IPRAVACAINE is a long-acting local anesthetic which anesthetic potency is similar to that of bupivacaine. It blocks the open state of human cardiac K+ channels.

RO4929097 (R-4733) is a small-molecule inhibitor of gamma-secretase (γ-secretase) with high oral bioavailability leading to the blockade of Notch signaling in tumor cells. This compound was co-developed by Roche and National Cancer Institute (NCI). RO4929097 had been in phase II clinical trials for the treatment of melanoma, colorectal cancer, and pancreatic cancer. However, these researches has been discontinued. Combination of RO4929097 and bevacizumab was well tolerated in phase I of clinical trial and can be considered in patients with recurrent malignant glioma.

Mipitroban (previously known as UP 11677), a thromboxane A2 receptor antagonist that was investigated to treat thrombosis. However, further studies were apparently discontinued.

FENPRINAST is a cromotyn-like bronchodilator used for the treatment of allergy and exercise-induced asthma.

Filibuvir (PF-868554), being developed by Pfizer, is an orally administered, non-nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase for the potential treatment of chronic hepatitis C (HCV) infection. Filibuvir is a potent and specific inhibitor of the virally encoded NS5B polymerase, and inhibited genotype 1 sub genomic HCV replication in the cell-based replicon system. In phase I and a IIa clinical trial in treatment-naïve patients infected with genotype 1 HCV, filibuvir monotherapy or in combination with pegylated IFNα2a/ribavirin (the standard of care [SoC] for HCV infection) for up to 4 weeks significantly reduced HCV RNA levels compared with placebo or SoC alone. However, company stopped development of the drug and the decision to halt development of the non-nucleoside polymerase inhibitor, which was in mid-stage testing, was not related to any safety issues.

Pretiadil is a thiadiazepine dioxide derivative patented by American pharmaceutical company Bristol-Myers Co. as a coronary vasodilating compound.

Prothixene is a thioxanthene derivative patented by Swiss multinational healthcare F. Hoffmann-La Roche & Co. as an antiemetic and neuroleptic agent. In preclinical models, prothixene shows patent antihistaminic activity. The central depressant activity of prothixene in the rotating rod test and the potentiation of thiopental narcosis and hypothermia in white mice (H strain) is one order lower than in the case of chlorprothixene. Prothixene has a higher protective effect in the supramaximal electric shock test with mice than promethazine and chlorprothixene. However, it has no effect on the reserpine ptosis in mice nor on the ulcerogenic action of reserpine in rats (Wistar strain). Its anti-serotonin activity is higher in vivo and in vitro than that of promethazine. The local irritation, tested on rabbits, is lower by 52% after prothixene application than after promethazine. Prothixene applied parenterally is more toxic to mice than promethazine. In oral administration, to mice, no differences in toxicity were found.

Dichloroxylenol is a bactericide, preservative and deodorant. It is often used in the preparation of antiseptic and deodorant lotions and bath preparations. Dichloroxylenol also showed slightly greater activity against S. aureus Oxoid 701/1 Lot 610254 than against Escherichia coli and Salmonella typhi, indicating a probable role for cell wall in the susceptibility of bacteria to dichloroxylenol. The efficacy of either povidone-iodine (Betadine) or dichloroxylenol (Septocid) intrauterine infusions on the treatment of endometritis and/or cervicitis in cows was examined. The recovery and conception rates obtained after Betadine treatment were better than those obtained after Septocid. Moreover, healthy cows and those inseminated before post-partum day 180, having no more than 4-7 previous services, responded well to either Betadine or Septocid treatment.

Obatoclax (GX15-070) is a novel BH3 mimetic pan Bcl- 2 inhibitor. The clinically studied formulation is as obatoclax mesylate (Box 1), a salt. It is only under study as an intravenous preparation. It functions to block BH3-mediated binding of Bcl-2, Bcl-XL, Mcl-1 and A1 to Bax and Bak. Bax and Bak thus are unopposed and able to dimerize to allow initiation of intrinsic apoptosis. Preclinically, obatoclax has been shown to reverse inhibition of Bax or Bak by Bcl-2, Bcl-XL, Bcl-w and Mcl-1. Obatoclax was discovered by Gemin X, which was acquired by Cephalon, which has since been acquired by Teva Pharmaceuticals. Obatoclax had been in phase III clinical trials by Gemin X Biotechnologies (subsidiary of Teva) for the treatment of non-small lung cancer (NSCLC). The compound received orphan drug designation in the U.S. in 2004 for the treatment of chronic lymphocytic leukemia (CLL). However, Teva discontinued the development of obatoclax in 2013.