Oxaprotiline (also known as hydroxymaprotiline) is a norepinephrine reuptake inhibitor and blocked the histamine H1 receptor. Oxaprotiline was studied in the treatment of hospitalized depressive patients. However, this drug has never been marketed.

Tomeglovir (BAY 38-4766) is a human cytomegalovirus (CMV) terminase complex inhibitor. Treatment with BAY 38-4766 reduced both viremia and DNAemia, as determined by a real-time PCR assay, following guinea pig cytomegalovirus (GPCMV) infection of cyclophosphamide-immunosuppressed strain 2 guinea pigs. BAY 38-4766 also reduced mortality following lethal GPCMV challenge in immunosuppressed Hartley guinea pigs. a combination of BAY 38-4766 with anti-cytomegalovirus drug ganciclovir showed antagonism. Interaction of viral DNA processing inhibitor 2-bromo-5,6-dichloro-1beta-D-ribofuranosyl benzimidazole (BDCRB) with BAY 38-4766 showed a mixed pattern of synergy and antagonism. Tomeglovir had been in phase II clinical trials by Bayer for the treatment of CMV infection. However, this development was discontinued.

ISALMADOL is an analgesic agent.

Oxadimedine, an antihistamine that was developed as a local anesthetic. Information about the current use of this compound is not available.

Letrazuril is the p-fluoro analogue of diclazuril, a benzeneacetonitrile which is active against Eimeria spp., the causative agent of coccidiosis in poultry. Letrazuril is better absorbed and unlike diclazuril produces detectable plasma drug levels in humans following oral administration. In experimental studies on neonatal mice infected with Cryptosporidium parvum, oral administration of letrazuril for 4 days reduced stool oocyst counts by 95-98%, with complete clearing of oocysts from the stool in 47% of animals receiving the higher dose. Letrazuril has the potential to be an effective agent in the treatment of AIDS-related Cryptosporidiosis, without associated major toxicity. Severely immunocompromised AIDS patients with refractory cryptosporidiosis may show a modest, short-lived response to letrazuril. Letrazuril had been in phase I clinical trials for the treatment of cryptosporidiosis. However, this study was discontinued.

Milameline (previously known as RU 35926/CI-979), a partial muscarinic agonist that was developed as a cognition-enhancing agent for the treatment of patients with Alzheimer's disease. In spite of this drug has achieved phase III clinical trials, further studies were apparently discontinued.

Arctigenin is a plant lignan extracted from Arctium lappa that has been shown to have estrogenic properties. In ER-positive MCF-7 cells, arctigenin efficiently inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced cell migration and invasion. Arctigenin confers anti-metastatic effects by inhibiting MMP-9 and uPA via the Akt, NF-κB and MAPK signaling pathways on breast cancer, regardless of ER expression. Intake of arctigenin could be an effective supplement for breast cancer patients. Arctigenin is a phenylpropanoid dibenzylbutyrolactone lignan compound possessing antitumor, anti-inflammatory, anti-influenza, antioxidant, antibacterial, and hypoglycaemic activities. Arctigenin exhibited significant antiproliferative activity against CCRF-CEM cells after 72 h treatment with IC50 values of 1.21 ± 0.15 um. It arrested CCRF-CEM cells in the S phase. It induced apoptosis in CCRF-CEM cells in a concentration- and time-dependent manner. Arctigenin is a good candidate for the development of novel agents against T-cell lymphoma. Arctigenin has been found to act as an agonist of adiponectin receptor 1 (AdipoR1). Arctigenin is an antagonist of MR and effectively decreases the Na/K-ATPase 1 gene expression, thus highlighting its potential as an anti-hypertensive drug lead compound.