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.

Propanocaine is a benzyl alcohol derivative with local anesthetics activity

Traxoprodil (CP-101,606) is a potent, selective N-Methyl-D-aspartate (NMDA) receptor (NR2B subunit) antagonist under development by Pfizer for its potential as a neuroprotectant in head injury and neurodegenerative disease. It is in phase II trials in the US and in phase I in Japan for the potential treatment of head injury, such as, Depressive Disorder, Major and Parkinson's Disease. CP-101,606 does not protect against glutamate-induced neurotoxicity in cultured cerebellar neurons, up to a dose of 10 uM. These results are consistent with CP-101,606 being a potent NMDA antagonist, selective for the type of NMDA receptor associated with the hippocampus. Some further investigation revealed that CP-101,606 was associated with a dose-related dissociation and amnesia. These results support the hypothesis that glutamate antagonists may be useful antidyskinetic agents. However, future studies will have to determine if the benefits of dyskinesia suppression can be achieved without adverse cognitive effects.

Naftypramide is a nonsteroidal anti-inflammatory drug. It was used in the treatment of gynecological inflammatory diseases.

Fenalcomine is a coronary vasodilator, cardiotonic and local anesthetic agent. It was studied in the treatment of angina pectoris.