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Head-to-head pharmacokinetic and pharmacodynamic comparison of subcutaneous versus intramuscular leuprorelin acetate formulations in male patients.

Publication ,  Conference
Moul, JW; McLane, JA; Atkinson, S; Concepcion, RS
Published in: Journal of Clinical Oncology
February 20, 2017

e589 Background: Leuprolide acetate (LA) is the standard-of-care luteinizing hormone-releasing hormone (LHRH) agonist used to suppress serum testosterone (T) in the treatment of advanced prostate cancer. There are currently two LA formulations available: a controlled-release implant injected subcutaneously (SC) or a microsphere intra-muscular (IM) injection. The study compared the pharmacokinetics/pharmacodynamics of both formulations at the same one-month dose. Methods: Thirty-two healthy men were randomized to receive a single 7.5 mg injection of SC-LA (n = 16) or IM-LA (n = 16) in this phase 1, open-label, parallel-group study. Serum LA, T, and luteinizing hormone (LH) were assessed. Results: The initial surge of LA was higher for IM-LA than SC-LA (Cmax 27±4.9 vs. 19±8.0 ng/mL, respectively), with a shorter t (1.0±0.4 vs. 2.1±0.8 hrs). Mean serum LA remained above the level of quantification (LOQ, 50 pg/mL) through Day 49 for SC-LA, whereas for IM-LA, mean serum LA dropped below the LOQ after Day 28. Median LH concentration remained low at Day 56 in the SC-LA group, whereas LH levels began to rise after Day 35 in the IM-LA group. Consequently, serum T began to increase by Day 42 in the IM-LA group. By Day 56, 13 SC-LA subjects maintained serum T levels ≤ 50 ng/dL vs. 0 in the IM-LA group. Both SC-LA and IM-LA were well tolerated, however SC-LA subjects experienced more mild injection site disorders compared to IM-LA. Conclusions: The initial surge of LA was higher for IM-LA than SC-LA (Cmax 27±4.9 vs. 19±8.0 ng/mL, respectively), with a shorter t (1.0±0.4 vs. 2.1±0.8 hrs). Mean serum LA remained above the level of quantification (LOQ, 50 pg/mL) through Day 49 for SC-LA, whereas for IM-LA, mean serum LA dropped below the LOQ after Day 28. Median LH concentration remained low at Day 56 in the SC-LA group, whereas LH levels began to rise after Day 35 in the IM-LA group. Consequently, serum T began to increase by Day 42 in the IM-LA group. By Day 56, 13 SC-LA subjects maintained serum T levels ≤ 50 ng/dL vs. 0 in the IM-LA group. Both SC-LA and IM-LA were well tolerated, however SC-LA subjects experienced more mild injection site disorders compared to IM-LA.

Duke Scholars

Published In

Journal of Clinical Oncology

DOI

EISSN

1527-7755

ISSN

0732-183X

Publication Date

February 20, 2017

Volume

35

Issue

6_suppl

Start / End Page

e589 / e589

Publisher

American Society of Clinical Oncology (ASCO)

Related Subject Headings

  • Oncology & Carcinogenesis
  • 3211 Oncology and carcinogenesis
  • 1112 Oncology and Carcinogenesis
  • 1103 Clinical Sciences
 

Citation

APA
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ICMJE
MLA
NLM
Moul, J. W., McLane, J. A., Atkinson, S., & Concepcion, R. S. (2017). Head-to-head pharmacokinetic and pharmacodynamic comparison of subcutaneous versus intramuscular leuprorelin acetate formulations in male patients. In Journal of Clinical Oncology (Vol. 35, pp. e589–e589). American Society of Clinical Oncology (ASCO). https://doi.org/10.1200/jco.2017.35.6_suppl.e589
Moul, Judd W., John A. McLane, Stuart Atkinson, and Raoul S. Concepcion. “Head-to-head pharmacokinetic and pharmacodynamic comparison of subcutaneous versus intramuscular leuprorelin acetate formulations in male patients.” In Journal of Clinical Oncology, 35:e589–e589. American Society of Clinical Oncology (ASCO), 2017. https://doi.org/10.1200/jco.2017.35.6_suppl.e589.
Moul JW, McLane JA, Atkinson S, Concepcion RS. Head-to-head pharmacokinetic and pharmacodynamic comparison of subcutaneous versus intramuscular leuprorelin acetate formulations in male patients. In: Journal of Clinical Oncology. American Society of Clinical Oncology (ASCO); 2017. p. e589–e589.
Moul, Judd W., et al. “Head-to-head pharmacokinetic and pharmacodynamic comparison of subcutaneous versus intramuscular leuprorelin acetate formulations in male patients.Journal of Clinical Oncology, vol. 35, no. 6_suppl, American Society of Clinical Oncology (ASCO), 2017, pp. e589–e589. Crossref, doi:10.1200/jco.2017.35.6_suppl.e589.
Moul JW, McLane JA, Atkinson S, Concepcion RS. Head-to-head pharmacokinetic and pharmacodynamic comparison of subcutaneous versus intramuscular leuprorelin acetate formulations in male patients. Journal of Clinical Oncology. American Society of Clinical Oncology (ASCO); 2017. p. e589–e589.

Published In

Journal of Clinical Oncology

DOI

EISSN

1527-7755

ISSN

0732-183X

Publication Date

February 20, 2017

Volume

35

Issue

6_suppl

Start / End Page

e589 / e589

Publisher

American Society of Clinical Oncology (ASCO)

Related Subject Headings

  • Oncology & Carcinogenesis
  • 3211 Oncology and carcinogenesis
  • 1112 Oncology and Carcinogenesis
  • 1103 Clinical Sciences