Bedaquiline (TMC-207, CAS: 843663-66-1) is a small molecule antibiotic used for the treatment of multidrug-resistant tuberculosis (MDR-TB). Bedaquiline was first approved by the US Food and Drug Administration (FDA) in 2012 under the brand name Sirturo. This article will provide an overview of bedaquiline, including its chemical properties, health benefits, potential effects, product mechanism, safety, side effects, dosing information, and a conclusion on its use.
Chemical Properties The chemical name for bedaquiline is N-(6-bromo-2-methoxy-3-quinoxalinyl)-2-nitro-1,3-thiazole-5-carboxamide. Its molecular formula is C32H31BrN4O3S, and it has a formula weight of 671.59 g/mol. The CAS number for this compound is 843663-66-1.
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Health Benefits Bedaquiline is primarily used for the treatment of MDR-TB, which is a form of tuberculosis that is resistant to at least two of the most commonly used anti-TB drugs. It works by inhibiting the activity of mycobacterial ATP synthase, which is an enzyme that is essential for the survival of Mycobacterium tuberculosis. By blocking the activity of ATP synthase, bedaquiline can help kill or slow the growth of MDR-TB bacteria, leading to improved outcomes for patients with this condition.
Potential Effects In clinical trials, bedaquiline has been shown to be highly effective at improving outcomes in patients with MDR-TB. It has also been found to be well-tolerated, with few serious side effects reported. Additionally, bedaquiline has demonstrated good pharmacokinetic properties, meaning it is well-absorbed and distributed throughout the body, and is metabolized and eliminated from the body in a predictable manner.
Product Mechanism Bedaquiline is a selective inhibitor of mycobacterial ATP synthase activity. It works by binding to the c-ring of ATP synthase, thereby preventing the synthesis of ATP molecules that are needed for the survival and growth of M. tuberculosis. By blocking the activity of ATP synthase, bedaquiline can help kill or slow the growth of MDR-TB bacteria.
Safety Overall, bedaquiline has been found to be safe and well-tolerated in clinical trials. However, like all medications, it does carry some risks of side effects and adverse events. Patients taking bedaquiline should be monitored regularly for any signs of liver dysfunction, cardiac abnormalities, or other serious side effects.
Side Effects Some of the most common side effects reported with bedaquiline include nausea, headache, dizziness, and chest pain. These side effects are usually mild to moderate in severity and go away on their own over time. More serious side effects, such as QT prolongation or hepatotoxicity, are rare but can occur in some patients.
Dosing Information Bedaquiline is typically taken orally, either with or without food. The recommended dose for patients with MDR-TB is 400 mg once daily for the first 2 weeks, followed by 200 mg three times weekly for the remainder of treatment. Patients should follow their healthcare provider's instructions carefully when taking this medication.
Conclusion Bedaquiline is a highly effective and well-tolerated medication used for the treatment of MDR-TB. As a selective inhibitor of mycobacterial ATP synthase activity, it helps kill or slow the growth of MDR-TB bacteria. While it does carry some risks of side effects and adverse events, overall, it has been found to be safe and effective in clinical trials. Patients taking bedaquiline should work closely with their healthcare providers to ensure proper dosing and monitoring for any potential side effects
