Pharmacokinetics and tolerability of a new a bioadhesive buccal testosterone tablet in testosterone deficient men
RJM Ross1, A Jabbar1, H Jones1, B Roberts1, K Dunkley1, A Long1, H Levine2 & DR Cullen1
Pharmacokinetics and tolerability of a new a bioadhesive buccal testosterone tablet in testosterone deficient men.
RJM Ross, A Jabbar, H Jones, B Roberts, K Dunkley, A Long, H Levine, DR Cullen
Objectives: A phase I single centre, open label study of the pharmacokinetics and tolerability of a buccal testosterone tablet (COL1621). Design: The study was approved by The South Sheffield Ethics Committee. Twelve testosterone deficient males were treated with the buccal tablet twice daily for 7 consecutive days. Results: After COL1621, the serum testosterone level increased to a peak concentration of 7.7 plus/minus 1.7 nanogram per millilitre at 4.8 plus/minus 5.8 hours and remained in the eugonadal range. Steady state was achieved within the first 24 hours and was maintained in the normal range. The Dihydrotestosterone (DHT) levels and Free tesosterone index followed a pattern very similar to that of testosterone. The serum testosterone / DHT ratio was within the normal male range throughout treatment. There was only one treatment-related adverse event (headache). Two thirds of patients indicated that treatment with COL 1621 was acceptable and that the tablet is convenient to use. Six patients (50.0%) preferred COL 1621 to their previous testosterone replacement therapy, 2 patients gave preference to their previous treatment and 3 patients found both treatments to be equally acceptable. Conclusion: We conclude that COL1621 can efficiently elevate serum Testosterone and Dihydrotesosterone levels in hypogonadal men within the first day of application, achieve a steady state within 24 hours and maintain serum T in the normal range with twice daily regimen. Buccal testosterone provides an effective alternative oral testosterone replacement therapy that gives physiological levels of testosterone and is well tolerated by the patients.