HE3286, a synthetic derivative of androst-5-ene-3β,7β,17β-triol (AET), a non-glucocorticoid anti-inflammatory metabolite of the adrenal steroid, dehydroepiandrosterone is under development by Harbor BioSciences as an anti-inflammatory; antiepileptic drugs; antihyperglycemic agent. HE3286 was studied in phase I clinical trials in Obese Adult Subjects, in Patients With Rheumatoid Arthritis in Patients With Active, Mild-to-Moderate Ulcerative Colitis, and in Patients With Type 2 Diabetes Mellitus. In all these studies were determined safety, tolerance, pharmacokinetics, and activity of HE3286. In addition, was shown that HE3286 acted via binding, regulation and/or activation of MAPK or ERK, or through modulation of NFκB. Experiments on animals have shown that the drug could have a neuroprotective influence in glaucoma, as well as other chronic neurodegenerations.

Piquindone is an antipsychotic pyrroloisoquinoline derivative that binds to dopamine D2 receptors. It is a potent D-2 antagonist. It has a low potential for extrapyramidal effects and tardive dyskinesia. Piquindone exhibited relatively weaker cataleptogenic and antistereotypic activity than haloperidol, and had minimal activity in a rat chronic stereotypy model of receptor supersensitivity. Piquindone almost as potent as haloperidol, with fewer or less intense extrapyramidal effects and low potential for tardive dyskinesia. Piquindone led to moderate but significant improvements in the positive symptoms of schizophrenia and to improvements in negative symptoms just below the level of statistical significance. Therapeutic efficacy of a piquindone antagonist in Tourette Syndrome can be achieved without production of disabling extrapyramidal-side effects.

Indotecan (LMP400) is a novel indenoisoquinoline derivative with specific topoisomerase I inhibition activity, developed by Division of Cancer Treatment and Diagnosis National Cancer Institute for cancer treatment. In preclinical studied Indotecan inhibited the cell growth of established mouse pheochromocytoma cell lines and primary human tumor tissue cultures. Low doses of Indotecan decreased the protein levels of hypoxia-inducible factor 1 (HIF-1α), one of a family of factors studied as potential metastatic drivers in these tumors. In vitro, Indotecan showed an increase in the growth-inhibitory effects in combination with other chemotherapeutic drugs that are currently used for the treatment of pheochromocytoma. Recently Indotecan has entered Phase I clinical trials for the treatment of cancer patients at the National Cancer Institute, and definite plans are being formulated to commence Phase II clinical trials.

Hexopyrronium is an antihistaminic agent. Its gastric antisecretory action was studied in human. Information about the current use of this drug is not available.

Propazolamide is a sulfonamide derivative patented by American Cyanamid Co. useful in the treatment of glaucoma and epilepsy and as oral diuretics. Propazolamide acts as a carbonic anhydrase inhibitor.

Conorphone (TR5109) is an opioid of mixed agonist-antagonist analgesic class. In animal models, conorphone demonstrated an analgesic activity in the same range as morphine, and lack of addiction liability. Conoprphone was evaluated in a clinical trial for postoperative pain in the oral surgery model and in patients with postepisiotomy pain. The 40 mg dose of conorphone resulted in a significant incidence of side effects such as drowsiness, dizziness, nausea, and vomiting.

Clovoxamine is an antidepressant and anxiolytic drug, acting as a serotonin and norepinephrine reuptake inhibitor. The drug was investigated in the double-blind clinical trials for the treatment of anxiety neurosis, where it was compared with diazepam, and found to have comparable efficacy but higher drop out rate.

Cloperidone is a quinazolinedione derivative with sedative and antihypertensive properties. Cloperidone was discovered in 1965 by Miles Laboratories. The activity of the compound was demonstrated by behavioral observations in dogs and cats, by rotarod and activity cage experiments in mice and in other models.