. The drug is metabolized to 2 biologically active substances, AFC (1-beta-D-arabinofuranosyl-5-fluorocytosine) and AFU (arabinofuranosyl-5-fluorouracil). Flurocitabine was tested against stomach cancer, pancreatic cancer, small cell lung cancer and AML, however, the development was terminated in the early phases.

Temarotene (also known as Ro 15-0778), the arotinoid with immunosuppressive and immunostimulatory activities. Temarotene was also studied as a chemopreventive agent. Information about the current development of this compound is not available.

Almestrone (7 alpha-methylestrone) is a synthetic steroidal estrogen. It is a precursor of several highly active steroidal hormones.

Sonolisib (PX-866) is a small-molecule inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. Sonolisib inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Inhibition of the PI3K pathway with Sonolisib leads to inhibition of cell growth and decreased activation of downstream targets in GBM, both in vitro and in vivo, using U87–tumor-bearing mice, including Akt, S6, and mTOR. Sonolisib was in phase II clinical trials by Oncothyreon for the treatment of glioblastoma multiforme and castration-resistant prostate cancer (CRPC). It was in phase I/II clinical trials for the treatment of malignant melanoma, non-small cell lung cancer and Head and neck cancer. In clinical trials, Sonolisib was well tolerated, with common side effects being diarrhea, nausea, vomiting, and elevated liver enzymes. However, no recent development has been reported.

Inecalcitol is a calcitriol analog with potential antineoplastic activity patented by a global pharmaceutical company Laboratoire Theramex. Inecalcitol is a potent agonist of vitamin D receptor (VDR). Inecalcitol was shown to be more potent than calcitriol in decreasing tumor cell growth and inducing apoptosis in a number of different model systems including models of breast cancer, prostate cancer, and squamous cell cancer. Importantly, at the doses shown to induce tumor regression in the animal models investigated, Inecalcitol had no major effect on blood calcium levels. In this phase I study, Inecalcitol was found to be well tolerated. Currently, Inecalcitol in combination with the cytotoxic drug, decitabine is undergoing a phase II clinical trial in patients with acute myeloid leukemia who are unfit to receive standard chemotherapy.