Amiflamine is a selective and reversible inhibitor of monoamine oxidase (MAO) type A which exerts a preferential effect on serotonin (5-HT) catabolism. The (+)-enantiomer is the active stereoisomer. In a series of p-aminosubstituted phenethylamines, the ( + )-enantiomer of the compound amiflamine (4-dimethylamino-2-a-dimethylphenethylamine) was found to be a potent, selective, and reversible MAO type A inhibitor. Amiflamine (FLA 336(+] and its two metabolites, FLA 788(+) and FLA 668(+) were found to be competitive inhibitors of the activity of monoamine oxidase-A in homogenates of human hypothalamus and liver obtained at autopsy. Ki values, determined at pH 7.2, were 1.3, 0.3 and 22 uM (liver) and 0.8, 0.2 and 14 uM (hypothalamus) for amiflamine, FLA 788(+) and FLA 668(+), respectively. Monoamine oxidase-B activity was only weakly inhibited by the compounds. This initial phase I study in six normal subjects showed that the new MAO inhibitor amiflamine can be tolerated in single oral doses up to 80 mg without significant pharmacologic effects. Doses up to 60 mg were tolerated without any subjective or objective effects.

Brallobarbital possessed the sedative and hypnotic properties and was a component of Vesparax that was used to treat sleep disorders. However, was revealed that brallobarbital was responsible for the problems in Vesparax intoxication.

Bometolol is a cardiospecific beta-adrenergic blocking drug that was never marketed.

Bisorcic is an N-acetyl-L-amino acid that is L-ornithine was developed as a hepatoprotective agent and was studied as a psychostimulant.

Guaiactamine was developed as antispasmodic therapeutic agents, and it has never been marketed.

CPI-613 is a lipoate derivative synthesized to be catalytically inert but to potentially mimic lipoate catalytic intermediates. The drug is in phase II of clinical trials for the treatment of Myelodysplastic syndromes; Pancreatic cancer; Small cell lung cancer; Solid tumors; Bile duct cancer; Acute Myeloid leukemia. The mechanism of CPI-613 action can be explained by (I) inhibition of tumor cell pyruvate dehydrogenase complex (PDC) through activation of pyruvate dehydrogenase kinases leading to inactivating phosphorylation of the E1alpha-subunit of PDC; and (II) inhibition of alpha-ketoglutarate dehydrogenase.

Guaisteine, a thiazolidine derivative that was used as an antitussive agent. This compound has never been marketed.

Simotaxel (MST-997) is a semi-synthetic, orally bioavailable, third-generation taxane derivative and microtubule-stabilizing agent, with potential antineoplastic activity. Simotaxel was being developed through a collaboration between Wyeth (later Pfizer) and Taxolog as a potential treatment for cancer. Upon administration, simotaxel binds to tubulin, promotes microtubule assembly and stabilization, and prevents microtubule depolymerization. This results in G2/M arrest, apoptosis and the inhibition of cell proliferation in susceptible tumor cells. This agent is a poor substrate for P-glycoprotein-related drug resistance mechanisms; therefore, it may be useful for treating multi-drug resistant tumors. MST-997 is more potent than paclitaxel and docetaxel and overcomes paclitaxel and docetaxel resistance in certain tumor cell types. Simotaxel is under investigation in clinical trial NCT00088647 (study evaluating MST-997 in advanced malignant solid tumors).

BLI 489 was developed by Wyeth as a 6-methylidene-penem β-lactamase inhibitor for the treatment of bacterial infections and urinary tract infections. BLI-489 has shown the promising clinical data, however, development of this drug, was discontinued.

Nitralamine is an antifungal agent.