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Combinations of positive allosteric modulators and nicotinic acetylcholine receptor agonists for treating ocular conditions

An agonist and ophthalmic technology, applied in drug combinations, sensory diseases, active ingredients of heterocyclic compounds, etc., can solve problems such as providing substantial efficacy and poor patient compliance

Pending Publication Date: 2021-04-09
OYSTER POINT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, none of these options provide substantial efficacy for most populations, and these options have poor patient compliance due to side effects including post-instillation stinging / burning and bad taste (dysgeusia)

Method used

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  • Combinations of positive allosteric modulators and nicotinic acetylcholine receptor agonists for treating ocular conditions
  • Combinations of positive allosteric modulators and nicotinic acetylcholine receptor agonists for treating ocular conditions
  • Combinations of positive allosteric modulators and nicotinic acetylcholine receptor agonists for treating ocular conditions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] An example of measuring potentiation is disclosed in Example 1, which describes an assay to evaluate nAChR agonists and PAMs in α4β2 nAchR expressed in Xenopuslaevis (African clawed frog) oocytes Law.

[0027] Considerations in selecting a PAM include, but are not limited to, toxicity, side effects associated with its use, and ability to exist in a stable and easily formulated physical form. Another consideration is the selectivity of PAMs for specific nAChR subtypes. PAMs that are selective for receptors comprising a specific peripheral nAChR subtype have a higher degree of functional affinity for this receptor than other peripheral nAChR subtypes. Selectivity may be associated with at least a 5-fold affinity difference in EC50 values, at least a 10-fold affinity difference in EC50 values, at least a 20-fold affinity difference in EC50 values, or at least a 50-fold affinity difference in EC50 values.

[0028] PAMs can enhance action by enhancing the potency and / or po...

Embodiment approach I-1

[0240] Embodiment I-1. A method of treating dry eye, increasing tear production, or reducing ocular discomfort in an individual in need thereof, the method comprising administering an effective amount of a nicotinic acetylcholine receptor (nAChR) agonist or A first dose and optionally one or more subsequent doses of a pharmaceutically acceptable salt, and an effective amount of a positive allosteric modulator (PAM) or a pharmaceutically acceptable salt thereof for the first dose and optionally One or more subsequent doses are administered into the nasal cavity of said individual in need thereof, wherein said nAChR agonist or a pharmaceutically acceptable salt thereof is varenicline or a pharmaceutically acceptable salt thereof or has the structure Compound 1, or a pharmaceutically acceptable salt thereof, wherein said method results in effective treatment of said individual in need thereof.

Embodiment approach I-2

[0241] Embodiment 1-2. A compound for use in a method of treating dry eye disease, increasing tear production, or reducing ocular discomfort in an individual in need thereof, wherein said compound is an nAChR agonist or a pharmaceutically acceptable salt, wherein the method comprises administering an effective amount of a first dose of an nAChR agonist or a pharmaceutically acceptable salt thereof and optionally one or more subsequent doses, an effective amount of a PAM or a pharmaceutically acceptable salt thereof The first dose and optionally one or more subsequent doses are administered into the nasal cavity of said individual in need thereof, wherein said nAChR agonist or a pharmaceutically acceptable salt thereof is varenicline or a pharmaceutically acceptable salt thereof salt or has structure Compound 1 or a pharmaceutically acceptable salt thereof.

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Abstract

Described herein are methods and pharmaceutical formulations for treating dry eye disease, increasing tear production, and reducing ocular discomfort.

Description

[0001] Cross References to Related Applications [0002] This application claims U.S. Provisional Application No. 62 / 696,268, filed July 10, 2018, U.S. Provisional Application No. 62 / 773,993, filed November 30, 2018, and U.S. Provisional Application No. 62 / 814,754, filed March 6, 2019 interests, the contents of these Provisional Applications are incorporated herein by reference in their entirety. technical field [0003] The present disclosure describes the use of nicotinic acetylcholine receptor agonists and positive allosteric modulators in the treatment of dry eye, ocular discomfort, and increased tear production. Background technique [0004] Dry eye disease is a multifactorial, age-related disorder of the ocular surface that causes severe pain, visual impairment, tear film hyperosmolarity and instability, inflammation, and corneal injury. Dry eye disease may be characterized by loss of homeostasis of the tear film. Although the prevalence of dry eye disease is difficu...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4439A61K31/4535A61K31/506A61K31/55A61P27/02
CPCA61K31/506A61K31/55A61K31/4535A61K31/4439A61K9/0043A61P27/02A61K2300/00A61P27/04A61K31/045A61K31/13A61K31/353A61K31/404A61K31/429A61K31/473A61K31/565A61K31/7048
Inventor J·A·诺伊
Owner OYSTER POINT PHARMA
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