Fleroxacin is an anti-bacterial agent developed for the treatment of uncomplicated cystitis in women, uncomplicated gonococcal infections, bacterial enteritis, and traveler's diarrea, urinary tract infection, pyelonephritis, skin, soft tissue, bone and joint infections, and lower respiratory tract infections. Fleroxacin acts on bacterials by inhibiting DNA gyrase and topoisomerase IV. Although the current status of the drug in Europe and in the USA is unknown, there is information about its approval and usage in China.

Nimustine is one of nitrosoureas used in the treatment of cancer. Nimustine alkylates and crosslinks DNA, thereby causing DNA fragmentation, inhibition of protein synthesis, and cell death. It is used in the treatment of brain tumor (in particular, high-grade gliomas), gastrointestinal cancers (stomach cancer, liver cancer, colorectal cancer), lung cancer, malignant lymphoma, chronic leukemia. Nimustine side effects are: leukopenia, thrombocytopenia, hypoproteinemia, anemia, Increased bleeding, proteinuria, interstitial pneumonia, anorexia, stomatitis, nausea, vomiting, general weakness, fever, headache, dizziness, seizures, alopecia, allergic reactions (rash).

Propentofylline is a selective inhibitor of adenosine transport and phosphodiesterase. For several years it has been well established in the geriatric therapy of the dog improving hemodynamics in cerebral and peripheral compartments. In human medicine clinical development of this pharmaceutical has already entered an advanced stage for the long-term therapy of patients with Alzheimer's disease and vascular dementia. In the brains of senile dogs and in human patients suffering from Alzheimer's disease comparable neuropathological findings can be made. In experimental models of vascular dementia and/or Alzheimer's disease it improves cognitive functions, inhibits inflammatory processes as well as excessive activation of microglia, formation of free radicals, cytocines and abnormal amyloid precursor proteins (APP). It stimulates synthesis and liberation of nerve growth factor (NGF) and reduces ischemic damage to the brain. In clinical studies in humans it improved cognitive functions as well as global functions and the ability to cope with tasks of routine daily life in patients suffering from Alzheimer's disease and vascular dementia. Possible mechanisms of action include a direct glial modulation to decrease a reactive phenotype, decrease glial production and release of damaging proinflammatory factors, and enhancement of astrocyte-mediated glutamate clearance. Net effects of propentofylline in vivo will be dependent on the concentrations of propentofylline and adenosine available and on the subtypes of adenosine receptors, phosphodiesterases, and nucleoside transporters present. In March, 2000 Aventis Pharma, announced that was discontinuing development of propentofylline as a possible treatment for Alzheimer's disease. The decision was a result of the company's portfolio review process which is intended to ensure that resources are devoted only to projects with a high potential for success.

Pirarubicin is a new kind of anthracene nucleus broad-spectrum antitumor antibiotic. This compound was rapidly incorporated into tumor cells, inhibiting DNA polymerase alpha, DNA topoisomerase II and subsequently DNA synthesis. Inhibition of RNA synthesis was also noted. It is indicated as an antineoplastic agent for the treatment of the following diseases: head and neck cancer, breast cancer, gastric cancer, urothelial cancer, ovarian cancer, uterine cancer, acute leukemia, malignant lymphoma. Among the side effects, cardiac toxicity, alopecia and disturbance of the digestive organs were mild.

Propoxur (Baygon) is a carbamate insecticide that has recently attracted considerable attention as a possible treatment option for addressing the bedbug epidemic. Propoxur is a non-systemic insecticide with a fast knockdown and long residual effect used against the turf, forestry, and household pests and fleas. The generally accepted mechanism of toxicity for propoxur involves the inhibition of cholinesterase. Propoxur is also used in pest control for other domestic animals, Anopheles mosquitoes, ants, gypsy moths, and other agricultural pests. It can also be used as a molluscicide. Several U.S. states have petitioned the Environmental Protection Agency (EPA) to use propoxur against bedbug infestations, but the EPA has been reluctant to approve indoor use because of its potential toxicity to children after chronic exposure.

Xibornol [6-(isoborn-2-yl)-3,4 xylenol] is a highly lipophilic and poorly soluble drug used as spray mouthwash for the local treatment of infection and inflammation of the throat and in the dental care, due to both its bacteriostatic activity, mainly against Gram positive micro-organisms and its antiviral properties. The drug concentration required for the therapeutic activity is 3% (w/v). Its poor water solubility makes difficult to set up drug formulations based on aqueous solvents, so xibornol is at present commercially available only as spray aqueous suspension. The self-microemulsifying approach was found to be effective to formulate stable and pharmaceutically acceptable liquid spray formulations of xibornol. The minimal inhibitory concentrations (MIC) and the minimal bactericidal concentrations (MBC) of xibornol against 100 strains of Staphylococcus aureus, clinically isolated have been evaluated in range between 2 ug/ml and 8 ug/ml. In the patients treated with xibornol (500 mg every 8 h for 7 days) any modification in phagocytosis frequency (PMF), phagocytosis index (PHI), nitroblue tetrazolium (NBT), reduction frequency (NRF), microbicidal activity and neutrophil mobility of PML, before, during and after the end of therapy wasn’t found.

WT-161 is a potent inhibitor of histone deacetylase (HDAC). It inhibits HDAC6, HDAC1, and HDAC2 with IC50 values of 0.4 nM, 8.35 nM, and 15.4 nM. The compound has demonstrated anti-tumor activity in preclinical models of multiple myeloma and breast cancer.

Pinaverium, known under the brand name DICETEL, is a spasmolytic agent used for functional gastrointestinal disorders. It is a quaternary ammonium compound that acts as an atypical calcium antagonist to restore normal bowel function. It is shown to relieve GI spasm and pain, transit disturbances and other symptoms related to motility disorders and may be considered as effective first-lline therapy for patients with irritable bowel syndrome (IBS). Pinaverium is also used to help relieve symptoms caused by certain disorders of the gallbladder associated with secretion of bile. Pinaverium bromide is the common ingredient in formulations, mostly as oral tablets. Although it is not a currently approved drug by the FDA, pinaverium is available in over 60 countries including Canada. DICETEL® (pinaverium bromide) is a calcium antagonist which inhibits the calcium influx by blocking the voltage-dependent calcium channel at the smooth muscle cell level. It possesses a high degree of selectivity for the intestinal smooth muscle.

Acetyldigoxin, a cardiac glycoside that has been studied in patients with congestive heart failure.

Monepantel (trade name Zolvix) is a new oral anthelmintic drug from a group of amino-acetonitrile derivatives with broad-spectrum activity against gastrointestinal nematodes of sheep, including adults and L4 larvae of the most important species. Monepantel have a novel mode of action involving a unique, nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunit ACR-23. Monepantel acts as a positive allosteric modulator of this receptor subunit, which is forced to open on stimulus but cannot close again, resulting in a constant uncontrolled flux of ions and finally in a depolarization of muscle cells leading to paralysis, spasmodic contractions of the anterior portion of the pharynx and ultimately death of adult nematodes. Monepantel-exposed C. elegans also exhibited molting defects and large vacuoles, characteristic for necrosis, are developed. Some nematode species lack ACR-23/MPTL-1 and predicted them to be Monepantel insensitive. Caenorhabditis nematodes equipped with ACR-23/MPTL-1 receptor subunits were found susceptible to Monepantel, whereas Pristionchus pacificus, closely related to these worms but lacking an ACR-23/MPTL-1 homolog, was tolerant. Monepantel shows an excellent tolerability in mammals and it is also active against multidrug-resistant parasites, indicating that its molecular target is absent or inaccessible in the host and is different from those of the classic anthelmintics. Safety pharmacological studies in rats indicate that MOP does not exert negative effects at a dose of 2000 mg/kg. Unfortunately, recent studies from New Zealand and Australia have reported that the efficacy of this new anthelmintic has declined markedly. Lack of efficacy of MOP was confirmed in the slaughtered sheep in which burdens of T. circumcincta and T. colubriformis showed no significant reductions. Whilst these two parasites now appear solidly resistant, the status of O. venulosum remains less clear.