Efficacy

Efficacy

ELIGARD® delivers powerful and sustained testosterone suppression that reflects current science.

ELIGARD® achieves low castration testosterone levels across all doses. In the United States, the biochemical and regulatory definition of castration is a serum testosterone (T) level <50 ng/dL.

This value is based on the sensitivity of the assays available when androgen deprivation therapy (ADT) was first developed 50 years ago. With the advent of current improved assays, it is possible to detect much lower T levels (<3 ng/dL).

Data were pooled from four prospective, open-label, fixed dose clinical trials in patients with advanced prostate cancer. Patients with no prior ADT were treated with one of four formulations of subcutaneous leuprolide acetate (ELIGARD®):

  • 7.5 mg every 28 days for 24 weeks (1-month formulation; n=120)
  • 22.5 mg every 84 days for 24 weeks (3-month formulation; n=117)
  • 30 mg every 112 days for 32 weeks (4-month formulation; n=90)
  • 45 mg every 168 days for 48 weeks (6-month formulation; n=111)

In the pooled patient population, 99%, 97%, 91% and 80% of patients reached nadir testosterone levels of ≤20, ≤10, ≤5, and ≤3 ng/dL respectively, at week 24. [1]

The mean proportions of time T suppression was maintained below each target were 100% for T ≤50 ng/dL, 94% to 99% for T ≤20 ng/dL, and 66% to 85% for T ≤10 ng/dL. [2]

Castration levels in 2-4 weeks

Testosterone levels increased above baseline during the first week, declining thereafter to baseline levels or below by the end of the second or third week in the majority of patients. Castration levels were generally reached within two to four weeks.

Castration levels maintained

Castration testosterone levels were maintained for the duration of the treatment with ELIGARD 7.5 mg. No increases above the castration level occurred in any of the patients.

Castration levels were maintained for the duration of treatment with ELIGARD 22.5 mg with only one patient demonstrating breakthrough following 1st injection; that patient remained at castration levels following the second injection.

Once castration levels were achieved with ELIGARD 30 mg, most (86/89) patients remained suppressed throughout the study.

Once castration levels were achieved with ELIGARD 45 mg, only one patient (< 1%) experienced a breakthrough, with testosterone levels > 50 ng/dL.

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ELIGARD (leuprolide acetate) for injectable suspension maintains castration testosterone levels across all four doses, including the longest duration available (6-month dose).

Table: Testosterone concentration over time

Serum PSA decrease

Serum PSA decreased in all patients in all studies whose baseline values were elevated above the normal limit. [1]

A total of 91% to 95% of patients achieved normal serum PSA values at study conclusion. [1]

Response to ELIGARD should be monitored by periodic measurement of serum concentrations of testosterone and prostate specific antigen.

Dose7.5 mg22.5 mg30 mg45 mg
Mean PSA reduction at study conclusion94%98%86%97%
Patients with normal PSA at study conclusion94%91%93%95%
In all studies, ELIGARD decreased serum PSA in all patients whose baseline values were elevated above normal. [1]
Table: Effect of ELIGARD® on serum PSA values
References
  1. ELIGARD® (leuprolide acetate) for injectable suspension, 7.5 mg, 22.5 mg, 30 mg, 45 mg prescribing information. Fort Collins, CO: Tolmar Therapeutics, Inc.; 2019

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.