PR-69 (Doranidazole) is a hypoxic radiosensitizer, and is a derivative of 2-nitroimidazole intended to reduce neurotoxicity due to its blood brain barrier (BBB) impermeability. Several studies have shown that doranidazole has a radiosensitizing effect under hypoxia, both in vitro and in vivo. Based on these studies, a phase III trial of doranidazole against advanced pancreatic cancer was performed; it was demonstrated that treatment with doranidazole following radiation significantly improved the tumor mass reduction rate and extended patient survival. Various results have suggested that doranidazole has promising potential for hypoxia-targeting chemoradiotherapy.

Kainic acid (kainate) is a natural marine acid present in some seaweed. Kainic acid is a potent neuroexcitatory amino acid that acts by activating receptors for glutamate, the principal excitatory neurotransmitter in the central nervous system. Kainic acid is commonly injected into laboratory animal models to study the effects of experimental ablation. Kainic acid is a direct agonist of the glutamic kainate receptors and large doses of concentrated solutions produce immediate neuronal death by overstimulating neurons to death. Such damage and death of neurons is referred to as an excitotoxic lesion. Thus, in large, concentrated doses kainic acid can be considered a neurotoxin, and in small doses of dilute solution kainic acid will chemically stimulate neurons. Kainic acid is utilised in primary neuronal cell cultures and acute brain slice preparations [5] to study of the physiological effect of excitotoxicity and assess the neuroprotective capabilities of potential therapeutics. Kainic acid is a potent central nervous system excitant that is used in epilepsy research to induce seizures in experimental animals, at a typical dose of 10–30 mg/kg in mice. In addition to inducing seizures, kainic acid is excitotoxic and epileptogenic. Kainic acid induces seizures via activation of kainate receptors containing the GluK2 subunit and also through activation of AMPA receptors, for which it serves as a partial agonist.

Quinafimide is an investigational compound that has been used in trials for the treatment of Amoebiasis and Helminthiasis. This phase 4 trial combined Quinfamide with the approved compound Mebendazole. The details of the mechanism of action are not known, but the overall effect is intraluminal immobilization of the Entamoeba.

Piperaquine is a bisquinoline antimalarial drug that was first synthesized in the 1960s and used extensively in China and Indochina as prophylaxis and treatment during the next 20 years. Usage declined in the 1980s as piperaquine-resistant strains of P. falciparum arose and artemisinin-based antimalarials became available. However, during the next decade, piperaquine was rediscovered by Chinese scientists as one of a number of compounds suitable for combination with an artemisinin derivative. The rationale for such artemisinin combination therapies (ACTs) was to provide an inexpensive, short-course treatment regimen with a high cure rate and good tolerability that would reduce transmission and protect against the development of parasite resistance. Piperaquine is characterized by slow absorption and a long biological half-life, making it a good partner drug with artemisinin derivatives which are fast acting but have a short biological half-life.

Clefamide is an aromatic ether and antiprotozoal agent that was used to treat and chemoprophylaxis of amoebiasis in the 1960s

Eprinomectin is 4"-deoxy-4"-epiacetylamino-avermectin B1. It is a semi-synthetic member of the avermectin family of macrocyclic lactones and consists of a mixture of two homologous components, B1a (not less than 90%) and B1b (not more than 10%), which differ by a single methylene group at C26. Eprinomectin is a member of the macrocyclic lactone class of endectocides which have a unique mode of action. Compounds of the class bind selectively and with high affinity to glutamate-gated chloride ion channels which occur in invertebrate nerve and muscle cells. This leads to an increase in the permeability of the cell membrane to chloride ions with hyperpolarization of the nerve or muscle cell, resulting in paralysis and death of the parasite. Compounds of this class may also interact with other ligand-gated chloride channels, such as those gated by the neurotransmitter gamma-aminobutyric acid (GABA). Molecular studies indicate that these drugs interact strongly not only with ligand-gated ion channels, the mode-of action receptors of nematodes and arthropods, but also with efflux ABC transporters. The margin of safety for compounds of this class is attributable to the fact that mammals do not have glutamate-gated chloride channels, the macrocyclic lactones have a low affinity for other mammalian ligand-gated chloride channels and they do not readily cross the blood-brain barrier. IVOMEC EPRINEX (eprinomectin) Pour-On is indicated for the treatment and control of gastrointestinal roundworms (including inhibited Ostertagia ostertagi), lungworms, grubs, sucking and biting lice, chorioptic and sarcoptic mange mites, and horn flies in beef and dairy cattle of all ages, including lactating dairy cattle.

Arteflene is the sesquiterpene peroxide. It is a synthetic derivative of yingzhaosuwas. Arteflene found negative in a battery of mutagenicity tests. It had low acute toxicity after oral or subcutaneous administration in pre-clinical studies. Experimentally arteflene proved to be a highly effective antimalarial drug. An open, non-comparative clinical trial was carried out in Nigeria and Burkina Faso to investigate the safety and efficacy of the arteflene in patients with mild malaria. The lower than expected effect was thought to be due to inadequate storage of the arteflene suspension. There were no withdrawals due to adverse events and no deaths. Arteflene had no major effect on TNF, IL-alpha or IL-6 cytokine release from mononuclear cells stimulated with malaria antigens or lipopolysaccharide and it did not affect cell viability. Arteflene only slightly suppressed cytoadherence of infected erythrocytes to melanoma cells. The therapeutic effect of Arteflene appears to be confined to its parasite killing activity. Single dose monotherapy with arteflene was not effective in curing children suffering from uncomplicated P. falciparum malaria in Gabon. Arteflene is reported to be more cytotoxic to primary rat hepatocytes than some non-endoperoxide antimalarials.

Oxantel is a narrow-spectrum anthelmintic effective against whipworms in dogs and cats. It is ineffective against other roundworms, flukes, tapeworms or external parasites. Oxantel acts on the nervous system of the worms as inhibitors of acetylcholinesterase. Oxantel, a cholinergic anthelmintic and fumarate reductase inhibitor, significantly inhibited biofilm formation by P. gingivalis and disrupted established biofilms at concentrations below its MIC against planktonic cells. Oxantel was more effective against P. gingivalis in biofilm than metronidazole, a commonly used antibiotic for periodontitis. When oxantel was administrated to human beings for the treatment of trichuriasis, no drug reaction or side effects were reported, and the results of hematologic, biochemical and urinary examinations didn’t reveal any significant drug-related changes.

Oxyclozanide is a salicylanilide anthelmintic, used for the treatment and control of fascioliasis in cattle, sheep, and goats. The mechanism of action of oxyclozanide is the uncoupling of oxidative phosphorylation in flukes. It is formulated as an oral drench containing oxyclozanide only or in combination with levamisole hydrochloride or oxfendazole or as a powder to be incorporated in the feed. The recommended doses are 10 to 15 mg oxyclozanide/kg BW for cattle and 15 mg oxyclozanide/kg BW for sheep and goats. The application was amended to exclude sheep milk and goat tissues and milk.

Ipronidazole is an antiprotozoal drug of the nitroimidazole class used in veterinary medicine. Ipronidazole (2-isopropyl-1-methyl-5-nitroimidazole) is used for the treatment of histomoniasis in turkeys and in swine dysentery.