See the DrugPatentWatch profile for tigecycline
Tigecycline, a broad-spectrum antibiotic, is known for its activity against drug-resistant bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE) [1]. However, the unique factors contributing to its resistance profile include:
1. **Efflux Pump Overexpression**: Bacteria can develop resistance to tigecycline by overexpressing efflux pumps, which are membrane transporters that pump antibiotics out of the bacterial cell [2]. This reduces the intracellular concentration of tigecycline, thereby reducing its effectiveness.
2. **Protein Production Modulation**: Bacteria can alter the production of proteins that are necessary for tigecycline to bind and exert its antibacterial effect [3]. This can lead to reduced susceptibility to tigecycline.
3. **Ribosomal Protection Proteins**: Some bacteria produce ribosomal protection proteins that can prevent tigecycline from binding to the bacterial ribosome, thereby inhibiting protein synthesis [4]. This can lead to resistance to tigecycline.
4. **Mutations in Bacterial Chromosome**: Mutations in the bacterial chromosome can lead to changes in the bacterial ribosome, which can reduce the binding of tigecycline and lead to resistance [5].
It's important to note that the overuse or misuse of tigecycline can contribute to the development of resistance [6]. Therefore, it's crucial to use this antibiotic judiciously and in accordance with clinical guidelines to prevent or delay the emergence of resistance.
Sources:
[1]
https://www.ncbi.nlm.nih.gov/books/NBK65763/
[2]
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2826659/
[3]
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3747631/
[4]
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3747631/
[5]
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3747631/
[6]
https://www.drugpatentwatch.com/antibiotic-resistance-database/tigecycline/