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Details for Patent: 5,910,510

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Details for Patent: 5,910,510

Title: Vision through photodynamic therapy of the eye
Abstract:Photodynamic therapy of conditions of the eye, especially those conditions characterized by unwanted neovasculature, such as age-related macular degeneration, results in enhanced visual acuity for treated subjects.
Inventor(s): Strong; H. Andrew (North Van, CA), Levy; Julia (Vancouver, CA), Huber; Gustav (Zurich, CH), Fsadni; Mario (Buelach, CH)
Assignee: QLT Phototherapeutics Inc (Vancouver, CA)
Filing Date:May 22, 1998
Application Number:09/083,480
Claims:1. A method to improve visual acuity in a human subject, which method comprises:

irradiating target ocular tissue in said subject with light emitted from a laser,

wherein said subject has been administered a formulation of a photoactive compound sufficient to permit an effective amount to localize in said target ocular tissue;

wherein the wavelength of the radiation is absorbed by the photoactive compound; and

wherein said radiation is conducted for a time and at an intensity sufficient to improve visual acuity in said subject;

wherein said irradiation is administered beginning about 5-30 minutes after said subject has been administered said formulation.

2. The method of claim 1 wherein said irradiation is administered beginning about 5 minutes after said subject has been administered said formulation.

3. The method of claim 1 wherein the eye of said subject contains unwanted neovasculature.

4. The method of claim 3 wherein the neovasculature is choroidal neovasculature.

5. The method of claim 1 wherein the photoactive agent is a polypyrrolic macrocycle.

6. The method of claim 5 wherein the photoactive agent is a green porphyrin, a hematoporphyrin derivative, a chlorin, or a phlorin.

7. The method of claim 6 wherein said photoactive compound is a green porphyrin.

8. The method of claim 7 wherein said green porphyrin is of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from the group consisting of carbalkoxyl (2-6C), alkyl (1-6C), arylsulfonyl (6-10C), cyano and --CONR.sup.5 CO-- wherein R.sup.5 is aryl (6-10C) or alkyl (1-6C);

each R.sup.3 is independently carboxyl, carboxyalkyl (2-6C) or a salt, amide, ester or acyl hydrazone thereof, or is alkyl (1-6C);

R.sup.4 is CH.dbd.CH.sub.2 or --CH(OR.sup.4')CH.sub.3 wherein R.sup.4' is H, or alkyl (1-6C) optionally substituted with a hydrophilic substituent.

9. The method of claim 8 wherein said green porphyrin is of the formula ##STR2## wherein each of R.sup.1 and R.sup.2 is independently carbalkoxyl (2-6C); one R.sup.3 is carboxyalkyl (2-6C) and the other R.sup.3 is the ester of a carboxyalkyl (2-6C) substituent; and

R.sup.4 is CH.dbd.CH.sub.2 or --CH(OH)CH.sub.3.

10. The method of claim 9 wherein said green porphyrin is of the formula ##STR3## and wherein R.sup.1 and R.sup.2 are methoxycarbonyl;

one R.sup.3 is --CH.sub.2 CH.sub.2 COOCH.sub.3 and the other R.sup.3 is CH.sub.2 CH.sub.2 COOH; and

R.sup.4 is CH.dbd.CH.sub.2 ; i.e., BPD-MA.

11. The method of claim 1 wherein said formulation is a liposomal preparation.

12. The method of claim 1 wherein said subject has been diagnosed with age-related macular degeneration (AMD).

13. The method of claim 1 wherein the subject has been diagnosed with a condition selected from the group consisting of macular degeneration, ocular histoplasmosis syndrome, myopia, and inflammatory diseases.

14. The method of claim 1 wherein said irradiation is administered at an irradiance of about 600 mW/cm.sup.2 to provide a total fluence of 50 J/cm.sup.2 -150 J/cm.sup.2 of said light.

15. The method of claim 2 wherein the eye of said subject contains unwanted neovasculature.

16. The method of claim 15 wherein the neovasculature is choroidal neovasculature.

17. The method of claim 2 wherein the photoactive agent is a polypyrrolic macrocycle.

18. The method of claim 17 wherein the photoactive agent is a green porphyrin, a hematoporphyrin derivative, a chlorin, or a phlorin.

19. The method of claim 18 wherein said photoactive compound is a green porphyrin.

20. The method of claim 17 wherein said green porphyrin is of the formula ##STR4## wherein each of R.sup.1 and R.sup.2 is independently selected from the group consisting of carbalkoxyl (2-6C), alkyl (1-6C), arylsulfonyl (6-10C), cyano and --CONR.sup.5 CO-- wherein R.sup.5 is aryl (6-10C) or alkyl (1-6C);

each R.sup.3 is independently carboxyl, carboxyalkyl (2-6C) or a salt, amide, ester or acyl hydrazone thereof, or is alkyl (1-6C);

R.sup.4 is CH.dbd.CH.sub.2 or --CH(OR.sup.4)CH.sub.3 wherein R.sup.4 is H, or alkyl (1-6C) optionally substituted with a hydrophilic substituent.

21. The method of claim 20 wherein said green porphyrin is of the formula ##STR5## wherein each of R.sup.1 and R.sup.2 is independently carbalkoxyl (2-6C); one R.sup.3 is carboxyalkyl (2-6C) and the other R.sup.3 is the ester of a carboxyalkyl (2-6C) substituent; and

R.sup.4 is CH.dbd.CH.sub.2 or --CH(OH)CH.sub.3.

22. The method of claim 21 wherein said green porphyrin is of the formula ##STR6## and wherein R.sup.1 and R.sup.2 are methoxycarbonyl;

one R.sup.3 is --CH.sub.2 CH.sub.2 COOCH.sub.3 and the other R.sup.3 is CH.sub.2 CH.sub.2 COOH; and

R.sup.4 is CH.dbd.CH.sub.2 ; i.e., BPD-MA.

23. The method of claim 2 wherein said formulation is a liposomal preparation.

24. The method of claim 2 wherein said subject has been diagnosed with age-related macular degeneration (AMD).

25. The method of claim 2 wherein the subject has been diagnosed with a condition selected from the group consisting of macular degeneration, ocular histoplasmosis syndrome, myopia, and inflammatory diseases.

26. The method of claim 2 wherein said irradiation is administered at an irradiance of about 600 mW/cm.sup.2 to provide a total fluence of 50 J/cm.sup.2 -150 J/cm.sup.2 of said light.
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