WO2019094390A1 – May 16, 2019 – METHODS FOR INDUCING PUPIL DILATION

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Inventors :

IFANTIDES, Cristos - 3425 Tejon Street, Denver, CO 80211

Owner :

THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE

Application Number :

WOUS18059469

Document Number :

WO2019094390A1

Priority Date :

November 10, 2017

Filing Date :

November 6, 2018

Date of Grant/ Publication :

May 16, 2019

Class :

; A61P27 / 08; A61B3 / 12; A61K31 / 00; A61K31 / 498; A61P27 / 00

Abstract

The present invention provides methods for inducing rapid and significant dilation of a subjects pupils. In certain embodiments, the method comprises upregulating the alpha-1 receptors in the eye of the subject, thereby increasing sensitivity to alpha-1 agonists. In other embodiments, such upregulation is achieved through administration of at least one compound selected from the group consisting of alpha-2 selective agonists and beta adrenoreceptor antagonists for a period of time prior to the intended time of dilation. After inducing the upregulation of alpha-1 receptors through the administration of at least one compound selected from the group consisting of alpha-2 selective agonists and beta adrenoreceptor antagonists, alpha-1 agonists can be administered to induce rapid and strong pupil dilation.

Claim(s)

1. A method of inducing dilation of at least one pupil of a subject, the method comprising administering to the subject a therapeutically effective amount of a first composition comprising at least one compound selected from the group consisting of alpha-2 selective agonists and beta adrenoreceptor antagonists, or a salt or solvate thereof; and a therapeutically effective amount of a second composition comprising at least one alpha- 1 agonist or a salt or solvate thereof.;
2. The method of claim 1, wherein the first composition comprises at least one compound selected from the group consisting of agmatine, amitraz, apraclonidine, atenolol, bisoprolol, cannabigerol, chloroethylclonidine, clonidine, brimonidine, butoxamine, detomidine, dexmedetomidine, fadolmidine, guanabenz, guanfacine, ICI-118,551, lofexidine, marsanidine, 7- Me-marsanidine, medetomidine, methamphetamine, metoprolol, mivazerol, nebivolol, 4- EMD, propranolol, rilmenidine, romifidine, SR 59230A, talipexole, tiamenidine, timolol, tizanidine, tolonidine, vortioxetine, xylazine, and xylometazoline, or a salt or solvate thereof.;
3. The method of claim 1, wherein the first composition comprises at least one compound selected from the group consisting of brimonidine and dexmedetomidine.;
4. The method of claim 1, wherein the second composition comprises at least one compound selected from the group consisting of cirazoline, epinephrine, etilefrine, metaraminol, methoxamine, midodrine, naphazoline, norepinephrine, oxymetazoline, phenylephrine, pseudoephedrine, tetrahydrozoline, synephrine, and xylometazoline, or a salt or solvate thereof.;
5. The method of claim 1, wherein the second composition comprises phenylephrine.;
6. The method of claim 1, wherein the first composition comprises at least one compound selected from the group consisting of alpha-2 selective agonists and beta adrenoreceptor antagonists at a concentration ranging from about 0.001% to about 50% (v/v).;
7. The method of claim 1, wherein the second composition comprises at least one alpha-1 agonist at a concentration ranging from about 0.001% to about 50% (v/v).;
8. The method of claim 1, wherein the composition is administered to the subject after the first composition.;
9. The method of claim 8, wherein the second composition is administered to the subject after a period of time ranging from about 1 hour to about 30 days after administration of the first composition.;
10. The method of claim 9, wherein the second composition is administered to the subject after a period of time ranging from about 1 day to about 10 days.;
11. The method of claim 8, wherein the first composition is administered to the subject two or more times before the second composition is administered.;
12. The method of claim 11, wherein the first composition is administered once per day for about 1 day to about 10 days.;
13. The method of claim 1, wherein the first composition is a pharmaceutical composition formulated for topical administration.;
14. The method of claim 13, wherein the first composition is a pharmaceutical composition formulated for topical administration to the eye of a subject.;
15. The method of claim 14, wherein the first composition is a pharmaceutical composition formulated in a form selected from the group consisting of an ophthalmic drop, ophthalmic ointment, ophthalmic gel, ophthalmic spray and ophthalmic lotion.;
16. The method of claim 1, wherein the second composition is a pharmaceutical composition formulated for topical administration.;
17. The method of claim 16, wherein the second composition is a pharmaceutical composition formulated for topical administration to the eye of a subject.;
18. The method of claim 17, wherein the second composition is a pharmaceutical composition formulated in a form selected from the group consisting of an ophthalmic drop, ophthalmic ointment, ophthalmic gel, ophthalmic spray, ophthalmic lotion, and ophthalmic intracameral injection.;
19. The method of claim 1, wherein the first composition and the second composition are administered to the subject topically or through intracameral injection.;
20. The method of claim 19, wherein the first composition and the second composition are administered directly to at least one portion of the eye of the subject.;
claim 21: 21. The method of claim 20, wherein the first composition and the second composition are administered to the subject directly to the cornea, iris, sclera, or anterior chamber of the subject.;
claim 22: 22. A kit comprising a therapeutically effective amount of a first composition comprising at least one compound selected from the group consisting of alpha-2 selective agonists and beta adrenoreceptor antagonists; and a therapeutically effective amount of a second composition comprising at least one alpha- 1 agonist.;
claim 23: 23. The kit of claim 22, wherein the first composition comprises at least one compound selected from the group consisting of agmatine, amitraz, apraclonidine, atenolol, bisoprolol, cannabigerol, chloroethylclonidine, clonidine, brimonidine, butoxamine, detomidine, dexmedetomidine, fadolmidine, guanabenz, guanfacine, ICI-118,551, lofexidine, marsanidine, 7- Me-marsanidine, medetomidine, methamphetamine, metoprolol, mivazerol, nebivolol, 4- EMD, propranolol, rilmenidine, romifidine, SR 59230A, talipexole, tiamenidine, timolol, tizanidine, tolonidine, vortioxetine, xylazine, and xylometazoline, or a salt or solvate thereof.;
claim 24: 24. The kit of claim 22, wherein the second composition comprises at least one compound selected from the group consisting of cirazoline, epinephrine, etilefrine, metaraminol, methoxamine, midodrine, naphazoline, norepinephrine, oxymetazoline, phenylephrine, pseudoephedrine, tetrahydrozoline, synephnne, and xylometazoline, or a salt or solvate thereof.;
claim 25: 25. The kit of claim 22, wherein the kit comprises at least two doses of the first composition.;
claim 26: 26. The kit of claim 22, wherein the kit comprises at least two doses of the second composition.;
claim 27: 27. The kit of claim 22, further comprising instructional materials containing instructions for inducing dilation of at least one pupil of a subject.

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