What is bedaquiline BDQ drug powder?: A Comprehensive Pharmacological Overview

October 8, 2025 •

5 min read

As the first new drug developed specifically for tuberculosis in over 40 years, bedaquiline represents a significant advancement in treating drug-resistant strains. While most patients are familiar with its oral tablet form, Sirturo, few understand its origin as bedaquiline BDQ drug powder—the critical active pharmaceutical ingredient (API) that must first be synthesized and purified before it can be formulated into a medicine. This review explores the nature of this essential raw material and its journey to becoming a potent clinical tool.

Quick Summary

Bedaquiline is a diarylquinoline antimycobacterial agent that inhibits ATP synthase in Mycobacterium tuberculosis and is reserved for multi-drug resistant tuberculosis treatment. The drug's active substance is a synthetic powder (API) that undergoes a complex formulation process, involving granulation and blending with excipients, to produce the final Sirturo tablets. Researchers also explore alternative powder formulations for improved delivery methods like inhalation.

Key Points

API for MDR-TB Drug: Bedaquiline BDQ drug powder is the active ingredient (API) of Sirturo, a medication used to treat multi-drug resistant tuberculosis (MDR-TB).
Unique Mechanism: It operates by inhibiting the ATP synthase enzyme in Mycobacterium tuberculosis, disrupting the bacteria's energy production and killing both active and dormant forms.
Complex Manufacturing: The powder is synthesized through a multi-step chemical process and purified to isolate the most active isomer.
Formulated into Tablets: The raw powder is combined with excipients and processed via methods like wet granulation to create the final oral tablets.
Risk of Resistance: Use of bedaquiline is reserved and must be part of a combination therapy to reduce the risk of resistance, which can develop through specific mutations.
Serious Side Effects: The drug has significant risks, including QT prolongation and liver issues, requiring careful monitoring during treatment.

What is Bedaquiline (BDQ) Drug Powder?

In pharmacology, a drug is defined by its active pharmaceutical ingredient (API), which is the substance responsible for its therapeutic effect. Bedaquiline BDQ drug powder is the API for the medication Sirturo, and it exists as a fine, synthetic, off-white powder. Chemically, it belongs to a novel class of compounds known as diarylquinolines. The standard formulation for use in medications is as bedaquiline fumarate, a salt form that enhances its physical and chemical stability.

Unlike the finished tablets, which contain additional inactive ingredients (excipients) to aid in absorption and stability, the raw BDQ powder is the concentrated, isolated compound. It is the starting material for all subsequent formulation steps in pharmaceutical manufacturing.

The Unique Mechanism of Action

Bedaquiline's efficacy stems from its distinctive mode of action, which targets the energy production machinery of Mycobacterium tuberculosis.

Inhibition of ATP Synthase: Bedaquiline specifically binds to and inhibits the proton pump of mycobacterial adenosine triphosphate (ATP) synthase. This enzyme is crucial for the bacteria's energy metabolism and survival.
Targeting Both Active and Dormant Cells: By disrupting the energy supply, bedaquiline is effective against both actively replicating and dormant forms of M. tuberculosis, which is a significant advantage over many older TB drugs.
No Cross-Resistance: Its unique mechanism means there is no known cross-resistance with existing anti-TB drugs that target other pathways, making it particularly valuable for treating multidrug-resistant tuberculosis (MDR-TB).

Manufacturing and Formulation of Bedaquiline

The creation of the final bedaquiline tablet is a multi-step process, beginning with the chemical synthesis of the BDQ powder.

Industrial Synthesis of Bedaquiline Fumarate

Chemical Synthesis: The bedaquiline API is synthesized through a series of complex chemical reactions. The initial synthesis method was known to be inefficient and yielded a mixture of isomers, which had to be separated.
Stereoselective Purification: The pure, active isomer of bedaquiline is separated and isolated. This process is complex but essential for ensuring the drug's potency and minimizing side effects.
Salt Formation: The purified bedaquiline is converted to its fumarate salt form to improve its stability and bioavailability. This results in the final BDQ drug powder ready for formulation.

From Powder to Oral Tablet: The Formulation Process

Once the bedaquiline fumarate powder is produced, it is combined with excipients to create the oral tablet dosage form (Sirturo).

Weighing and Blending: The bedaquiline powder is precisely weighed and blended with excipients like lactose monohydrate, microcrystalline cellulose, and starch.
Granulation: A wet granulation process is often used to produce uniform, compressible granules from the blended powder.
Drying and Milling: The granules are dried to remove moisture and then milled to a consistent particle size.
Lubrication and Compression: A lubricant is added to the granules before they are compressed into tablets using a high-speed press.
Coating and Packaging: The final tablets are coated and packaged for distribution.

Bedaquiline Powder (API) vs. Finished Product (Sirturo) Comparison


Feature	Bedaquiline Powder (API)	Finished Product (Sirturo Tablet)
Physical State	Fine, white to off-white powder	Uncoated, round, biconvex tablet
Composition	Pure bedaquiline fumarate	Bedaquiline fumarate plus excipients (lactose, cellulose, etc.)
Purpose	Raw material for manufacturing	Oral medication for patients
Handling	Handled in controlled pharmaceutical manufacturing settings	Handled by pharmacists and patients
Solubility	Very low solubility in water	Formulated for optimal absorption after oral administration
Safety Concerns	Industrial handling precautions	Side effects in patients, including QT prolongation and hepatotoxicity

Potential for Alternative Formulations

Researchers are investigating new ways to deliver bedaquiline that may offer advantages over oral tablets, particularly for pediatric use or to reduce side effects.

Inhalable Dry Powder: Studies have explored the development of inhalable dry powder formulations to deliver the drug directly to the lungs, potentially reducing systemic side effects and improving treatment outcomes for pulmonary TB.
Long-Acting Injectables: Long-acting injectable formulations, in which the bedaquiline powder is incorporated into a microsuspension, are also under preclinical development.

Clinical Use and Important Considerations

Bedaquiline (Sirturo) is a potent treatment, but its use comes with important considerations:

Reserved Use: The drug is reserved for cases of multi-drug resistant tuberculosis (MDR-TB) and is always used as part of a combination therapy regimen to prevent the development of resistance.
Serious Side Effects: Potential serious side effects include QT prolongation (a heart rhythm abnormality) and hepatotoxicity (liver damage), necessitating careful cardiac and liver monitoring throughout treatment.
Resistance: While its mechanism is novel, resistance to bedaquiline can emerge through mutations, primarily affecting efflux pump mechanisms. Vigilant drug-susceptibility testing is crucial.

Conclusion

Bedaquiline BDQ drug powder is far more than just a chemical compound; it is the raw, potent heart of a critical medication for combating multi-drug resistant tuberculosis. Its journey from a synthesized powder to a carefully formulated tablet demonstrates the complexity and importance of pharmaceutical manufacturing and underscores the distinction between an active substance and its finished product. Ongoing research into new delivery methods, such as inhalable powders, shows promise for further optimizing its therapeutic impact. Given its power and associated risks, BDQ remains a vital tool in combination therapies for MDR-TB, demanding careful monitoring and strategic use to maintain its effectiveness against one of the world's most resilient infectious diseases.

: https://www.newtbdrugs.org/pipeline/compound/bedaquiline-0

: https://www.ncbi.nlm.nih.gov/books/NBK247434/

: https://www.goodrx.com/sirturo/what-is

: https://medlineplus.gov/druginfo/meds/a613022.html

: https://www.ncbi.nlm.nih.gov/books/NBK247415/bin/part3-m3.pdf

: https://www.thelancet.com/journals/lanmic/article/PIIS2666-5247(23)00321-X/fulltext

: https://pmc.ncbi.nlm.nih.gov/articles/PMC6836091/

: https://pdfs.semanticscholar.org/dbac/6bb22f3aac61d4bd230a406d7534adfe6c47.pdf

: https://ijprajournal.com/issue_dcp/Formulation%20and%20Evaluation%20of%20Immediate%20Release%20tablets%20of%20Bedaquiline.pdf

: https://www.sciencedirect.com/science/article/pii/S2213716521000497

: https://rsc.niaid.nih.gov/sites/default/files/bedaquiline_sirturo_pi-jan-2017.pdf

: https://ec.europa.eu/health/documents/community-register/2021/20210326150900/anx_150900_en.pdf

: https://www.jnj.com/media-center/press-releases/u-s-fda-approves-new-pediatric-formulation-of-sirturoo-bedaquiline-as-part-of-combination-therapy-to-treat-children-with-pulmonary-multidrug-resistant-tuberculosis

: https://pmc.ncbi.nlm.nih.gov/articles/PMC6437534/

: https://pubchem.ncbi.nlm.nih.gov/compound/Bedaquiline-Fumarate

: https://www.researchgate.net/figure/Industrial-synthesis-of-bedaquiline-fumarate_fig4_361191775

: https://pmc.ncbi.nlm.nih.gov/articles/PMC7045498/

: https://pmc.ncbi.nlm.nih.gov/articles/PMC6963887/

: https://www.sciencedirect.com/science/article/pii/S2213716521000497

: https://www.newtbdrugs.org/pipeline/compound/bedaquiline-0

: https://www.mayoclinic.org/drugs-supplements/bedaquiline-oral-route/description/drg-20060714

: https://www.sciencedirect.com/science/article/pii/S2666524724001496

Frequently Asked Questions

The bedaquiline BDQ drug powder is the active ingredient used to manufacture the final medication, Sirturo, which is prescribed as part of a combination therapy to treat pulmonary multi-drug resistant tuberculosis (MDR-TB).

No, the bedaquiline powder is the active pharmaceutical ingredient (API) in its raw, purified state. Sirturo tablets are the finished pharmaceutical product, which combines the bedaquiline powder with inactive excipients for oral administration.

Bedaquiline works by inhibiting the proton pump of the mycobacterial ATP synthase enzyme. This action disrupts the energy metabolism of the M. tuberculosis bacteria, leading to bacterial death.

Yes, while the oral tablet is the standard form, research has explored alternative formulations using bedaquiline powder, including inhalable dry powders and long-acting injectable microsuspensions, to potentially improve delivery.

Serious side effects include QT prolongation (a type of heart rhythm abnormality) and hepatotoxicity (liver damage). Patients on bedaquiline therapy must undergo regular cardiac and liver function monitoring.

The manufacturing process involves several steps: weighing and blending the BDQ powder with excipients, forming granules (often using a wet granulation method), drying the granules, and compressing them into tablets.

Bedaquiline is reserved for drug-resistant tuberculosis and is used in combination therapy to limit the emergence of drug resistance. Its powerful and unique mechanism of action makes it a last-resort option when other treatments fail.