Luteinizing hormone-releasing hormone agonists such as leuprolide acetate (LA) are the most frequently utilized treatment of advanced prostate cancer as the regimen for achieving androgen deprivation therapy (ADT).
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The efficacy of LA is determined by extent of testosterone (T) suppression in prostate cancer patients. Although, the historical castrate T suppression target has been defined as < 50 ng/dl, this level may not be as low as required to deliver equivalent suppression as achieved by surgical castration. Recent studies have demonstrated that a T level as low as 20 ng/dl may produce improved clinical outcomes.
LA is available in long-acting formulations that deliver active drug over the course of 1-6 months from a single-dose administration. The technologies utilized to provide sustained drug delivery differ: one mode of administration uses microspheres, which encapsulate the drug and are injected as a suspension intramuscularly; another mode of administration uses a liquid polymer that creates a single, solid depot after injection subcutaneously. This article will review the safety and efficacy of both 6-month LA formulations, as well as their impact in prostate cancer treatment.
As the understanding of optimal T castrate level evolves and may be refined pending new data from contemporaneous trials, achievement and maintenance of T levels well below 50 ng/dl may be important in evaluating potential differences in ADT regimens.
Expert opinion on drug metabolism & toxicology 2015 Sep [Epub]
E David Crawford, Judd W Moul, Oliver Sartor, Neal D Shore
a 1 University of Colorado Cancer Center, University of Colorado Health Sciences Center, Urologic Oncology Department , Mail Stop F710, 1665 N Ursula Street, Rm 1004, P O Box 6510, Aurora, CO 80045, USA +1 720 848 0195 ; +1 720 848 0203