Healthy VolunteersPhase 1NCT05195892
Investigate Bioequivalence of Alpelisib Granule and Film-coated Tablet Formulation and the Food Effect of Alpelisib Granule Formulation in Adult Healthy Volunteers
A Phase 1 study testing Treatment A, Treatment B and Treatment C in people with Healthy Volunteers, run by Novartis Pharmaceuticals at 1 site in United Kingdom.
Trial summary
The purpose of this study is to assess bioequivalence of the granule formulation of alpelisib as compared to the film-coated tablet formulation in healthy volunteers in the fed state. In addition, the food effect of the granule formulation will be investigated between the fed state and the fasted state. Read more about this study
- Who is it for?
- Ages 18 years and olderHealthy volunteers can take part
- Conditions the study is for
- Healthy Volunteers
- What is being tested?
- Treatment A, Treatment B and Treatment C
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 33 participants
- Where
- 1 siteUnited Kingdom
- Study dates
- 3 Feb 2022to 9 Nov 2022
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 years and older
- All sexes
- Healthy volunteers accepted
- Adult, Older adult
Who may be able to join
- Male or female participants 18 and 55 years of age
- Female participants must be postmenopausal or not of child bearing potential.
- Participants must weigh 50 kg - 120 kg and have BMI= 18.0-30.0 kg/m2
- Participants should be in good health as determined by no clinically significant findings from the medical history, physical examination, vital signs, and ECG.
- Participant must have laboratory values (including fasting plasma glucose and HgbA1C) within the reference range at the local laboratory
- At screening, and at baseline visit of each Period, participant has vital signs which are within the protocol defined ranges
Who cannot join
- Women of childbearing potential
- Sexually active male participant with partner(s) of women of childbearing potential, UNLESS agree to comply with highly effective contraception AND use a condom
- Participant with
- significant illness, including infections, or hospitalization within the 30 days prior to dosing.
- diabetes mellitus or participants with fasting plasma glucose (FPG) levels > 100 mg/dL or >5.55 mmol/L.
- clinically significant risk of developing diabetes mellitus during the study
Show all 23Show fewer
- Use of:
- tobacco products within 3 months prior to first dosing
- drug or alcohol abuse within 12 months prior to first dose
- alcohol within 48 hours prior to the dosing of each treatment period.
- any prescription or non-prescription, herbal medication, dietary supplements or vitamins during 14 days prior to dosing..
- History of :
- clinically significant hematologic, renal, endocrinologic, pulmonary, cardiovascular, hepatic, or allergic disease, medically documented. including uncontrolled hypertension, interstitial lung disease, or other causes of dyspnea, acute pancreatitis within 1 year of screening or past medical
- chronic pancreatitis.
- cardiac disease
- immunodeficiency diseases
- malignancy of any organ system carcinoma of the skin or in situ cervical cancer), within 5 years,
- erythema multiform (EM), Steven-Johnson-Syndrome (SJS) or Toxic Epidermal Necrolysis (TEN).
- history or presence of
- any surgical or medical condition which might significantly alter the absorption, distribution, metabolism or excretion of drugs.
- clinically significant ECG abnormalities or a family prolonged QT-interval syndrome.
- chronic infection with Hepatitis B (HBV) or Hepatitis C (HCV).
- Other inclusion/exclusion criteria may apply
Trial locations and contacts
1 site in 1 country.
United Kingdom1 site
Novartis Investigative Site
Belfast, Northern Ireland, BT9 6AD
About this study
Official title: A Single-center, Randomized, Open-label, Three-period Crossover Study to Investigate the Bioequivalence of Alpelisib Granule and Film-coated Tablet Formulation, and the Food Effect of Alpelisib Granule Formulation in Adult Healthy Volunteers
The purpose of this study is to assess bioequivalence of the granule formulation of alpelisib as compared to the film-coated tablet formulation in healthy volunteers in the fed state. In addition, the food effect of the granule formulation will be investigated between the fed state and the fasted state.
Read the detailed description
This is a single-center, randomized, open-label, three-period six-sequence crossover study.
The study consists of a screening period followed by Periods 1, 2, and 3 and a safety follow-up. Randomization occurs at the beginning of Period 1, whereby every participant who passes the screening will be randomized to one of 6 sequences with 1:1:1:1:1:1 randomization ratio. Each sequence consists of a permutation of three treatments: A, B and C. The order of the sequence of the treatments (A, B, C) will be determined by randomization to the assigned sequence.
A total of 60 participants will be enrolled with approximately 10 participants per sequence, in order to obtain at least 48 evaluable participants for comparison of the granule formulation in fed status and the film-coated tablet formulation in fed status.
- Conditions
- Healthy Volunteers
- Being tested
- Treatment A, Treatment B, Treatment C
- Keywords
- adult, bioequivalence, food effect, three-period six sequence crossover, alpelisib, BYL719
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
Treatment ADrug
Single oral dose of alpelisib film-coated tablet at 50 mg in fed state
Treatment BDrug
Single oral dose of alpelisib granule at 50 mg in fed state
Treatment CDrug
Single oral dose of alpelisib granule at 50 mg in fasted state
| Study group | Role | What they receive |
|---|---|---|
| Sequence 1 | Experimental | Participants will receive a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A) in period 1 followed by a single oral dose of alpelisib granule at 50 mg in fed state (treatment B) in period 2 and a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C) in period 3. Receives: Drug: Treatment A; Drug: Treatment B; Drug: Treatment C |
| Sequence 2 | Experimental | Participants will receive a single oral dose of alpelisib granule at 50 mg in fed state (treatment B) in period 1 followed by a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C) in period 2 followed by a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A) in period 3. Receives: Drug: Treatment A; Drug: Treatment B; Drug: Treatment C |
| Sequence 3 | Experimental | Participants will receive a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C) in period 1 followed by a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A) in period 2 followed by a single oral dose of alpelisib granule at 50 mg in fed state (treatment B) in period 3. Receives: Drug: Treatment A; Drug: Treatment B; Drug: Treatment C |
| Sequence 4 | Experimental | Participants will receive a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C) in period 1 followed by a single oral dose of alpelisib granule at 50 mg in fed state (treatment B) in period 2 followed by a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A). Receives: Drug: Treatment A; Drug: Treatment B; Drug: Treatment C |
| Sequence 5 | Experimental | Participants will receive a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A) in period 1 followed by a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C) in period 2 followed by a single oral dose of alpelisib granule at 50 mg in fed state (treatment B). Receives: Drug: Treatment A; Drug: Treatment B; Drug: Treatment C |
| Sequence 6 | Experimental | Participants will receive a single oral dose of alpelisib granule at 50 mg in fed state (treatment B) in period 1 followed by a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A) in period 2 followed by a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C). Receives: Drug: Treatment A; Drug: Treatment B; Drug: Treatment C |
What is being measured
The primary outcome is the main question the study is designed to answer.
Maximum concentration (Cmax) of alpelisib for Treatment A and Treatment B
Blood samples will be collected at specified time points to compare Cmax of the test formulation (Treatment B: granule formulation in fed state) versus the reference formulation (Treatment A: the film-coated tablet formulation in fed state). PK parameters will be calculated using noncompartmental data analysis of plasma concentration-time data
Measured: Period 1, 2 and 3 at pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12. 24, 48, 72 and 96 hours post-dose
Secondary outcomes (2)
Maximum concentration (Cmax) of alpelisib for Treatment B and Treatment C
Blood samples will be collected at specified time points to compare Cmax of the granule formulation in the fed state (Treatment B) versus the granule formulation in the fasted state (Treatment C). PK parameters will be calculated using noncompartmental data analysis of plasma concentration-time data.
Measured: Period 1, 2 and 3 at pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12. 24, 48, 72 and 96 hours post-dose
Area under plasma concentration time curve (AUC) from zero to 96 hours post dose of alpelisib for Treatment A, Treatment B and Treatment C
Blood samples will be collected at specified time points to calculate AUC0-96 of alpelisib after a single oral dose of alpelisib film coated tablet formulation in fed state (Treatment A), after a single oral dose of alpelisib granule formulation in fed state (Treatment B), after a single oral dose of alpelisib granule formulation in fasted state (Treatment C). PK parameters will be calculated using noncompartmental data analysis of plasma concentration-time data
Measured: Period 1, 2 and 3 at pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12. 24, 48, 72 and 96 hours post-dose
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted19 Jan 2022
- Study start3 Feb 2022
- Primary completion9 Nov 2022
- Study completion9 Nov 2022
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Publications (1)Papers the sponsor has linked to this study.
- Other trials for Healthy VolunteersStudies of the same condition, open and under way.
- More trials run by Novartis PharmaceuticalsThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Enrolment
- 33 participants (actual)
Sponsor and investigators
- Lead sponsor
- Novartis Pharmaceuticals
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Novartis Pharmaceuticals, Study director, Novartis Pharmaceuticals
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT05195892
- Sponsor's protocol ID
- CBYL719F12101
- Status last verified
- Dec 2022
- First submitted
- 4 Jan 2022
- Last updated
- 28 Dec 2022
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- No
- FDA-regulated device
- No
- Individual data sharing
- No
Publications
Burmeister Getz E, Niglis S, Papadimitriou A, Statelova M, Ren X, Nakhla K, Sharaby S, Tariq M, Garbuio L, Bakhsh S. Predicting and Confirming Bioequivalence of Alpelisib Oral Granules and Tablets for Patients With PIK3CA-Related Disorders. AAPS PharmSciTech. 2025 Apr 30;26(5):121. doi: 10.1208/s12249-025-03109-4.
PubMed 40307580
Study at a glance
From the registry record, last updated by the sponsor on 28 Dec 2022. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Single-center, Randomized, Open-label, Three-period Crossover Study to Investigate the Bioequivalence of Alpelisib Granule and Film-coated Tablet Formulation, and the Food Effect of Alpelisib Granule Formulation in Adult Healthy Volunteers
- ClinicalTrials.gov ID
- NCT05195892
- Acronym / sponsor ID
- CBYL719F12101
- Conditions
- Healthy Volunteers
- Keywords
- adult, bioequivalence, food effect, three-period six sequence crossover, alpelisib, BYL719
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 33 participants (actual)
- Lead sponsor
- Novartis PharmaceuticalsIndustry (pharma, biotech, devices)
- Study start
- 3 Feb 2022 (actual)
- Primary completion
- 9 Nov 2022 (actual)
- Study completion
- 9 Nov 2022 (actual)
- First posted
- 19 Jan 2022 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
The purpose of this study is to assess bioequivalence of the granule formulation of alpelisib as compared to the film-coated tablet formulation in healthy volunteers in the fed state. In addition, the food effect of the granule formulation will be investigated between the fed state and the fasted state.
Detailed description
This is a single-center, randomized, open-label, three-period six-sequence crossover study.
The study consists of a screening period followed by Periods 1, 2, and 3 and a safety follow-up. Randomization occurs at the beginning of Period 1, whereby every participant who passes the screening will be randomized to one of 6 sequences with 1:1:1:1:1:1 randomization ratio. Each sequence consists of a permutation of three treatments: A, B and C. The order of the sequence of the treatments (A, B, C) will be determined by randomization to the assigned sequence.
A total of 60 participants will be enrolled with approximately 10 participants per sequence, in order to obtain at least 48 evaluable participants for comparison of the granule formulation in fed status and the film-coated tablet formulation in fed status.
Study design
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 6
| Arm | Type | Receives |
|---|---|---|
| Sequence 1 | Experimental | Drug: Treatment A, Drug: Treatment B, Drug: Treatment CParticipants will receive a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A) in period 1 followed by a single oral dose of alpelisib granule at 50 mg in fed state (treatment B) in period 2 and a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C) in period 3. |
| Sequence 2 | Experimental | Drug: Treatment A, Drug: Treatment B, Drug: Treatment CParticipants will receive a single oral dose of alpelisib granule at 50 mg in fed state (treatment B) in period 1 followed by a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C) in period 2 followed by a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A) in period 3. |
| Sequence 3 | Experimental | Drug: Treatment A, Drug: Treatment B, Drug: Treatment CParticipants will receive a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C) in period 1 followed by a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A) in period 2 followed by a single oral dose of alpelisib granule at 50 mg in fed state (treatment B) in period 3. |
| Sequence 4 | Experimental | Drug: Treatment A, Drug: Treatment B, Drug: Treatment CParticipants will receive a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C) in period 1 followed by a single oral dose of alpelisib granule at 50 mg in fed state (treatment B) in period 2 followed by a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A). |
| Sequence 5 | Experimental | Drug: Treatment A, Drug: Treatment B, Drug: Treatment CParticipants will receive a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A) in period 1 followed by a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C) in period 2 followed by a single oral dose of alpelisib granule at 50 mg in fed state (treatment B). |
| Sequence 6 | Experimental | Drug: Treatment A, Drug: Treatment B, Drug: Treatment CParticipants will receive a single oral dose of alpelisib granule at 50 mg in fed state (treatment B) in period 1 followed by a single oral dose of alpelisib film-coated tablet at 50 mg in fed state (treatment A) in period 2 followed by a single oral dose of alpelisib granule at 50 mg in fasted state (treatment C). |
Who may qualify
- Ages
- 18 years and older
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult, Older adult
Key inclusion criteria (6 listed)
- Male or female participants 18 and 55 years of age
- Female participants must be postmenopausal or not of child bearing potential.
- Participants must weigh 50 kg - 120 kg and have BMI= 18.0-30.0 kg/m2
- Participants should be in good health as determined by no clinically significant findings from the medical history, physical examination, vital signs, and ECG.
- Participant must have laboratory values (including fasting plasma glucose and HgbA1C) within the reference range at the local laboratory
Key exclusion criteria (23 listed)
- Women of childbearing potential
- Sexually active male participant with partner(s) of women of childbearing potential, UNLESS agree to comply with highly effective contraception AND use a condom
- Participant with
- significant illness, including infections, or hospitalization within the 30 days prior to dosing.
- diabetes mellitus or participants with fasting plasma glucose (FPG) levels > 100 mg/dL or >5.55 mmol/L.
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| Treatment ASingle oral dose of alpelisib film-coated tablet at 50 mg in fed state | Drug | Sequence 1, Sequence 2, Sequence 3, Sequence 4, Sequence 5, Sequence 6 |
| Treatment BSingle oral dose of alpelisib granule at 50 mg in fed state | Drug | Sequence 1, Sequence 2, Sequence 3, Sequence 4, Sequence 5, Sequence 6 |
| Treatment CSingle oral dose of alpelisib granule at 50 mg in fasted state | Drug | Sequence 1, Sequence 2, Sequence 3, Sequence 4, Sequence 5, Sequence 6 |
Primary outcome
Maximum concentration (Cmax) of alpelisib for Treatment A and Treatment B
Time frame: Period 1, 2 and 3 at pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12. 24, 48, 72 and 96 hours post-dose
Blood samples will be collected at specified time points to compare Cmax of the test formulation (Treatment B: granule formulation in fed state) versus the reference formulation (Treatment A: the film-coated tablet formulation in fed state). PK parameters will be calculated using noncompartmental data analysis of plasma concentration-time data
2 secondary outcomes
Maximum concentration (Cmax) of alpelisib for Treatment B and Treatment C
Time frame: Period 1, 2 and 3 at pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12. 24, 48, 72 and 96 hours post-dose
Area under plasma concentration time curve (AUC) from zero to 96 hours post dose of alpelisib for Treatment A, Treatment B and Treatment C
Time frame: Period 1, 2 and 3 at pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12. 24, 48, 72 and 96 hours post-dose
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 28 Dec 2022.
- Derived from this study: PubMed 40307580Burmeister Getz E, Niglis S, Papadimitriou A, Statelova M, Ren X, Nakhla K, Sharaby S, Tariq M, Garbuio L, Bakhsh S. Predicting and Confirming Bioequivalence of Alpelisib Oral Granules and Tablets for Patients With PIK3CA-Related Disorders. AAPS PharmSciTech. 2025 Apr 30;26(5):121. doi: 10.1208/s12249-025-03109-4.
- Individual participant dataSharing planned: No
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Novartis Pharmaceuticals study director
Novartis Pharmaceuticals
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing Treatment A, Treatment B and Treatment C in people with Healthy Volunteers, run by Novartis Pharmaceuticals at 1 site in United Kingdom.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 6 inclusion and 23 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 28 Dec 2022. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in United Kingdom. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Maximum concentration (Cmax) of alpelisib for Treatment A and Treatment B (time frame: Period 1, 2 and 3 at pre-dose and 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12. 24, 48, 72 and 96 hours post-dose). It is what the study was designed to measure, not a finding.
Where can I read the original study information?
On the ClinicalTrials.gov record for NCT05195892, which also lists 1 linked publication.
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 28 Dec 2022.