Acreozast is an orally active antiallergic agent, which has anti-inflammatory activity. It was undergoing phase II clinical trials in Japan for the following condition: Asthma and Atopic dermatitis. Toyobo discontinued the development of acreozast in 1996.

Tazanolast, an anti-allergic and anti-asthmatic agent with selective mast-cell stabilising effects, was developed jointly by Wakamoto and Torii Pharmaceuticals.

Tepoxalin is a nonsteroidal anti-inflammatory drug approved for veterinary use in the United States and many other countries. Marketed under the brand name Zubrin, Tepoxalin is indicated for the control of pain and inflammation associated with osteoarthritis in dogs. Tepoxalin has an unique property as an NSAIDs that suppresses both cyclooxygenase and lipoxygenase.

Acefylline is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. Acephylline piperazine is a theophylline derivative with a direct bronchodilator action. It has the advantages over theophylline in being far less toxic and producing minimal gastric irritation. It is indicated for the treatment of asthma, emphysema, acute and chronic bronchitis associated with bronchospasm.Acefylline relaxes smooth muscles, relieves bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular calcium. Sodium phenobarbital is a non-selective central nervous system depressant that is primarily used as sedative-hypnotic.

Repirinast is an antiallergic drug developed and introduced into the market in Japan in 1987. It is a histamine release inhibitor. It has demonstrated effectiveness for treating bronchial asthma in humans.

Clorprenaline is a β2-adrenergic receptor agonist. As a bronchodilator it has been used for the treatment of bronchial asthma, bronchitis and other respiratory diseases. It is a potential new lean meat-boosting feed additive because it can promote animal muscular mass growth and decrease fat accumulation.

Oxatomide is a H1-histamine receptor antagonist developed for the treatment of broad spectrum of allergic and other hypersensitivity reactions. The drug is currently marketed in Japan, Taiwan, Italy, Portugal, Indonesia, Argentina, South Africa.

Etofylline [7-(2-hydroxyethyl)theophylline] is a N-7-substituted derivative of theophylline, a smooth muscle relaxant. Etofylline is used to relieve bronchoconstriction. It may act as a phosphodiesterase inhibitor and adenosine receptor antagonist.

Leukotriene D4 (LTD4, 5(S)-hydroxy-6(R)-S-cysteinylglycyl-7,9,11,14-(E, E, Z, Z)-eicosatetraenoic acid) is a pro-inflammatory mediator produced by eosinophils and mast cells, that is known to mediate its effects through specific cell-surface receptors belonging to the G-protein-coupled receptor family, namely the high-affinity CysLT (cysteinyl leukotriene) receptor. LTD4 is associated with the pathogenesis of several inflammatory disorders, such as asthma and inflammatory bowel disease. LTD4 is triggering many processes central to asthma – mucus secretion, bronchoconstriction and increased vascular permeability. Potent LTD4 antagonists protect (by about 50%) against exercise- and allergen-induced bronchoconstriction, suggesting that leukotrienes contribute to bronchoconstrictor responses. Leukotriene D4 has been used in trials studying the diagnostic of Asthma and Allergic Rhinitis.

Formoterol is a long-acting selective beta2-adrenergic receptor agonist (beta2-agonist). Inhaled formoterol fumarate acts locally in the lung as a bronchodilator. In vitro studies have shown that formoterol has more than 200-fold greater agonist activity at beta2-receptors than at beta1- receptors. Although beta2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors in the heart, there are also beta2-receptors in the human heart comprising 10%-50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective beta2- agonists may have cardiac effects. The pharmacologic effects of beta2-adrenoceptor agonist drugs, including formoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibits the release of pro-inflammatory mast-cell mediators such as histamine and leukotrienes. Formoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness. The relevance of these in vitro and animal findings to humans is unknown. Formoterol is used for use as long-term maintenance treatment of asthma in patients 6 years of age and older with reversible obstructive airways disease, including patients with symptoms of nocturnal asthma, who are using optimal corticosteroid treatment and experiencing regular or frequent breakthrough symptoms requiring use of a short-acting bronchodilator. Not indicated for asthma that can be successfully managed with occasional use of an inhaled, short-acting beta2-adrenergic agonist. Also used for the prevention of exercise-induced bronchospasm, as well as long-term treatment of bronchospasm associated with COPD. Marketed as Foradil Aerolizer.