Nemonoxacin is a non-fluorinated quinolone antibiotic in clinical development in an oral and intravenous formulation. It exhibits potent antibacterial activities against Gram-positive, Gram-negative, and atypical pathogens, especially methicillin-resistant Staphylococcus aureus. The molecule inhibits bacterial DNA synthesis by forming a ternary complex with a DNA molecule and gyrase and topoisomerase IV enzymes, thus blocking bacterial DNA supercoiling. Nemonoxacin is developed by TaiGen Biotechnology Company and has reached worldwide approval in 2014 and is marketed under the name Taigexyn®.

Cetiedil is effective potassium channel blocker used as a peripheral vasodilator to treat patients with painful crises in sickle cell anemia and pain in the extremities caused by an arterial disease. Known pharmacological properties of the drug include vascular smooth muscle relaxation, inhibition of phosphodiesterase with the consequent increase in circulating cyclic AMP concentration, blockade of the effect of bradykinin and serotonin, analgesia, inhibition of platelet aggregation and the decrease of plasma and blood viscosity and plasma fibrinogen level. The antisickling effect of cetiedil is explained mainly in the light of the changes it induces in the activities of membrane-bound ATPases and the permeability properties of the erythrocyte membrane to cations and anions.

Hematoporphyrin (Photodyn), a porphyrin prepared from hemin, is used as a photosensitizer in photodynamic therapy. Photodynamic therapy is based on the use of light-sensitive photosensitizers. Photoactivation causes the formation of singlet oxygen, which produces peroxidative reactions that can cause cell damage and death. Hematoporphyrin was used as the therapeutic agent in patients with manic-depressive reactions and in patients with involutional melancholia. One of the last studies has shown, that Hematoporphyrin-Photodynamic therapy (PDT) combined with stent placement is an effective and safe treatment for extrahepatic cholangiocarcinoma (EHCC).

Mitiglinide is a drug for the treatment of type 2 diabetes currently marked under tradename Glufast. Glufast® is available as the tablet for oral use, containing 5 mg or 10 mg of Mitiglinide calcium hydrate. The recommended dose is 10 mg three times daily just before each meal (within 5 minutes). Mitiglinide was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 29, 2004, and is currently co-marketed in Japan by Kissei and Takeda. Mitiglinide is a rapid-acting insulin secretion-stimulating agent, its belongs to the meglitinide (glinide) class of blood glucose-lowering drugs. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells.

Mazaticol is an anti-acetylcholine agent used in Japan for the treatment of Parkinson's syndrome.

Sulfobromophthalein (BSP) is a dye with a high affinity for organic anion transporting polypeptides (OATPs) and has been used as a substrate for multidrug resistance associated protein 2 (Mrp2). BSP is transported into hepatocytes by OATPs and, after conjugation to glutathione, is excreted into bile by Mrp2.3 It was found to inhibit the aldo-keto reductase ARK1C20. Sulfobromophthalein (BSP) is used in diagnosis of hepatic disorders.It is also used for the quantitative determination of proteins.

Orazamide, which is composed of one molecule of 5-aminoimidazole-4-carboxamide (AICA), one molecule of orotic acid and two molecules of water, is used clinically for the treatment of hepatitis and cirrhosis The nucleoside of AICA (AICAR) is internalized and becomes phosphorylated by adenosine kinase to form AICAR mono-phosphate (AICA ribotide, ZMP), an intermediate in the late steps of de novo purine biosynthesis. In hepatocytes, AICA can inhibit the fatty acid synthesis, sterol synthesis, and gluconeogenesis.

Ozagrel is a thromboxane A2 synthesis inhibitor used for the treatment of cerebral vasospasm and asthma due to its antiplatelet and anti-inflammation properties.

Incadronate (Disodium Cycloheptylaminomethylene diphosphate) is used to treat malignancy-associated hypercalcemia (MAH) in Japan. Experiments on rodents have revealed that this drug could be an effective agent for the treatment of various arthritic conditions, including human rheumatoid arthritis. In addition was shown, that incadronate induced growth inhibition and apoptotic death of pancreatic cancer cells. Incadronate also inhibited migration presumably by preventing the activation of Rho by lysophosphatidic acid. Thus, this drug can be of value in regimens for the treatment of pancreatic cancer.

Hippuric Acid is an acyl glycine produced by the conjugation of benzoic acid and glycine, found as a normal component in urine as a metabolite of aromatic compounds from food. Increased urine hippuric acid content may have antibacterial effects. Hippuric Acid is used therapeutically in the form of its salts (hippurates of calcium and ammonium). It is an ingredient of FDA-approved drug Hiprex (methenamine hippurate tablets USP). Each yellow capsule-shaped tablet of Hiprex contains 1 g Methenamine Hippurate which is the Hippuric Acid Salt of Methenamine (hexamethylene tetramine). The tablet also contains inactive ingredients. Hiprex (methenamine hippurate tablets USP) has antibacterial activity because the methenamine component is hydrolyzed to formaldehyde in acid urine. Hippuric acid has some antibacterial activity and also acts to keep the urine acid. The drug is generally active against E. coli, enterococci and staphylococci. Enterobacter aerogenes is generally resistant. The urine must be kept sufficiently acid for urea-splitting organisms such as Proteus and Pseudomonas to be inhibited. Hiprex is indicated for prophylactic or suppressive treatment of frequently recurring urinary tract infections when long-term therapy is considered necessary.