RO-5028442 (RG7713) is a potent and highly selective arginine vasopressin receptor 1A (V1a) antagonist. This compound has been studied for use in autistic spectrum disorder. A phase I study in adult male high-functioning autistic patients has been completed in 2016 and showed that blockade of the V1a receptor may improve social communication in adults with high-functioning ASD. Eye-tracking results showed an increase in biological motion orienting preference. Only mild or moderate adverse events were reported.

Broxaterol is a β2 adrenoreceptor agonist used for the treatment of respiratory disease. Broxaterol produced a significant clinical improvement, an increase in FEV1 and a decrease in supplemental anti-asthmatic drugs used in patients with reversible airflow obstruction and in asthmatic children. The increases in FEV1 versus baseline were significantly maintained after the end of the treatment. Prompt disappearance of the asthmatic attack with significant improvement in lung function was observed in children. In two long-term controlled trials, the respiratory effects of broxaterol nebulizer solution were significantly greater than placebo. Moreover, broxaterol by metered dose inhaler was more effective than salbutamol after 3 months follow-up, showing the absence of tachyphylaxis. In long-term clinical evaluation, broxaterol has been shown to be well tolerated, with an incidence of adverse reactions equal to or less than that reported in the literature for other beta 2-agonists. The side effects most frequently associated with broxaterol were tremor, nervousness, and palpitations.

PF-03893787 is potent and selective histamine H4 receptor (H4R) antagonist. It has comparable binding affinity to the human histamine H3 receptor. PF-03893787 was found to have significant affinity for the hERG channel. Novartis initiates a phase II extension trial in Atopic dermatitis. Studies exploring the utility of PF-3893787 in patients would be reported in due course, being the potential indications of asthma, pruritus, inflammatory skin diseases and pain, among others.