Pamatolol is a beta-Adrenergic receptor antagonist was studied as an Antiarrhythmic agent. The phase I clinical trial has shown that the drug was relatively cardioselective in man. Information about the further development of this drug is not available.

LASINAVIR, a hydroxyethylene derivative, is highly specific human immunodeficiency virus (HIV) protease inhibitor with an IC50 of 1 nM. Its clinical development was discontinued.

Cefuroxime Pivoxetil is an ester prodrug of cefuroxime, a semisynthetic, broad-spectrum, beta-lactamase-resistant, second-generation cephalosporin with antibacterial activity. Cefuroxime binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Cicarperone is decahydroquinoline derivative with local anesthetic action. In ex vivo models Cicarperone protected anesthetized guinea-pigs against ouabain-induced ventricular fibrillation and increased the lethal dose of ouabain. Unlike most drugs with local anesthetic properties, Cicarperone did not depress contractions in isolated atria but increased them. Cicarperone reduces the spontaneous frequency, maximum follow frequency and conduction velocity of rabbit isolated atria. Cicarperone had no blocking action on the chronotropic or positive inotropic actions of isoprenaline on isolated atrial muscle. In vivo evaluation of Cicarperone in anesthetized dogs shows that Cicarperone caused small dose-related bradycardia and a large dose-related decrease in peripheral vascular resistance. Ciclactate has never been marketed in the US and EU.

Merimepodib has immunosuppressive activity. It targets hepatitis C indirectly through the inhibition of inositol monophosphate dehydrogenase, which exerts an acute antiproliferative effect on lymphocyte proliferation due to their almost exclusive dependence on the de novo pathway for synthesis of guanosine. Phase II clinical trial study of merimepodib for the treatment of HCV infection and psoriasis were completed. The poor pharmacokinetic-pharmacodynamic results have resulted in discontinuation of clinical trials.

Alvespimycin (17-desmethoxy-17-N,N-dimethylaminoethylamino-geldanamycin) (17-DMAG; NSC 707545) is an inhibitor of the molecular chaperone heat shock protein HSP90. Alvespimycin is a derivative of antineoplastic benzoquinone antibiotic geldanamycin. Alvespimycin binds to HSP90, a chaperone protein that aids in the assembly, maturation and folding of proteins. Subsequently, the function of Hsp90 is inhibited, leading to the degradation and depletion of its client proteins such as kinases and transcription factors involved with cell cycle regulation and signal transduction. Alvespimycin was studied in clinical trials for the treatment of solid tumors and hematologic malignancies however its development was discontinued.

Carprazidil is oxadiazolopyrimidine derivative patented by pharmaceutical company Hoffmann-La Roche as a direct vasodilator and potent antihypertensive agent. In clinical trials, Carprazidil was evaluated in patients with moderate to severe arterial hypertension. Following the addition of Carprazidil to pre-existing therapy with diuretics and beta-blockers or sympatholytics, blood pressure in most of the patients was normalized within one month. Heart rate was only slightly increased. Orthostatic hypotension was not observed. Weight gain or oedema formation occurred in 14 patients within the first four weeks, but could be controlled satisfactorily by intensified diuretic therapy. After a mean duration of treatment of 2.8 months, plasma volume and plasma and urine sodium were unaltered, and plasma potassium was slightly decreased. Plasma renin activity was doubled, whereas plasma aldosterone concentrations were unaltered. No adverse side effects on hematological parameters, liver or renal function were observed, nor was antinuclear antibody detected.

Diphenan is p-benzyl-phenyl-carbamate. Various workers have reported that diphenan will rid children of oxyurids and it has been claimed to be nontoxic and tasteless and to have the advantage of being a vermicide as opposed to a vermifuge. An attempt has been made to assess the efficacy of diphenan as a vermicide. Diphenan was given far in excess of the normal dosage. Subsequent examnation showed few cures and these mostly in lightly infested children. The condition of many was unchanged and that of some worse after treatment. No toxic reactions were encountered. Moreover, diphenan was found to have no detectable anthelmintic effect when given in high dosage in the treatment of enterobiasis.

Bamnidazole was developed as an antiprotozoal agent against Tryhomonas, however, has never been marketed.

Alestramustine is the l-alanine ester form of estramustine, a combination of the nitrogen mustard normustine coupled via a carbamate to estradiol, with antineoplastic activity. Upon conversion of alestramustine to estramustine, estramustine binds to microtubule-associated proteins (MAPs) and beta tubulin, thereby interfering with microtubule dynamics and leading to microtubule disassembly and cell cyle arrest. Due to the estrogen moiety, this agent is able to selectively bind to and be taken up by estrogen receptor-positive cells.