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Alpelisib

  • 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 Alpelisib does in the body

PIQRAY is indicated in combination with fulvestrant for the treatment of adults with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer as detected by an FDA-approved test following progression on or after an endocrine-based regimen.

From the FDA-approved label: Alpelisib is an inhibitor of phosphatidylinositol-3-kinase (PI3K) with inhibitory activity predominantly against PI3Kα. Gain-of-function mutations in the gene encoding the catalytic α-subunit of PI3K (PIK3CA) lead to activation of PI3Kα and Akt-signaling, cellular transformation and the generation of tumors in in vitro and in vivo models. In breast cancer cell lines, alpelisib inhibited the phosphorylation of PI3K downstream targets, including Akt and showed activity in cell lines harboring a PIK3CA mutation. In vivo, alpelisib inhibited the PI3K/Akt signaling pathway and reduced tumor growth in xenograft models, including models of breast cancer.

Why people take it. PIQRAY is indicated in combination with fulvestrant for the treatment of adults with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer as detected by an FDA-approved test following progression on or after an endocrine-based regimen.

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
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 · 08W5N2C97Q · read 2026-08-29

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 197 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.

Stand-in result

A stand-in result is a number measured because the real result takes too long.

A picture of it, and where the picture fails

It is like judging a journey by the speedometer rather than by arriving.

Where that stops being true. Speed does predict arrival. Many stand-in results do not predict the real one.

What people get wrong. A stand-in result is often reported as the result itself.

A surrogate endpoint substituted for a clinical endpoint, valid only where the substitution has been shown to hold.

Enzyme

An enzyme is a protein that speeds up one chemical change.

A picture of it, and where the picture fails

An enzyme is like a machine on a production line doing one cut.

Where that stops being true. A machine is switched on and off by a person. Enzymes are controlled by the cell.

What people get wrong. Enzymes are thought to be used up. They are not; they work again and again.

A catalytic protein that lowers the activation energy of a specific reaction.

Receptor

A receptor is a part of a cell that a signal fits into.

A picture of it, and where the picture fails

A receptor is like a lock waiting for one key.

Where that stops being true. A lock either opens or does not. A receptor can be half-triggered, or worn out.

What people get wrong. Fitting a receptor is read as causing a benefit. It causes a step, and nothing more.

A protein that binds a specific ligand and converts that binding into a cellular response.

Pathway

A pathway is a chain of steps inside a cell, each one setting off the next.

A picture of it, and where the picture fails

A pathway is like a row of dominoes.

Where that stops being true. Dominoes fall one way. Pathways loop back and can switch themselves off.

What people get wrong. Changing one step is read as changing the outcome. Other steps often absorb it.

An ordered series of molecular interactions producing a defined cellular change.

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.

16 weeks clinical response

The study did not show it

Who was studied
NCT04817956
How many people
3000
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. Oral

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

Accrual of patients to ComboMATCH treatment trials

The study did not show it

Who was studied
NCT05564377
How many people
2900
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. Oral

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

Percentage of patients that are treated based on their molecular tumor profile

The study did not show it

Who was studied
NCT02925234
How many people
1550
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. Oral

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

Number of participants who experience at least 1 Dose Limiting Toxicity (DLT)

The study did not show it

Who was studied
NCT05768139
How many people
880
Study design
Phase 1/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. Oral

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

Progression Free Survival (PFS) in Patients with PIK3CA WT and PIK3CA MT Breast Cancer

The study did not show it

Who was studied
NCT05501886
How many people
701
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
Living longer, or avoiding a major event
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. Oral

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

Progression-free Survival (PFS) Per Investigator Assessment in the PIK3CA Mutant Cohort

The study did not show it

Who was studied
NCT02437318
How many people
572
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
Living longer, or avoiding a major event
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. Oral

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 happened in peopleRead from sources, not yet reviewed

How close this is to real life

The top step is something a person would feel or care about. The bottom is a guess from software. Filled steps are where evidence exists for this substance.

  1. Living longer, or avoiding a major event Evidence recorded. Death, a heart attack, a stroke, a hospital stay.4 registered measures of this kind. 2 written-up studies measured this and did not show a benefit.
  2. What a body can do day to day No evidence recorded. Walking, dressing, breathing, recovering.No registered study measures this.
  3. Measured performance No evidence recorded. How much was lifted, how far was run, how fast.No registered study measures this.
  4. Symptoms and quality of life No evidence recorded. Pain, tiredness, mood, sleep, as the person rated it.No registered study measures this.
  5. A number that stands in for health Evidence recorded. Cholesterol, blood sugar, bone density. A stand-in, not the thing itself.1 registered measure of this kind.
  6. A step measured inside a person Evidence recorded. Something measured in human tissue or human cells.A human record sits on the stored organism ladder.
  7. Animals Evidence recorded. Mice, rats, dogs. Useful for ideas, not proof about people.Stored records in Mouse. A result in animals says what to test next. It does not say what happens in people.
  8. Cells in a dish Evidence recorded. Cells or chemistry on a bench, far from a whole body.Stored mechanism abstracts describe steps measured in cells or tissue.
  9. A guess from software No evidence recorded. Nobody measured it. RNAWiki never publishes one as a finding.RNAWiki stores no prediction for this record. Software can suggest a link. RNAWiki does not publish one as a finding.

Higher on these steps means closer to something a person would feel. It does not mean better done.

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

Felt, measured, or meaningful

Three different things that get called the same word. Registered studies measured all three, and mixing them is how a blood test becomes a health claim.

Felt

Things a person could notice without a test.

No registered study measured anything of this kind.

Measured

Things only a test, a scale or a device shows.

  • sub study maximum observed drug concentration for midazolam

Meaningful

Things that change how a life goes, not only a number.

  • progression free survival
  • part 2 progression free survival
  • progression free survival rate at 4 months
  • progression free survival in the study groups

A registered study says what someone planned to measure. It does not say what they found. A number moving is not the same as a life going better. The two are shown apart here.

Felt, but not shown to help. A person notices a change. No study showed it leads anywhere good.

Measured, but not felt. A number moves. The person notices nothing. Both can be true.

Measured, but not shown to matter. A number moves in the good direction. Nobody showed that lives went better.

Matters, but takes years. The result that counts may take longer than anyone would keep watching.

Names that fit none of the three (35)
  • phase ib incidence of dose limiting toxicities in cycle 1
  • dose limiting toxicities phase ib
  • maximum tolerated dose and/or recommended phase ii dose
  • dose escalation incidence of dose limiting toxicity
  • incidence of dose limiting toxicities
  • that are treated based on their molecular tumor profile
  • objective tumor response
  • stable disease
  • treatment related grade 3 and serious adverse events
  • hotspot mutated genes by scheduled timepoint
  • screening in target mutation variant allele frequency
  • partial response in the extension phase
  • dose limiting toxicities and dlt equivalent toxicities
  • overall response rate in cdk4/6 inhibitor naive
  • overall response rate
  • incidence proportion of hyperglycemia
  • dose limiting toxicity
  • descriptive statistics of adverse events
  • hyperglycemia free rate for
  • ki67

These are harms, study-process measures, or names the rules did not recognise. They are shown rather than dropped.

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

How long anything takes

Nine different lengths of time that get confused with each other. None of them is worked out from another.

  1. Before anything is noticed. RNAWiki does not store this separately, and never works it out from another figure on this page.

  2. Before a test result moves. RNAWiki does not store this separately, and never works it out from another figure on this page.

  3. Before performance moves. RNAWiki does not store this separately, and never works it out from another figure on this page.

  4. How long the result was watched. No finished study window is recorded for a study that tested this substance.

  5. How long people took it. How long people actually took it is not stored. The study window is not the same thing.

  6. How long people were followed. Follow-up length is not stored separately. It is never read off the study window, which would be a different thing.

  7. How fast the body clears it. 8 to 9 hours hours

    Read from the label, which states: “Elimination The half-life of alpelisib is predicted to be 8 to 9 hours.”

  8. How long effects linger. RNAWiki does not store this separately, and never works it out from another figure on this page.

  9. Beyond the studies. Nothing is recorded about the long term.

    The longest finished study sets the edge of what anyone measured.

A study window is not how long people took it, and neither is how long they were followed. Where RNAWiki holds only one of the three, it shows one.

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.

  • VIJOICE is indicated for the treatment of adult and pediatric patients 2 years of age and older with severe manifestations of PIK3CA-Related Overgrowth Spectrum (PROS) who require systemic therapy. This indication is approved under accelerated approval based on response rate and duration of response.

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 efficacy of PIQRAY in pediatric patients have not been established.”

    US prescribing information · b20b4e18-7a4b-4500-a08f-06c6dab0ee5b · read 2026-08-30

  • On older people, the label states: “Of 284 patients who received PIQRAY in the SOLAR-1 trial, 117 patients were ≥ 65 years of age and 34 patients were ≥ 75 years of age.”

    US prescribing information · b20b4e18-7a4b-4500-a08f-06c6dab0ee5b · read 2026-08-30

  • On people who are pregnant, the label states: “Risk Summary PIQRAY is used in combination with fulvestrant.”

    US prescribing information · b20b4e18-7a4b-4500-a08f-06c6dab0ee5b · read 2026-08-30

  • On people who are breastfeeding, the label states: “PIQRAY is used in combination with fulvestrant.”

    US prescribing information · b20b4e18-7a4b-4500-a08f-06c6dab0ee5b · read 2026-08-30

  • On people with reduced kidney function, the label states: “The effect of severe renal impairment (CLcr < 30 mL/min) on alpelisib pharmacokinetics is unknown [see Clinical Pharmacology (12.3)] .”

    US prescribing information · b20b4e18-7a4b-4500-a08f-06c6dab0ee5b · 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 for a different goal

The studies measured something else entirely.

On this record: Some registered studies measured things that match no goal on this page.

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 (10)
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

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: S1, S3, S4.

No source is stored against this line.

What is in the pack

Sold as tablet, granule, given by the 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.

Reports sent to a regulator

  • 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.

Alpelisib appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 1799 reaction mentions were counted. One report can name several reactions.

The recorded terms (10)
  • hyperglycaemia — 497 reaction mentions
  • rash — 403 reaction mentions
  • diarrhoea — 223 reaction mentions
  • blood glucose increased — 173 reaction mentions
  • nausea — 158 reaction mentions
  • malignant neoplasm progression — 99 reaction mentions
  • decreased appetite — 68 reaction mentions
  • stomatitis — 62 reaction mentions
  • breast cancer metastatic — 58 reaction mentions
  • weight decreased — 58 reaction mentions
  • open-targets-adr · recorded 2026-06-24 · a recorded source, not a stored snapshot

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

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

  • 13 products list this as an active ingredient in the United States drug directory. 13 of them contain it and nothing else.

    FDA National Drug Code directory · 0078-0701 · read 2026-08-29

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

    FDA National Drug Code directory · 0078-0701 · read 2026-08-29

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

    US prescribing information · b20b4e18-7a4b-4500-a08f-06c6dab0ee5b · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · b20b4e18-7a4b-4500-a08f-06c6dab0ee5b · read 2026-08-29

  • PIQRAY is oral at 3 DOSAGE FORMS AND STRENGTHS Tablets: 50 mg, 150 mg, and 200 mg alpelisib 50 mg: Light pink, unscored, round and curved with beveled edges film-coated tablet, imprinted with “L7” on one side and “NVR” on the other side.…, recorded as fda label in effect 2025-12-15 in the United States.

    US prescribing information · b20b4e18-7a4b-4500-a08f-06c6dab0ee5b · 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.

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 Alpelisib 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.

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 Alpelisib 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.

How many documents were read

  • 2 documents were read for this substance.

    RNAWiki source record

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

    RNAWiki source record

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

    RNAWiki source record

  • 2 of them state the same volumeOfDistribution, and they agree.

    RNAWiki source record

Where else this substance is registered

FDA substance identifier (UNII)
08W5N2C97Q
RxNorm concept
2169300

Checks this page had to pass

  • Passed

    Identity resolved

    no open identity hold

  • Passed

    No unresolved merge across substance families

    no quarantine open

  • Passed

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    Trial roles classified for highlighted evidence

    No registered study is classified as testing this substance.

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  • Passed

    Safety mode resolved

    Suppression classes recorded: S1, S3, S4.

  • 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.

What the approval register records

  • 3 approved applications cover products containing this substance. The earliest was NDA212526, approved 20190524 to NOVARTIS.

    Drugs@FDA application register · NDA212526 · read 2026-08-29

  • Marketing status on the register: prescription.

    Drugs@FDA application register · NDA212526 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 20190524.

    FDA National Drug Code directory · 0078-0701 · 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

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  • What was measured, goal by goal — found nothing in the sources checked.
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  • 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.
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Recorded evidence blocks (14)

What did Alpelisib's largest trial (2900 people) and its longest (11 years) measure?


2900 people in Alpelisib's largest registered study, 11 years in its longest registered window, measuring Sub-study: Maximum observed Drug Concentration (Cmax) for Midazolam. ClinicalTrials.gov · 2026-09-01

38 phase2, 22 phase1, 10 phase3, 9 na or unstated, 2 na, 1 early phase1, 1 phase4; NCT02925234; 2027-12; no ageing endpoint recorded. Last human test completed 2026, NCT06083038.

Interpretation These counts include studies where Alpelisib was a comparison treatment, a background treatment or an exposure in an observational study, and the longest window may be a planned end date. Trial roles have not yet been classified for this record.

Show the evidence
  • phase2
    38
  • phase1
    22
  • phase3
    10
  • na or unstated
    9
  • na
    2
  • early phase1
    1
2 more recorded rows
  • phase4
    1
  • Last recorded human test NCT06083038
    2026-04-21

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

From mouse to human: where has Alpelisib shown lifespan?


mouse: lifespan and human: biomarker (74): the rungs where Alpelisib has a recorded finding. Europe PMC and ClinicalTrials.gov · organism ladder · 2026-09-01

Interpretation Sub-study: Maximum observed Drug Concentration (Cmax) for Midazolam — the recorded outcome words.

Yeast C. elegans Drosophila Mouse lifespanRat Dog Non-human primate Human biomarker
Show the evidence
  • mouse
    lifespan
  • human NCT05646862
    biomarker; Sub-study: Maximum observed Drug Concentration (Cmax) for Midazolam; 74

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

17 of Alpelisib's trials stopped: safety, accrual/recruitment, funding/business, sponsor decision unspecified, other?


safety (3), accrual/recruitment (5), funding/business (2), sponsor decision unspecified (2) and other (5): Alpelisib's stop wording, clustered. ClinicalTrials.gov · 2026-09-01

"early termination due to Sponsor decision (slow recruitment)"; 17 of 74 registered studies

Show the evidence

Trial

  • NCT01602315
    terminated; "early termination due to Sponsor decision (slow recruitment)"
  • NCT02620839
    terminated; "Funding"
  • NCT02734615
    terminated; "Sponsor's decision"
  • NCT03284957
    terminated; "Sponsor decision to prematurely stop the study, not linked to any safety concern."
  • NCT03386162
    terminated; "Study was halted Prematurely for low recruitment."
  • NCT03439046
    terminated; "Novartis terminated the trial early because the collected data were sufficient to perform the analysis stated for the primary endpoint."
11 further recorded trials
  • NCT03601507
    terminated; "Novartis has chosen to withdraw support for this trial"
  • NCT04216472
    terminated; "\<75% participation"
  • NCT04251533
    terminated; "The study was terminated following a strategic decision to halt recruitment due to persistently slow enrollment. This decision was not driven by any new or unexpected safety concerns."
  • NCT04729387
    terminated; "Sponsor Decision"
  • NCT04801966
    terminated; "low recruitment"
  • NCT04862143
    terminated; "Study early terminated due to low enrollment compared to the anticipated figures"
  • NCT04899349
    terminated; "Study was early terminated due to slow recruitment and emerging data showing that prophylactic use of metformin may prevent or reduce the incidence of all-grades alpelisib-related hyperglycemia. The decision was not driven by safety…"
  • NCT04967248
    terminated; "Low recruitment"
  • NCT05238831
    withdrawn; "Withdrawn due to a change in therapeutic interventions."
  • NCT05472220
    withdrawn; "Sponsor funding"
  • NCT05967286
    withdrawn; "Other - Protocol moved to Withdrawn"

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

Human studies of Alpelisib used Alpelisib 150 MG Oral Tablet [Piqray] — over how long?


studies of Alpelisib used the recorded amount. ClinicalTrials.gov · 2026-09-01

3 recorded entries; human; also "Alpelisib 150 MG Oral Tablet [Piqray]", "Alpelisib 150 mg [Piqray], 2 overencapsulated tablets (total: 300 mg)", "Alpelisib 300 mg"

Show the evidence

human

  • NCT05392608
    Alpelisib 150 MG Oral Tablet [Piqray]
  • NCT05733455
    Alpelisib 150 mg [Piqray], 2 overencapsulated tablets (total: 300 mg)
  • NCT06354088
    Alpelisib 300 mg

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

Alpelisib's half-life is 8 to 9 hours — which schedules were studied?


8 to 9 hours, the half-life Alpelisib's label states. openfda-label · b20b4e18-7a4b-4500-a08f-06c6dab0ee5b · 2026-08-30

Show the evidence
  • half life
    8 to 9 hours hours; Elimination The half-life of alpelisib is predicted to be 8 to 9 hours.
  • tmax
    In adult patients who received PIQRAY 300 mg once daily in the SOLAR-1 trial, population approach derived mean steady-state alpelisib [coefficient of variation (CV%)] for C max was 2480 (23%) ng/mL and AUC 0-24hr was 33224 (21%) ng*h/mL. Absorption The median time to reach peak plasma concentration (T max ) ranged between 2.0 to 4.0 hours.
  • metabolism
    Metabolism Alpelisib is primarily metabolized by chemical and enzymatic hydrolysis to form its metabolite BZG791 and followed by CYP3A4 mediated hydroxylation.

recorded 2026-08-30 · last checked 2026-09-04

Which of accrual of to combomatch treatment trials, assignment of to combomatch treatment trials and at least one on treatment adverse events did Alpelisib's trials measure?


accrual of to combomatch treatment trials, assignment of to combomatch treatment trials and at least one on treatment adverse events lead 40 outcome terms across Alpelisib's trials. ClinicalTrials.gov · 2026-09-01

dose escalation incidence of dose limiting toxicity, incidence of dose limiting toxicities, that are treated based on their molecular tumor profile, objective tumor response, stable disease and treatment related grade 3 and serious adverse events follow.

Show the evidence
  • phase ib incidence of dose limiting toxicities in cycle 1
    1
  • dose limiting toxicities phase ib
    1
  • maximum tolerated dose and/or recommended phase ii dose
    1
  • dose escalation incidence of dose limiting toxicity
    1
  • incidence of dose limiting toxicities
    1
  • that are treated based on their molecular tumor profile
    1
14 more recorded rows
  • objective tumor response
    1
  • stable disease
    1
  • treatment related grade 3 and serious adverse events
    1
  • progression free survival
    1
  • hotspot mutated genes by scheduled timepoint
    1
  • screening in target mutation variant allele frequency
    1
  • partial response in the extension phase
    1
  • dose limiting toxicities and dlt equivalent toxicities
    1
  • part 2 progression free survival
    1
  • overall response rate in cdk4/6 inhibitor naive
    1
  • progression free survival rate at 4 months
    1
  • overall response rate
    1
  • incidence proportion of hyperglycemia
    1
  • dose limiting toxicity
    1

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

Which of Alpelisib's 33 ongoing trials reports first?


33 registered trials of Alpelisib are open; earliest completion 2026-05. ClinicalTrials.gov · 2026-09-01

Percentage of patients that are treated based on their molecular tumor profile; Number of Participants with Dose Limiting Toxicities (DLTs) and DLT-Equivalent Toxicities; latest 2033-05-02

Show the evidence

Trial

  • NCT02925234
    "The Drug Rediscovery Protocol (DRUP Trial)"; n 1550; "Percentage of patients that are treated based on their molecular tumor profile"; 2027-12
  • NCT04085653
    "Managed Access Programs for BYL719, Alpelisib"
  • NCT04188548
    "A Study of LY3484356 in Participants With Advanced or Metastatic Breast Cancer or Endometrial Cancer"; n 379; "Number of Participants with Dose Limiting Toxicities (DLTs) and DLT-Equivalent Toxicities"; 2027-12
  • NCT04208178
    "Study of Alpelisib (BYL719) in Combination With Trastuzumab and Pertuzumab as Maintenance Therapy in Patients With HER2-positive Advanced Breast Cancer With a PIK3CA Mutation"; n 19; "Part 1: Incidence of dose limiting toxicities (DLTs) for each dose level"; 2027-02-26
  • NCT04524000
    "Study Assessing the Efficacy and Safety of Treatment With Alpelisib Plus Fulvestrant in Japanese Men and Postmenopausal Women With Advanced Breast Cancer"; n 24; "[Part 1] The incidence of Dose Limiting Toxicities (DLTs) of alpelisib in combination with fulvestrant"; 2027-02-27
  • NCT04544189
    "Study Assessing the Efficacy and Safety of Treatment With Alpelisib Plus Fulvestrant Versus Placebo Plus Fulvestrant in Chinese Men and Postmenopausal Women With Advanced Breast Cancer"; n 69; "Progression Free Survival (PFS)"; 2027-01-29
14 further recorded trials
  • NCT04589650
    "Study Assessing the Efficacy, Safety and PK of Alpelisib (BYL719) in Pediatric and Adult Patients With PIK3CA-related Overgrowth Spectrum"; n 206; "Proportion of Participants Randomized to Alpelisib With a Confirmed Objective Response by BIRC in Group 1 and Group 2"; 2031-01-09
  • NCT04762979
    "Alpelisib (BYL719) in Combination With Continued Endocrine Therapy Following Progression on Endocrine Therapy in Hormone Receptor Positive, HER2 Negative, PIK3CA Mutant Metastatic Breast Cancer"; n 44; "Progression-Free Survival (PFS)"; 2026-05
  • NCT04980833
    "Study Assessing Long-term Safety and Efficacy of Alpelisib in Patients With PIK3CA-Related Overgrowth Spectrum (PROS) Who Previously Participated in Study CBYL719F12002 (EPIK-P1)"; n 41; "Prospective period only: Proportion of participants with new or worsening grade ≥3 treatment emergent adverse events (AEs)"; 2027-08-20
  • NCT05038735
    "Study to Assess the Efficacy and Safety of Alpelisib Plus Fulvestrant in Participants With HR-positive (HR+), HER2-negative, Advanced Breast Cancer After Treatment With a CDK4/6 Inhibitor and an Aromatase Inhibitor."; n 210; "Progression-free survival (PFS) based on BIRC assessments and using RECIST v1.1 criteria"; 2027-02-26
  • NCT05063786
    "Trastuzumab + Alpelisib +/- Fulvestrant vs Trastuzumab + CT in Patients With PIK3CA Mutated Previously Treated HER2+ Advanced BrEasT Cancer (ALPHABET)"; n 27; "Progression Free Survival (PFS)"; 2026-06
  • NCT05090358
    "Preventing High Blood Sugar in People Being Treated for Metastatic Breast Cancer"; n 15; "Hyperglycemia-free rate for participants"; 2027-10-08
  • NCT05143229
    "Alpelisib And Sacituzumab Govitecan For Treatment Of Breast Cancer"; n 18; "Recommended phase II dose (RP2D) of alpelisib + sacituzumab govitecan"; 2026-12
  • NCT05154487
    "A Study of Alpelisib and Fulvestrant to Treat Endometrial Cancer"; n 51; "Response rate"; 2028-11-01
  • NCT05230810
    "Clinical Trial of Alpelisb and Tucatinib in Patients With PIK3CA-Mutant HER2+ Metastatic Breast Cancer."; n 40; "Phase Ib Safety and Tolerability of alpelisib and tucatinib combination, summary of all AEs and SAEs on study as evaluated by NCI-CTCAE v 5.0"; 2026-06-30
  • NCT05293470
    "A Post Marketing Surveillance on Piqray in Korea"; n 900; "Incidence of AEs"; 2027-05-12
  • NCT05392608
    "SEQUence of Endocrine Therapy in Advanced Luminal Breast Cancer (SEQUEL-Breast)"; n 130; "Progression-free survival (PFS)"; 2028-03
  • NCT05501886
    "Gedatolisib Plus Fulvestrant With or Without Palbociclib vs Standard-of-Care for the Treatment of Patients With Advanced or Metastatic HR+/HER2- Breast Cancer (VIKTORIA-1)"; n 701; "Progression Free Survival (PFS) in Patients with PIK3CA WT and PIK3CA MT Breast Cancer"; 2026-12-31
  • NCT05508906
    "Phase 1b Study of OP-1250 (Palazestrant) in Combination With Ribociclib, Alpelisib, Everolimus, or Atirmociclib in ER+, HER2- Breast Cancer"; n 190; "Dose Limiting Toxicities (DLTs)"; 2028-01-31
  • NCT05563220
    "Open-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Participants With Metastatic Breast Cancer"; n 435; "Number of Participants with DLTs Observed During the First Cycle"; 2028-12-28

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

Which running trial of Alpelisib could settle lifespan?


NCT04762979 measures Progression-Free Survival (PFS), reading out 2026-05.

9 open trials; n 44; "Alpelisib (BYL719) in Combination With Continued Endocrine Therapy Following Progression on Endocrine Therapy in Hormone Receptor Positive, HER2 Negative, PIK3CA Mutant Metastatic Breast Cancer"

Show the evidence

Trial

  • NCT04762979
    "Alpelisib (BYL719) in Combination With Continued Endocrine Therapy Following Progression on Endocrine Therapy in Hormone Receptor Positive, HER2 Negative, PIK3CA Mutant Metastatic Breast Cancer"; n 44; "Progression-Free Survival (PFS)"; 2026-05
  • NCT05063786
    "Trastuzumab + Alpelisib +/- Fulvestrant vs Trastuzumab + CT in Patients With PIK3CA Mutated Previously Treated HER2+ Advanced BrEasT Cancer (ALPHABET)"; n 27; "Progression Free Survival (PFS)"; 2026-06
  • NCT05501886
    "Gedatolisib Plus Fulvestrant With or Without Palbociclib vs Standard-of-Care for the Treatment of Patients With Advanced or Metastatic HR+/HER2- Breast Cancer (VIKTORIA-1)"; n 701; "Progression Free Survival (PFS) in Patients with PIK3CA WT and PIK3CA MT Breast Cancer"; 2026-12-31
  • NCT04544189
    "Study Assessing the Efficacy and Safety of Treatment With Alpelisib Plus Fulvestrant Versus Placebo Plus Fulvestrant in Chinese Men and Postmenopausal Women With Advanced Breast Cancer"; n 69; "Progression Free Survival (PFS)"; 2027-01-29
  • NCT05038735
    "Study to Assess the Efficacy and Safety of Alpelisib Plus Fulvestrant in Participants With HR-positive (HR+), HER2-negative, Advanced Breast Cancer After Treatment With a CDK4/6 Inhibitor and an Aromatase Inhibitor."; n 210; "Progression-free survival (PFS) based on BIRC assessments and using RECIST v1.1 criteria"; 2027-02-26
  • NCT05392608
    "SEQUence of Endocrine Therapy in Advanced Luminal Breast Cancer (SEQUEL-Breast)"; n 130; "Progression-free survival (PFS)"; 2028-03
3 further recorded trials
  • NCT05646862
    "A Study Evaluating the Efficacy and Safety of Inavolisib Plus Fulvestrant Compared With Alpelisib Plus Fulvestrant in Participants With HR-Positive, HER2-Negative, PIK3CA Mutated, Locally Advanced or Metastatic Breast Cancer Post CDK4/6i and Endocrine Combination Therapy"; n 420; "Blinded Independent Central Review (BICR)-Assessed Progression Free Survival (PFS)"; 2029-03-30
  • NCT05826964
    "Levels of Circulating Tumor DNA as a Predictive Marker for Early Switch in Treatment for Patients With Metastatic (Stage IV) Breast Cancer"; n 24; "Progression-Free Survival 1 (PFS1) Among Participants in Step 2"; 2029-07-31
  • NCT05625087
    "Detection of Tumor DNA in the Blood of Patients Receiving Standard Therapy for Hormone Receptor-positive (HR+) Non-HER2 Expressing (HER2-) Metastatic Breast Cancer as a Tool to Select Those Who May Benefit From the Next Course of Fulvestrant in Combination With Alpelisib or Ribociclib"; n 162; "Progression-Free Survival in the study groups"; 2030-06

Which 6 trials of Alpelisib posted no result?


Posted no result
6 of 6 completed trials
Registrations
NCT02624557, NCT02058381, NCT02077933, NCT05733455, NCT03207529 and NCT05294289
Completion dates
oldest 2017-10-01; newest 2024-06-28
Show the evidence

Trial

  • NCT02624557
    2017-10-01
  • NCT02058381
    2018-06-19
  • NCT02077933
    2019-04-12
  • NCT05733455
    2023-12-01
  • NCT03207529
    2023-12-31
  • NCT05294289
    2024-06-28

At the median, Alpelisib's trials enrolled 50 people — anything larger?


Median enrolment
50
Largest enrolment
2900
Registered trials counted
71

What do 1799 spontaneous reports say about Alpelisib — 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.

Alpelisib appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 1799 reaction mentions were counted: hyperglycaemia 497; rash 403; diarrhoea 223; blood glucose increased 173. open-targets-adr · CHEMBL2396661 · 2026-06-24

Show the evidence
  • hyperglycaemia
    497
  • rash
    403
  • diarrhoea
    223
  • blood glucose increased
    173
  • nausea
    158
  • malignant neoplasm progression
    99
4 more recorded rows
  • decreased appetite
    68
  • stomatitis
    62
  • breast cancer metastatic
    58
  • weight decreased
    58

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

Alpelisib and CYP3A4, BCRP and P-GP: shared by which compounds?


CYP3A4, BCRP and P-GP appear in Alpelisib's recorded interaction sentences, 11 in all. openfda-label+europepmc · 2026-08-30

Interpretation pharmacokinetics

Show the evidence
  • CYP2B6 pharmacokinetics
    CYP3A4, CYP2C8, CYP2C9, CYP2C19 and CYP2B6 Substrates: Coadministration of repeated doses of alpelisib 300 mg with a single-dose of sensitive substrates of CYP3A4 (midazolam), CYP2C8 (repaglinide), CYP2C9 (warfarin), CYP2C19 (omeprazole) and CYP2B6 (bupropion), administered as a cocktail did not show clinically significant pharmacokinetic interactions.
  • CYP2C19 pharmacokinetics
    CYP3A4, CYP2C8, CYP2C9, CYP2C19 and CYP2B6 Substrates: Coadministration of repeated doses of alpelisib 300 mg with a single-dose of sensitive substrates of CYP3A4 (midazolam), CYP2C8 (repaglinide), CYP2C9 (warfarin), CYP2C19 (omeprazole) and CYP2B6 (bupropion), administered as a cocktail did not show clinically significant pharmacokinetic interactions.
  • CYP2C8 pharmacokinetics
    CYP3A4, CYP2C8, CYP2C9, CYP2C19 and CYP2B6 Substrates: Coadministration of repeated doses of alpelisib 300 mg with a single-dose of sensitive substrates of CYP3A4 (midazolam), CYP2C8 (repaglinide), CYP2C9 (warfarin), CYP2C19 (omeprazole) and CYP2B6 (bupropion), administered as a cocktail did not show clinically significant pharmacokinetic interactions.
  • CYP2C9 pharmacokinetics
    CYP3A4, CYP2C8, CYP2C9, CYP2C19 and CYP2B6 Substrates: Coadministration of repeated doses of alpelisib 300 mg with a single-dose of sensitive substrates of CYP3A4 (midazolam), CYP2C8 (repaglinide), CYP2C9 (warfarin), CYP2C19 (omeprazole) and CYP2B6 (bupropion), administered as a cocktail did not show clinically significant pharmacokinetic interactions.

CYP3A4

  • pharmacokinetics
    Metabolism Alpelisib is primarily metabolized by chemical and enzymatic hydrolysis to form its metabolite BZG791 and followed by CYP3A4 mediated hydroxylation.
  • pharmacokinetics
    CYP3A4-mediated metabolites (12%) and glucuronides amounted to approximately 15% of the dose.
  • pharmacokinetics
    CYP3A4, CYP2C8, CYP2C9, CYP2C19 and CYP2B6 Substrates: Coadministration of repeated doses of alpelisib 300 mg with a single-dose of sensitive substrates of CYP3A4 (midazolam), CYP2C8 (repaglinide), CYP2C9 (warfarin), CYP2C19 (omeprazole) and CYP2B6 (bupropion), administered as a cocktail did not show clinically significant pharmacokinetic interactions.
  • pharmacokinetics
    Effect of CYP3A4 Inducers on Alpelisib: Coadministration of repeat doses of rifampin (a strong CYP3A4 inducer) with a single 300 mg dose of alpelisib decreased alpelisib C max by 38% and AUC by 57%, respectively.
  • pharmacokinetics
    Coadministration of repeat doses of efavirenz (a moderate CYP3A4 inducer) with a single 300 mg dose of alpelisib is expected to decrease alpelisib AUC by 30% or less.
  • pharmacokinetics
    Model-Informed Approaches Coadministration of repeat doses of ketoconazole (a strong CYP3A4 inhibitor) with a single 300 mg dose of alpelisib is expected to increase alpelisib AUC by 37% or less.
1 more recorded row
  • CYP3A4 pharmacokinetics
    No clinically significant differences in pharmacokinetics of everolimus (a substrate of CYP3A4 and P-gp) were observed when coadministered with alpelisib.

recorded 2026-08-30 · last checked 2026-09-04

Was Alpelisib studied with fasting?


fasting is named in Alpelisib's label sentences: "Fasting plasma glucose trended higher with alpelisib (mean ± SD 93 ± 11 mg/dL) versus placebo (84 ± 5 mg/dL); mean fasting serum insulin increased nearly fivefold (23 ± 12 vs. 5 ± 3 μU/mL, respectively), and HOMA of insulin resistance (IR) scores were 5.4 ± 3.1 for alpelisib and 1.1 ± 0.6 for…" openfda-label+europepmc · 2026-08-30

1 recorded statement; fasting

Show the evidence
  • fasting
    Fasting plasma glucose trended higher with alpelisib (mean ± SD 93 ± 11 mg/dL) versus placebo (84 ± 5 mg/dL); mean fasting serum insulin increased nearly fivefold (23 ± 12 vs. 5 ± 3 μU/mL, respectively), and HOMA of insulin resistance (IR) scores were 5.4 ± 3.1 for alpelisib and 1.1 ± 0.6 for placebo.

recorded 2026-08-30 · last checked 2026-09-04

What is recorded about Alpelisib and autophagy?


"Alpelisib (BYL719), a selective PI3Kα inhibitor, has shown promise, but its efficacy is often hampered by compensatory survival mechanisms, including autophagy." — where Alpelisib and autophagy appear together. Europe PMC · pathway abstract search · 2026-07-13

autophagy, mTOR; PMID 41043199, 42621428, 42680443

Show the evidence

autophagy

  • PMID 41043199
    "Alpelisib (BYL719), a selective PI3Kα inhibitor, has shown promise, but its efficacy is often hampered by compensatory survival mechanisms, including autophagy."
  • PMID 41043199
    "This study assesses the therapeutic potential of alpelisib as a monotherapy and in combination with an autophagy inhibitor for PI3K-mutated NSCLC."
  • PMID 41043199
    "Alpelisib significantly reduced cell viability in human NSCLC cell lines in a dose- and time-dependent manner, with enhanced markers of autophagy and apoptosis, with pronounced effects in PI3K-mutant H460 cells."

mTOR

  • PMID 42621428
    "Alpelisib is a US Food and Drug Administration-approved p110α catalytic subunit of phosphoinositide 3-kinase α (PIK3CA) inhibitor for severe manifestations of PIK3CA-related overgrowth spectrum, and inhibits upstream of sirolimus in the phosphoinositide 3-kinase (PI3K)-mTOR pathway."
  • PMID 42680443
    "We are now able to use mTOR inhibitors like sirolimus, PI3K inhibitors like alpelisib and MEK inhibitors like trametinib for targeted therapy of vascular anomalies, often in conjunction with interventional and surgical management."
  • "In xenografts, PAC-XL outperformed cetuximab, BGT226 and alpelisib, including complete regressions, while reducing hyperglycemia and weight loss caused by systemic PI3K/mTOR inhibition."

recorded 2026-07-13 · last checked 2026-09-04

Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL2396661
PubChem CID
56649450
CAS number
1217486-61-7
RxCUI
2169285
InChIKey
STUWGJZDJHPWGZ-LBPRGKRZSA-N
Also called
Byl-719, BYL719, BYL-719A-1214(S)-N1-(4-METHYL-5-(2-(1,1,1-TRIFLUORO-2-METHYLPROPAN-2-YL)PYRIDIN-4-YL)THIAZOL-2-YL)PYRROLIDINE-1,2-DICARBOXAMIDE, NVP-BYL719, PIQRAY, Vijoice, (S)-PYRROLIDINE-1,2-DICARBOXYLIC ACID 2-AMIDE 1-(4-METHYL-5-(2-(2,2,2-TRIFLUORO-1,1-DIMETHYLETHYL)-PYRIDIN-4-YL)THIAZOL-2-YL)AMIDE, ALPELISIB [JAN], ALPELISIB [MI], ALPELISIB [ORANGE BOOK], ALPELISIB [USAN], Alpelisib [WHO-DD]
Trade name
Vijoice / Piqray
Sources (11)

Sources

  • ClinicalTrials.gov clinicaltrials.gov ·
  • ClinicalTrials.gov ClinicalTrials.gov API v2 snapshot 2026-09-01T09:00:05 ·
  • this record's own fields 2,3,5 ·
  • Europe PMC dose-response search ·
  • Europe PMC pathway abstract search ·
  • Europe PMC search ·
5 more sources

ChEMBL ATC CC BY-SA · ClinicalTrials.gov — US Government work · Europe PMC — metadata only, under the recorded legal gate · Open Targets 26.06 — CC0 · derived from this page's own recorded fields; no external licence · 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: 5 required field(s) not terminal: Why people use it, Best-supported result, Most important common problem, Biggest unanswered question, Human evidence
  • public claims reviewed: 0 reviewed claim(s); drafts are never rendered
  • source coverage passed: 11 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.