Table 2 Study of biodistribution revealed that weekly systemic delivery of fulvestrant at 5 mg dose results in excessive level of drug in every major organ. Similarly, a significant amount of drug was found in all organs but not in the plasma when mice were systemically treated with 1 mg dose per week. In contrast, the level of fulvestrant in major organs was below the limit of detection when delivered locally via silastic tubing. The IMFP could not be collected in mice that were implanted with fulvestrant-loaded tubings because it was difficult to determine where the tubings touched the fat pad once the tumors, adjoined with the tubings, were removed.
ng fulvestrant per gram of organ | Treatment | ||
|---|---|---|---|
5 mg/week SQ injection | 1 mg/week SQ injection | fulvestrant-loaded tubing | |
(systemic) | (systemic) | (local) | |
IMFP | 3,945 ± 1,134 | 2.93 ± 2.93 | N.A. |
heart | 2,896 ± 2,478 | 152.90 ± 31.43 | N.D. |
lung | 5,793 ± 3,651 | 120.80 ± 39.61 | N.D. |
liver | 1,247 ± 929 | 41.95 ± 13.90 | N.D. |
kidney | 1,389 ± 798 | 170.70 ± 21.31 | N.D. |
plasma* | 128 ± 13 | <3.64 ng/ml | <3.64 ng/ml |