Claims for Patent: 8,106,029

Summary for Patent: 8,106,029

Title:	Use of A.sub.2A adenosine receptor agonists
Abstract:	Myocardial imaging methods are provided that are accomplished by administering doses of a pharmaceutical composition comprising one or more adenosine A.sub.2A receptor agonists, in particular regadenoson, useful for, among other indications, myocardial imaging and coronary vasodilation, in an amount sufficient to achieve at least a minimal increase in average coronary peak flow velocity.
Inventor(s):	Gordi; Toufigh (Sunnyvale, CA), Olmsted; Ann Walls (Palo Alto, CA), Lieu; Hsiao Dee (Burlingame, CA), Belardinelli; Luiz (Palo Alto, CA)
Assignee:	Gilead Sciences, Inc. (Foster City, CA)
Application Number:	12/637,583
Patent Claims:	1. A method of producing coronary vasodilation in a human in need thereof comprising administering to the human a single intravenous (iv) bolus dose of a pharmaceutical composition comprising: a) regadenoson, a compound named (1-{9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, which has the formula: ##STR00002## and b) at least one pharmaceutical excipient wherein the composition has a pH of from about 6 to about 8; wherein the single dose of the pharmaceutical composition is administered in an amount that is sufficient to increase the average coronary peak flow velocity by at least about 16.5 cm/sec to about 105 cm/sec. 2. The method of claim 1, wherein the single dose of the pharmaceutical composition further comprises a member selected from the group consisting of water, distilled water, de-ionized water, saline, buffer solutions, normal isotonic saline solution, dextrose in water, and combinations thereof. 3. The method of claim 2, wherein the single dose of the pharmaceutical composition further comprises a buffer solution and the buffer is selected from the group consisting of dibasic sodium phosphate, dibasic sodium phosphate dehydrate, monobasic sodium phosphate monohydrate, and combinations thereof. 4. The method of claim 3, wherein the buffer is dibasic sodium phosphate and monobasic sodium phosphate monohydrate. 5. The method of claim 4, wherein the single dose of the pharmaceutical composition further comprises EDTA. 6. The method of claim 5, wherein the single dose of the pharmaceutical composition further comprises propylene glycol in an amount from about 5% to about 25% (w:v). 7. The method of claim 6, wherein the propylene glycol is present in an amount from about 8% to about 20% (w:v). 8. The method of claim 7, wherein the single dose of the pharmaceutical composition comprises from about 10 to about 500 micrograms of regadenoson. 9. The method of claim 8, wherein the single dose of the pharmaceutical composition comprises from about 0.05 to about 60 .mu.g/kg of regadenoson. 10. The method of claim 1, wherein the single dose of the pharmaceutical composition is administered in about 10 to about 20 seconds. 11. The method of claim 1, wherein the amount of the single dose of the pharmaceutical composition is sufficient to raise the average coronary peak flow velocity by an amount ranging from about 16.5 to about 77.0 cm/sec. 12. A method of performing myocardial perfusion imaging of a human in need thereof, said method comprising: 1) administering to the human a single intravenous (iv) bolus dose of a pharmaceutical composition comprising: a) regadenoson, a compound named (1-{9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, which has the formula: ##STR00003## and b) at least one pharmaceutical excipient wherein the composition has a pH of from about 6 to about 8; wherein the single dose of the pharmaceutical composition is administered in an amount that is sufficient to increase the average coronary peak flow velocity by at least about 16.5 cm/sec to about 105 cm/sec; 2) administering at least one radionuclide; and 3) imaging the myocardium of the human, wherein said imaging is conducted at least concomitantly with process steps 1 and 2. 13. The method of claim 12, wherein the single dose of the pharmaceutical composition and the radionuclide are administered to the human simultaneously. 14. The method of claim 12, wherein the single dose of the pharmaceutical composition and the radionuclide are administered to the human separately. 15. The method of claim 12, wherein the myocardium imaging begins no sooner than about 1 minute from the time the single dose of the pharmaceutical composition is administered to the human.