PD37-02 PHASE 2 RESULTS OF NOVEL ORAL TESTOSTERONE REPLACEMENT THERAPY (TSX-002) IN SYMPTOMATIC HYPOGONAGAL MEN

Abstract

You have accessJournal of UrologySexual Function/Dysfunction/Andrology: Medical and Non-Surgical Therapy I1 Apr 2015PD37-02 PHASE 2 RESULTS OF NOVEL ORAL TESTOSTERONE REPLACEMENT THERAPY (TSX-002) IN SYMPTOMATIC HYPOGONAGAL MEN Michael Oefelein, and Guru Betageri Michael OefeleinMichael Oefelein More articles by this author , and Guru BetageriGuru Betageri More articles by this author View All Author Informationhttps://doi.org/10.1016/j.juro.2015.02.2264AboutPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookTwitterLinked InEmail INTRODUCTION AND OBJECTIVES Due to poor water solubility of testosterone and a high first pass metabolism, testosterone replacement therapy (TRT) has been provided via an inconvenient parenteral route (injections, topical patches or gels). TSX-002 is a novel, pro-liposomal oral formulation of un-modified testosterone, which when hydrated forms liposomes that are capable of being absorbed by the intestinal lacteals, thus, bypassing the portal vein and hepatic metabolism. Proof of concept has been established and Phase 2 twice daily dosing is the subject matter of this trial (NCT01717768). METHODS 17 symptomatic hypogonadal (T<300ng/dl) men were enrolled in an open-label twice daily dosing regimen of TSX-002 (120 mg) and dosed for 15 days. The primary end-point is the proportion of study subjects who maintain testosterone average concentrations (Cavg0-24) between 300 and 1050 ng/dl. Bio-analytical analysis was performed at Celerion (Lincoln, NE) using Liquid-liquid extraction with analysis/detection by LC-MS/MS. An intention to treat analysis was performed. RESULTS The average testosterone concentration (Cavg0-24) on Day 1 and 15 are (Cavg = 384.77 ng/dL) and(Cavg = 306.47 ng/dL), respectively. The DHT/testosterone ratio ranged from 0.1 to 0.25 over 24 hours, which is within the normal range of 0.05 to 0.33. No T-levels above 1500 ng/dL were observed. No Serious Adverse Events (SAE) were reported. No study subject withdrew for any drug-related reason. CONCLUSIONS 120 mg TSX-002 administered orally twice daily normalized testosterone levels, and maintained a normal DHT/T ratio in symptomatic hypogonadal men. No SAEs or supra-physiological T levels (T> 1500) were observed. The pro-liposomal formulation of unmodified T safely restores physiological levels of testosterone via twice daily oral administration. Mean pharmacokinetic parameters of serum total testosterone after 120 mg TSX-002 Day 1 Tmax Cmax Cavg24 Mean 12.8 hr 850.6 ng/dL 384.8 ng/dL Standard Deviation 9.1 hr 322.6 ng/dL 118.1 ng/dL Day 15 Mean 9.5 hr 710.6 ng/dL 306.5 ng/dL Standard Deviation 9.2 hr 321.4 ng/dL 90.8 ng/dL © 2015 by American Urological Association Education and Research, Inc.FiguresReferencesRelatedDetails Volume 193Issue 4SApril 2015Page: e770 Advertisement Copyright & Permissions© 2015 by American Urological Association Education and Research, Inc.MetricsAuthor Information Michael Oefelein More articles by this author Guru Betageri More articles by this author Expand All Advertisement Advertisement PDF DownloadLoading ...