Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Reexamination Certificate
2001-05-09
2003-07-22
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
C514S573000, C514S913000
Reexamination Certificate
active
06596765
ABSTRACT:
BACKGROUND OF THE INVENTION
The prior art describes the use of prostaglandin analogs containing a ring structure in the omega chain for reducing intraocular pressure. A representative patent in this area is U.S. Pat. No. 5,321,128 to Stjernschantz. These compounds contain a hydroxy group or keto group as a substituent at the 15-position. Also, one subset of these compounds contains an unsubstituted phenyl group substituted on carbon atom number 17 of the omega chain and the absence of carbons 18-20. These types of structures, where the conventional prostaglandin carbons 18-20 and their equivalent are absent are named by Stjernschantz as 18,19,20-trinor prostaglandins.
One of the above-described type of compounds, latanoprost, is now sold commercially as an IOP (intraocular pressure) reducing eye drop. The clinical dosage is 1.5 &mgr;g per dose as an eye drop, once a day. This is the U.S. FDA approved dosage. The provided liquid composition product can contain 0.005% latanoprost used at a dosage of one drop, or about 30 &mgr;l, providing 1.5 &mgr;g per dose. Latanoprost is named by Stjernschantz as 13,14-dihydro-17-phenyl-18,19,20-trinor-PGF
2
&agr; isopropyl ester.
Another compound of this family known to date is 13,14-dihydro-15-oxo-17-phenyl-18,19,20-trinor PGF
2
&agr; isopropyl ester, hereinafter referred to as 15-keto latanoprost.
The above noted patent describes a wide potential dosage range as therapeutically active. For example, see column 5, lines 33-66 of the '128 patent (“The composition contains about 0.1-30 &mgr;g, especially 1-10 &mgr;g, per application of the active substance . . . ”). Even so, the lowest dosage used in the '128 patent for any test compound for evaluating IOP reduction in humans or monkeys is 1.0 &mgr;g per eye. For 15-keto latanoprost in the '128 patent, the tested dosage in healthy human volunteers is 5 &mgr;g per eye and is 3 &mgr;g in the monkey eye. Latanoprost is tested in the '128 patent at a dosage of 1.0 &mgr;g per eye in healthy human volunteers and at a dosage of 10.4 &mgr;g in the monkey eye.
Latanoprost at its clinical concentration can cause pigmentation of the iris, a mild IOP spike and/or mild hyperemia.
SUMMARY OF THE INVENTION
It has been discovered that 15-keto latanoprost can be used in an unusually low dosage for reduction of IOP. Another embodiment of the present invention is the use of 15-keto latanoprost at a dosage up to about the clinical dosage of latanoprost. 15-keto latanoprost does not cause iridic pigmentation, an initial IOP spike nor any hyperemia at the dosages described herein. Still another embodiment of the present invention is the use of 15-keto latanoprost for maintaining IOP reduction over an extended time following an initial rapid IOP reduction bought about by another IOP reducing agent, such as latanoprost.
The embodiments of the present invention involve treatment of glaucoma where IOP reduction is needed and the lowering of IOP for purposes other than treatment of glaucoma.
This application describes other 15-keto prostaglandins useable at low dosages for treating ocular hypertension and glaucoma.
REFERENCES:
patent: 5296504 (1994-03-01), Stjernschantz et al.
patent: 5321128 (1994-06-01), Stjernschantz et al.
patent: 5422368 (1995-06-01), Stjernschantz et al.
patent: 5422369 (1995-06-01), Stjernschantz et al.
patent: 5578618 (1996-11-01), Stjernschantz et al.
patent: 5627208 (1997-05-01), Stjernschantz et al.
patent: 5849791 (1998-12-01), Stjernschantz et al.
patent: 6030999 (2000-02-01), Stjernschantz et al.
Tsuyoshi Habe et al. “Role of the Intraocular Metabolite in Intraocular Pressure Reducing Effect of Prostaglandin F2&agr; Analogue Latanoprost in Monkeys” Clinical Report vol. 28. No. 11: 3505-3509 Oct. 1994 and translation.
Hiroyoshi Osama “Comparatie study of intraocular pressure lowering effects of 0.005% latanoprost and 0.005% 15-keto-latanoprost in monkeys” Study No. YG-Oc-5056 and translation, 1994.
Hiroyoshi Osama “Intraocular pressure lowering effect of 15-keto acid of latanoprost by perfusion in the anterior chamber of monkeys” Study No. YG-Oc-5057 and translation, 1994.
Hiroyoshi Osama “Intraocular pressure lowering effect of 15-keto acid of latanoprost by intravitreal injection in normal monkeys” Study No. YG-Oc-5058 and translation, 1994.
Tsuyoshi Habe “Metabolite concentration profiled in aqueous humor following an ocular administration of3-H-Latanoprost in monkey” Study No.: MRLata99001 and translation, 1994.
Tohru Hirato and Tetsuo Deguchi “Effects of intra-anterior chamber perfusion with 2 ng/mL solution of 13,14-dihydro-15-keto-17-phenyl-18,19,20-trinor-PGF2&agr; (15—keto acid of latanoprost) on intraocular pressure in monkeys” Study No. YG-Oc-5063 and translation, 1994.
Tetsuo Deguchi “Comparison of intraocular pressure lowering effects of 0.0005% 13,14-dihydro-15-keto-17-phenyl-18,19,20-trinor-PGF2&agr;-isopropyl ester (15-keto-latanoprost) and 0.0005% 13,14-dihydro-17-phenyl-18,19,20-trinor-PGF2&agr;- isopropyl ester (latanoprost) in monkeys”, Study No. YG-Oc-5062 and translation, 1994.
Hiroyoshi Osama “Investigation of signifcance of the presence of 13,14-dihydro-15-keto type metabolite produced from latanoprost in the eye after instillation of latanoprost intraocular pressure lowering maintenance effect of 15-keto-latanoprost” Study No. YG-Oc-5060 and translation, 1994.
Fay Zohreh
Sucampo AG
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