Leuprolide (Lupron)

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General information

Class/mechanism: GnRH (gonadotropin-releasing hormone)/LHRH (luteinizing hormone releasing hormone) agonist; inhibits gonadotropin secretion, decreasing circulating levels of LH (luteinizing hormone) and FSH (follicle stimulating hormone), and suppressing synthesis of ovarian and testicular steroids.[1][2][3][4][5][6]
Route: IM
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1][4]

Diseases for which it is used

Patient drug information

Information about dementia risk

  • Khosrow-Khavar F, Rej S, Yin H, Aprikian A, Azoulay L. Androgen Deprivation Therapy and the Risk of Dementia in Patients With Prostate Cancer. J Clin Oncol. 2017 Jan 10;35(2):201-207. link to original article PubMed
    • 30,903 patients searched in the United Kingdom's Clinical Practice Research Datalink. Mean follow-up of 4.3 years, (3.6 standard deviation).
    • Not statistically different incidence of dementia 7.4 (ADT) vs. 4.4 (no ADT) per 1,000 person-years; adjusted hazard ratio, 1.02; 95% CI, 0.87 to 1.19).
    • Does Androgen Deprivation Therapy Raise the Risk for Dementia? Jan 06, 2017 ASCO Connection: "Dr. Azoulay said that the varying findings from previous studies might be the result of methodological issues, such as exposure lag periods and immortal time bias."
  • Nead KT, Gaskin G, Chester C, Swisher-McClure S, Dudley JT, Leeper NJ, Shah NH. Androgen Deprivation Therapy and Future Alzheimer's Disease Risk. J Clin Oncol. 2016 Feb 20;34(6):566-71. link to original article PubMed ASCO Post article
    • 16,888 patients, with 2,397 (14.2%) receiving ADT. "We used a previously validated and implemented text-processing pipeline to analyze electronic medical record data in a retrospective cohort of patients at Stanford University and Mt. Sinai hospitals." Median follow-up 2.7 years (interquartile range 1.0-5.4 years).
    • Statistically significant increased risk of Alzheimer's dementia in ADT patients. "Propensity score–matched analysis (hazard ratio, 1.88; 95% CI, 1.10 to 3.20; P = .021) and traditional multivariable-adjusted Cox regression analysis (hazard ratio, 1.66; 95% CI, 1.05 to 2.64; P = .031) both supported a statistically significant association between ADT use and Alzheimer’s disease risk. We also observed a statistically significant increased risk of Alzheimer’s disease with increasing duration of ADT (P = .016)."
    • 125 new diagnoses of Alzheimer’s disease
  • Nead KT, Gaskin G, Chester C, Swisher-McClure S, Leeper NJ, Shah NH. Association Between Androgen Deprivation Therapy and Risk of Dementia. JAMA Oncol. 2017 Jan 1;3(1):49-55. link to original article PubMed ASCO Post article
    • "A text-processing method was used to analyze electronic medical record data" for 9,272 patients at Stanford. 1826 (19.7%) patients received ADT. Median follow-up 3.4 years (interquartile range 1.0-7.2 years)
    • Statistically significant increased risk of dementia in ADT patients (7.9%) vs. non-ADT patients (3.5%). Overall incidence of dementia was 4.4% at 5 years.

Management checklist

  • Basic/comprehensive metabolic panel including glucose and liver function tests (LFTs), bone density, vitamin D 25, lipid panel, testosterone, EKG (if on other QT prolonging medications)

History of changes in FDA indication

  • 4/09/1985: Initial FDA approval for palliative treatment of advanced prostate cancer.

Also known as

  • Code names: A-43818, TAP-144
  • Generic names: leuprolide acetate, leuprorelin, leuprorelin acetate
  • Brand names: Carcinil, Depo-Eligard, Eligard, Enanton, Enantone, Enantone-Gyn, Ginecrin, Leuplin, Leupromer, Leuprorelin, Leuren, Lorelin Depot, Lucrin, Lucrin Depot, Lupard Depot, Lupoide Depot, Lupride Depot, Luprodex Depot, Lupron, Lupron Depot, Procren, Procrin, Prostap, Trenantone, Uno-Enantone, Valeuprox, Viadur

References

  1. 1.0 1.1 1.2 Leuprolide (Lupron) package insert
  2. Leuprolide (Lupron) package insert (locally hosted backup)
  3. Lupron manufacturer's website
  4. 4.0 4.1 4.2 Leuprolide (Eligard) package insert
  5. Leuprolide (Eligard) package insert (locally hosted backup)
  6. Eligard manufacturer's website
  7. Leuprolide (Lupron) patient drug information (Chemocare)
  8. Leuprolide (Lupron) patient drug information (UpToDate)