Activity of KRM 1648 or rifabutin alone or in combination with clarithromycin against Mycobacterium avium complex in human alveolar macrophages

Int J Tuberc Lung Dis. 1997 Oct;1(5):460-7.

Abstract

Setting: The activity of KRM 1648 (KRM), a new benzoxazinorifamycin, and rifabutin (RBT), alone or in combination with clarithromycin (CLA), was evaluated against Mycobacterium avium complex (MAC) that multiplied in human alveolar macrophages (AM).

Design: AM were recovered by bronchoalveolar lavage, incubated in RPMI 1640 medium with 10% human AB serum, infected with four strains of MAC (of non-acquired immune deficiency syndrome [AIDS] origin), and then treated with each drug alone or in combination. After incubation for 7 days, colony forming units in each well were counted on 7H10 agar.

Results: Although concentrations between 0.2 microgram/ml and 20 micrograms/ml of both rifamycins showed clear dose-dependent activities against all MAC strains tested, only 20 micrograms/ml of each drug had modest bactericidal effect. In combination with 2.0 micrograms/ml of CLA, however, 0.2 microgram/ml of both drugs caused a bactericidal response against two of the four MAC strains examined.

Conclusion: According to this human alveolar macrophage model of MAC infection, KRM and RBT in combination with CLA was found to be a promising candidate against human pulmonary MAC infection, and deserves clinical evaluation.

Publication types

  • Clinical Trial
  • Comparative Study
  • Controlled Clinical Trial

MeSH terms

  • Adult
  • Anti-Bacterial Agents / pharmacology*
  • Antibiotics, Antitubercular / pharmacology*
  • Bronchoalveolar Lavage
  • Cells, Cultured
  • Clarithromycin / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Female
  • Humans
  • L-Lactate Dehydrogenase / drug effects
  • L-Lactate Dehydrogenase / metabolism
  • Macrophages, Alveolar / drug effects*
  • Macrophages, Alveolar / metabolism
  • Macrophages, Alveolar / microbiology
  • Male
  • Microbial Sensitivity Tests
  • Middle Aged
  • Mycobacterium avium Complex / drug effects*
  • Mycobacterium avium Complex / growth & development
  • Reference Values
  • Rifabutin / pharmacology*
  • Rifamycins / pharmacology*
  • Smoking

Substances

  • Anti-Bacterial Agents
  • Antibiotics, Antitubercular
  • Rifamycins
  • KRM 1648
  • Rifabutin
  • L-Lactate Dehydrogenase
  • Clarithromycin