July 24, 2016
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Mechanism Of Action

Mitotane is an adrenal cytotoxic agent with an unknown mechanism of action. Mitotane modifies the peripheral metabolism of steroids and directly suppresses the adrenal cortex. A reduction in 17-hydroxycorticosteroids in the absence of decreased corticosteroid concentrations and increased formation of 6-β-hydroxycortisol have been reported.


The pharmacodynamics of mitotane are unknown.



Following oral administration of LYSODREN, 40% of the dose is absorbed.


Mitotane is found in most tissues of the body; however, fat is the primary site of distribution.


Following discontinuation of mitotane, the plasma terminal half-life ranges from 18 to 159 days (median 53 days).


Mitotane is converted to a water-soluble metabolite.


No unchanged mitotane is found in urine or bile. Approximately 10% of the administered dose is recovered in the urine as a water-soluble metabolite. A variable amount of metabolite (1%-17%) is excreted in the bile.

Last reviewed on RxList: 3/28/2016
This monograph has been modified to include the generic and brand name in many instances.

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