Azlocillin: A Potential Lyme Cure Forbidden in the USA
Azlocillin is classified as an acylampicillin and is known for its broad-spectrum antibacterial activity, effective against both Gram-positive and Gram-negative bacteria, including strains like Pseudomonas aeruginosa and Escherichia coli
Mechanism: It works by inhibiting penicillin-binding proteins (PBPs), which are essential for bacterial cell wall synthesis, thereby leading to cell lysis and death.
Azlocillin, a semisynthetic β-lactam antibiotic, has emerged as a potential treatment for Lyme disease, particularly in cases where patients exhibit drug-tolerant bacteria.
The cell wall of B. burgdorferi, a spiral bacteria which causes Lyme Disease, is primarily composed of peptidoglycan (PG), which provides structural integrity and protection against osmotic pressure. The PG consists of glycan chains linked by peptides, forming a mesh-like structure that is crucial for maintaining the shape of the bacterium
Despite its promising laboratory results, azlocillin is currently not available for human use in the United States due to its discontinued marketing and lack of clinical trials for Lyme disease.
Efficacy Against Lyme Disease
Recent studies, particularly those conducted by Stanford Medicine, have shown that azlocillin effectively kills Borrelia burgdorferi, the bacterium responsible for Lyme disease. Research indicates that it can eliminate both the active and drug-tolerant forms of the bacteria in vitro and in mouse models. The combination of azlocillin with cefotaxime has been noted to enhance its efficacy against persistent bacterial forms, which are often responsible for lingering symptoms in patients.
Laboratory Findings
- Complete Elimination: Azlocillin has been shown to completely eradicate B. burgdorferi at the onset of infection in laboratory settings.
- Effectiveness Against Persisters: It has demonstrated the ability to kill drug-tolerant persister cells, which contribute to chronic Lyme disease symptoms experienced by some patients.
Regulatory Status
Azlocillin was previously marketed under the name Azlin in the U.S., but its approval was discontinued. Currently, it is not available for clinical use, as no pharmaceutical companies are pursuing its development further. The lack of ongoing production and research into its application for Lyme disease treatment poses a significant barrier to its availability.
Challenges and Considerations
Despite azlocillin’s potential, several challenges hinder its clinical application:
- Allergy Concerns: It cannot be used in patients with penicillin allergies.
- Administration Method: Azlocillin is only available intravenously, complicating its use compared to orally administered antibiotics.
- Lack of Human Trials: There have been no published human studies validating its effectiveness or safety specifically for Lyme disease, which limits its acceptance in clinical practice.
Obstacles to Availability
The situation with azlocillin’s FDA status and availability is frustrating. Here’s an explanation of why it’s not currently available in the United States despite being FDA-approved:
1. Discontinued Production: Although azlocillin was previously FDA-approved, it is no longer manufactured or marketed in the United States. Pharmaceutical companies sometimes discontinue production of drugs for various reasons, such as low demand, manufacturing costs, or shifting market priorities[12].
2. Repurposing Challenges: While azlocillin shows promise for Lyme disease treatment, it was originally approved for other uses. Repurposing an existing drug for a new indication requires additional research, clinical trials, and regulatory approvals, which can be time-consuming and expensive[12][14].
3. Development of Oral Formulation: The researchers are working with a company to develop an oral form of azlocillin specifically for Lyme disease treatment. The original FDA approval was likely for an intravenous formulation, which is less convenient for widespread use in Lyme disease patients[12].
4. Pending Clinical Trials: Before azlocillin can be made available for Lyme disease treatment, it needs to undergo human clinical trials to demonstrate its safety and efficacy for this specific use. These trials are planned but have not yet been conducted[12][14].
5. Regulatory Process: Even with previous FDA approval, introducing azlocillin as a Lyme disease treatment would require going through the regulatory process again, including submitting new drug applications and potentially conducting additional safety studies[14].
6. Commercial Considerations: The potential market size for Lyme disease treatment and the associated development costs may influence pharmaceutical companies’ decisions to pursue bringing azlocillin back to market[15].
The process of making azlocillin available for Lyme disease treatment is ongoing, but it requires navigating complex regulatory, scientific, and commercial challenges. This explains the frustrating gap between its promising lab results and its current unavailability in the United States.
Conclusion
While azlocillin shows promise as a treatment option for Lyme disease, especially for patients resistant to standard therapies, significant hurdles remain before it can be considered a viable treatment option in the U.S. Its current unavailability and the absence of human trial data underscore the need for further research and development in this area.
Read More
[1] https://danielcameronmd.com/late-stage-lyme-disease-treatment-azlocillin/
[2] https://drugs.ncats.io/drug/HUM6H389W0
[3] https://toku-e.com/blog/the-promise-of-azlocillin-and-cefotaxime-for-lyme-disease/
[4] https://med.stanford.edu/news/all-news/2020/03/potential-treatment-for-lingering-lyme-disease.html
[5] https://pmc.ncbi.nlm.nih.gov/articles/PMC10483257/
[6] https://www.medicalnewstoday.com/articles/lyme-disease-treatment
[7] https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=12260
[8] https://danielcameronmd.com/new-treatments-for-lyme-disease/
[9] https://www.nature.com/articles/s41598-020-59600-4
[10] https://www.treatlyme.net/guide/hygromycin-a-and-azlocillin-for-lyme-disease
[11] https://www.nature.com/articles/s41598-020-59600-4
[12] https://scopeblog.stanford.edu/2020/03/30/lyme-disease-bacteria-eradicated-by-new-drug-in-early-tests/
[13] https://www.treatlyme.net/guide/hygromycin-a-and-azlocillin-for-lyme-disease
[14] https://med.stanford.edu/news/all-news/2020/03/potential-treatment-for-lingering-lyme-disease.html
[15] https://palyme.org/emerging-treatments/
[16] https://danielcameronmd.com/late-stage-lyme-disease-treatment-azlocillin/
[17] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10244525/
[18] https://medlineplus.gov/ency/article/001407.htm