BROTIANIDE is salicylanilide derivative used to treat fascioliasis in sheep. A dose of 7 mg/kg of brotianide shows 91-99% activity against 7-14 weeks old flukes; however, its activity against 6 weeks old flukes is weak (50-90%). It also possesses 85-90% activity against paramphistomes in sheep and cattle. The maximum tolerated dose of brotianide is 27 mg/kg in sheep.

Bromofos is an organic thiophosphate used as pesticide and insecticide for apple-pest control. Bromophos possesses remarkable stability in alkaline media and extremely low mammalian toxicity. The oral toxicity for small rodents is 3.75 to 13.4 mg/kg. body wt. Bromofos acts as contact and stomach poison. Very good efficacy is obtained against flies and their larvae, especially against parasitic species on sheep. Bromopros in sheep dip soln. is as effective as diazinon. It is effective in stables for fly control, depending on the surface, for up to 14 weeks.

Bromoxanide shows high activity against 6-week-old worms of F. hepatica and the nematode Hae- monchus contortus at very low doses.

Salazosulfamide was studied for the treatment of ankylosing spondylitis. It was found that salazosulfamide efficacy is associated with N-acetyltransferase 1 polymorphisms and in particularly, NAT1 AA/GG genotype at 263 locus. However, future studies should be conducted to investigate these issues.

Amuvatinib (formerly known as MP470) is an oral multi-targeted tyrosine kinase inhibitor, which play critical roles in transducing growth signals to cancer cells. It suppresses c-MET, c-RET and the mutant forms of cKIT, PDGFR and FLT3. It also disrupts DNA repair likely through suppression of homologous recombination protein Rad51, an important survival pathway in many human cancers. In vitro and in vivo data have demonstrated amuvatinib synergy with DNA damaging agents including etoposide and doxorubicin. Overall, in the amuvatinib clinical development program, over 200 subjects were exposed to at least one dose of amuvatinib. In the Phase 1b clinical study in combination with carboplatin and etoposide, responses in small cell lung cancer (SCLC), neuroendocrine as well as other tumor types were observed. Human pharmacokinetic data suggest that co-administration of amuvatinib did not alter exposures of standard of care agents including carboplatin, etoposide, doxorubicin, paclitaxel, topotecan or erlotinib as measured by overall exposure. In the first-in-human study, durable clinical benefit was observed in the gastrointestinal stromal tumors (GIST) with modulation of Rad51 observed in skin punch biopsies. In clinical trials, amuvatinib has demonstrated a wide therapeutic window and shows minimal toxicity in the expected therapeutic dose range, despite suppressing several signaling pathways within cells. However, in spite of this, this drug was discontinued, because it was not pre-specified primary endpoints in the clinical proof of concept (cPOC) stage. But the combination of MP470 and Erlotinib, which target the HER family/PI3K/Akt pathway may represent a novel therapeutic strategy for prostate cancer.

Zicronapine (formerly known as Lu 31-130), an oral antipsychotic that was studied for the treatment of schizophrenia. The drug was used in a phase III clinical trial.

Diproteverine is a calcium channel blocking agent. Diproteverine provoked a dose-dependent inhibition of LHRH-stimulated luteinizing hormone release. Diproteverine does not modify mean blood pressure. Diproteverine administered with and without pharmacologic autonomic blockade in the conscious dog causes dose-related depressant effects on sinus node function and atrioventricular conduction without producing significant vasodilatation. Diproteverine caused a redistribution of the available coronary blood flow, to the benefit of an ischemic area of the myocardium. The combination of the reduction in heart rate, to lower cardiac oxygen demand, with the beneficial action on coronary blood flow should result in diproteverinebeing particularly beneficial for the treatment of angina pectoris.

Cetaben has been identified as an anti-atherosclerotic hypolipidaemic substance. Cetaben is a unique, PPARα-independent peroxisome proliferator with hypolipidemic activity that inhibits cholesterol synthesis in the human hepatoma Hep-G2 cells resulting in reversible changes in Golgi morphology. Cetaben represents an exceptional type of peroxisome proliferator, specifically affecting peroxisomes, without having a negative influence on the processes of peroxisome biogenesis. Cetaben raised only the peroxisomal enzymes, acyl-CoA oxidase, glycerone-phosphate acyltransferase, D-amino-acid oxidase, catalase, and urate oxidase. Cetaben sodium has being shown to be an antiatherosclerotic agent.

Guanisoquin was found to be an effective antihypertensive agent that inhibited the monoamine oxidase.