Nabazenil is a synthetic cannabinoid receptor agonist, which has anticonvulsant properties. Nabazenil was undergoing preclinical trials with HG Pars in the USA.

FILENADOL is an analgesic drug with antinociceptive and anti-inflammatory properties. It reduces the hyperalgesic effects of inflammatory mediators besides inhibiting partially the synthesis of eicosanoids.

Azamethiphos, an organothiophosphate insecticide, initially was used in 1991 for the treatment against sea lice. However, because of reduced sensitivity in 1999, the use of this compound was terminated. Azamethiphos was re-introduced in 2008; it’s the main component of Salmosan, a pesticide presently used for treatment against sea lice. Salmosan is applied as a bath treatment and then released into the surrounding seawater

Sulbenox is substituted tetrahydrobenzothiophene derivative patented by American Cyanamid Co as the animal growth-promoting agent. In preclinical studies, Sulbenox found to be an effective growth promoter in sheep, mice, and rats.

Propizepine is a benzodiazepinone derivative patented by Laboratoires U.P.S.A. as antidepressive, antihistaminic, antianaphylactic, thymoanaleptic, antiserotonine, antispasmodic, and analgetic compound. Propizepine used in France for the treatment of depression in the 1970s.

Pentomone is a nonsteroidal antiandrogen developed by Lilly Company for postmenopausal patients with metastatic breast cancer who have been previously treated with tamoxifen. It is a prostate growth inhibitor.

Cytochalasin B is a cell-permeable alkaloid, isolated from a fungus Helminthosporium dematioideum. Cytochalasin B is an inhibitor of actin polymerization through binding to the fast-growing (barbed) end of F-actin filaments. Cytochalasin is used in studies of actin polymerization, cell division, and cell movement. The compound also inhibits glucose transporters GLUT1,3 and 4 and was investigated in a clinical trial to prevent restenosis after angioplasty surgery.

Erizepine is a compound with neuroleptic activity. Erizepine is considered to bind dopamine receptors.

R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta, FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2. In addition, this agent exhibits anti-proliferative activity by initiating mitotic arrest and inducing apoptosis. In the presence of R1530, polyploid cancer cells underwent apoptosis or became senescent which translated into potent in vitro and in vivo efficacy. Normal proliferating cells were resistant to R1530-induced polyploidy thus supporting the rationale for cancer therapy by induced polyploidy. Mitotic checkpoint kinase BubR1 was found downregulated during R1530-induced exit from mitosis, a likely consequence of PLK4 inhibition. R1530 strongly inhibited human tumor cell proliferation and growth factor-driven proliferation of endothelial and fibroblast cells. Significant tumor growth inhibition was demonstrated in a lung cancer xenograft model with a range of once daily, weekly and twice-weekly doses of R1530. Daily doses were most effective in the lung cancer model and also had significant growth inhibitory effects in models of colorectal, prostate, and breast tumors. Tumor regression occurred in all models treated with the maximum tolerated daily dose. The doses of 25 and 50 mg/kg QD resulted in biologically significant increased survival in all tested models. After oral administration in nude mice, R1530 showed good tissue penetration. R1530 had been in phase I clinical trials by Hoffmann-La Roche, Inc. for the treatment of advanced solid tumors. However, the clinical development of R1530 was discontinued.