Bedaquiline

Bedaquiline is a diarylquinoline antimycobacterial drug [see Microbiology (12.4) ] .

• SIRTURO is a diarylquinoline antimycobacterial drug indicated as part of combination therapy in the treatment of adult and pediatric patients (2 years and older and weighing at least 8 kg) with pulmonary tuberculosis (TB) due to Mycobacterium tuberculosis resistant to at least rifampin and isoniazid. SIRTURO is a diarylquinoline antimycobacterial drug indicated as part of combination therapy in adult and pediatric patients (2 years and older and weighing at least 8 kg) with pulmonary tuberculosis (TB) due to Mycobacterium tuberculosis resistant to at least rifampin and isoniazid.ICD-10: A15.9

• None. None.contraindicated

Administer SIRTURO by directly observed therapy (DOT). ( 2.1 ) Emphasize need for compliance with full course of therapy. ( 2.1 ) Prior to administration, obtain ECG, liver enzymes and electrolytes. Obtain susceptibility information for the background regimen against Mycobacterium tuberculosis isolate if possible. ( 2.2 ) Only use SIRTURO in combination with at least 3 other drugs to which the patient's TB isolate has been shown to be susceptible in vitro. If in vitro testing results are unavailable, may initiate SIRTURO in combination with at least 4 other drugs to which patient's TB isolate is likely to be susceptible. ( 2.1 ) Recommended dosage in adult patients: 400 mg (4 of the 100 mg tablets OR 20 of the 20 mg tablets) once daily for 2 weeks followed by 200 mg (2 of the 100 mg tablets OR 10 of the 20 mg tablets) 3 times per week (with at least 48 hours between doses) for 22 weeks. ( 2.3 ) Recommended dosage in pediatric patients (2 years and older and weighing at least 8 kg) is based on body weight. ( 2.4 ) Take SIRTURO tablets with food. ( 2.6 ) See full prescribing information for the different methods of administration of SIRTURO 20 mg tablet and administration of the 100 mg tablet. 2.1 Important Administration Instructions Administer SIRTURO by directly observed therapy (DOT). Only use SIRTURO in combination with at least three other drugs to which the patient's TB isolate has been shown to be susceptible in vitro.

A mortality imbalance was seen in clinical trials in SIRTURO-treated patients with pulmonary TB due to Mycobacterium tuberculosis resistant to at least rifampin. ( 5.2 ) Hepatotoxicity may occur with use of SIRTURO. Monitor liver-related laboratory tests. Discontinue SIRTURO if evidence of liver injury occurs. ( 5.4 ) 5.1 QTc Prolongation SIRTURO prolongs the QTc interval [see Clinical Pharmacology (12.2) ] . Use with drugs that prolong the QTc interval may cause additive QTc prolongation [see Adverse Reactions (6) ] . In Study 4, where SIRTURO was administered with the QTc prolonging drugs clofazimine and levofloxacin, 5% of patients in the 40-week SIRTURO treatment group experienced a QTc ≥500 ms and 43% of patients experienced an increase in QTc ≥60 ms over baseline. Of the clofazimine- and levofloxacin-treated patients in the 40-week control arm, 7% of patients experienced a QTc ≥500 ms and 39% experienced an increase in QTc ≥60 ms over baseline. Obtain an ECG before initiation of treatment, 2 weeks after initiation, during treatment, as clinically indicated and at the expected time of maximum increase in the QTc interval of the concomitantly administered QTc prolonging drugs (as applicable). Obtain electrolytes at baseline and during treatment and correct electrolytes as clinically indicated.

The following serious adverse reactions are discussed elsewhere in the labeling: QTc Prolongation [see Warnings and Precautions (5.1) and Clinical Pharmacology (12.2) ] Mortality Imbalance in Clinical Trials [see Warnings and Precautions (5.2) ] Hepatotoxicity [see Warnings and Precautions (5.4) ] Drug Interactions [see Warnings and Precautions (5.5) ] The most common adverse reactions reported in 10% or more adult patients treated with SIRTURO in Study 1 were nausea, arthralgia, headache, hemoptysis and chest pain. ( 6.1 ) The most common adverse reactions reported in 10% or more adult patients treated with SIRTURO (40-week arm) in Study 4 were QTc prolongation, nausea, vomiting, arthralgia, transaminases increased, abdominal pain, pruritus, dizziness, headache, chest pain, rash, insomnia, dry skin, and palpitations. ( 6.1 ) The most common adverse reactions reported in 10% or more of pediatric patients (12 years to less than 18 years of age) treated with SIRTURO were arthralgia, nausea and abdominal pain. ( 6.1 ) The most common adverse reaction reported in 10% or more of pediatric patients (5 years to less than 12 years of age) treated with SIRTURO was elevation in liver enzymes. ( 6.1 ) The most common adverse reaction reported in 10% or more of pediatric patients (2 years to less than 5 years of age) treated with SIRTURO was vomiting. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Janssen Therapeutics, Division of Janssen Products, LP at 1-800-JANSSEN (1-800-526-7736) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

Lactation: Breastfeeding is not recommended unless infant formula is not available. If an infant is exposed to bedaquiline through breast milk, monitor for signs of bedaquiline-related adverse reactions, such as hepatotoxicity. ( 6 , 8.2 ) Pediatrics: The safety and effectiveness of SIRTURO in pediatric patients less than 2 years of age and/or weighing less than 8 kg have not been established. ( 8.4 ) Use with caution in patients with severe hepatic impairment and only when the benefits outweigh the risks. Monitor for SIRTURO-related adverse reactions. ( 8.6 ) Use with caution in patients with severe renal impairment. ( 8.7 ) 8.1 Pregnancy Risk Summary Available data from published literature of SIRTURO use in pregnant women are insufficient to evaluate a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. There are risks associated with active TB during pregnancy (see Clinical Considerations ) . Reproduction studies performed in rats and rabbits have revealed no evidence of harm to the fetus due to oral administration of bedaquiline to pregnant rats and rabbits during organogenesis at exposures up to 6 times the clinical dose based on AUC comparisons (see Data ) . The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown.

Metabolism

Pharmacokinetics (PK) parameters The pharmacokinetic properties of bedaquiline are summarized in Table 5 as mean (SD) in adult patients. Table 5: Model-Derived Pharmacokinetic Parameters of Bedaquiline and M2 (mean [SD]) after Multiple Doses of SIRTURO at the Recommended Dosing Regimen Pharmacokinetic Parameters Bedaquiline SD=Standard Deviation Absorption Food effect High fat meal (22 grams of fat, 558 total Kcal) increased C max and AUC by 2-fold.

There is no experience with the treatment of acute overdose with SIRTURO. Take general measures to support basic vital functions including monitoring of vital signs and ECG (QTc interval) in case of deliberate or accidental overdose. It is advisable to contact a poison control center to obtain the latest recommendations for the management of an overdose. Since bedaquiline is highly protein-bound, dialysis is not likely to significantly remove bedaquiline from plasma.

• Dec 28, 2012NDANDA204384Janssen Therap

1. 1Electrocardiogram Qt Prolonged22016%
2. 2Off Label Use17012%
3. 3Hepatotoxicity14911%
4. 4Anaemia14510%
5. 5Neuropathy Peripheral966.9%
6. 6Nausea926.6%
7. 7Death735.2%
8. 8Intentional Product Use Issue725.2%
9. 9Vomiting705.0%
10. 10Dyspnoea463.3%
11. 11Dizziness433.1%
12. 12Decreased Appetite423.0%
13. 13Hypokalaemia402.9%
14. 14Headache342.4%
15. 15Asthenia332.4%

The 10 most recently updated of 100 ClinicalTrials.gov registrations naming Bedaquiline as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Pharmacokinetic Study to Evaluate Anti-mycobacterial Activity of TMC207 in Combination With Background Regimen (BR) of Multidrug Resistant Tuberculosis (MDR-TB) Medications for Treatment of Children/Adolescents With Pulmonary MDR-TB
  Recruiting · Phase 2 · Interventional · 60 enrolled · Janssen Research & Development, LLC
  NCT02354014updated 2026-06-05
• Bedaquiline Roll-out Evidence in Contacts and People Living With HIV to Prevent TB
  Recruiting · Phase 2 · Phase 3 · Interventional · 2,530 enrolled · Johns Hopkins University
  NCT06568484updated 2026-06-03
• Bacteriophage Therapy for Mycobacterium Abscessus Pulmonary Infection
  Enrolling by invitation · Phase 1 · Interventional · 1 enrolled · Vancouver Coastal Health
  NCT07228702updated 2026-06-03
• Bactericidal Activity of TBD09 in Combination With Other Drugs in Pulmonary Tuberculosis
  Recruiting · Phase 2 · Interventional · 150 enrolled · Gates Medical Research Institute
  NCT07525427updated 2026-06-03
• Safety and Efficacy Evaluation of 4-month Regimen of OPC-167832, Delamanid and Bedaquiline in Participants With Drug-Susceptible Pulmonary TB
  Completed · Phase 2 · Interventional · 122 enrolled · Otsuka Pharmaceutical Development & Commercialization, Inc.
  NCT05221502updated 2026-05-26
• Bactericidal Activity and Safety of Nicotinamide in Combination With Bedaquiline, Pretomanid, and Linezolid in Drug-susceptible Pulmonary Tuberculosis
  Recruiting · Phase 2 · Interventional · 165 enrolled · Gates Medical Research Institute
  NCT07517445updated 2026-05-22
• Efficacy and Safety Evaluation of Two to Four Months of Treatment With the Combination Regimens of DBOS and PBOS in Adults With Pulmonary Tuberculosis
  Terminated · Phase 2 · Interventional · 93 enrolled · Gates Medical Research Institute
  NCT05971602updated 2026-05-20
• Bedaquiline Enhanced Post ExpOsure Prophylaxis for Leprosy
  Recruiting · Phase 3 · Interventional · 124,000 enrolled · Institute of Tropical Medicine, Belgium
  NCT05597280updated 2026-05-19
• Trial of Novel Regimens for the Treatment of Pulmonary Tuberculosis
  Recruiting · Phase 2 · Interventional · 315 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT06192160updated 2026-05-19
• Finding the Optimal Regimen for Mycobacterium Abscessus Treatment
  Recruiting · Phase 2 · Phase 3 · Interventional · 300 enrolled · The University of Queensland
  NCT04310930updated 2026-05-11

Frequently asked questions

How does Bedaquiline work?

Bedaquiline is a diarylquinoline antimycobacterial drug [see Microbiology (12.4) ] .

What is Bedaquiline used for?

According to FDA labeling, Bedaquiline carries indications including: SIRTURO is a diarylquinoline antimycobacterial drug indicated as part of combination therapy in the treatment of adult and pediatric patients (2 years and older and weighing at least 8 kg) with pulmonary tuberculosis (TB) due to Mycobacterium tuberculosis resistant to at least rifampin and isoniazid. SIRTURO is a diarylquinoline antimycobacterial drug indicated as part of combination therapy in adult and pediatric patients (2 years and older and weighing at least 8 kg) with pulmonary tuberculosis (TB) due to Mycobacterium tuberculosis resistant to at least rifampin and isoniazid.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bedaquiline?

Bedaquiline is classified as Other drugs for treatment of tuberculosis, Diarylquinoline Antimycobacterial, Enzyme Inhibitors.

What are the brand names for Bedaquiline?

Bedaquiline is marketed under brand names including Sirturo.

What are the contraindications for Bedaquiline?

Bedaquiline labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.