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Alosetron

  • 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 Alosetron does in the body

A tablet for severe diarrhoea-predominant irritable bowel syndrome in women, prescribed only under a special programme

The gut uses serotonin to drive movement, secretion and the sensation of pain. Alosetron blocks one particular serotonin receptor on gut nerves, so transit slows, less fluid is secreted and the gut becomes less sensitive to stretch — which is exactly what someone with severe diarrhoea and cramping needs. The same slowing can go too far, producing severe constipation, and in rare cases the blood supply to a segment of colon becomes inadequate.

What happened in people

Global symptom improvement relative risk 1.60 (95% CI 1.44 to 1.76) across 4,170 patients in eight trials

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 the ischaemic colitis is caused by the constipation; serious constipation complications were not significantly increased while ischaemic colitis was

Where it acts
Enteric nervous system; 5-HT3 receptors on intrinsic and extrinsic afferent neurons of the gastrointestinal tract
Kind of result
Symptoms and quality of life
Supervision
Professional supervision is normally required. A regulator classifies this substance in a way that restricts how it is supplied.

What the registries record it as

  • The substance registry classes this as chemical.

    FDA substance registry · 2F5R1A46YW · read 2026-08-29

  • Its recorded molecular formula is C17H18N4O•HCl, weighing 330.81 g/mol.

    US prescribing information · 3ac203a2-4c55-deac-e063-6394a90aa165 · read 2026-08-30

Where each sentence above came from

No recorded sentence describes the change this makes in a way that stands on its own. The page opens with what it is taken for instead, and the recorded explanation follows below.

Shown as the opening line on this page.

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

The four opening statements run to 111 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.

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.

Absolute difference

An absolute difference is how many more people in a hundred were affected.

A picture of it, and where the picture fails

It is like counting heads in two rooms of a hundred.

Where that stops being true. Heads are easy to count. Study results carry a margin of error too.

What people get wrong. It is confused with a percentage change, which can look far larger.

The arithmetic difference in event rates between arms.

Confidence interval

A confidence interval is the range the true answer is likely to sit in.

A picture of it, and where the picture fails

It is like a weather forecast giving a range rather than one number.

Where that stops being true. A forecast range covers tomorrow. This one covers what the study could resolve.

What people get wrong. The middle number is read as the answer. A range crossing zero means no change is still possible.

An interval estimate that would contain the true parameter in a stated proportion of repeated studies.

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.

Global improvement in irritable bowel syndrome symptoms, and adequate relief of pain and discomfort

The study showed what it set out to show

Who was studied
Meta-analysis of eight randomised placebo-controlled trials of alosetron
How many people
4170
Study design
Meta-analysis of 12-week multicentre randomised placebo-controlled trials
Compared against
A dummy treatment
Kind of result
A number that stands in for health
What was found
Global improvement relative risk 1.60 (95% CI 1.44 to 1.76), P < 0.001; adequate relief of pain and discomfort 1.31 (1.20 to 1.43), P < 0.001; women 1.34 (1.21 to 1.48), men 1.23 (1.02 to 1.47)
Repeated elsewhere
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 pooled population was 80 per cent female with only 2.6 per cent constipation-predominant disease, so the male and constipation-predominant estimates rest on small subsets. Tolerability differed from placebo, relative risk 1.19 (1.07 to 1.31).

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

Form and route. Oral tablet, 0.5 mg twice daily with cautious escalation to 1 mg twice daily

Interval reported. 95% CI 1

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

Adjudicated incidence of ischaemic colitis and serious complications of constipation in alosetron users, in trials and in post-marketing surveillance

The study showed what it set out to show

Who was studied
Blinded expert adjudication of ischaemic colitis and constipation complications
How many people
19
Study design
Systematic review with blinded case adjudication of trial and post-marketing reports
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Trials: ischaemic colitis 0.15 per cent versus 0.0 per cent, P = 0.03; no significant difference in serious complications of constipation. Post-marketing: 1.1 ischaemic colitis and 0.66 serious constipation complications per 1,000 patient-years
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. Post-marketing rates depend on an exposure denominator derived from the restricted prescribing programme, and on the adjudication panel's exclusion criteria for cases judged inconsistent or not drug-associated.

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

Form and route. Oral tablet, 0.5 mg twice daily with cautious escalation to 1 mg twice daily

Interval reported. Not recorded in this summary

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

What we know
RNAWiki holds 2 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

    Alosetron

    What a person takes: Oral tablet, 0.5 mg twice daily with cautious escalation to 1 mg twice daily.

    The measurement behind this step

    Oral alosetron hydrochloride, started at the lowest dose and escalated only after four weeks if symptoms are inadequately controlled and constipation has not occurred. Extensively metabolised by CYP1A2, making fluvoxamine a contraindication and requiring caution with other CYP1A2 inhibitors.

  2. Getting in

    An oral tablet, started at the lowest dose

    Taken by mouth, beginning at a low dose and increased only if symptoms are not controlled and constipation has not developed.

    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

    Oral alosetron hydrochloride, initiated at 0.5 mg twice daily with escalation to 1 mg twice daily only after four weeks if tolerated. Extensively metabolised by CYP1A2, so fluvoxamine is contraindicated and ciprofloxacin requires caution.

  3. Reaching the cell

    Reaches the nerve networks of the gut wall

    It reaches the nerve cells embedded in the wall of the intestine and the sensory fibres running from the gut to the spinal cord.

    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

    Distributes to enteric neurons of the myenteric and submucosal plexuses and to extrinsic vagal and spinal afferent terminals, where 5-HT3 receptors are expressed.

  4. What it acts on

    Blocks the 5-HT3 ion channel

    It plugs a serotonin-operated channel on those nerves, so the serotonin the gut releases can no longer excite them.

    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

    Selective antagonism at the 5-HT3 receptor, a ligand-gated cation channel. Blocking it prevents serotonin-evoked depolarisation of enteric and afferent neurons, rather than modulating a second-messenger cascade.

  5. The change it makes

    Transit slows, secretion falls, sensation dulls

    The gut moves contents more slowly, secretes less fluid, and reports less discomfort from stretching — all three at once.

    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

    Reduced excitatory 5-HT3 signalling slows colonic transit, reduces intestinal secretion and raises the threshold for visceral afferent firing on distension. The three effects are inseparable properties of the same blockade, which is why constipation is not a side effect but the same effect taken further.

  6. What that does for a person

    Symptom relief in most; ischaemic colitis in about one per thousand patient-years

    Global symptoms improved in substantially more patients than on placebo. Ischaemic colitis occurred in roughly one patient per thousand treated for a year, and in the trials every case resolved.

    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

    Measured: relative risk 1.60 (95% CI 1.44 to 1.76) for global symptom improvement across 4,170 patients. Measured: ischaemic colitis 0.15 per cent versus 0.0 per cent in pooled trials (P = 0.03), post-adjudication rate 1.1 per 1,000 patient-years, all 19 trial cases reversible without long-term sequelae.

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

What we know
The record describes 5 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.

  • Women with severe diarrhoea-predominant irritable bowel syndrome who have failed conventional therapy, prescribed by clinicians enrolled in the programme. It is not indicated in men or in constipation-predominant disease.

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 have not been established.”

    US prescribing information · 3ac203a2-4c55-deac-e063-6394a90aa165 · read 2026-08-30

  • On older people, the label states: “In some studies in healthy men or women, plasma concentrations were elevated by approximately 40% in individuals 65 years and older compared to young adults [see Warnings and Precautions (5.1) ] .”

    US prescribing information · 3ac203a2-4c55-deac-e063-6394a90aa165 · read 2026-08-30

  • On people who are pregnant, the label states: “Risk Summary The available data with alosetron hydrochloride use in pregnant women are insufficient to draw conclusions about any drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes.”

    US prescribing information · 3ac203a2-4c55-deac-e063-6394a90aa165 · read 2026-08-30

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

    US prescribing information · 3ac203a2-4c55-deac-e063-6394a90aa165 · read 2026-08-30

  • On people with reduced liver function, the label states: “Due to the extensive hepatic metabolism of alosetron, increased exposure to alosetron and/or its metabolites is likely to occur in patients with hepatic impairment.”

    US prescribing information · 3ac203a2-4c55-deac-e063-6394a90aa165 · read 2026-08-30

  • On people with reduced kidney function, the label states: “(creatinine clearance 4 mL/min to 56 mL/min) has no effect on the renal elimination of alosetron due to the minor contribution of this pathway to elimination.”

    US prescribing information · 3ac203a2-4c55-deac-e063-6394a90aa165 · read 2026-08-30

Where the result stopped carrying

  • Approved February 2000 and voluntarily withdrawn in November 2000, nine months later
  • The original indication covered irritable bowel syndrome in women broadly; the reintroduced one covers severe diarrhoea-predominant disease after conventional therapy has failed
  • The mechanism of the ischaemic colitis remains unresolved between a direct vascular effect and a consequence of slowed transit
  • 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

Oral tablet, 0.5 mg twice daily with cautious escalation to 1 mg twice daily

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

Professional supervision is normally required. A regulator classifies this substance in a way that restricts how it is supplied.

Quoted from a source

Where this came from

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

Suppression classes recorded: S6.

No source is stored against this line.

What is in the pack

Oral alosetron hydrochloride, started at the lowest dose and escalated only after four weeks if symptoms are inadequately controlled and constipation has not occurred. Extensively metabolised by CYP1A2, making fluvoxamine a contraindication and requiring caution with other CYP1A2 inhibitors.

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

Constipation is the commonest adverse effect and is the same pharmacology as the therapeutic action taken further. The serious harms are ischaemic colitis — 0.15 per cent against 0.0 per cent on placebo in pooled trials, post-adjudication rate 1.1 per 1,000 patient-years, with all 19 trial cases reversible without long-term sequelae — and serious complications of constipation at 0.66 per 1,000 patient-years, which were not significantly increased over placebo in the trials. The drug is contraindicated in constipation, ischaemic colitis, Crohn's disease, ulcerative colitis, diverticulitis, adhesions and strictures, and must be stopped immediately if constipation or rectal bleeding occurs. Prescribing is restricted to enrolled clinicians.

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

Oral tablet, 0.5 mg twice daily with cautious escalation to 1 mg twice daily

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

Extensively metabolised by CYP1A2, making fluvoxamine a contraindication and requiring caution with other CYP1A2 inhibitors.

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

  • 18 products list this as an active ingredient in the United States drug directory. 18 of them contain it and nothing else.

    FDA National Drug Code directory · 73190-035 · read 2026-08-29

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

    FDA National Drug Code directory · 73190-035 · read 2026-08-29

  • The regulator's established pharmacologic class for it is serotonin 3 receptor antagonists [moa] and serotonin-3 receptor antagonist [epc].

    FDA National Drug Code directory · 73190-035 · read 2026-08-29

  • 9 published labels name it as an active ingredient. 9 of them describe this substance alone, which is where its own label text on this page comes from.

    US prescribing information · 3ac203a2-4c55-deac-e063-6394a90aa165 · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · 3ac203a2-4c55-deac-e063-6394a90aa165 · read 2026-08-29

  • Alosetron Hydrochloride is oral at 3 DOSAGE FORMS AND STRENGTHS 0.5 mg and 1 mg tablets Alosetron tablets USP, 0.5 mg (0.562 mg alosetron hydrochloride, USP equivalent to 0.5 mg alosetron), are white, oval shaped, film coated tablets debossed with “AN248…, recorded as fda label in effect 2025-09-09 in the United States.

    US prescribing information · 3ac203a2-4c55-deac-e063-6394a90aa165 · read 2026-08-30

  • Recorded price in US: 1.949–3.61824 USD per one unit as the pricing file counts it — a tablet, capsule, patch or single item, across 8 priced products whose strengths and pack forms differ, as of 2026-08-26, paid by retail pharmacies buying the product, as surveyed by the Centers for Medicare & Medicaid Services. It is not a list price, an insurance price, or what anyone pays at a counter..

    Recorded source · 2026-08-26 · read 2026-08-28

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.

Self-experiment planning is not offered for a prescription or clinician-supervised medicine. The questions below are for a clinician or pharmacist.

Questions worth asking

  • Which of the trials of Alosetron 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 the ischaemic colitis is caused by the constipation; serious constipation complications were not significantly increased while ischaemic colitis was

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 women-only indication reflects absence of efficacy in men — the pooled male estimate is 1.23 (1.02 to 1.47) and significant

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 spontaneous reports alone could have supported a rate; the denominator comes from the restricted prescribing programme

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.

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 Alosetron 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.

Ischaemic colitis in 0.15 per cent against 0.0 per cent on placebo
In plain words
In pooled trials, ischaemic colitis occurred in about 1.5 patients per thousand on alosetron and in none on placebo. Every one of the 19 cases resolved without lasting damage.
What was measured
Adjudicated incidence of ischaemic colitis and serious complications of constipation, alosetron versus placebo
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
A blinded expert adjudication reviewed clinical trial report forms and FDA MedWatch forms for every reported case of ischaemic colitis or serious complication of constipation, with the panel unaware of treatment assignment, rating diagnostic accuracy and likelihood of medication association against pre-specified criteria; cases inconsistent with the reported diagnosis or not possibly drug-associated were excluded from the incidence calculation. Pooled trial data showed ischaemic colitis in 0.15 per cent on alosetron against 0.0 per cent on placebo (P = 0.03), with no significant difference in serious complications of constipation. All 19 alosetron-treated patients with ischaemic colitis had reversible colitis without long-term sequelae.
Source
Chang L et al. Am J Gastroenterol 2006;101:1069-1079
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
1.1 ischaemic colitis cases per 1,000 patient-years after adjudication
In plain words
From post-marketing data, about one patient in a thousand treated for a year developed ischaemic colitis, and about two-thirds of one in a thousand had a serious complication of constipation.
What was measured
Post-adjudication rate of ischaemic colitis and serious complications of constipation per 1,000 patient-years
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Post-marketing surveillance data, subjected to the same blinded adjudication, gave a post-adjudication rate of 1.1 cases of ischaemic colitis per 1,000 patient-years of alosetron use and 0.66 serious complications of constipation per 1,000 patient-years. The authors conclude that the incidence of both is very low and rarely associated with long-term sequelae or serious morbidity. This is what a restricted-access programme buys: an exposure denominator that spontaneous reporting cannot supply, so a numerator of case reports becomes a rate that a patient and a clinician can weigh against a symptom burden.
Source
Chang L et al. Am J Gastroenterol 2006;101:1069-1079
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
Relative risk 1.60 for global symptom improvement across 4,170 patients
In plain words
Pooling eight trials, patients on alosetron were about 60 per cent more likely to report global improvement and about 30 per cent more likely to get adequate relief of pain.
What was measured
Pooled relative risk for global symptom improvement and for adequate relief of pain and discomfort
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
A meta-analysis of eight multicentre randomised placebo-controlled 12-week trials including 4,170 patients with irritable bowel syndrome (80 per cent female, all meeting Rome criteria, only 2.6 per cent constipation-predominant) found alosetron significantly more effective than placebo for global improvement in symptoms across the three trials reporting it, relative risk 1.60 (95% CI 1.44 to 1.76, P < 0.001). Across the six trials reporting adequate relief of pain and discomfort the relative risk was 1.31 (95% CI 1.20 to 1.43, P < 0.001), and by sex 1.34 (1.21 to 1.48) in women and 1.23 (1.02 to 1.47) in men. Tolerability differed from placebo, relative risk 1.19 (1.07 to 1.31, P < 0.001).
Source
Efficacy and tolerability of alosetron for the treatment of irritable bowel syndrome in women and men: a meta-analysis. Clin Ther 2008;30:884-901
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
Nine months on the market, then eighteen months off, then back with conditions
In plain words
Approved February 2000, withdrawn November 2000, returned June 2002 with prescribing restricted to enrolled clinicians and a narrow patient group.
What was measured
Not recorded
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Alosetron was approved in February 2000 for irritable bowel syndrome in women, voluntarily withdrawn in November 2000 after reports of ischaemic colitis and serious complications of constipation, and reintroduced in 2002 under a restricted prescribing programme requiring prescriber enrolment, a patient-physician agreement and a narrowed indication: severe diarrhoea-predominant disease in women who have failed conventional therapy. Drugs@FDA records NDA 021107 for LOTRONEX in Prescription marketing status, with several generic applications also approved. What changed between 2000 and 2002 was not the drug or the risk but the size and definition of the exposed population, and the existence of a system that counts it.
Source
Drugs@FDA NDA 021107 (LOTRONEX) — Prescription; Chang L et al. Am J Gastroenterol 2006;101:1069-1079
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
Whether the ischaemia is a vascular effect or a constipation effect is unresolved
In plain words
Nobody has established whether alosetron restricts blood flow to the colon directly, or whether the severe constipation it causes is what starves the tissue.
What was measured
That alosetron-associated ischaemic colitis is caused by the constipation the drug produces
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Two mechanisms are compatible with the data. Alosetron slows colonic transit, and severe constipation can raise intraluminal pressure enough to compromise mucosal perfusion — which would make ischaemic colitis a downstream consequence of the intended pharmacology rather than a separate action. Alternatively, 5-HT3 receptors are present on enteric neurons regulating vasomotor tone, so a direct effect on splanchnic perfusion is possible. The adjudicated analysis found ischaemic colitis significantly increased while serious complications of constipation were not significantly different between arms, which sits awkwardly with a purely constipation-mediated account. The two are not distinguished by the clinical data, and the distinction matters for whether the risk is dose-limitable.
Source
Chang L et al. Am J Gastroenterol 2006;101:1069-1079
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
It works in men too, and the label does not cover them
In plain words
The pooled trials show a significant benefit in men as well as women. The indication is restricted to women, which is a risk decision rather than an efficacy finding.
What was measured
That the women-only indication reflects a lack of efficacy in men
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
The meta-analysis reported adequate relief of pain and discomfort in both sexes: relative risk 1.34 (95% CI 1.21 to 1.48) in women and 1.23 (1.02 to 1.47) in men, both significant. The trials were 80 per cent female, so the male estimate is less precise, but it is not null. The restriction of the indication to women therefore reflects the composition of the safety data and the population in which the benefit-risk case was made, not a demonstrated absence of efficacy in men. Recording it as "alosetron does not work in men" would misstate the evidence; recording it as "the benefit-risk case was only made in women" is accurate.
Source
Efficacy and tolerability of alosetron for the treatment of irritable bowel syndrome in women and men: a meta-analysis. Clin Ther 2008;30:884-901
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
Blinded re-adjudication cut the case count before any rate was computed
In plain words
An expert panel that did not know who was on the drug reviewed each reported case and discarded those that were not really ischaemic colitis or not plausibly drug-related.
What was measured
Not recorded
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
The adjudication panel comprised experts in epidemiology and functional bowel disorders, reviewed the primary trial report forms and MedWatch forms for each case, was blinded to whether the patient received alosetron or placebo, and applied pre-specified criteria to rate both diagnostic accuracy and the plausibility of a drug association. Cases inconsistent with the reported diagnosis or not possibly drug-associated were removed before the incidence rates were computed. That procedure is what separates the resulting figure — 1.1 per 1,000 patient-years — from a raw count of spontaneous reports. It is the same instrument that reversed the tegaserod decision on the same page of this file, applied here in the same direction rather than the opposite one.
Source
Chang L et al. Am J Gastroenterol 2006;101:1069-1079
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

How many documents were read

  • 9 documents were read for this substance.

    RNAWiki source record

  • 9 of them state the same halfLife, and they agree.

    RNAWiki source record

  • 9 of them state the same bioavailability, and they agree.

    RNAWiki source record

  • 9 of them state the same tMax, and they agree.

    RNAWiki source record

  • 9 of them state the same proteinBinding, and they agree.

    RNAWiki source record

Where else this substance is registered

FDA substance identifier (UNII)
2F5R1A46YW
RxNorm concept
403975

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    Suppression classes recorded: S6.

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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

  • 7 approved applications cover products containing this substance. The earliest was NDA021107, approved 20000209 to LEGACY.

    Drugs@FDA application register · NDA021107 · read 2026-08-29

  • Marketing status on the register: discontinued and prescription.

    Drugs@FDA application register · NDA021107 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 20160711.

    FDA National Drug Code directory · 73190-035 · read 2026-08-29

What is missing or unclearRead from sources, not yet reviewed

What to learn next

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What is not here

7 questions this page could not answer

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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.

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 5-HT3 antagonist withdrawn nine months after approval over ischaemic colitis and complications of constipation, and returned in 2002 under restricted prescribing once the harms were quantified — a post-adjudication rate of 1.1 cases of ischaemic colitis per 1,000 patient-years, all 19 trial cases reversible without long-term sequelae, against a relative risk of 1.60 for global symptom improvement.

Recorded evidence blocks (8)

On the Alosetron label: indicated for what?


"LOTRONEX is indicated only for women with severe diarrhea-predominant irritable bowel syndrome (IBS) who have: chronic IBS symptoms (generally lasting 6 months or longer), had anatomic or biochemical abnormalities of the gastrointestinal tract excluded, and not responded adequately to conventional therapy.…": indications and usage on Alosetron's label. DailyMed label · 35cbb9d5-639b-207a-e054-00144ff88e88 · 2026-06-30

3 registered trials of Alosetron — at which phases?


Registered studies posting no result
2 of 3

3 registered studies of Alosetron: 2 phase3, 1 phase4. CLINICALTRIALS_SNAPSHOT · 2026-09-01

37 with a PubMed record

Show the evidence
  • phase3
    2
  • phase4
    1
  • completed
    3

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

Alosetron's half-life is 1.5 hours — which schedules were studied?


1.5 hours, the half-life Alosetron's label states: "The terminal elimination half-life of alosetron is approximately 1.5 hours (plasma clearance is approximately 600 mL/min)." DailyMed label · 35cbb9d5-639b-207a-e054-00144ff88e88 · 2026-06-30

tmax 1 hour; bioavailability 50 %.

Show the evidence
  • half life pharmacokinetics
    1.5 hours; The terminal elimination half-life of alosetron is approximately 1.5 hours (plasma clearance is approximately 600 mL/min).
  • tmax pharmacokinetics
    1 hour; Following oral administration of a 1 mg alosetron dose to young men, a peak plasma concentration of approximately 5 ng/mL occurred at 1 hour.
  • bioavailability pharmacokinetics
    50 %; Absorption: Alosetron was rapidly absorbed after oral administration with a mean absolute bioavailability of approximately 50% to 60% (approximate range, 30% to >90%).
  • metabolism pharmacokinetics
    Metabolism and Elimination: Plasma concentrations of alosetron increase proportionately with increasing single oral doses up to 8 mg and more than proportionately at a single oral dose of 16 mg.

recorded 2026-06-30 · last checked 2026-09-04

Which 2 trials of Alosetron posted no result?


Posted no result
2 of 2 completed trials
Registrations
NCT00067561 and NCT00067457
Completion dates
oldest 2005-01; newest 2005-12
Show the evidence

Trial

  • NCT00067561
    2005-01
  • NCT00067457
    2005-12

At the median, Alosetron's trials enrolled 700 people — anything larger?


Median enrolment
700
Largest enrolment
702
Registered trials counted
3

What do 19 spontaneous reports say about Alosetron — 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.

Alosetron appears in spontaneous reports to regulators. Across the 8 most-reported reaction terms, 19 reaction mentions were counted: nausea 4; abdominal pain 3; colitis ischaemic 3; constipation 3. FAERS via Open Targets · CHEMBL1110 · 2026-06-24

Show the evidence
  • nausea
    4
  • abdominal pain
    3
  • colitis ischaemic
    3
  • constipation
    3
  • haemorrhoids
    2
  • intestinal obstruction
    2
2 more recorded rows
  • faecal occult blood positive
    1
  • mean platelet volume decreased
    1

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

Which 8 reactions does Alosetron's label not list?


abdominal pain, colitis ischaemic and constipation and 5 more reported for Alosetron, absent from its label. FAERS via Open Targets · CHEMBL1110 · 2026-06-24

2 label terms; 8 reported and unlisted; 35cbb9d5-639b-207a-e054-00144ff88e88

Show the evidence
  • abdominal pain
    count not stated
  • colitis ischaemic
    count not stated
  • constipation
    count not stated
  • faecal occult blood positive
    count not stated
  • haemorrhoids
    count not stated
  • intestinal obstruction
    count not stated
2 more recorded rows
  • mean platelet volume decreased
    count not stated
  • nausea
    count not stated

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

Alosetron and CYP3A4, CYP1A2 and CYP2C9: shared by which compounds?


CYP3A4, CYP1A2 and CYP2C9 appear in Alosetron's recorded interaction sentences, 8 in all. DailyMed label · 35cbb9d5-639b-207a-e054-00144ff88e88 · 2026-06-30

CYP1A2, CYP2C19, CYP2C9, CYP2C9, CYP2E1, CYP3A4; 7 shared nodes; drug_interactions

Show the evidence

Interaction statement

  • drug_interactions
    In vivo data suggest that alosetron is primarily metabolized by cytochrome P450 (CYP) 1A2, with minor contributions from CYP3A4 and CYP2C9.
  • drug_interactions
    CYP1A2 inhibitors: Avoid concomitant uses because of increased exposure and half-life of alosetron.
  • drug_interactions
    ( 4.3 , 7.1 ) CYP3A4 inhibitors: Use with caution in combination due to increased exposure of alosetron.
  • drug_interactions
    ( 7.2 ) 7.1 CYP1A2 Inhibitors Fluvoxamine is a known strong inhibitor of CYP1A2 and also inhibits CYP3A4, CYP2C9, and CYP2C19.
  • drug_interactions
    Concomitant administration of alosetron and moderate CYP1A2 inhibitors, including quinolone antibiotics and cimetidine, has not been evaluated, but should be avoided unless clinically necessary because of similar potential drug interactions.
  • drug_interactions
    7.2 CYP3A4 Inhibitors Ketoconazole is a known strong inhibitor of CYP3A4.
2 more recorded rows
  • Interaction statement drug_interactions
    Coadministration of alosetron and strong CYP3A4 inhibitors such as clarithromycin, telithromycin, protease inhibitors, voriconazole, and itraconazole has not been evaluated but should be undertaken with caution because of similar potential drug interactions.
  • Interaction statement drug_interactions
    In an in vivo metabolic probe study, alosetron did not inhibit CYP2E1 but did produce 30% inhibition of both CYP1A2 and N-acetyltransferase.
  • CYP1A2
    FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Golodirsen, Tinidazole
  • CYP2C19
    FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Golodirsen, Naldemedine, Etravirine

CYP2C9

  • FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Golodirsen, Tinidazole, Naldemedine
  • FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Golodirsen, Tinidazole, Naldemedine
  • CYP2E1
    FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, Rasagiline, Tinidazole, Naldemedine, Methylnaltrexone, Metaxalone, Uridine triacetate

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

recorded 2026-06-30 · last checked 2026-09-04

Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL1110
PubChem CID
2099
CAS number
122852-42-0
RxCUI
85248
InChIKey
JSWZEAMFRNKZNL-UHFFFAOYSA-N
Development code
A03AE01, GR 68755C
Also called
ALOSETRON HYDROCHLORIDE, Lotrpnex, ALOSETRON [MI], ALOSETRON [VANDF], Alosetron [WHO-DD], alosetron [INN]
Salt form
Alosetron hcl
Trade name
Lotronex
Sources (5)

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

Index-quality checks
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  • 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: 5 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

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