In vivo studies have established that sangivamycin was phosphorylated and incorporated into the nucleic acids of mouse tissues. When ³H-labeled sangivamycin was administered to mice by i.p. injection, the major component of drug in liver, heart, brain, and red blood cells was sangivamycin 5′-monophosphate; whereas, in spleen and kindey, the larger proportion of the drug was recovered as unmetabolized sangivamycin. Small amounts of sangivamycin 5′-diphosphate were identified in all tissues, but sangivamycin 5′-triphosphate was detected only in red blood cells. There was incorporation of sangivamycin into RNA and DNA of all tissues except brain, where labeling occurred only in RNA.

The half-life of sangivamycin in mouse blood was 50 hr after i.p. injection. Labeled sangivamycin was retained in tissues for at least 12 days, presumably because of its intracellular phosphorylation. The main route of excretion appeared to be the kidneys; 40% of the drug-derived radioactivity was accounted for in the urine over a period of 12 days.