11/11/2019 Tuberculosis Drugs and Mechanisms of Action | NIH: National Institute of Allergy and Infectious Diseases

 (/) 

Diseases & Conditions (/diseases-conditions)      Tuberculosis (/diseases-conditions/tuberculosis)

Tuberculosis Drugs and Mechanisms of

Action
First-Line Treatment of TB for Drug-Sensitive TB

Shown here are the four drugs in the standard regimen of rst-line drugs. Also shown are the dates these four drugs were discovered—all more than 40
years ago.
Credit: NIAID

Tuberculosis, which results from an infection with Mycobacterium tuberculosis, can be cured with a combination of rst-line
drugs taken daily for several months. 

Multidrug-Resistant Tuberculosis (MDR TB) and Second-Line

Treatments

https://www.niaid.nih.gov/diseases-conditions/tbdrugs 1/4
11/11/2019 Tuberculosis Drugs and Mechanisms of Action | NIH: National Institute of Allergy and Infectious Diseases

MDR TB occurs when a Mycobacterium tuberculosis strain is resistant to isoniazid and rifampin, two of the most powerful rst-line drugs. To cure MDR
TB, healthcare providers must turn to a combination of second-line drugs, several of which are shown here. Second-line drugs may have more side
effects, the treatment may last much longer, and the cost may be up to 100 times more than rst-line therapy. MDR TB strains can also grow resistant to
second-line drugs, further complicating treatment.
Credit: NIAID

Extensively Drug-Resistant Tuberculosis (XDR TB) - Options

for Treatment

Bedaquiline and Delamanid are new drugs. Ethambutol, Pyrazinamide, Thioamides, Cycloserine, Para-aminosalicylic acid, Streptomycin, and Clofazimine
are possibly effective. Kanamycin, Capreomycin and Amikacin are injectable second-line.
Credit: NIAID

XDR TB occurs when a Mycobacterium tuberculosis strain is resistant to isoniazid and rifampin, two of the most powerful
rst-line drugs, as well as key drugs of the second line regimen—any uoroquinolone and at least one of the three injectable
drugs shown above. XDR TB strains may also be resistant to additional drugs, greatly complicating therapy.

New Candidate TB Drugs Under Development

https://www.niaid.nih.gov/diseases-conditions/tbdrugs 2/4
11/11/2019 Tuberculosis Drugs and Mechanisms of Action | NIH: National Institute of Allergy and Infectious Diseases

Several new types of TB drugs currently under development are shown here. NIAID has supported the development of ve of these compounds, SQ-109,
PA-824 (Pretomanid), Sutezolid, Linezolid, and Meropenem, which are denoted by asterisks (*) above.
Credit: NIAID

Mechanisms of Action of Current TB Drugs

Thioamides, Nitroimidazoles, Ethambutol, and Cycloserine act on cell wall synthesis. Diarylquinoline inhibits ATP synthase. PAS, Fluoroquinolones, Cyclic
Peptides and Aminoglycosides act on the DNA.
Credit: NIAID

Tuberculosis drugs target various aspects of Mycobacterium tuberculosis biology, including inhibition of cell wall synthesis,
protein synthesis, or nucleic acid synthesis. For some drugs, the mechanisms of action have not been fully identi ed.

Mechanisms of Action of TB Drugs Under Development

https://www.niaid.nih.gov/diseases-conditions/tbdrugs 3/4
11/11/2019 Tuberculosis Drugs and Mechanisms of Action | NIH: National Institute of Allergy and Infectious Diseases

Nitroimidazoles, SQ-109,, Meropenem, and Benzothiazinones act on cell wall synthesis. Imidazopyridine Amide inhibits ATP synthesis. Rifamycins,
Oxazolidinones and Macrolides act on DNA.
Credit: NIAID

Tuberculosis drugs target various aspects of Mycobacterium tuberculosis biology, including inhibition of cell wall synthesis,
protein synthesis, or nucleic acid synthesis. For some drugs, the mechanisms of action have not been fully identi ed.

About the Illustrations

The photo of Mycobacterium tuberculosis is from the Centers for Disease Control and Prevention (http://wayback.archive-

it.org/7761/20160909192435/http://phil.cdc.gov/phil/home.asp) , CDC/Dr. Ray Butler, Janice Carr. This illustration is in the
public domain. Please credit the National Institute of Allergy and Infectious Diseases (NIAID).

Additional TB Information
Working Group on New TB Drugs (http://wayback.archive-

it.org/7761/20160909192435/http://www.newtbdrugs.org/pipeline.php)
Handbook of Anti-Tuberculosis Agents (http://wayback.archive-

it.org/7761/20160909192435/http://www.tballiance.org/newscenter/research_papers/TB_DB_Final.pdf) pdf  (PDF)
2008
TB Alliance (http://wayback.archive-it.org/7761/20160909192435/http://www.tballiance.org/)


Content last reviewed on April 19, 2016

https://www.niaid.nih.gov/diseases-conditions/tbdrugs 4/4