Rosiptor (AQX-1125) is a once daily, orally administered small molecule being developed by Aquinox Pharmaceuticals for the treatment of asthma, bladder pain syndrome/interstitial cystitis (IC/BPS) and chronic prostatitis/chronic pelvic pain syndrome. AQX-1125 is the only clinical-stage, orally administered, SHIP1 activator. AQX-1125 significantly reduces the late response to allergen challenge, with a trend to reduce airway inflammation. AQX-1125 was safe and well tolerated and merits further investigation in inflammatory disorders. AQX-1125 has been used in trials studying the treatment of COPD, atopic dermatitis, interstitial cystitis, and bladder pain syndrome. However, the development has been discontinued.

AZD-3043, a short-acting intravenous anesthetic/sedative agent. This drug was initially invented by Theravance and then developed by AstraZeneca as a positive allosteric modulator of the γ-aminobutyric acid type A (GABA(A)) receptor containing a metabolically labile ester moiety. Phase I clinical trials for use this compound in anesthesia was completed in Sweden and the UK, but further development was discontinued.

Echinomycin is a cyclic peptide of the family of quinoxaline antibiotics that was originally isolated from Streptomyces echinatus. It is thought to act as a bifunctional DNA intercalator. Echinomycin has a binding site size of four base pairs. The strong binding sites for echinomycin contain the central two-base-pair sequence 5'-CG-3'. Echinomycin interferes with HIF-1 DNA binding in a sequence-specific fashion. It was brought into clinical trials by the NCI 20 years ago based on its antitumor activity. It has been extensively tested in phase I-II clinical trials. Nausea, vomiting, reversible liver enzyme abnormalities, and allergic reactions were the most common toxicities encountered. However, minimal or no antitumor activity was found in phase II clinical trials.

MK-6186 is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) which displays subnanomolar potency against wild-type (WT) HIV virus and the two most prevalent NNRTI-resistant RT mutants (K103N and Y181C) in biochemical assays. In addition, it showed excellent antiviral potency against K103N and Y181C mutant viruses. In 2010 MK-6186 was studied in phase I clinical trials but no further development reports were published.

Praziquantel, (-)- is oxopyrazinoisoquinoline derivative and a levorotated isomer of Praziquantel patented by Merck Patent G.m.b.H. as anthelmintics agent. In rabbits infested with S. japonicum, the therapeutic effect of Praziquantel, (-)-was greater than that of dl-praziquantel as rated by the number of the worms in tissues and by liver damage. Histopathological examination showed that liver egg granulomas in the levo-praziquantel group were fewer in no. and smaller in size and were predominantly composed of Pseudotubercles instead of eosinophilic abscesses. Levo-praziquantel is therapeutically superior to praziquantel, while dextro-praziquantel is almost ineffective.

Piprocurarium is a curarimimetic. It is antagonized by neostigmine. Piprocurarium is strongly vagolytic, producing tachicardia. Its duration of action is shorter than that of d-tubocurare and longer than that of succinylcholine. Piprocurarium is not hypotensive, is only slightly histaminogenic, is nonirritating to the veins, and can be mixed with all the anesthetic drugs. Piprocurarium has been offered for clinical trial as a brief-acting, nondepolarizing neuromuscular blocking drug. The drug appears to be anything but short acting. A persistent tachycardia and elevation in systolic and diastolic pressure invariably follows its intravenous injection. Alarming electrocardiographic changes occur, characterized by AV dissociation, depression of the ST segment, supraventricular tachycardia and, at times, inversion of the T waves. In view of these circulatory effects, it is doubtful that the drug will be useful clinically.