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Rolapitant

  • Prescription medicine
  • Given by a clinician
  • 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 Rolapitant does in the body

VARUBI ® is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.

From the FDA-approved label: Rolapitant is a selective and competitive antagonist of human substance P/NK1 receptors. Rolapitant does not have significant affinity for the NK2 or NK3 receptors or for a battery of other receptors, transporters, enzymes and ion channels. Rolapitant is also active in animal models of chemotherapy-induced emesis.

Why people take it. VARUBI ® is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.

What happened in people

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

A fixed RNAWiki sentence

Where this came from

Wording RNAWiki always uses, not a finding about this substance.

No reviewed claim names a result for any goal on this record.

No source is stored against this line.

The limit that matters most

Not recorded.

Where it acts
Not recorded.
Kind of result
No result is published, so no kind of result applies yet
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 · 57O5S1QSAQ · read 2026-08-29

  • Its recorded molecular formula is C25H26F6N2O2, weighing 554.95.

    US prescribing information · a52896cd-4a98-49b8-82db-bf1985a64d97 · read 2026-08-30

Where each sentence above came from

The use the label states, quoted from it. No plain-language version of this sentence has been written.

The use the label states, quoted from it. It is written for a clinician, not for a reader without medical training.

No statement of the main limit is recorded.

The four opening statements run to 136 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.

Biomarker

A biomarker is a number from a test that stands in for something about health.

A picture of it, and where the picture fails

A biomarker is like a fuel gauge.

Where that stops being true. A gauge is wired to the tank. Many biomarkers are only loosely tied to health.

What people get wrong. A better number is read as a better life. Several medicines improved a number and helped nobody.

A measurable indicator used as a substitute for a clinical outcome of interest.

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.

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.

No Emetic Episodes and No Rescue Medication

The study did not show it

Who was studied
NCT01500226
How many people
1369
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

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. No limitation is recorded for this study.

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

Form and route. Intravenous

Interval reported. Not recorded in this summary

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

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

No emetic episodes regardless of rescue medication use.

The study did not show it

Who was studied
NCT00539721
How many people
619
Study design
Phase 2
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

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. No limitation is recorded for this study.

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

Form and route. Intravenous

Interval reported. Not recorded in this summary

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

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

No Emetic Episodes and No Rescue Medication

The study did not show it

Who was studied
NCT01500213
How many people
555
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

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. No limitation is recorded for this study.

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

Form and route. Intravenous

Interval reported. Not recorded in this summary

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

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

No Emetic Episodes and No Rescue Medication

The study did not show it

Who was studied
NCT01499849
How many people
532
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

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. No limitation is recorded for this study.

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

Form and route. Intravenous

Interval reported. Not recorded in this summary

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

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

The primary efficacy endpoint is the overall complete response rate (no emesis and no use of rescue medication from 0 through 120 hours following initiation of cisplatin-based chemotherapy).

The study did not show it

Who was studied
NCT00394966
How many people
450
Study design
Phase 2
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

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. No limitation is recorded for this study.

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

Form and route. Intravenous

Interval reported. Not recorded in this summary

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

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

Complete Remission (CR) Rate

The study did not show it

Who was studied
NCT07442890
How many people
238
Study design
Not applicable
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

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. No limitation is recorded for this study.

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

Form and route. Intravenous

Interval reported. Not recorded in this summary

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

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot
What we know
RNAWiki holds 6 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 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.

  • VARUBI ® is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.

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: “The safety and effectiveness of VARUBI have not been established in pediatric patients.”

    US prescribing information · a52896cd-4a98-49b8-82db-bf1985a64d97 · read 2026-08-30

  • On older people, the label states: “Of the 1294 subjects treated with VARUBI, 25% were 65 years and over, while 5% were 75 and over.”

    US prescribing information · a52896cd-4a98-49b8-82db-bf1985a64d97 · read 2026-08-30

  • On people who are pregnant, the label states: “Risk Summary The limited data with VARUBI use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes.”

    US prescribing information · a52896cd-4a98-49b8-82db-bf1985a64d97 · read 2026-08-30

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

    US prescribing information · a52896cd-4a98-49b8-82db-bf1985a64d97 · read 2026-08-30

  • On people with reduced liver function, the label states: “No dosage adjustment is needed in patients with mild (Child-Pugh Class A) or moderate (Child-Pugh Class B) hepatic impairment.”

    US prescribing information · a52896cd-4a98-49b8-82db-bf1985a64d97 · read 2026-08-30

Where the result stopped carrying

  • 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

Given by a clinician

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

Intravenous

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

Sold as emulsion, tablet, given by the intravenous, oral route.

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 takeNothing found in the sources checked

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.

Nothing found in the sources checked

No harm is recorded against this substance in the sources RNAWiki checked. Finding nothing is not the same as showing there is nothing.

The sources listed were searched and held nothing. That is not the same as nothing existing.

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

Intravenous

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

Not recorded.

Nothing recorded

Where this came from

RNAWiki holds nothing here and says so rather than guessing.

Nothing further is recorded about which forms are sold.

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. 4 of them contain it and nothing else.

    FDA National Drug Code directory · 70720-101 · read 2026-08-29

  • They are sold as powder and tablet, taken oral.

    FDA National Drug Code directory · 70720-101 · read 2026-08-29

  • The regulator's established pharmacologic class for it is breast cancer resistance protein inhibitors [moa], cytochrome p450 2d6 inhibitors [moa] and neurokinin 1 antagonists [moa].

    FDA National Drug Code directory · 70720-101 · read 2026-08-29

  • 1 published label names 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 · a52896cd-4a98-49b8-82db-bf1985a64d97 · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · a52896cd-4a98-49b8-82db-bf1985a64d97 · read 2026-08-29

  • Varubi is oral at 3 DOSAGE FORMS AND STRENGTHS Tablets: 90 mg rolapitant; film-coated, blue capsule shaped, debossed with T0101 on one side and 100 on the other side., recorded as fda label in effect 2020-08-19 in the United States.

    US prescribing information · a52896cd-4a98-49b8-82db-bf1985a64d97 · 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 Rolapitant 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

What nobody knows yet

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

How much did people take in the studies?

The sources RNAWiki checked hold nothing for this field.

Why it matters. A result belongs to an amount. Without the amount the result floats free.

What would answer it

A stored source that records 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 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 Rolapitant 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.

Where else this substance is registered

FDA substance identifier (UNII)
57O5S1QSAQ
RxNorm concept
1665503

Checks this page had to pass

  • Passed

    Identity resolved

    no open identity hold

  • Passed

    No unresolved merge across substance families

    no quarantine open

  • Passed

    Every public sentence names a source

    The opening statement carries the origin: Quoted from a stored source.

  • Not passed

    Trial roles classified for highlighted evidence

    No registered study is classified as testing this substance.

  • Passed

    No internal keys in reader text

    enforced by the copy-contract test over the rendered page

  • Not passed

    Safety mode resolved

    No register row and no identity class settled the question.

  • Passed

    Canonical metadata present

    slug and display name present

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.

  1. Withdrawn, in European Union; no reason is published (EMA Medicine.csv)

What the approval register records

  • 2 approved applications cover products containing this substance. The earliest was NDA206500, approved 20150901 to TERSERA.

    Drugs@FDA application register · NDA206500 · read 2026-08-29

  • Marketing status on the register: discontinued and prescription.

    Drugs@FDA application register · NDA206500 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 20151007.

    FDA National Drug Code directory · 70720-101 · read 2026-08-29

What is missing or unclearRead from sources, not yet reviewed

What to learn next

Ordered by what would most change how you read this page, starting with what is easiest to misunderstand.

This order is fixed in code and does not count clicks or time on the page.

What is not here

9 questions this page could not answer

These sections were prepared and left out because there was nothing to put in them. They are listed rather than hidden, so the gaps in this record are visible.

  • What was measured, goal by goal — found nothing in the sources checked.
  • How close this is to real life — found nothing in the sources checked.
  • The path through the body — found nothing in the sources checked.
  • Felt, measured, or meaningful — found nothing in the sources checked.
  • How long anything takes — found nothing in the sources checked.
  • What it may clash with — found nothing in the sources checked.
  • Other ways to the same goal — found nothing in the sources checked.
  • Claims that go past the evidence — found nothing in the sources checked.
  • What changed on this page — found nothing in the sources checked.

The record as stored

The full record, for auditing

Everything above is built from what is below. This layer keeps the technical vocabulary, record identifiers and every stored row, so a reader who wants to check the page can.

Recorded evidence blocks (10)

On the Rolapitant label: indicated for what?

"VARUBI ® is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. VARUBI is a substance P/neurokinin 1 (NK1) receptor…": indications and usage on Rolapitant's label. DailyMed label · a52896cd-4a98-49b8-82db-bf1985a64d97 · 2020-08-19

11 registered trials of Rolapitant — at which phases?

Registered studies posting no result
6 of 11

11 registered studies of Rolapitant: 5 phase2, 3 phase1, 3 phase3. CLINICALTRIALS_SNAPSHOT · 2026-09-01

20 with a PubMed record

Show the evidence
  • phase2
    5
  • phase1
    3
  • phase3
    3
  • completed
    9
  • terminated
    1
  • withdrawn
    1

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

2 of Rolapitant's trials stopped: other?

other (2): Rolapitant's stop wording, clustered. CLINICALTRIALS_SNAPSHOT · 2026-09-01

"Terminated per PI's request"; 2 of 11 registered studies

Show the evidence

Trial

  • NCT02732015
    terminated; "Terminated per PI's request"
  • NCT03960151
    withdrawn; "Compound was sold by funder and development ceased."

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

Rolapitant's half-life is 169 to 183 hours — which schedules were studied?

169 to 183 hours, the half-life Rolapitant's label states: "Elimination Following single oral doses (4.5 to 180 mg) of rolapitant, the mean terminal half-life (t 1/2 ) of rolapitant ranged from 169 to 183 hours (approximately 7 days), and was independent of dose." DailyMed label · a52896cd-4a98-49b8-82db-bf1985a64d97 · 2020-08-19

tmax 30 minutes.

Show the evidence
  • half life pharmacokinetics
    169 to 183 hours; Elimination Following single oral doses (4.5 to 180 mg) of rolapitant, the mean terminal half-life (t 1/2 ) of rolapitant ranged from 169 to 183 hours (approximately 7 days), and was independent of dose.
  • tmax pharmacokinetics
    30 minutes; Absorption Following a single oral dose administration of 180 mg VARUBI under fasting conditions to healthy subjects, rolapitant was measurable in plasma within 30 minutes and the peak plasma concentration (C max ) for rolapitant which was reached in about 4 hours and mean C max was 968 ng/mL (%CV:28%).
  • metabolism pharmacokinetics
    Metabolism Rolapitant is metabolized primarily by CYP3A4 to form a major active metabolite, M19 (C4-pyrrolidine-hydroxylated rolapitant).

recorded 2020-08-19 · last checked 2026-09-04

Which 5 trials of Rolapitant posted no result?

Posted no result
5 of 5 completed trials
Registrations
NCT00506545, NCT00394966, NCT02285647, NCT02382666 and NCT02434861
Completion dates
oldest 2007-10; newest 2015-08
Show the evidence

Trial

  • NCT00506545
    2007-10
  • NCT00394966
    2008-03
  • NCT02285647
    2015-05
  • NCT02382666
    2015-08
  • NCT02434861
    2015-08

At the median, Rolapitant's trials enrolled 102 people — anything larger?

Median enrolment
102
Largest enrolment
1369
Registered trials counted
11

What do 484 spontaneous reports say about Rolapitant — 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.

Rolapitant appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 484 reaction mentions were counted: flushing 91; dyspnoea 74; infusion related reaction 64; erythema 55. FAERS via Open Targets · CHEMBL3707330 · 2026-06-24

Show the evidence
  • flushing
    91
  • dyspnoea
    74
  • infusion related reaction
    64
  • erythema
    55
  • feeling hot
    45
  • dizziness
    38
4 more recorded rows
  • nausea
    35
  • back pain
    29
  • chest discomfort
    27
  • abdominal discomfort
    26

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

Which 10 reactions does Rolapitant's label not list?

abdominal discomfort, back pain and chest discomfort and 7 more reported for Rolapitant, absent from its label. FAERS via Open Targets · CHEMBL3707330 · 2026-06-24

2 label terms; 10 reported and unlisted; a52896cd-4a98-49b8-82db-bf1985a64d97

Show the evidence
  • abdominal discomfort
    count not stated
  • back pain
    count not stated
  • chest discomfort
    count not stated
  • dizziness
    count not stated
  • dyspnoea
    count not stated
  • erythema
    count not stated
4 more recorded rows
  • feeling hot
    count not stated
  • flushing
    count not stated
  • infusion related reaction
    count not stated
  • nausea
    count not stated

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

Rolapitant and CYP2D6, CYP3A4 and BCRP: shared by which compounds?

CYP2D6, CYP3A4 and BCRP appear in Rolapitant's recorded interaction sentences, 8 in all. DailyMed label · a52896cd-4a98-49b8-82db-bf1985a64d97 · 2020-08-19

CYP2D6, CYP2D6, CYP3A4, CYP3A4, BCRP, P-gp; 6 shared nodes; drug_interactions

Show the evidence

Interaction statement

  • drug_interactions
    Rolapitant is a moderate CYP2D6 inhibitor.
  • drug_interactions
    The inhibition of CYP2D6 persisted on Day 28 with a 2.3-fold increase in dextromethorphan concentrations, the last time point measured.
  • drug_interactions
    The inhibitory effect of rolapitant on CYP2D6 is expected to persist beyond 28 days for an unknown duration following administration of VARUBI [see Clinical Pharmacology (12.3) ] .
  • drug_interactions
    Oral rolapitant is an inhibitor of Breast-Cancer-Resistance Protein (BCRP) and p-glycoprotein (P-gp).
  • drug_interactions
    Rolapitant, given as a single oral dose, is not an inhibitor or inducer of CYP3A4 [see Clinical Pharmacology (12.3) ] .
  • drug_interactions
    Therefore, no dosage adjustment for dexamethasone (CYP3A4 substrate) is needed when co-administered with VARUBI [see Dosage and Administration (2) ] .
2 more recorded rows
  • Interaction statement drug_interactions
    Table 4: Clinically Relevant Interactions Affecting Drugs Co-Administered with VARUBI CYP2D6 Substrates Narrow Therapeutic Index Drugs (Thioridazine and Pimozide) Clinical Impact: Increased plasma concentrations of thioridazine and pimozide are associated with serious and/or life-threatening events of QT prolongation and Torsades de Pointes.
  • Interaction statement drug_interactions
    Intervention: VARUBI is contraindicated in patients taking CYP2D6 substrates with a narrow therapeutic index such as thioridazine and pimozide.

CYP2D6

  • FINGOLIMOD LAURYL SULFATE, Darunavir Propylene Glycolate, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Fluoxetine
  • FINGOLIMOD LAURYL SULFATE, Darunavir Propylene Glycolate, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Fluoxetine

CYP3A4

  • FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Beclometasone, Rasagiline, Sofpironium
  • FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Beclometasone, Rasagiline, Sofpironium
  • BCRP
    TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Deoxycholic acid, Golodirsen, Naldemedine, Eravacycline, Omadacycline
  • P-gp
    FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, Darunavir Propylene Glycolate, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Vincristine

recorded 2020-08-19 · last checked 2026-09-04

Where do the label and the trials disagree about Rolapitant?

"withdrawn" against "approved": withdrawal status vs register status for Rolapitant.

EMA_MEDICINE_REGISTER, Drugs@FDA; 1 recorded pair

Show the evidence
  • EMA_MEDICINE_REGISTER EMEA/H/C/004196
    withdrawn; 2026-09-04
  • Drugs@FDA NDA206500
    approved; 2026-08-28
Where it is registered

Where it’s registered

Withdrawn, in European Union; no reason is published (EMA Medicine.csv)

Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL3707330
PubChem CID
16203739
CAS number
914462-92-3
RxCUI
1673367
InChIKey
FIVSJYGQAIEMOC-ZGNKEGEESA-N
Also called
ROLAPITANT HYDROCHLORIDE, 1,7-DIAZASPIRO(4.5)DECAN-2-ONE, 8-(((1R)-1-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)ETHOXY)METHYL)-8-PHENYL-, MONOHYDROCHLORIDE, MONOHYDRATE, (5S,8S)-, ROLAPITANT HYDROCHLORIDE [MI], ROLAPITANT HYDROCHLORIDE [ORANGE BOOK], ROLAPITANT HYDROCHLORIDE [USAN], Rolapitant hydrochloride monohydrate [WHO-DD]
Salt form
Rolapitant hcl h20, Rolapitant hydrochloride monohydrate
Development code
SCH-619734, SCH619734
Trade name
Varubi, Varuby
Sources (6)

Sources

ChEMBL 37 — CC BY-SA 3.0 Unported · ClinicalTrials.gov — US Government work · EMA medicine register · 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

Index-quality checks
  • identity passed: no open identity hold
  • required summary fields resolved: 4 required field(s) not terminal: Why people use it, Best-supported result, Biggest unanswered question, Human evidence
  • public claims reviewed: 0 reviewed claim(s); drafts are never rendered
  • source coverage passed: 6 source rows
  • no critical contamination: no quarantine open
  • canonical metadata passed: slug and display name present
  • no raw internal fields: enforced by the copy-contract test over the rendered page

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.