Pretomanid (PA-824) is an experimental anti-tuberculosis drug. Pretomanid is a bicyclic nitroimidazole-like molecule with a very complex mechanism of action. It is active against both replicating and hypoxic, non-replicating Mycobacterium tuberculosis. As a potential TB therapy, it has many attractive characteristics - most notably its novel mechanism of action, its activity in vitro against all tested drug-resistant clinical isolates, and its activity as both a potent bactericidal and a sterilizing agent in mice. In addition, the compound shows no evidence of mutagenicity in a standard battery of genotoxicity studies, no significant cytochrome P450 interactions, and no significant activity against a broad range of Gram-positive and Gram-negative bacteria. This compound has been developed by TB Alliance and is a potential cornerstone of future TB and drug-resistant TB treatment regimens. It is currently undergoing Phase III clinical trials.

PRIFTIN® (rifapentine) is indicated in adults and children 12 years and older for the treatment of active pulmonary tuberculosis (TB) caused by Mycobacterium tuberculosis. PRIFTIN must always be used in combination with one or more antituberculosis (anti-TB) drugs to which the isolate is susceptible. Rifapentine is an antibiotic that inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. And it acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death. It is bactericidal and has a very broad spectrum of activity against most gram-positive and gram-negative organisms (including Pseudomonas aeruginosa) and specifically Mycobacterium tuberculosis. Because of rapid emergence of resistant bacteria, use is restricted to treatment of mycobacterial infections and a few other indications. Rifampin is well absorbed when taken orally and is distributed widely in body tissues and fluids, including the CSF. It is metabolized in the liver and eliminated in bile and, to a much lesser extent, in urine, but dose adjustments are unnecessary with renal insufficiency. Rifapentine has shown higher bacteriostatic and bactericidal activities especially against intracellular bacteria growing in human monocyte-derived macrophages.

ETHAMBUTOL HYDROCHLORIDE is an oral chemotherapeutic agent which is specifically effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Ethambutol inhibits RNA synthesis and decreases tubercle bacilli replication. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of MAC are sensitive to ethambutol. Ethambutol inhibits arabinosyl transferases which is involved in cell wall biosynthesis. By inhibiting this enzyme, the bacterial cell wall complex production is inhibited. This leads to an increase in cell wall permeability. ETHAMBUTOL HCl is indicated for the treatment of pulmonary tuberculosis. It should not be used as the sole antituberculous drug, but should be used in conjunction with at least one other antituberculous drug.

Idramantone (Kemantane) is a biologically active compound first synthesized and pharmacologically studied at the V. V. Zakusov Science Research Institute of Pharmacology, Russian Academy of Medical Sciences. Idramantone has immunostimulatory properties, which are particularly effective in the treatment of autoimmune diseases of the vascular system of the limbs, chronic bronchitis, bronchial asthma, aphthous stomatitis, herpes, and others. Idramantone also has an antiparkinsonism action. The compound has antiamnestic properties, which experimental data indicate are comparable in strength to those of memantine. Idramantone has cerebrovascular properties, increasing the blood supply in the ischemic brain. In addition, Idramantone and its derivatives are used in the electronics industry.

Cyacetacide is a biochemical used in the past as an anti-tuberculosis agent and currently used in Russia to for the treatment of various forms of tubercular lesions of the eye: keratitis, scleritis, uveitis, chorioretinitis, tuberculosis-allergic diseases and eye diseases of non-tubercular origin. Cyacetacide has also been used to derive compounds that may have antitumor properties.

Dihydroisocodeine is an opioid derivative. Dihydroisocodeine is much less toxic for rabbits than codeine, and in these and other animals its convulsant action is less marked. The minimum analgesic dose for cats is considerably less than for codeine. In the 1930s it was clinically investigated for cough relief, where it has no demonstrable clinical superiority over standard codeine in the usual therapeutic dosage.

Sulfoxone is a water-soluble sulfone and is a competitive inhibitor of the bacterial enzyme dihydropteroate synthetase. Sulfoxone under the brand name Diasone was used as an antileprosy drug, for treatment of dermatitis herpetiformis, and to treat pulmonary tuberculosis. Presently, usage of diasone has been discontinued.

CAPRYLYL GLUCOSIDE is a mild and non-denaturing detergent for the solubilization and reconsititution of membrane bound proteins. Treatment with 1.2% N-octylglucoside for 5 min completely inhibited HIV-1 infectivity. CAPRYLYL GLUCOSIDE being nontoxic and inexpensive agent in inhibiting Staphylococcus epidermidis and Pseudomonas aeruginosa adhesion to conventional and silicone-hydrogel contact lenses. CAPRYLYL GLUCOSIDE was tested for the treatment of pulmonary tuberculosis. It was shown, that surfactant is proficient in removing Mycobacterium tuberculosis shield. Thus, it may also enhance the effectiveness of antibiotics and the immune system's response in the treatment of pulmonary tuberculosis.

Fudosteine is a derivative of cysteine developed and approved in Japan for the treatment of such diseases as bronchial asthma, chronic bronchitis, pulmonary emphysema, bronchiectasis, pulmonary tuberculosis, pneumoconiosis, atypical mycobacterial disease and diffuse panbronchiolitis. Fudosteine acts as a mucoactive agent, enabling mucin secretion. Although exact mechanism of action is unknown, it is supposed that fudosteine inhibits MUC5AC expression.

Methaniazide (metaniazide) is the methanesulfonate derivative of isoniazid with antibacterial properties. It is used used primarily as a tuberculostatic. It remains the treatment of choice for tuberculosis.