TY - JOUR
T1 - Tonapofylline
T2 - A selective adenosine-1 receptor antagonist for the treatment of heart failure
AU - Ensor, Christopher R.
AU - Russell, Stuart D.
PY - 2010/10
Y1 - 2010/10
N2 - Importance of the field: The heart failure and cardiorenal syndromes are major public health hazards, affecting one in five persons during their lifetime. Alternatives to traditional loop-diuretics, including vasopressin and adenosine A1 receptor antagonists are now in development. Areas covered in this review: The pathophysiologic rationale for the use of tonapofylline, an intravenous and oral adenosine A1 receptor antagonist, in patients with heart failure and/or the cardiorenal syndrome are reviewed. A comprehensive review of published literature describing its medicinal chemistry, pharmacokinetics, efficacy, safety and tolerability are provided. We searched the Medline/PubMed and Embase databases for the terms 'BG9928', 'tonapofylline', 'Adentri', 'adenosine', 'heart failure', 'renal failure' and 'cardiorenal syndrome' from 1 January 1992 to the present. References from pertinent manuscripts were also reviewed for additional relevant content. What the reader will gain: The reader will better appreciate the potential role of tonapofylline in patients with heart failure and/or the cardiorenal syndrome. Additionally, the reader will gain an understanding of the current state of drug development and the rationale for the need for continued research. Take home message: Tonapofylline promotes natriuresis and diuresis, and may preserve glomerular filtration rate in patients with heart failure. Additionally, pilot data indicate that tonapofylline may be renoprotective in the setting of concomitant treatment with a loop-diuretic. Adverse effects were generally mild.
AB - Importance of the field: The heart failure and cardiorenal syndromes are major public health hazards, affecting one in five persons during their lifetime. Alternatives to traditional loop-diuretics, including vasopressin and adenosine A1 receptor antagonists are now in development. Areas covered in this review: The pathophysiologic rationale for the use of tonapofylline, an intravenous and oral adenosine A1 receptor antagonist, in patients with heart failure and/or the cardiorenal syndrome are reviewed. A comprehensive review of published literature describing its medicinal chemistry, pharmacokinetics, efficacy, safety and tolerability are provided. We searched the Medline/PubMed and Embase databases for the terms 'BG9928', 'tonapofylline', 'Adentri', 'adenosine', 'heart failure', 'renal failure' and 'cardiorenal syndrome' from 1 January 1992 to the present. References from pertinent manuscripts were also reviewed for additional relevant content. What the reader will gain: The reader will better appreciate the potential role of tonapofylline in patients with heart failure and/or the cardiorenal syndrome. Additionally, the reader will gain an understanding of the current state of drug development and the rationale for the need for continued research. Take home message: Tonapofylline promotes natriuresis and diuresis, and may preserve glomerular filtration rate in patients with heart failure. Additionally, pilot data indicate that tonapofylline may be renoprotective in the setting of concomitant treatment with a loop-diuretic. Adverse effects were generally mild.
KW - Adenosine
KW - Cardiorenal syndrome
KW - Heart failure
KW - Tonapofylline
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U2 - 10.1517/14656566.2010.514605
DO - 10.1517/14656566.2010.514605
M3 - Review article
C2 - 20807184
AN - SCOPUS:77956574334
SN - 1465-6566
VL - 11
SP - 2405
EP - 2415
JO - Expert opinion on pharmacotherapy
JF - Expert opinion on pharmacotherapy
IS - 14
ER -