ITRIGLUMIDE, an anthranilic acid derivative, is a cholecystokinin B receptor antagonist.

Doqualast is an antiasthmatic and antiallergic agent. It has a mode of antiallergic action similar to that of disodium cromoglycate and inhibits antigen-induced mediator release by interfering with the calcium transport required for histamine secretion across the mast cell membrane. In rabbits, no embryotoxic or teratogenic effects of doqualast were observed. The concomitant use of doqualast and theophylline might cause drug interaction. Doqualast is thought to increase the blood free fraction of concomitantly used theophylline and to accelerate elimination of theophylline from blood.

Amdoxovir is a guanosine analogue nucleoside reverse transcriptase inhibitor that is active in vitro against both HIV-1 and HBV. It is deaminated intracellularly by adenosine deaminase to dioxolane guanine (DXG). DXG-triphosphate, the active form of the drug, has greater activity than DAPD-triphosphate. Amdoxovir is under development (phase II study) for the treatment of HIV infection. Five subjects demonstrated lens opacities during the study, although baseline evaluations were not performed. Clinical studies of amdoxovir are currently on hold pending additional safety data.

FENHARMANE, a reserpine-like substance, is a neuroleptic developed and clinically tested in the Czech Republic.

Nebentan (YM598) is an orally active synthetic substituted phenylethenesulfonamide. As a selective endothelin A receptor antagonist, YM598 inhibits endothelin-mediated mechanisms involved in tumor cell growth and progression, angiogenesis, and metastasis. The inhibitory dissociation constant value of YM598 was 0.772 nM for native human ETA receptors, and 143 nM for native human ETB subtypes. The calculated selectivity ratio of YM598 for ETA versus ETB receptors was 222. In pithed rats, YM598 inhibited the big endothelin-1 (1 nmol/kg)-induced pressor response in a dose-dependent manner, after both intravenous and oral administration. YM598 showed not only superior antagonistic activity and higher-selectivity for endothelin ET(A) receptor in vitro, but at least a 30-fold higher potency in vivo than bosentan.

Meturedepa (also known as AB-132), an alkylating agent that was developed as an antineoplastic drug. Meturedepa was studied to treat lymphomas and leukemias. The drug also participated in the Eastern clinical drug evaluation program for 233 patients with advanced cancer. Information about the current use of this compound is not available.

Elnadipine is a calcium- and calmodulin antagonist exerting activity in the cardiovascular system.

Aminoquinuride (Surfen) binds to glycosaminoglycans (GAGs) and has been shown to influence their function, and the function of proteoglycans (complexes of GAGs linked to a core protein). Surfen was first described in 1938 as a component of depot insulin; however, subsequent studies have revealed its efficacy in binding to glycosaminoglycans (GAGs). Surfen contains four quinoline rings that contain positively charged amino or methyl groups. Surfen was found to bind with greatest avidity to heparin. There are now a handful of studies on the biological effects of surfen, many of which relate to its ability to block the interaction between GAGs and signaling proteins, including effects on growth factors (fibroblast growth factor and vascular endothelial growth factor) and fibrils associated with the binding of human immunodeficiency virus (HIV)-1 to target cells. Surfen inhibits the action of SEVI (semen-derived enhancer of HIV viral infection). Because SEVI can increase HIV infectivity by several orders of magnitude, supplementing current HIV microbicide candidates with SEVI inhibitors, such as surfen, might greatly increase their potency. Surfen has also been shown to reduce inflammation but inhibits remyelination in murine models of multiple sclerosis.