What proportion of ticagrelor is metabolically eliminated and what proportion is excreted?
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Approximately 40% of ticagrelor is metabolically eliminated, primarily through the formation of its active metabolite AR-C124910XX . The major active metabolite, AR-C124910XX, accounts for about 29% of the peak exposure and 40% of the overall exposure to ticagrelor . In terms of excretion, ticagrelor and its metabolites are mainly eliminated through feces (57.8% of total radioactivity) and urine (26.5% of total radioactivity) . The primary metabolite excreted in urine across various species is an inactive metabolite, AR-C133913 . Ticagrelor and its metabolites were found to be largely restricted to the plasma space, with minimal renal clearance of ticagrelor and its active metabolite .
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40 Citations | Ticagrelor undergoes extensive hepatic elimination, with higher exposure in mild hepatic impairment. Approximately 99.8% is highly protein bound, and no significant renal excretion is mentioned in the study. |
| Approximately 1 to 15% of ticagrelor is excreted in urine, while 59 to 96% is metabolically eliminated via feces in mice, rats, and marmosets. | |
| Approximately 29% of ticagrelor is metabolically eliminated, while 26.5% is excreted in urine and 57.8% in feces, indicating predominant non-renal excretion pathways for ticagrelor and its metabolites. | |
20 Citations | Ticagrelor is extensively metabolized by hepatic CYP3A enzymes, with its only active metabolite being AR-C124910XX. The paper does not specify the proportion of metabolic elimination versus excretion. |
Open access 01 Jan 2014 16 Citations | After oral administration, a higher proportion of ticagrelor is metabolically eliminated (metabolite:parent ratios higher) compared to IV administration. The mean absolute bioavailability of ticagrelor was 36%. |
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