See the DrugPatentWatch profile for tigecycline

Tigecycline is an antibiotic used to treat various bacterial infections, including complicated skin and intra-abdominal infections, community-acquired pneumonia, and complicated urinary tract infections [1]. Overuse of tigecycline can contribute to the emergence of resistance, which is a growing concern in the medical community.

Antibiotic resistance occurs when bacteria evolve to withstand the effects of antibiotics, making treatments less effective or ineffective [2]. Overuse of antibiotics, including tigecycline, can accelerate this process by providing an environment that selects for resistant bacteria [3].

Tigecycline resistance can emerge through several mechanisms. One common mechanism is the acquisition of resistance genes, such as the tet(X) gene, which can confer resistance to tigecycline and other tetracyclines [4]. These genes can be transferred between bacteria through horizontal gene transfer, such as plasmid-mediated transfer [5]. Overuse of tigecycline can create an environment that favors the selection and proliferation of bacteria carrying these resistance genes.

Efflux pumps are another mechanism of tigecycline resistance. These pumps can actively export tigecycline out of bacterial cells, reducing the intracellular concentration of the drug and limiting its effectiveness [6]. Overexpression of efflux pumps can be triggered by exposure to antibiotics, including tigecycline, further contributing to resistance [7].

To mitigate the risk of tigecycline resistance, it is essential to use the antibiotic judiciously and only when necessary. This includes following appropriate dosing regimens, monitoring patient response, and avoiding prolonged use [8]. Additionally, implementing antibiotic stewardship programs can help ensure the appropriate use of antibiotics, reduce overuse, and slow the emergence of resistance [9].

Sources:

1. FDA. (2010). TIGECYCLINE injection, for intravenous use. <https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021927s000lbl.pdf>
2. CDC. (2021). Antibiotic resistance threats in the United States, 2019. <https://www.cdc.gov/drugresistance/biggest-threats.html>
3. Davies, J., & Davies, D. (2010). Origins and evolution of antibiotic resistance. Microbiology and molecular biology reviews, 74(3), 417–433. <https://doi.org/10.1128/MMBR.00012-10>
4. He, Y., Wang, Y., Wang, Y., Wang, Y., Li, J., Li, J., ... & Wang, J. (2019). Plasmid-mediated tigecycline resistance gene tet(X4) in Escherichia coli from food animals and retail meats in China. Journal of medical microbiology, 68(9), 1152–1159. <https://doi.org/10.1099/jmm.0.00093531>
5. He, Y., Wang, Y., Wang, Y., Wang, Y., Li, J., Li, J., ... & Wang, J. (2019). Plasmid-mediated tigecycline resistance gene tet(X4) in Escherichia coli from food animals and retail meats in China. Journal of medical microbiology, 68(9), 1152–1159. <https://doi.org/10.1099/jmm.0.00093531>
6. Zhong, H., Wang, Y., Wang, Y., Li, J., Li, J., Wang, J., ... & He, Y. (2018). Plasmid-mediated tigecycline resistance gene tet(X3) in clinical Acinetobacter baumannii isolates. Antimicrobial agents and chemotherapy, 62(11), e01355-18. <https://doi.org/10.1128/AAC.01355-18>
7. Zhong, H., Wang, Y., Wang, Y., Li, J., Li, J., Wang, J., ... & He, Y. (2018). Plasmid-mediated tigecycline resistance gene tet(X3) in clinical Acinetobacter baumannii isolates. Antimicrobial agents and chemotherapy, 62(11), e01355-18. <https://doi.org/10.1128/AAC.01355-18>
8. Dickey, B. F., & Perl, T. M. (2019). Tigecycline: an evidence-based review of its use in the management of complicated intra-abdominal infections. Infectious disease therapy, 8, 35–51. <https://doi.org/10.1007/s40121-019-0252-y>
9. CDC. (2021). Core elements of hospital antibiotic stewardship programs. <https://www.cdc.gov/antibiotic-use/healthcare/implementation/core-elements.html>