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Fig 1.

Flow diagram of the study.

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Fig 1 Expand

Fig 2.

Noncontact specular microscopy images of corneal endothelium before and after ripasudil administration in instilled eye.

In 3 of 6 typical healthy subjects, before administration (Top row), 1.5 hours after the initial administration on day 0 (Second row), 6 hours after the initial administration on day 0 (Third row), and before the final administration on day 7 (Bottom row), in subject 1 (Left column), subject 2 (Middle column), and subject 5 (Right column). Before ripasudil administration, corneal endothelial cells showed regular hexagonal monolayer with clear cell borders in all subjects (Top row). One and half hours after ripasudil administration, endothelial cell showed irregular and indistinct cell borders with guttae like dark cells in subjects 1 (Left, second) and 2 (Middle, second). In subject 5, no analyzable image was obtained by noncontact specular microscopy (Right, second). At 6 hours post-dose or later, corneal endothelial morphology returned to normal in subjects 1 and 2. Some guttae like dark cells were still observed in subject 5 at 6 hours on day 0 (Right, third) and prior to the final administration on day 7 (Right, bottom).

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Fig 2 Expand

Fig 3.

Contact specular microscopy images of corneal endothelium before and after ripasudil administration in instilled eye.

In 3 of 6 typical healthy subjects, before administration (Top row), 1.5 hours after the initial administration on day 0 (Second row), 6 hours after the initial administration on day 0 (Third row), and before the final administration on day 7 (Bottom row), in subject 1 (Left column), subject 2 (Middle column), and subject 5 (Right column). Before ripasudil administration, wide-field contact specular microscopy revealed regular hexagonal monolayer of corneal endothelial cells in all subjects (Top row). One and half hours after ripasudil administration, corneal endothelial cells showed indistinct cell borders with a very few dark cells (Second row), but characteristic morphology of guttae was not observed. These morphological changes were detected in common in all subjects. At 6 hours post-dose or later, corneal endothelial morphology came back to normal in all subjects (Third and bottom rows).

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Fig 3 Expand

Table 1.

Endothelial Cell Density Examined by Noncontact Specular Microscopy Before and After the Administrations of Ripasudil in Instilled Eye.

N/A = not able to be calculated or unreliable data, SD = standard deviation. Values are the number of corneal endothelial cells (/mm2).

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Table 1 Expand

Table 2.

Endothelial Cell Density Examined by Contact Specular Microscopy Before and After the Administrations of Ripasudil in Instilled Eye.

N/A = not able to be calculated or unreliable data, SD = standard deviation. Values are the number of corneal endothelial cells (/mm2).

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Table 2 Expand

Table 3.

Central Corneal Thickness Before and After the Administrations of Ripasudil in Instilled Eye.

SD = standard deviation. Values are the central corneal thickness (μm) examined by Pentacam Scheimpflug topography.

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Table 3 Expand

Table 4.

Corneal Volume of 5mm Diameter Area of Central Cornea Before and After the Administrations of Ripasudil in Instilled Eye.

SD = standard deviation. Values are the corneal volume of 5mm diameter area (mm3).

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Table 4 Expand

Table 5.

Endothelial Cell Density Examined by Noncontact Specular Microscopy Before and After the Administrations of Ripasudil in Non-instilled Eye.

SD = standard deviation. Time points indicate administrations of ripasudil in instilled eye. Values are the number of corneal endothelial cells (/mm2).

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Table 5 Expand

Table 6.

Endothelial Cell Density Examined by Contact Specular Microscopy Before and After the Administrations of Ripasudil in Non-instilled Eye.

SD = standard deviation. Time points indicate administrations of ripasudil in instilled eye. Values are the number of corneal endothelial cells (/mm2).

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Table 6 Expand

Table 7.

Central Corneal Thickness in Non-instilled Eye.

SD = standard deviation. Time points indicate administrations of ripasudil in instilled eye. Values are the central corneal thickness measured by Pentacam Scheimpflug topography (μm).

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Table 7 Expand

Table 8.

Corneal Volume of 5mm Diameter Area of Central Cornea in Non-instilled Eye.

SD = standard deviation. Time points indicate administrations of ripasudil in instilled eye. Values are the corneal volume (mm3).

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Table 8 Expand

Fig 4.

Corneal pachymetry mapping in instilled eye.

Corneal pachymetry mapping of subject 4 on day 0 before administration (Top left), 1.5 hours (Top right) and 6 hours (Bottom left) after the initial administration and on day 7 prior to the final administration (Bottom right) of ripasudil in instilled eye. Throughout the observation period, there was no change of corneal thickness of the center and peripheral cornea.

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Fig 4 Expand

Fig 5.

Noncontact specular microscopy images of corneal endothelium before and after ripasudil administration in non-instilled eye.

In 3 of 6 typical healthy subjects, before administration (Top row), 1.5 hours after the initial administration on day 0 (Second row), 6 hours after the initial administration on day 0 (Third row), and before the final administration on day 7 (Bottom row) of ripasudil in non-instilled eye, in subject 1 (Left column), subject 2 (Middle column), and subject 5 (Right column). Throughout the observation period, there were no morphological changes of corneal endothelial cells in non-instilled eye.

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Fig 5 Expand

Fig 6.

Contact specular microscopy images of corneal endothelium before and after ripasudil administration in non-instilled eye.

In 3 of 6 typical healthy subjects, before administration (Top row), 1.5 hours after the initial administration on day 0 (Second row), 6 hours after the initial administration on day 0 (Third row), and before the final administration on day 7 (Bottom row) of ripasudil in non-instilled eye, in subject 1 (Left column), subject 2 (Middle column), and subject 5 (Right column). Throughout the observation period, there were no morphological changes of corneal endothelial cells in non-instilled eye.

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Fig 6 Expand