Peptide compositions and methods of use
Inventors
BESIRLI, Cagri G. • Bridges, Alexander J. • FRESHLEY, John K. • Hunke, William A. • JOHNSON, Linda L. • Smith, Francis X. • SYLVAIN, Ethan • Zacks, David N.
Assignees
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Publication Number
US-10829518-B2
Publication Date
2020-11-10
Expiration Date
Abstract
Provided herein are compositions including peptides, pharmaceutical preparations thereof, and methods of preventing photoreceptor death therewith and protecting of retinal cells, including, but not limited to, photoreceptors and retinal pigment epithelium, from Fas- or TRAIL-mediated apoptosis.
Core Innovation
The patent describes aqueous, ocularly deliverable peptide formulations containing Compound 1, including a C-terminally amidated derivative of Met-12 and pharmaceutically acceptable salts. The formulations include an excipient for ocular delivery and are presented as pharmaceutical compositions for use in preventing extrinsic-pathway retinal cell apoptosis mediated by Fas or TRAIL.
The patent states that Compound 1 provides improved formulation behavior and/or efficacy compared with Met-12, citing better solubility and compatibility with micelles in the formulation context. The described formulation approach supports ocular delivery to one or more retinal targets including photoreceptors, retinal pigment epithelium (RPE), and retinal ganglion cells.
The patent documents ocular disease and model contexts including retinal detachment, age-related macular degeneration, glaucoma, and other retinal settings, and associates the treatment concept with reduction of apoptosis. In 661W cells, Compound 1 is described as blocking FasL-induced caspase-8 activation with a reported potency difference versus Met-12, and in rat retinal detachment models it reduces TUNEL+ apoptotic cells and is described as outperforming Met-12.
Claims Coverage
The independent claims identified in the partial content are clm-00001, clm-00008, and clm-00016. Across these, the patent covers an ocularly deliverable pharmaceutical composition containing a specified peptide compound (or salt) in an excipient system, and ocular therapeutic methods for treating retinal detachment and macular degeneration using a therapeutically effective amount of that compound (or salt).
Pharmaceutical composition with excipient and specified compound (or salt)
A pharmaceutical composition comprising an excipient and a compound having the formula, or a pharmaceutically acceptable salt thereof.
Treatment of retinal detachment by administering therapeutically effective compound (or salt)
A method for treating retinal detachment in an individual having a detached retina, comprising administering to the individual a therapeutically effective amount of a compound having the formula, or a pharmaceutically acceptable salt thereof.
Treatment of macular degeneration by administering therapeutically effective compound (or salt)
A method for treating macular degeneration in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of a compound having the formula, or a pharmaceutically acceptable salt thereof.
The claim coverage centers on pharmaceutical compositions and ocular therapeutic administration of Compound 1 and pharmaceutically acceptable salts. The composition claim anchors the excipient-containing formulation, while the method claims cover treating retinal detachment and macular degeneration by administering a therapeutically effective amount to an individual.
Stated Advantages
Improved formulation behavior and/or efficacy versus Met-12 is stated, attributed to better solubility and micelle-compatible behavior.
Reduction of TUNEL+ apoptotic retinal cells is documented in retinal detachment models, and Compound 1 is described as outperforming Met-12.
Blocking FasL-induced caspase-8 activation in 661W cells is described, with reported increased potency versus Met-12.
Documented Applications
Preventing extrinsic-pathway retinal cell apoptosis mediated by Fas or TRAIL using aqueous ocularly deliverable peptide formulations of Compound 1.
Treating retinal detachment in an individual having a detached retina by administering Compound 1 (or a pharmaceutically acceptable salt) as described in the method claims and supported by retinal detachment model outcomes.
Treating macular degeneration in an individual in need thereof, including age-related macular degeneration subtypes, with Compound 1 administration as described in the method claims.
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