BACKGROUNDPatients with high pulse pressures have an increased risk for cardiovascular events. Drugs that selectively decrease high pulse pressure may be of interest for these patients. Such drugs have a more pronounced effect on large arteries than on resistance vessels.OBJECTIVETo compare the selectivity to large arteries of the new nitric oxide donor sinitrodil with the classic nitrate isosorbide dinitrate in healthy young men in order to investigate whether it is possible to develop drugs that act more selectively on large arteries.DESIGNThe study had a double-blind, 5-way cross-over design. In randomized order, subjects received a single oral dose of 10 mg sinitrodil, 20 mg sinitrodil, 40 mg sinitrodil, isosorbide dinitrate and placebo. Measurements were performed before and 45 min after administration of the drugs. Between each drug administration, at least 3 days of wash-out was allowed.METHODSThe effects of the drugs on large arteries and resistance vessels were assessed by their effects on brachial artery compliance and total peripheral resistance, respectively.RESULTSBrachial artery compliance increased gradually with increasing doses of sinitrodil (by 10, 20 and 27% with 10, 20 and 40 mg sinitrodil, respectively). Total peripheral resistance index decreased with isosorbide dinitrate (by 11%) and 40 mg sinitrodil (by 7%), while it remained unchanged with 10 mg and 20 mg sinitrodil.CONCLUSIONSThe results of this study show that it may be possible to develop drugs with a higher selectivity for large arteries. Such drugs may be good candidates to decrease high pulse pressure without substantially decreasing mean and diastolic blood pressures.

01 Feb 1999·European Journal of Pharmaceutical SciencesQ2 · MEDICINE

In vitro skin permeation of Sinitrodil, a member of a new class of nitrovasodilator drugs

Q2 · MEDICINE

Article

Author: P. Minghetti ; M.V. Monzani ; L. Montanari ; A. Casiraghi

Clinical trials have shown the potential of benzoxazinones, a new class of organic nitrates, in cardiovascular therapy. In particular Sinitrodil possesses a coronary vascular selectivity greater than that of Nitroglycerin and isosorbide dinitrate. The objective of this study was a preliminary evaluation of the ability of these new organic nitrate derivatives to reach therapeutical steady-state plasma concentrations following a transdermal administration. In vitro permeation studies through human stratum corneum and epidermis have been conducted on two members of this class: Sinitrodil (ITF 296) and ITF 1129. Comparative studies have also been carried out with Nitroglycerin, Isosorbide dinitrate and Nicorandil. Two different fixed concentrations were tested: 0.08% w/v solution and saturated solution. Sinitrodil could be considered a good candidate for transdermal administration on the basis of the in vitro permeation results and of the known therapeutical plasma concentration.

01 Feb 1999·European Journal of Pharmaceutical SciencesQ2 · MEDICINE

Pharmacokinetics of ITF 296 (Sinitrodil) a novel organic nitrate, in healthy volunteers

Q2 · MEDICINE

Article

Author: Marco Sardina ; M.Valmen Monzani ; Alberto Sala ; Giuseppina Coltro

ITF 296 is a new orally active nitrate acting selectively on large arterial vessels over a wide range of doses. In healthy volunteers it causes less reduction in vascular resistance and less venodilatation than classic nitrates. Its pharmacokinetic profile was evaluated after intravenous infusion and oral (solution and immediate-release tablet) administration in a randomised cross-over design on 11 healthy volunteers. The plasma levels of ITF 296 and its metabolite ITF 1124 were determined by a HPLC method. The drug is rapidly distributed (mean steady-state distribution volume 53+/-17 liters) and eliminated (half-life of about 25 minutes) both after intravenous and oral administration. The total clearance is 2. 31+/-0.46 l/min. The oral solution of ITF 296 is well absorbed (Cmax=0.057 microg/ml, tmax=30 min) but it undergoes a first-pass effect (F=25%). The tablet, developed only for Phase 1 clinical studies, is characterised by an immediate release (Cmax=0.057 microg/ml, tmax=30 min). The extent of its absolute and relative bioavailability is about 14% and 53% respectively.

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Indication	Highest Phase	Country/Location	Organization	Date
Angina Pectoris	Phase 2	IT	Italfarmaco SpA	-
Angina Pectoris	Phase 2	-	Italfarmaco SA	-
Hypertension	Phase 2	IT	Italfarmaco SpA	-
Myocardial Infarction	Phase 2	-	Italfarmaco SA	-
Myocardial Ischemia	Phase 2	EU	-	-

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