Rifamycin antibiotics and the mechanisms of their failure

Rebekah A. Adams, Gabrielle Leon, Natalia M. Miller, Saira P. Reyes, Chantal H. Thantrong, Alina M. Thokkadam, Annabel S. Lemma, Darshan M. Sivaloganathan, Xuanqing Wan, Mark P. Brynildsen

Research output: Contribution to journalReview articlepeer-review

28 Scopus citations


Rifamycins are a class of antibiotics that were first discovered in 1957 and are known for their use in treating tuberculosis (TB). Rifamycins exhibit bactericidal activity against many Gram-positive and Gram-negative bacteria by inhibiting RNA polymerase (RNAP); however, resistance is prevalent and the mechanisms range from primary target modification and antibiotic inactivation to cytoplasmic exclusion. Further, phenotypic resistance, in which only a subpopulation of bacteria grow in concentrations exceeding their minimum inhibitory concentration, and tolerance, which is characterized by reduced rates of bacterial cell death, have been identified as additional causes of rifamycin failure. Here we summarize current understanding and recent developments regarding this critical antibiotic class.

Original languageEnglish (US)
Pages (from-to)786-798
Number of pages13
JournalJournal of Antibiotics
Issue number11
StatePublished - Nov 2021

All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • Pharmacology


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