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Netarsudil

  • Prescription medicine
  • Prescription only
  • Identity checked
  • Sources last checked 2026-09-04

This page shows what was measured, who it was measured in, and what that does not settle.

What Netarsudil does in the body

Netarsudil blocks the enzyme that keeps those cables under tension.

Fluid leaves the eye mainly through a spongy mesh at the base of the iris. In glaucoma that mesh stiffens, because the cells in it are holding themselves tight with an internal scaffolding of protein cables. The cells relax, the mesh opens, and fluid drains through the route it was always meant to use.

Why people take it. High pressure inside the eye, treated at the blocked drain itself

What happened in people

Non-inferiority to twice-daily timolol in the per-protocol population with maximum baseline IOP below 25 mmHg, across 1,167 randomised patients

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

The recorded finding that sits closest to something a person would notice. Written into the record, not signed off, and it carries no population or interval.

The limit that matters most

That netarsudil works by relaxing the trabecular meshwork — the approved label states the exact mechanism is unknown

Where it acts
The trabecular meshwork and Schlemm’s canal — the eye’s main drain, and the actual site of disease in open-angle glaucoma
Kind of result
The kind of result is not recorded
Supervision
RNAWiki has not recorded a supervision or regulatory status for this substance.

What the registries record it as

  • The substance registry classes this as chemical.

    FDA substance registry · VL756B1K0U · read 2026-08-29

Where each sentence above came from

A person wrote this explanation into the record, with the studies named in the path below.

The recorded use, written for a reader without medical training. Not signed off.

A limit recorded against this substance. Not signed off as a reviewed claim.

The four opening statements run to 95 words.

Words this page uses

Four words worth knowing first

Chosen from what this page shows, with each one explained before the word it depends on.

Placebo

A placebo is a dummy treatment given so the real one can be compared with it.

A picture of it, and where the picture fails

A placebo is like a blank control in an experiment.

Where that stops being true. A blank does nothing. People given a placebo often do get better.

What people get wrong. A placebo effect is read as imaginary. The improvement is measured and real.

An inactive intervention matched in appearance to the test intervention, used to control for non-specific effects.

Comparator

A comparator is whatever the treatment was measured against.

A picture of it, and where the picture fails

It is like the other runner in a race.

Where that stops being true. A race has one winner. A study can show both arms improved.

What people get wrong. Results are read without asking what the other group got. Beating nothing is not beating a treatment.

The control condition against which the experimental intervention is assessed.

Randomisation

Randomisation means chance decides who gets which treatment.

A picture of it, and where the picture fails

It is like a coin toss deciding the groups.

Where that stops being true. A coin toss is fair once. Fairness here comes from doing it for everyone.

What people get wrong. It is thought to make groups identical. It makes them similar on average, including on things nobody measured.

Allocation of participants to arms by a chance process, so that unmeasured factors are balanced in expectation.

What happened in peopleRead from sources, not yet reviewed

What happened in people

Each card is one study: the exact question it asked, who was in it, and whether it showed what it set out to show.

Non-inferiority of netarsudil 0.02% once daily to timolol 0.5% twice daily on intraocular pressure

The study did not show it

Who was studied
ROCKET-1 (NCT02207491)
How many people
411
Study design
Double-masked, randomised, non-inferiority, 3-month
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Non-inferiority met in the per-protocol population with maximum baseline IOP < 25 mmHg as a POST HOC outcome measure; not met across the full enrolled range
Repeated elsewhere
Partially Replicated

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. The population in which the drug can claim to match timolol was defined after the results were seen. Conjunctival hyperemia occurred in 53% (108 of 203) against 8% (17 of 208) on timolol, P < .0001.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Topical ophthalmic solution 0.02%, instilled once daily in the evening

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

Non-inferiority to timolol in the per-protocol population with maximum baseline IOP < 25 mmHg

The study showed what it set out to show

Who was studied
ROCKET-2 (NCT02207621)
How many people
756
Study design
Double-masked, randomised, multicentre, parallel-group, non-inferiority, 12-month
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Non-inferiority met; mean IOP at 8 AM 17.9 to 18.8 mmHg (netarsudil once daily), 17.2 to 18.0 (twice daily) and 17.5 to 17.9 (timolol) over 12 months
Repeated elsewhere
Partially Replicated

What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.

The limits of this study, and where it came from

Main limit. Conjunctival hyperemia 61% and 66% against timolol’s 14%; cornea verticillata 26% and 25% against 1%; conjunctival haemorrhage 20% and 19% against 1%. A separate non-interventional Corneal Observation Study was run for patients developing verticillata.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Topical ophthalmic solution 0.02%, instilled once daily in the evening

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

Intraocular pressure with once-daily netarsudil against twice-daily timolol in patients with baseline IOP below 30 mmHg

The study showed what it set out to show

Who was studied
ROCKET-4 (NCT02558374)
How many people
708
Study design
Randomised, double-masked, phase 3, 6-month
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Reported by the label as demonstrating up to 5 mmHg reductions, with reductions similar to timolol for baseline IOP < 25 mmHg and up to 3 mmHg worse than timolol at morning time points for baseline IOP ≥ 25 mmHg
Repeated elsewhere
Partially Replicated

What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.

The limits of this study, and where it came from

Main limit. The stratification by baseline pressure at 25 mmHg recurs across all three registration studies and is the boundary of the drug’s demonstrated equivalence. Every comparison is against timolol, never against a prostaglandin analogue.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Topical ophthalmic solution 0.02%, instilled once daily in the evening

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

What we know
RNAWiki holds 3 written-up human studies for this substance, each with the question it asked.
How we know it
Each card names the study, the number of people and what the study set out to measure.
What this does not prove
These summaries were written by a person and have not been signed off as reviewed claims.
Why it matters
A study that failed is as informative as one that worked, and both are here.
What we still do not know
No reviewed claim exists, so no exact population, effect size or interval is published yet.

What it changes in the bodyRead from sources, not yet reviewed

The path through the body

From what a person takes to what changes. A solid line is a step measured in people. A dashed line is a step nobody has measured that way.

  1. Start

    Netarsudil

    What a person takes: Topical ophthalmic solution 0.02%, instilled once daily in the evening.

    The measurement behind this step

    A once-daily evening drop of an ester prodrug, cleaved by ocular esterases during corneal passage to the more potent active metabolite netarsudil-M1. Evening dosing was used throughout the registration programme. Supplied as the dimesylate salt.

  2. Getting in

    One drop in the evening, containing a disguised molecule

    What is in the bottle is not what does the work. A chemical group is attached that gets cut off inside the eye, releasing a more potent version.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step

    Netarsudil dimesylate 0.02% is instilled once daily in the evening. The molecule is an ester of 2,4-dimethylbenzoic acid, and ocular esterases cleave it to netarsudil-M1, which is a more potent Rho kinase inhibitor than the parent. The ester exists to carry the compound across the cornea, as in the prostaglandin analogues.

  3. Reaching the cell

    It reaches the mesh at the base of the iris

    The active form reaches the spongy tissue where fluid normally leaves the eye — the tissue that is actually blocked in this disease, and that no earlier drug touched.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step

    Netarsudil-M1 reaches the trabecular meshwork and the inner wall of Schlemm’s canal, the site of the outflow resistance that defines open-angle glaucoma. Every earlier drug class acts either on aqueous production at the ciliary body or on the uveoscleral pathway, both anatomically distinct from this tissue.

  4. What it acts on

    It blocks the enzyme holding the cells under tension

    The cells in that mesh keep themselves taut with internal protein cables. One enzyme maintains the tension. Netarsudil blocks it.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step

    Netarsudil-M1 inhibits Rho-associated coiled-coil containing protein kinase, which phosphorylates myosin light chain and the myosin phosphatase targeting subunit to sustain actomyosin contractility. Inhibition permits dephosphorylation, disassembling actin stress fibres and focal adhesions in trabecular meshwork cells. The drug also inhibits the norepinephrine transporter, a second and pharmacologically separate activity.

  5. The change it makes

    The mesh relaxes and the drain opens

    With the tension released, the tissue becomes less stiff and the spaces in it widen. Fluid leaves through the route it was always supposed to use.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step

    Loss of cell contractility and extracellular matrix tension reduces outflow resistance and increases conventional outflow facility. Netarsudil additionally lowers episcleral venous pressure, the back-pressure against which the conventional pathway drains, and reduces aqueous production through norepinephrine transporter inhibition. The label declines to commit to any of this, stating that the exact mechanism is unknown.

  6. What that does for a person

    Pressure falls, and holds for a year

    Pressure drops by up to five millimetres of mercury and stays down across twelve months. The comparison it was tested against is timolol, not the stronger modern drops.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step

    The label reports up to 5 mmHg reductions with once-daily evening dosing. In the twelve-month study, mean pressure at 8 AM fell from a baseline of 22.5 to 22.6 mmHg to 17.9 to 18.8 mmHg on once-daily netarsudil against 17.5 to 17.9 on timolol, sustained throughout. Non-inferiority was demonstrated only in the population with maximum baseline pressure below 25 mmHg.

  7. What that does for a person

    The same relaxation reddens the surface vessels

    The enzyme being blocked also keeps blood vessels in the white of the eye constricted. Blocking it dilates them, which is why more than half of patients get red eyes.

    Measured in people. Written by a person from the study named beside the step. Not signed off as a reviewed claim.

    The measurement behind this step

    Rho kinase inhibition relaxes vascular smooth muscle in conjunctival vessels, producing hyperemia in 53% of patients in the controlled trials, 61% at twelve months on once-daily dosing and 66% on twice-daily, against 8% to 14% on timolol. Six per cent of patients discontinued for hyperemia. Cornea verticillata occurred in about a quarter of patients at twelve months and conjunctival haemorrhage in about a fifth, against 1% each on timolol.

No suggested links are held for this record, so nothing is hidden from this path.

What we know
The record describes 6 steps from taking it to an effect in a person.
How we know it
Each step names the study behind it in the technical detail beside it.
What this does not prove
A change inside the body is a reason to look. It is not a result in a person.
Why it matters
A reader can see exactly where the chain stops being measured in people.
What we still do not know
No reviewed claim binds any of these steps to a named population.

What is missing or unclearRead from sources, not yet reviewed

Were people like you studied?

RNAWiki cannot tell whether a study fits you. It can show who was in it, and where the result stops carrying.

Who was studied

People similar to this profile were included.

  • Adults with open-angle glaucoma or ocular hypertension, usually after or alongside a prostaglandin analogue. The label reports it works less well than timolol in patients whose starting pressure is 25 mmHg or above.

Who is missing from the studies

  • Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

What the label states about particular groups

  • On pediatric, the label states: “Safety and effectiveness in pediatric patients below the age of 18 years have not been established.”

    US prescribing information · 7d4f0e3a-5b86-4c43-982a-813b22ae7e22 · read 2026-08-30

  • On older people, the label states: “No overall differences in safety or effectiveness have been observed between elderly and other adult patients.”

    US prescribing information · 7d4f0e3a-5b86-4c43-982a-813b22ae7e22 · read 2026-08-30

  • On people who are pregnant, the label states: “Risk Summary There are no available data on RHOPRESSA use in pregnant women to inform any drug associated risk; however, systemic exposure to netarsudil from ocular administration is low [see Clinical Pharmacology ( 12.3 ) ] .”

    US prescribing information · 7d4f0e3a-5b86-4c43-982a-813b22ae7e22 · read 2026-08-30

  • On people who are breastfeeding, the label states: “Risk Summary There are no data on the presence of RHOPRESSA in human milk, the effects on the breastfed infant, or the effects on milk production.”

    US prescribing information · 7d4f0e3a-5b86-4c43-982a-813b22ae7e22 · read 2026-08-30

Where the result stopped carrying

  • ROCKET-1 did not meet non-inferiority across its full enrolled range; the claim rests on a post hoc restricted population
  • The label states that above 25 mmHg baseline pressure, netarsudil gives smaller morning reductions than timolol, by as much as 3 mmHg
  • More than half of patients develop red eyes and 6% stop the drug for that alone
  • About a quarter develop corneal deposits over a year, a finding that required its own dedicated observational sub-study
  • This is a scope explorer, not a diagnosis engine.
  • It shows who was studied so you can see whether people similar to you were included.

RNAWiki cannot tell whether a study fits you. It can show who was in it.

What it would be like to takeRead from sources, not yet reviewed

Why it might seem to do nothing

A real effect and a noticed effect are different things. These are the recorded reasons the two come apart.

It was studied in different people

The people in the studies were not much like the reader.

On this record: Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

The evidence may simply be wrong

Small early studies often do not hold up.

On this record: RNAWiki has not yet published a reviewed conclusion for this use.

Other reasons RNAWiki checked and found nothing for (11)
It was studied for a different goal
The studies measured something else entirely. Nothing in this record points to this reason.
A different form was studied
The studied form is not the form on the shelf. Nothing in this record points to this reason.
There was nothing to correct
Where a level is already normal, topping it up may change nothing. Nothing in this record points to this reason.
Something else had to happen too
In the studies it was paired with training, a diet or another treatment. Nothing in this record points to this reason.
The change is too small to feel
A real change can still sit below what a person notices. Nothing in this record points to this reason.
Day-to-day swing hides it
Sleep, food, stress and time of day move most numbers more than this would. Nothing in this record points to this reason.
Not enough time yet
The studies ran longer than the person has waited. Nothing in this record points to this reason.
It was not taken as studied
Missed days change the result, and studies count them. Nothing in this record points to this reason.
Something else changed at the same time
Two changes at once cannot be told apart afterwards. Nothing in this record points to this reason.
The product may not be what it says
Contents of a sold product are not always what the label states. Nothing in this record points to this reason.
No recorded reason
RNAWiki has nothing stored that would explain it. Nothing in this record points to this reason.

None of these is a reason to take more. Taking more is not a step this page ever suggests.

What it would be like to takeRead from sources, not yet reviewed

What taking it involves

The recorded facts about getting hold of it and using it. Nothing here is a suggestion about what you should do.

How it is supplied

Prescription only

Quoted from a source

Where this came from

Copied from a source RNAWiki stored, with the source named.

Read from the recorded approval status.

No source is stored against this line.

Form and route

Topical ophthalmic solution 0.02%, instilled once daily in the evening

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

The form and route recorded on this substance.

No source is stored against this line.

Who oversees it

RNAWiki has not recorded a supervision or regulatory status for this substance.

Quoted from a source

Where this came from

Copied from a source RNAWiki stored, with the source named.

No register row and no identity class settled the question.

No source is stored against this line.

What is in the pack

A once-daily evening drop of an ester prodrug, cleaved by ocular esterases during corneal passage to the more potent active metabolite netarsudil-M1. Evening dosing was used throughout the registration programme. Supplied as the dimesylate salt.

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

Recorded notes on how this is sold and what that means for what is in the pack.

No source is stored against this line.

Where it is registered

Regulatory records are listed in the technical disclosure at the foot of this page.

Counted from records

Where this came from

A count of rows RNAWiki holds. It describes our records, not your body.

Register entries are stored per jurisdiction and shown with their dates.

No source is stored against this line.

Why people stop

Not recorded.

Nothing recorded

Where this came from

RNAWiki holds nothing here and says so rather than guessing.

No record of why people stopped taking it is stored for this substance.

No source is stored against this line.

What it would be like to takeRead from sources, not yet reviewed

What can go wrong

Sorted by where each line came from. A regulator's label and a report somebody sent in are not the same kind of fact.

Worth asking a clinician aboutWritten into the record from the studies named on this page

Conjunctival hyperemia in 53% of patients, with 6% discontinuing because of it, rising to 61% and 66% for once- and twice-daily dosing at twelve months against 14% on timolol. Corneal verticillata, instillation site pain and conjunctival haemorrhage each at approximately 20% in the label, with verticillata at 26% and haemorrhage at 20% in the twelve-month study against 1% each on timolol. Instillation site erythema, corneal staining, blurred vision, increased lacrimation, eyelid erythema and reduced visual acuity also reported. No systemic beta-blockade and no respiratory or cardiac contraindications. The hyperemia and the corneal deposits are both direct consequences of the mechanism rather than formulation problems, so neither is addressable by reformulation.

Nobody counted how many people took this and were fine, so this cannot be turned into a rate.

Where this came from

Over a long time. No completed tested study window is recorded, so long-term effects are not established by the registry record.

Groups the studies covered thinly. Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

What is missing or unclearRead from sources, not yet reviewed

Does the exact form matter?

Evidence belongs to the exact thing that was tested. A different salt, a different mixture or a different preparation is a different question.

The form that was studied

Topical ophthalmic solution 0.02%, instilled once daily in the evening

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

The form used in the studies cited on this page.

No source is stored against this line.

What is sold

Evening dosing was used throughout the registration programme. Supplied as the dimesylate salt.

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

Recorded notes on which forms are sold and how they compare.

No source is stored against this line.

What is recorded as being sold

  • 4 products list this as an active ingredient in the United States drug directory. 3 of them contain it and nothing else.

    FDA National Drug Code directory · 70727-497 · read 2026-08-29

  • They are sold as powder and solution/ drops, taken ophthalmic and topical.

    FDA National Drug Code directory · 70727-497 · read 2026-08-29

  • The regulator's established pharmacologic class for it is rho kinase inhibitor [epc] and rho kinase inhibitors [moa].

    FDA National Drug Code directory · 70727-497 · read 2026-08-29

  • 2 published labels name it as an active ingredient. 1 of them describe this substance alone, which is where its own label text on this page comes from.

    US prescribing information · 7d4f0e3a-5b86-4c43-982a-813b22ae7e22 · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · 7d4f0e3a-5b86-4c43-982a-813b22ae7e22 · read 2026-08-29

  • Rhopressa is ophthalmic at 3 DOSAGE FORMS AND STRENGTHS Ophthalmic solution containing netarsudil 0.02% (0.2 mg/mL)., recorded as fda label in effect 2026-01-20 in the United States.

    US prescribing information · 7d4f0e3a-5b86-4c43-982a-813b22ae7e22 · read 2026-08-30

Evidence carries across two names for one substance. It does not carry across a salt, a mirror form or a mixture.

What it would be like to takeRead from sources, not yet reviewed

What you could measure

This one is decided with a clinician, so this section holds questions to ask rather than a plan to run.

RNAWiki could not confidently classify this substance, so no self-experiment plan is offered.

Questions worth asking

  • Which of the trials of Netarsudil studied people like me?
  • What was measured, and for how long?
  • Was the result a laboratory value or a health outcome?
  • What would we watch for, and when would we stop?

Tracking can show whether something changed for you. It cannot show what caused it.

RNAWiki records evidence. It does not say whether this substance is right for you.

What is missing or unclearRead from sources, not yet reviewed

Claims that go past the evidence

Things said about this substance that sound reasonable, and the exact step that is missing between the evidence and the claim.

Goes past the evidence

That netarsudil works by relaxing the trabecular meshwork — the approved label states the exact mechanism is unknown

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

Goes past the evidence

That a novel outflow mechanism justifies 84 times the acquisition cost of generic latanoprost, which lowers pressure more in indirect comparison

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

Goes past the evidence

That the ROCKET-1 non-inferiority result is equivalent in weight to ROCKET-2’s; one was pre-specified and the other post hoc

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

Goes past the evidence

That non-inferiority to timolol implies comparability with the prostaglandin analogues, which the drug has never been tested against as a primary comparison

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

What is missing or unclearRead from sources, not yet reviewed

What nobody knows yet

Open questions, each with why it is open and what would close it.

Missing populations

Which groups were under-represented in the studies has not been recorded.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Missing long-term data

No completed tested study window is recorded.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

No reviewed conclusion

RNAWiki has not yet published a reviewed conclusion for this use.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Missing interaction studies

No interaction was found in the registers checked. Not finding one is not the same as showing there is none.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Formulation uncertainty

Several salts, forms or products of Netarsudil are recorded. Results from one form may not transfer to another.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Mechanism not reviewed

No reviewed mechanism story exists for this substance.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

What happened in peopleRead from sources, not yet reviewed

Check any of this yourself

Every line above traced back to the study it came from. This is the technical layer, and the vocabulary changes here.

Every line above can be traced to the study named beside it. Follow the link and read it.

ROCKET-1 met its endpoint only as a post hoc analysis in a subgroup
In plain words
Two trials in 1,167 patients tested whether netarsudil matched timolol. In the first one, the answer across the full pressure range was no, and the claim of non-inferiority comes from an analysis of a narrower group decided on after the results were in.
What was measured
Non-inferiority to timolol in the per-protocol population with maximum baseline IOP below 25 mmHg
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
ROCKET-1 (411 patients) and ROCKET-2 (756 patients) were double-masked randomised non-inferiority trials enrolling 1,167 patients in total, comparing netarsudil 0.02% once daily against timolol 0.5% twice daily, with an additional netarsudil twice-daily arm in ROCKET-2. The published report states that netarsudil once daily was non-inferior to timolol in the per-protocol population with maximum baseline intraocular pressure below 25 mmHg in both studies — and specifies that this was the primary outcome measure and population in ROCKET-2, and a post hoc outcome measure in ROCKET-1. ROCKET-1 did not meet non-inferiority across its full enrolled range. The restriction is not a footnote: it defines the population in which the drug can claim to match a sixty-year-old generic.
Source
Serle JB et al., Am J Ophthalmol 2018;186:116-127 (ROCKET-1 NCT02207491 and ROCKET-2 NCT02207621)
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
The label says it works worse than timolol above 25 mmHg
In plain words
The prescribing information states it plainly: in patients whose starting pressure was 25 millimetres of mercury or higher, netarsudil lowered morning pressure less than timolol did, by as much as three millimetres.
What was measured
Mean intraocular pressure reduction at morning time points, stratified by baseline pressure above and below 25 mmHg
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
The Clinical Studies section states that across three randomised controlled trials — Study 301 (NCT02207491), Study 302 (NCT02207621) and Study 304 (NCT02558374) — netarsudil 0.02% once daily in the evening produced up to 5 mmHg reductions in pressure. For patients with baseline pressure below 25 mmHg, reductions were similar to timolol 0.5% twice daily. For patients at or above 25 mmHg, netarsudil resulted in smaller mean reductions at the morning time points than timolol at the Day 43 and Day 90 visits, with the difference as high as 3 mmHg favouring timolol. Studies 301 and 302 enrolled patients with baseline pressure below 27 mmHg and Study 304 below 30 mmHg. A drug that underperforms a generic beta-blocker at the pressures where treatment is most urgent has a narrower place than its approval implies.
Source
RHOPRESSA (netarsudil ophthalmic solution) 0.02% US prescribing information, Clinical Studies section (NDA 208254)
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
Half the eyes go red, and 6% of patients stop because of it
In plain words
Conjunctival redness affected 53% of patients in the controlled trials and 61% over twelve months. On timolol it was 8% to 14%. Six in a hundred patients stopped the drug because of the redness alone.
What was measured
Incidence of conjunctival hyperemia and discontinuation for hyperemia, netarsudil against timolol
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
In the ROCKET-1 and ROCKET-2 three-month report, conjunctival hyperemia was the most frequent adverse event, ranging from 50% (126 of 251, ROCKET-2) to 53% (108 of 203, ROCKET-1) for netarsudil once daily, 59% (149 of 253, ROCKET-2) for twice daily, against 8% (17 of 208, ROCKET-1) to 11% (27 of 251, ROCKET-2) for timolol (P<.0001 for netarsudil against timolol). At twelve months in ROCKET-2 the figures were 61% once daily, 66% twice daily and 14% for timolol. The label records 53% and states that 6% of patients discontinued therapy because of conjunctival hyperemia. The hyperemia follows directly from Rho kinase inhibition relaxing conjunctival vascular smooth muscle, so it is inseparable from the mechanism.
Source
Serle JB et al., Am J Ophthalmol 2018;186:116-127; Kahook MY et al., Am J Ophthalmol 2019;200:130-137 (ROCKET-2 12-month)
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim
A quarter of patients develop deposits in the cornea
In plain words
Whorl-shaped deposits build up in the surface layer of the cornea in about a quarter of patients over a year. On timolol it happens to one in a hundred. Patients do not notice them; a clinician has to look.
What was measured
Incidence of cornea verticillata and conjunctival haemorrhage at 12 months, netarsudil against timolol
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
In the twelve-month ROCKET-2 study of 756 patients — netarsudil once daily 251, twice daily 254, timolol 251 — corneal deposits (cornea verticillata) occurred in 26%, 25% and 1% respectively. Conjunctival haemorrhage, typically petechial, occurred in 20%, 19% and 1%. All three findings were generally scored as mild. The study ran a separate non-interventional Corneal Observation Study specifically for patients who developed verticillata, which is an acknowledgement that the finding needed dedicated follow-up rather than routine adverse event capture. The label summarises corneal verticillata, instillation site pain and conjunctival haemorrhage together at approximately 20%. Verticillata are asymptomatic in most patients and reported as reversible on discontinuation, which is reassuring and also means the true incidence outside a trial depends entirely on whether anyone is looking.
Source
Kahook MY et al., Am J Ophthalmol 2019;200:130-137 (ROCKET-2, 12 months)
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
Twelve-month durability with no loss of effect
In plain words
Over a full year, netarsudil held pressure in the same range as timolol, without the drift that beta-blockers can show. The pressures achieved were within about a millimetre of each other throughout.
What was measured
Mean intraocular pressure at 8 AM sustained over 12 months, three arms
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
In the twelve-month ROCKET-2 study, mean intraocular pressure at 8 AM decreased from a baseline of 22.5 to 22.6 mmHg to 17.9 to 18.8 mmHg with netarsudil once daily, 17.2 to 18.0 mmHg with netarsudil twice daily and 17.5 to 17.9 mmHg with timolol, sustained across twelve months. ROCKET-4 separately compared once-daily netarsudil against twice-daily timolol over six months in patients with baseline pressure below 30 mmHg. The durability result is real and is the strongest thing on this page. It is also a comparison against timolol, which the independent pooled analysis of 114 trials ranks sixth of fourteen first-line agents, more than a millimetre below the prostaglandin analogues.
Source
Kahook MY et al., Am J Ophthalmol 2019;200:130-137; Khouri AS et al., Am J Ophthalmol 2019;204:97-104 (ROCKET-4)
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim
The first drug aimed at the tissue that actually fails
In plain words
For a hundred years, glaucoma drugs turned down fluid production or opened a side route. None of them touched the drain that is the actual problem. This is the first one that does, and the label still says the exact mechanism is unknown.
What was measured
That netarsudil works by relaxing the trabecular meshwork — the design rationale for the whole drug class, supported by cell and perfusion work, and described by the approved label as unknown
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Open-angle glaucoma is a disease of increased outflow resistance at the trabecular meshwork and the inner wall of Schlemm’s canal. Beta-blockers and carbonic anhydrase inhibitors reduce aqueous production. Prostaglandin analogues increase uveoscleral outflow, a secondary route. Neither addresses the conventional pathway. Rho kinase inhibition disassembles actin stress fibres and focal adhesions in trabecular meshwork cells, reducing cell contractility and tissue stiffness and increasing conventional outflow facility, and netarsudil additionally inhibits the norepinephrine transporter and lowers episcleral venous pressure. The FDA label commits to none of this in detail: its Mechanism of Action section reads in full that netarsudil is a Rho kinase inhibitor believed to reduce intraocular pressure by increasing outflow of aqueous humour through the trabecular meshwork, and that the exact mechanism is unknown. A field-changing target and an explicitly unresolved mechanism are stated on the same page.
Source
RHOPRESSA (netarsudil ophthalmic solution) 0.02% US prescribing information, Mechanism of Action 12.1 (NDA 208254)
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
contested
Review state
Written into the record, not signed off as a reviewed claim
Eighty-four times generic latanoprost, for non-inferiority to timolol
In plain words
A millilitre costs pharmacies US$131.76. A millilitre of generic latanoprost costs US$1.57 and lowers pressure more in indirect comparison. The clinical case for the difference is the mechanism, not the measurement.
What was measured
That a novel mechanism justifies an eighty-four-fold price difference against the incumbent, when the supporting trial claims non-inferiority to a still cheaper drug in a restricted population
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
In the CMS acquisition-cost survey effective 19 August 2026, netarsudil is listed as a single brand product at US$131.76 per millilitre. In the same survey on the same date, generic latanoprost is US$1.57 across 13 products, generic timolol US$1.06 across 65, and generic dorzolamide US$0.8910 across 23 — ratios of 84, 124 and 148. The clinical evidence supporting that price is non-inferiority to timolol in the population with baseline pressure below 25 mmHg, with the ROCKET-1 non-inferiority analysis being post hoc. Netarsudil is absent from the network meta-analysis of 114 randomised trials that ranks the first-line drops, because it was approved after that analysis was published, so no independent pooled estimate places it against the alternatives. The argument for the drug is that it acts on a pathway nothing else reaches and therefore adds to a prostaglandin analogue rather than overlapping with it. That argument is mechanistically sound and it is not the same thing as a measured comparative advantage.
Source
CMS National Average Drug Acquisition Cost survey effective 19 August 2026; Serle JB et al., Am J Ophthalmol 2018;186:116-127; Li T et al., Ophthalmology 2016;123:129-140
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
contested
Review state
Written into the record, not signed off as a reviewed claim

Where else this substance is registered

FDA substance identifier (UNII)
VL756B1K0U
RxNorm concept
1992868

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What is missing or unclearRead from sources, not yet reviewed

How this medicine reached us

Kept near the foot of the page. A historical event moves up only when it changes something about this substance today.

What the approval register records

  • 2 approved applications cover products containing this substance. The earliest was NDA208254, approved 20171218 to ALCON LABS INC.

    Drugs@FDA application register · NDA208254 · read 2026-08-29

  • Marketing status on the register: prescription.

    Drugs@FDA application register · NDA208254 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 20171218.

    FDA National Drug Code directory · 70727-497 · read 2026-08-29

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The older medicine-wide conclusion held in this record

Written for a clinical reader, and about the medicine as a whole rather than about one indication, population and set of trials. RNAWiki does not treat it as a programme conclusion and no reviewer has signed it off in that form. It is here word for word because it is what the record holds.

A Rho kinase and norepinephrine transporter inhibitor that relaxes the trabecular meshwork to open the eye’s main drain, non-inferior to timolol only in the restricted population with baseline pressure below 25 mmHg — a post hoc analysis in ROCKET-1 and the pre-specified one in ROCKET-2 — while causing conjunctival hyperemia in 53% of patients, corneal deposits in around a quarter, and costing US$131.76 per millilitre against generic latanoprost’s US$1.57.

Recorded evidence blocks (7)

On the Netarsudil label: indicated for what?


"RHOPRESSA is indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. RHOPRESSA ® is a Rho kinase inhibitor indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.": indications and usage on Netarsudil's label. DailyMed label · 7d4f0e3a-5b86-4c43-982a-813b22ae7e22 · 2026-01-20

20 registered trials of Netarsudil — at which phases?


Registered studies posting no result
6 of 20

20 registered studies of Netarsudil: 11 phase2, 8 phase3, 4 phase4, 1 phase1. CLINICALTRIALS_SNAPSHOT · 2026-09-01

25 with a PubMed record

Show the evidence
  • phase2
    11
  • phase3
    8
  • phase4
    4
  • phase1
    1
  • completed
    15
  • unknown
    2
3 more recorded rows
  • active not recruiting
    1
  • recruiting
    1
  • terminated
    1

recorded 2026-09-01 · last checked 2026-09-04

Why did Netarsudil's trial NCT03971357 stop?


1 recorded trial of Netarsudil stopped. CLINICALTRIALS_SNAPSHOT · 2026-09-01

"variance of outcome measures was substantially greater than anticipated in the statistical plan"; 1 of 20 registered studies

Show the evidence
  • Trial NCT03971357
    terminated; "variance of outcome measures was substantially greater than anticipated in the statistical plan"

recorded 2026-09-01 · last checked 2026-09-04

Human studies of Netarsudil used AR-13324 Ophthalmic Solution 0.01% — over how long?


Human studies of Netarsudil used "AR-13324 Ophthalmic Solution 0.01%". ClinicalTrials.gov · 2026-09-01

11 recorded entries; human; ophthalmic; also "AR-13324 Ophthalmic Solution 0.02%", "AR-13324 Ophthalmic Solution 0.04%", "AR-13324 Ophthalmic Solution 0.02% BID"

Show the evidence

human

  • NCT01528787
    AR-13324 Ophthalmic Solution 0.01%
  • NCT01528787
    AR-13324 Ophthalmic Solution 0.02%
  • NCT01528787
    AR-13324 Ophthalmic Solution 0.04%
  • NCT02207621
    AR-13324 Ophthalmic Solution 0.02% BID
  • NCT02874846
    ophthalmic; Netarsudil ophthalmic solution 0.02%
  • NCT03808688
    Netarsudil Ophthalmic Solution 0.02%
5 more recorded rows
  • human NCT03844945
    Netarsudil Ophthalmic Solution 0.01%
  • human NCT03844945
    Netarsudil Ophthalmic Solution 0.04%
  • human NCT05660447
    Netarsudil 0.02% Ophthalmic Solution [RHOPRESSA]
  • human NCT06441643
    Netarsudil 0.02% Ophthalmic Solution
  • human NCT06441643
    Netarsudil 0.02%/Latanoprost 0.005% Ophthalmic Solution

recorded 2026-09-01 · last checked 2026-09-04

At the median, Netarsudil's trials enrolled 107.5 people — anything larger?


Median enrolment
107.5
Largest enrolment
756
Registered trials counted
20

What do 141 spontaneous reports say about Netarsudil — and not say?


These are reports people sent to a regulator. They do not show the medicine caused the reaction. Nobody counted how many people took the medicine and reported nothing. The same event can be reported more than once, and many reports are incomplete. News coverage, lawsuits and new warnings change how often people report. A count is not a rate and not a risk.

Netarsudil appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 141 reaction mentions were counted: conjunctival hyperaemia 33; visual acuity reduced 24; corneal oedema 20; intraocular pressure increased 14. FAERS via Open Targets · CHEMBL4594250 · 2026-06-24

Show the evidence
  • conjunctival hyperaemia
    33
  • visual acuity reduced
    24
  • corneal oedema
    20
  • intraocular pressure increased
    14
  • vision blurred
    13
  • cornea verticillata
    8
4 more recorded rows
  • eye irritation
    8
  • conjunctivitis allergic
    7
  • eye pruritus
    7
  • lacrimation increased
    7

recorded 2026-06-24 · last checked 2026-09-04

Which 10 reactions does Netarsudil's label not list?


conjunctival hyperaemia, conjunctivitis allergic and cornea verticillata and 7 more reported for Netarsudil, absent from its label. FAERS via Open Targets · CHEMBL4594250 · 2026-06-24

2 label terms; 10 reported and unlisted; 7d4f0e3a-5b86-4c43-982a-813b22ae7e22

Show the evidence
  • conjunctival hyperaemia
    count not stated
  • conjunctivitis allergic
    count not stated
  • cornea verticillata
    count not stated
  • corneal oedema
    count not stated
  • eye irritation
    count not stated
  • eye pruritus
    count not stated
4 more recorded rows
  • intraocular pressure increased
    count not stated
  • lacrimation increased
    count not stated
  • vision blurred
    count not stated
  • visual acuity reduced
    count not stated

recorded 2026-06-24 · last checked 2026-09-04

Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL4594250
PubChem CID
66599893
CAS number
1254032-66-0
RxCUI
1992864
InChIKey
OURRXQUGYQRVML-AREMUKBSSA-N
Development code
AR-11324 FREE BASE, AR-13324
Also called
NETARSUDIL DIMESYLATE, Netarsudil mesilate, NETARSUDIL DIMESYLATE [MI], NETARSUDIL DIMESYLATE [ORANGE BOOK], NETARSUDIL MESYLATE [ORANGE BOOK], NETARSUDIL MESYLATE [USAN], Netarsudil mesilate [WHO-DD], ROCKLATAN COMPONENT NETARSUDIL DIMESYLATE
Trade name
Netarsudil dimesylate component of rocklatan, Rhokiinsa, Rhopressa, Roclanda
Salt form
Netarsudil mesylate
Sources (6)

Sources

ChEMBL 37 — CC BY-SA 3.0 Unported · ChEMBL ATC CC BY-SA · ClinicalTrials.gov — US Government work · Open Targets 26.06 — CC0 · mixed register set; per-register licences in docs/specs/corpus-20k-sources.md · openFDA / DailyMed — US Government work

How these records are assembled · Which registers were checked

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This is a record of evidence. It is not medical advice, and it does not say this substance suits you. Nothing here says any substance on RNAWiki is appropriate for a child.