Exposing Novel Anti-Tuberculosis Drug Mechanism

The foundational basis of a novel class of anti-tuberculosis drug discovered paves the way for a new concept in the ongoing fight against TB.

Scientists from Hackensack Meridian Center for Discovery and Innovation working with collaborators from across the globe revealed the action of mechanism of a new anti-tuberculosis drug pathway that they helped develop.

The new study reported in the journal Proceedings of the National Academy of Sciences shows that the enzyme inhibitor triaza-coumarin, or TA-C, is metabolized by the Tuberculosis (TB) germs, making it effective in inhibiting the disease from within like in a "Trojan horse" attack.

Drug-Resistant Tuberculosis - Types, Causes, Symptoms, Diagnosis, Treatment and Prevention
Drug-resistant tuberculosis (TB) is a globally serious infectious disease caused by the bacterium Mycobacterium tuberculosis. It occurs as multidrug-resistant or MDR TB or in its more severe form, extensively drug-resistant or XDR TB.

‘New drugs are needed to fight against the drug-resistant strains of Tuberculosis.’

"The scientists at the CDI who specialize in tuberculosis and other mycobacteria are at the vanguard of their specialty," said David Perlin, PhD., the chief scientific officer and senior vice president of the CDI.

Bacterial metabolism can cause intrinsic drug resistance but it also converts inactive parent drugs to bioactive derivatives, as prodrugs.

These "prodrugs" are biologically inactive compounds which are broken down by the bacteria to create the effective by-product compounds within the bacterial cell.

New Blood Test can Predict Who are at High Risk for Tuberculosis
Novel blood test for tuberculosis (TB) diagnosis can also be used for identifying people who are at a highest risk of developing the disease. The test, called Actiphage, detects Mycobacterium tuberculosis in the blood.

This new Mycobacterium tuberculosis dihydrofolate reductase (DHFR) inhibitor drug discovered with moderate affinity for intra-bacterial metabolism of TA-C boosts its on-target activity by two orders of magnitude.

The TB germ takes up and metabolizes the TA-C - but the by-products inhibit its function from within. This is the first 'prodrug-like' antimycobacterial that possesses baseline activity in the absence of intracellular bio-activation.

Short Course Therapy Effective for Tuberculosis
New study concluded one month TB therapy as effective as 6-month standard regimen.

This promising direction of research about the novel class of DHFR inhibitors uncovers a new antibacterial drug discovery concept that can be crucial in the ongoing fight against TB.

Anti-Tuberculosis Medication Safe Even at High Dose
Higher dose of the anti-tuberculosis drug Rifampicin is safe and can also lead to a shorter treatment for tuberculosis and less resistance.

Source-Medindia