 With once-weekly treatment in participants with pulmonary TB, mean plasma AUC0-inf was 296, 410, and 477 μghmL after 600, 900, and 1200 mg doses administered without food, and Cmax was 12, 15, and 19 μgmL. The bioavailability of rifapentine was 70 in healthy adult volunteers who were given a single 600-mg dose. Food total, 850 calories 33 g protein, 55 g fat, and 58 g carbohydrate increases AUC0-inf by 43 and Cmax by 44 compared with fasting conditions. Rifapentine and its 25-desacetyl metabolite are 98 and 93 protein-bound in serum, primarily to albumin. Rifapentine is metabolized to 25-desacetyl rifapentine by an esterase enzyme present in the liver and blood. The half-life of rifapentine is 14 to 17 hours and the half-life of 25-desacetyl rifapentine is 13 hours. Rifapentine is excreted in bile and eliminated in feces, and 10 rifapentine is excreted unchanged in urine. The microbiologically active metabolite contributes 40 of the overall activity of the drug. The MIC of rifapentine against M. tuberculosis is 0.05 μgmL 0.25 μgmL for 25-desacetyl rifapentine. Single-dose rifapentine PK parameters are similar in healthy females and males. 