Shin-Ichi Momomura1, Yoshihiko Saito2, Yoshio Yasumura3, Kazuhiro Yamamoto4, Yasushi Sakata5, Masao Daimon6, Koichiro Kinugawa7, Hiroshi Okamoto8, Naoki Dohi9, Issei Komuro10. 1. Division of Cardiovascular Medicine, Saitama Medical Center, Jichi Medical University. 2. First Department of Internal Medicine, Nara Medical University. 3. Department of Cardiology, Amagasaki Chuo Hospital. 4. Division of Cardiovascular Medicine, Department of Molecular Medicine and Therapeutics, Tottori University. 5. Department of Cardiovascular Medicine, Osaka University. 6. Department of Clinical Laboratory, The University of Tokyo. 7. Second Department of Internal Medicine, University of Toyama. 8. Department of Cardiovascular Medicine, Hokkaido University. 9. Research and Development Department, Toa Eiyo. 10. Department of Cardiovascular Medicine, The University of Tokyo.
Abstract
BACKGROUND: TY-0201 (TY) is a transdermal formulation of bisoprolol that is the free base of bisoprolol fumarate (BO), a drug widely used to treat chronic heart failure (CHF). The objectives of this phase II study were to evaluate the efficacy and safety of TY when switching from oral BO to TY in patients with CHF whose drug therapy was optimized, and to determine the dose conversion rate of BO to TY.Methods and Results: The efficacy and safety of once daily TY patch use for 16 weeks was investigated in 40 patients with CHF who were stabilized with an optimized drug treatment, including BO, after switching from BO to TY at the dose conversion rate of 5:8. The pre-switch left ventricular ejection fraction was 50.13±11.09% (mean±SD). The post-switch value was 50.87±10.79% after 16 weeks, which was not significantly different, with similar results for other efficacy and safety parameters. The 16-week study was continued for all patients without changing doses after switching to TY. No cardiovascular deaths, hospitalizations for worsening HF, or significant safety concerns were observed. CONCLUSIONS: Efficacy was maintained without significant safety concerns in patients with CHF who were stabilized with BO treatment after switching to TY, suggesting the appropriateness of the dose conversion rate.
BACKGROUND:TY-0201 (TY) is a transdermal formulation of bisoprolol that is the free base of bisoprolol fumarate (BO), a drug widely used to treat chronic heart failure (CHF). The objectives of this phase II study were to evaluate the efficacy and safety of TY when switching from oral BO to TY in patients with CHF whose drug therapy was optimized, and to determine the dose conversion rate of BO to TY.Methods and Results: The efficacy and safety of once daily TY patch use for 16 weeks was investigated in 40 patients with CHF who were stabilized with an optimized drug treatment, including BO, after switching from BO to TY at the dose conversion rate of 5:8. The pre-switch left ventricular ejection fraction was 50.13±11.09% (mean±SD). The post-switch value was 50.87±10.79% after 16 weeks, which was not significantly different, with similar results for other efficacy and safety parameters. The 16-week study was continued for all patients without changing doses after switching to TY. No cardiovascular deaths, hospitalizations for worsening HF, or significant safety concerns were observed. CONCLUSIONS: Efficacy was maintained without significant safety concerns in patients with CHF who were stabilized with BO treatment after switching to TY, suggesting the appropriateness of the dose conversion rate.