Metoxepin was developed as an antiemetic, neuroleptic and antihistamine agent. This drug has never been marketed.

Mofegiline (MDL 72,974A or (E)-2-(4-fluorophenethyl)-3-fluoroallylamine, hydrochloride), is a selective and irreversible inhibitor of monoamine oxidase type B (MAO-B) both in vitro and in vivo. In addition, mofegiline inhibits semicarbazide-sensitive amine oxidase activity from human serum and saphenous vein. In phase II studies, MDL 72,974A is proving to be a useful adjunct to conventional therapy of Parkinson's disease. It seems mofegiline development was discontinued.

Resorantel (HOE 296V) is an anthelmintic agent. Resorantel was found to be highly effective against Houttuynia struthionis (a tapeworm, parasite of the small intestine) in ostriches. Resorantel also showed anthelmintic efficacy against Thysaniezia giardi and Avitellina spp. (both tapeworms) when tested in sheep. Similar results have been found in goats and cattle.

Omonasteine was used in sequential peptide ligation for the synthesis of the BRD7 bromodomain.

Cefedrolor is a broad-spectrum cephalexin antibiotic patented by pharmaceutical company Bristol-Myers Co.

Vidupiprant, also known as AMG 853, is an orally bioavailable and potent dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors. Vidupiprant inhibits PGD2-induced down modulation of CRTH2 on CD16- granulocytes in human whole blood as well as PGD2-induced cAMP response in platelets. It inhibits PGD2-induced airway constriction in vivo. Also inhibits BRD4 (Kd = 170 nM). AMG 853 as an add-on to inhaled corticosteroid therapy demonstrated no associated risks but was not effective at improving asthma symptoms or lung function in patients with inadequately controlled moderate-to-severe asthma. AMG 853 has been discontinued due to poor efficacy.

Rotigaptide (previously known as ZP123) originally was developed by Zealand Pharma as a stable antiarrhythmic peptide analog, which maintains gap junction intercellular communication. Then this drug was licensed to Wyeth Pharmaceuticals where it studied in phase II clinical trials in patients with coronary artery disease and with atrial fibrillation. However, these researches have been discontinued.

Benurestat is a urease inhibitor, which as was shown in experiments on rats, could decrease in the urinary excretion of ammonia with experimental P. mirabilis genitourinary tract infection.

Actodigin is a semisynthetic cardiac glycoside compounded from digitoxigenin and one molecule of glucose. In addition, unlike the naturally occurring glycosides, the C-2 instead of the C-3 atom of the lactone ring is attached to the steroid nucleus. Actodigin is a cardiovascular agent. When injected at 30 min invervals into dogs with barbiturate-induced heart failure, actodigin caused a marked positive inotropic action of short duration. It converted arrhythmia to normal sinus rhythm. Actodigin effectively and quickly reduced the ventricular rate in patients with atrial fibrillation. Actodigin, because of its rapid onset and brief duration of action, may be useful in controlling the ventricular rate in patients with atrial fibrillation.