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Non-Clinical Toxicology

Non-Clinical Toxicology

Carcinogenesis, mutagenesis, impairment of fertility

Two-year carcinogenicity studies were conducted with leuprolide acetate in rats and mice.

In rats, a dose-related increase of benign pituitary hyperplasia and benign pituitary adenomas was noted at 24 months when the drug was administered subcutaneously at high daily doses (0.6 to 4 mg/kg). There was a significant but not dose-related increase of pancreatic islet-cell adenomas in females and of testicular interstitial cell adenomas in males (highest incidence in the low dose group).

In mice, no leuprolide acetate-induced tumors or pituitary abnormalities were observed at a dose as high as 60 mg/kg for two years.

Patients have been treated with leuprolide acetate for up to three years with doses as high as 10 mg/day and for two years with doses as high as 20 mg/day without demonstrable pituitary abnormalities.

No carcinogenicity studies have been conducted with ELIGARD.

Mutagenesis

Mutagenicity studies have been performed with leuprolide acetate using bacterial and mammalian systems and with ELIGARD 7.5 mg in bacterial systems. These studies provided no evidence of a mutagenic potential.

IMPORTANT SAFETY INFORMATION

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ELIGARD®, (leuprolide acetate) for injectable suspension, is indicated for the palliative treatment of advanced prostate cancer.

ELIGARD is contraindicated in patients with hypersensitivity to GnRH, GnRH agonists, or any of the components of ELIGARD. Anaphylactic reactions to synthetic GnRH or GnRH agonists have been reported in the literature. Transient increase in serum levels of testosterone during treatment may result in worsening of symptoms or onset of new signs and symptoms during the first few weeks of treatment, including bone pain, neuropathy, hematuria, bladder outlet obstruction, ureteral obstruction, or spinal cord compression. Monitor patients at risk closely and manage as appropriate.

Hyperglycemia and an increased risk of developing diabetes have been reported in men receiving GnRH agonists. Monitor blood glucose level and manage according to current clinical practice. Increased risk of myocardial infarction, sudden cardiac death and stroke has also been reported with use of GnRH agonists in men. Monitor for cardiovascular disease and manage according to current clinical practice. Androgen deprivation therapy may prolong the QT/QTc interval. Consider risks and benefits. May cause fetal harm. Convulsions have been observed in patients taking leuprolide acetate with or without a history of predisposing factors. Manage convulsions according to current clinical practice.

ELIGARD may impair fertility in males of reproductive potential.

The most common injection site adverse events are transient burning and stinging, pain, bruising, and erythema. The most common systemic adverse events include mild to severe hot flashes/sweats, malaise and fatigue, weakness, myalgia, dizziness, clamminess, testicular atrophy, and gynecomastia. As with other GnRH agonists, other adverse reactions, including decreased bone density and rare cases of pituitary apoplexy have been reported.

See package insert for full prescribing and safety information.

Please see full Prescribing Information for ELIGARD and full Prescribing Information for ELIGARD with Pre-connected Syringe System.