Burapitant (SSR-240,600) is a drug developed by Sanofi-Aventis which was one of the first compounds developed that acts as a potent and selective antagonist for the NK1 receptor. Burapitant inhibited the binding of radioactive substance P to tachykinin NK1 receptors in human lymphoblastic IM9 cells, human astrocytoma U373MG cells, and human brain cortex. It also showed a subnanomolar affinity for guinea pig NK1 receptors but was less potent on rat and gerbil NK1 receptors. Burapitant inhibited [Sar(9),Met(O2)(11)]substance P-induced inositol monophosphate formation in human astrocytoma U373MG cells. Burapitant (0.1-10 mg/kg i.p. or p.o.) antagonized the excitatory effect of i.c.v. infusion of [Sar(9),Met(O2)(11)]substance P (SP) on the release of acetylcholine in the striatum of anesthetized and awake guinea pigs. This antagonistic action was still observed after repeated administration of Burapitant (5 days, 10 mg/kg p.o., once a day). Burapitant (10 mg/kg i.p.) inhibited the phosphorylation of the cAMP response element-binding protein in various brain regions induced by i.c.v. administration of [Sar9,Met(O2)(11)]SP. While burapitant itself did not proceed beyond early clinical trials and was never developed for clinical use in humans, promising animal results from this and related compounds have led to a number of novel drugs from this class that has now been introduced into medical use.

N-(4-Ethylphenyl)-3-(Hydroxymethyl)-N-Isobutyl-4-(Tetrahydro-2h-Pyran-4-Ylmethoxy)Benzenesulfonamide (also known as GSK2981278) is a highly potent and selective inverse agonist of RORγ under development for the topical treatment of psoriasis. Preclinical data showed that GSK2981278 significantly inhibited the production of the Th17 signature cytokines in multiple in vitro and human tissue‐based systems. GSK2981278 may block the transcriptional activity of RORγt, leading to local suppression of cytokine expression and ultimately, improvement in psoriasis. Unfortunately in phase I clinical trial clinical assessment results showed no improvement of psoriatic lesions following treatment with GSK2981278.

SPK-843 is a water-soluble partricin derivative patented by SPA Societa Prodotti Antibiotici S.p.A. and developed by Aparts and Kaken for the potential treatment of systemic fungal infections. In preclinical models, SPK-843 shows in vitro inhibitory activity comparable to or better than that of Amphotericin B against Candida spp., Cryptococcus neoformans, and Aspergillus spp. SPK-843 exhibits dose-dependent efficacy on murine pulmonary aspergillosis models. SPK-843 doses of higher than 1.0 mg/kg of body weight exhibit no renal toxicities and a tendency toward better survival prolongation than the estimated maximum tolerated doses of amphotericin B (Fungizone) and liposomal amphotericin B.