Your browser doesn't support javascript.
loading
Safety and bactericidal activity of rifalazil in patients with pulmonary tuberculosis.
Dietze, R; Teixeira, L; Rocha, L M; Palaci, M; Johnson, J L; Wells, C; Rose, L; Eisenach, K; Ellner, J J.
Afiliação
  • Dietze R; Núcleo de Doenças Infecciosas Centro Biomédico, Universidade Federal de Espírito Santo, Vitória, Brazil. rdietze@npd.ufes.br
Antimicrob Agents Chemother ; 45(7): 1972-6, 2001 Jul.
Article em En | MEDLINE | ID: mdl-11408210
Rifalazil, also known as KRM-1648 or benzoxazinorifamycin, is a new semisynthetic rifamycin with a long half-life of approximately 60 h. Rifalazil has potent bactericidal activity against Mycobacterium tuberculosis in vitro and in animal models of tuberculosis (TB). Prior studies in healthy volunteers showed that once-weekly doses of 25 to 50 mg of rifalazil were well tolerated. In this randomized, open-label, active-controlled phase II clinical trial, 65 subjects with sputum smear-positive pulmonary TB received one of the following regimens for the first 2 weeks of therapy: 16 subjects received isoniazid (INH) (5 mg/kg of body weight) daily; 16 received INH (5 mg/kg) and rifampin (10 mg/kg) daily; 17 received INH (5 mg/kg) daily plus 10 mg of rifalazil once weekly; and 16 received INH (5 mg/kg) daily and 25 mg of rifalazil once weekly. All subjects were then put on 6 months of standard TB therapy. Pretreatment and day 15 sputum CFU of M. tuberculosis were measured to assess the bactericidal activity of each regimen. The number of drug-related adverse experiences was low and not significantly different among treatment arms. A transient decrease in absolute neutrophil count to less than 2,000 cells/mm(3) was detected in 10 to 20% of patients in the rifalazil- and rifampin-containing treatment arms without clinical consequences. Decreases in CFU counts were comparable among the four treatment arms; however, the CFU results were statistically inconclusive due to the variability in the control arms. Acquired drug resistance did not occur in any patient. Studies focused on determining a maximum tolerated dose will help elucidate the full anti-TB effect of rifalazil.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Rifamicinas / Tuberculose Pulmonar / Antibióticos Antituberculose Tipo de estudo: Clinical_trials Limite: Adolescent / Adult / Female / Humans / Male Idioma: En Revista: Antimicrob Agents Chemother Ano de publicação: 2001 Tipo de documento: Article País de afiliação: Brasil País de publicação: Estados Unidos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Rifamicinas / Tuberculose Pulmonar / Antibióticos Antituberculose Tipo de estudo: Clinical_trials Limite: Adolescent / Adult / Female / Humans / Male Idioma: En Revista: Antimicrob Agents Chemother Ano de publicação: 2001 Tipo de documento: Article País de afiliação: Brasil País de publicação: Estados Unidos