R207910
Encyclopedia
R207910 is an experimental diarylquinoline anti-tuberculosis
drug, which was discovered by Koen Andries
and his team at Janssen Pharmaceutica
. It was described for the first time in 2004 at the Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC
) meeting Late-Breaker Session, after the drug had been in development for over 7 years, and a trial of 47 patients showed that it is effective in the treatment of M. tuberculosis.
TMC207 has been successfully applied in a phase II efficacy study and is marketed by Tibotec
and the TB alliance
.
for ATP synthase
, which is unlike the quinolone
s, whose target is DNA gyrase
.
Tuberculosis
Tuberculosis, MTB, or TB is a common, and in many cases lethal, infectious disease caused by various strains of mycobacteria, usually Mycobacterium tuberculosis. Tuberculosis usually attacks the lungs but can also affect other parts of the body...
drug, which was discovered by Koen Andries
Koen Andries
Koen Andries is a Belgian scientist working at Janssen Pharmaceutica and professor at the University of Antwerp. In 2005 he and his team published a discovery about a new di-Aryl-Quinoline-based drug which promises a shorter and simpler treatment for Tuberculosis .-Career:He graduated as a...
and his team at Janssen Pharmaceutica
Janssen Pharmaceutica
Janssen Pharmaceutica is pharmaceutical company, established in Belgium in 1953 by Paul Janssen. Its headquarters are located in Beerse, in the Campine region of the province of Antwerp, Belgium. It was created not as a subsidiary of a chemical factory but solely with the aim of conducting...
. It was described for the first time in 2004 at the Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC
American Society for Microbiology
The American Society for Microbiology is a professional organization for scientists who study viruses, bacteria, fungi, algae, and protozoa as well as other aspects of microbiology. Microbiology is the study of organisms too small to be seen with the naked eye and which must be viewed with a...
) meeting Late-Breaker Session, after the drug had been in development for over 7 years, and a trial of 47 patients showed that it is effective in the treatment of M. tuberculosis.
TMC207 has been successfully applied in a phase II efficacy study and is marketed by Tibotec
Tibotec
Tibotec is a pharmaceutical company with a focus on research and development for the treatment of infectious diseases such as HIV , and Hepatitis C...
and the TB alliance
TB Alliance
The Global Alliance for TB Drug Development is a non-profit organization dedicated to the discovery and development of new, faster-acting and affordable tuberculosis medicines....
.
Mode of action
R207910 affects the proton pumpProton pump
A proton pump is an integral membrane protein that is capable of moving protons across a cell membrane, mitochondrion, or other organelle. Mechanisms are based on conformational changes of the protein structure or on the Q cycle.-Function:...
for ATP synthase
ATP synthase
right|thumb|300px|Molecular model of ATP synthase by X-ray diffraction methodATP synthase is an important enzyme that provides energy for the cell to use through the synthesis of adenosine triphosphate . ATP is the most commonly used "energy currency" of cells from most organisms...
, which is unlike the quinolone
Quinolone
The quinolones are a family of synthetic broad-spectrum antibiotics. The term quinolone refers to potent synthetic chemotherapeutic antibacterials....
s, whose target is DNA gyrase
DNA gyrase
DNA gyrase, often referred to simply as gyrase, is an enzyme that relieves strain while double-stranded DNA is being unwound by helicase. This causes negative supercoiling of the DNA...
.