Alvespimycin (17-desmethoxy-17-N,N-dimethylaminoethylamino-geldanamycin) (17-DMAG; NSC 707545) is an inhibitor of the molecular chaperone heat shock protein HSP90. Alvespimycin is a derivative of antineoplastic benzoquinone antibiotic geldanamycin. Alvespimycin binds to HSP90, a chaperone protein that aids in the assembly, maturation and folding of proteins. Subsequently, the function of Hsp90 is inhibited, leading to the degradation and depletion of its client proteins such as kinases and transcription factors involved with cell cycle regulation and signal transduction. Alvespimycin was studied in clinical trials for the treatment of solid tumors and hematologic malignancies however its development was discontinued.

Ondelopran (also known as LY2196044) was developed as orally available opioid receptor antagonist for the treatment of alcoholism. This drug completed clinical trials phase III where was assess its efficacy and safety in the treatment of alcohol dependence in adult outpatients.

IRAMPANEL, an oxazole derivative, is a dual non-competitive antagonist of the AMPA receptor and neuronal voltage-gated sodium channel blocker. It was under development for the potential treatment of stroke and other neurological disorders, including epilepsy and pain.

IRLOXACIN, a fluorinated quinolone derivative, is an antibacterial agent with proved activity against both gram-positive and gram-negative bacteria.

Pirenperone, a quinazoline derivative, is a selective antagonist at serotonin receptor 2A binding sites. The liposoluble compound pirenperone has been studied in a variety of behavioral tests including the sensitive d-lysergic acid diethylamide (LSD) cue discrimination assay, in which it served as a potent LSD-antagonist. Pirenperone also proved to be an effective antagonist of serotonin-mediated behavioral responses including the head twitch response thought to be mediated by serotonin receptors.

FIDUXOSIN is a selective alpha1-adrenoceptor antagonist with higher affinity for alpha1A-adrenoceptors and for alpha1D-adrenoceptors than for alpha1B-adrenoceptors. It was in clinical trials for the treatment of benign prostatic hyperplasia.

Pirinidazole was found to be the compound from a series of 5-nitroimidazoles with the broadest action against protozoans. Its effect against trichomonads is the most pronounced. The comparison of the effective doses of different 5-nitroimidazoles against Trichomonas fetus demonstrates that the compound Pirinidazole is slightly superior to Tinidazole, distinctly superior to Metronidazole, and very much superior to Nitrimidazine. Some toxicological data of Pirinidazole show that the compound is well tolerated.

Varlitinib (Alternative Names: ARRY-334543; ARRY-543; ASLAN-001; Varlitinib tosylate) is a small molecule based reversible pan-HER inhibitor of EGFR, HER2 and HER4. In response to the binding of various ligands, these kinases undergo heterodimerisation and homodimerization, resulting in activation of numerous growth factor signaling pathways, by inhibiting the activation of the HER receptors via drug, effects such as shrinkage of the tumor and longer survival can be anticipated. In a large variety of cancers, the overexpression and/or constitutive activation of EGFR and HER2 are often observed and frequently correlate with poor clinical prognosis. Licensed from Array BioPharma with global rights for all indications, varlitinib is being developed as first-in-class drug for cholangiocarcinoma, gastric and colorectal cancer, and as best-in-class drug for breast cancer.

Goxalapladib (SB-677116) is a selective inhibitor of Lipoprotein associated phospholipase A2 (Lp-PLA2).

Pentisomide is an agent structurally related to disopyramide. Pentisomide is a class-I antiarrhythmic agent with a marked effect on depolarization (action of class Ia and Ic) and on repolarization. Pentisomide dose-dependently inhibited ischaemia-reperfusion arrhythmia. Pentisomide had been in phase II clinical trial for the treatment of arrhythmias. The electrophysiologic effects of pentisomide were investigated after intravenous and oral application in patients with drug refractory atrioventricular nodal tachycardia and patients with orthodromic atrioventricular re-entrant tachycardia. If intravenous pentisomide did not prevent induction of the tachycardia, oral pentisomide was not effective either. Long-term treatment with pentisomide had to be discontinued because of possible side effects.