Study Assessing the Efficacy and Safety of Alpelisib Plus Fulvestrant or Letrozole, Based on Prior Endocrine Therapy, in Patients With PIK3CA Mutant, HR+, HER2- Advanced Breast Cancer Who Have Progressed on or After Prior Treatments

NCT ID: NCT03056755

Last Updated: 2026-01-13

Study Results

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Basic Information

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Recruitment Status

COMPLETED

Clinical Phase

PHASE2

Total Enrollment

383 participants

Study Classification

INTERVENTIONAL

Study Start Date

2017-08-29

Study Completion Date

2024-11-12

Brief Summary

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This was a Phase II, multicenter, open-label, three-cohort, non-comparative study of alpelisib plus endocrine therapy (either fulvestrant or letrozole) in subjects (pre- and post-menopausal women and men) with HR-positive, HER2-negative aBC harboring PIK3CA mutation(s) in the tumor, whose disease had progressed on or after prior treatments.

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Detailed Description

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The study comprised two phases:

1. Core Phase: included a treatment phase for all subjects from first subject first treatment (FSFT) until disease progression, unacceptable toxicity, or death until 18 months post last subject first treatment (LSFT) + 1 month safety follow-up (total 19 months post LSFT), discontinuation from the study treatment for any other reason, or sponsor terminates the study. At the start of the Core Phase, subjects were assigned to Cohort A, Cohort B, or Cohort C based on previous therapy as follows:

* Cohort A: alpelisib (300 mg oral QD) + fulvestrant (500 mg intramuscular (IM)) to subjects whose last prior treatment was a CDK4/6i plus any AI;
* Cohort B: alpelisib (300 mg oral QD) + letrozole (2.5 mg oral QD) to subjects whose last prior treatment was a CDK4/6i plus fulvestrant;
* Cohort C: alpelisib (300 mg oral QD)+ fulvestrant (500 mg IM) to subjects who failed prior AI based therapy and whose last prior treatment was systemic chemotherapy or endocrine therapy (as monotherapy or in combination with targeted treatment except CDK 4/6i + AI). Endocrine therapy included letrozole, fulvestrant and CDK 4/6 inhibitor plus fulvestrant.
2. Extension Phase: included a treatment phase starting at the end of the treatment Core Phase until last subject last visit(LSLV) (up to 36 months). Following the end of the Core Phase, subjects continuing to derive benefit from study treatment who were not eligible for Post-Study Drug Supply (PSDS) in their country based on local regulations were re-consented and transitioned to the Extension Phase. Subjects continued on their existing study treatment assigned in the Core Phase until disease progression/lack of clinical benefit or any other reason for which the subject may have been discontinued from study treatment. If PSDS became available for a subject, the subject was to be discontinued from the study and to access treatment via PSDS. When subjects discontinued treatment for any reason, the end of treatment visit was performed after discontinuation of the medication , followed by safety follow-up 30 days after last dose.

A total of 340 subjects were planned to be enrolled, with approximately 112 subjects in each cohort. In the Core Phase, 379 subjects were analyzed, with 127 subjects in Cohort A, 126 subjects in Cohort B, and 126 subjects in Cohort C. In the Extension Phase, 11 subjects were analyzed, with 1 subject in Cohort A and 10 subjects in Cohort C.

Conditions

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Breast Cancer

Study Design

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Allocation Method

NON_RANDOMIZED

Intervention Model

PARALLEL

Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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Cohort A: Pre-treated with CDK 4/6i + AI

Participants who received any Cyclin-Dependent Kinases 4 and 6 inhibitor (CDK 4/6i) plus aromatase inhibitor (AI) as immediate prior treatment will receive alpelisib + fulvestrant

Group Type EXPERIMENTAL

Alpelisib

Intervention Type DRUG

300 mg of alpelisib film-coated tablets administered orally once daily

Fulvestrant

Intervention Type DRUG

500 mg of fulvestrant via intramuscular injection administered on Days 1, 15 on Cycle 1 and Day 1 at each cycle thereafter. Cycle=28 days

Goserelin

Intervention Type DRUG

3.6 mg of goserelin via injectable subcutaneous implant administered every 28 days. Only for men in Cohort B and premenopausal women.

Leuprolide

Intervention Type DRUG

7.5 mg of leuprolide via injectable intramuscular depot administered every 28 days. Only for men in cohort B and premenopausal women.

Cohort B: Pre-treated with CDK 4/6i + fulvestrant

Patients who received any CDK 4/6i plus fulvestrant as immediate prior treatment will receive alpelisib + letrozole

Group Type EXPERIMENTAL

Alpelisib

Intervention Type DRUG

300 mg of alpelisib film-coated tablets administered orally once daily

Letrozole

Intervention Type DRUG

2.5 mg of letrozole film-coated tablets administered orally once daily

Goserelin

Intervention Type DRUG

3.6 mg of goserelin via injectable subcutaneous implant administered every 28 days. Only for men in Cohort B and premenopausal women.

Leuprolide

Intervention Type DRUG

7.5 mg of leuprolide via injectable intramuscular depot administered every 28 days. Only for men in cohort B and premenopausal women.

Cohort C: Pre-treated with systemic chemotherapy or ET

Participants who received systemic chemotherapy or endocrine therapy (ET) (as monotherapy or in combination with targeted treatment except CDK 4/6i + AI) as immediate prior treatment will receive alpelisib + fulvestrant.

Group Type EXPERIMENTAL

Alpelisib

Intervention Type DRUG

300 mg of alpelisib film-coated tablets administered orally once daily

Fulvestrant

Intervention Type DRUG

500 mg of fulvestrant via intramuscular injection administered on Days 1, 15 on Cycle 1 and Day 1 at each cycle thereafter. Cycle=28 days

Goserelin

Intervention Type DRUG

3.6 mg of goserelin via injectable subcutaneous implant administered every 28 days. Only for men in Cohort B and premenopausal women.

Leuprolide

Intervention Type DRUG

7.5 mg of leuprolide via injectable intramuscular depot administered every 28 days. Only for men in cohort B and premenopausal women.

Interventions

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Alpelisib

300 mg of alpelisib film-coated tablets administered orally once daily

Intervention Type DRUG

Fulvestrant

500 mg of fulvestrant via intramuscular injection administered on Days 1, 15 on Cycle 1 and Day 1 at each cycle thereafter. Cycle=28 days

Intervention Type DRUG

Letrozole

2.5 mg of letrozole film-coated tablets administered orally once daily

Intervention Type DRUG

Goserelin

3.6 mg of goserelin via injectable subcutaneous implant administered every 28 days. Only for men in Cohort B and premenopausal women.

Intervention Type DRUG

Leuprolide

7.5 mg of leuprolide via injectable intramuscular depot administered every 28 days. Only for men in cohort B and premenopausal women.

Intervention Type DRUG

Other Intervention Names

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BYL719

Eligibility Criteria

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Inclusion Criteria

* Subject was an adult male or female ≥ 18 years of age.
* Subjects with histologically and/or cytologically confirmed diagnosis of estrogen receptor (ER)-positive and/or progesterone receptor (PgR)-positive breast cancer by local laboratory.
* Subjects with a confirmed human epidermal growth factor receptor-2 (HER2)-negative aBC.
* Subjects with gene encoding the p110alpha catalytic subunit of PI3K (phosphatidylinositol-3-kinase) (PIK3CA) mutation.
* In case of women, both premenopausal and postmenopausal subjects were allowed to be included in this study.
* Subjects with documented evidence of tumor progression on or after:

i. Cyclin-Dependent Kinase 4 and 6 inhibitor (CDK4/6i) treatment as last treatment regimen in Cohorts A and B.

ii. aromatase inhibitor (AI) treatment (either in adjuvant or metastatic setting) and received systemic chemotherapy or ET (monotherapy or combination except CDK4/6i + AI) as last treatment regimen in Cohort C. Upon completion of enrollment of Cohort B, subjects who received CDK4/6i + fulvestrant as immediate prior therapy were eligible for Cohort C.

iii. No more than 2 prior anticancer therapies for aBC. iv. Received no more than 1 prior regimen of chemotherapy for the treatment of advanced/metastatic disease was permitted.

v. Recovered to grade 1 or better from any adverse events (AEs) related to previous anticancer therapy prior to study entry (except alopecia or other toxicities not considered a safety risk for the subject at the investigator's discretion).

* Subjects with:

i. Measurable disease, i.e., at least 1 measurable lesion as per RECIST v1.1 criteria; or ii. If no measurable disease was present, at least 1 predominantly lytic bone lesion had to be present.
* Subjects with adequate bone marrow and coagulation function, liver function and renal function as shown by laboratory values.
* Subjects with Eastern Cooperative Oncology Group (ECOG) performance status score of ≤ 2.

Exclusion Criteria

* Subjects with a known hypersensitivity to alpelisib, fulvestrant, letrozole, goserelin, or leuprolide or to any of their excipients.
* Subjects with prior treatment with any PI3K inhibitor (PI3Ki).
* Subjects with central nervous system (CNS) involvement unless they met all of the following criteria:

i. At least 4 weeks from prior therapy completion (including radiation and/or surgery) to starting the study treatment, ii. Clinically stable CNS tumor at the time of screening untreated or without evidence of progressions for at least 4 weeks after treatment as determined by clinical examination and brain imaging (magnetic resonance imaging (MRI) or computed tomography (CT) during screening period and stable low dose of steroids for 2 weeks prior to initiating study treatment.
* Subjects with an established diagnosis of diabetes mellitus type I or uncontrolled type II.
* Any concurrent severe and/or uncontrolled medical conditions that would, in the investigator's judgment, contraindicate subject participation in the study (e.g., chronic active hepatitis, severe hepatic impairment, etc.).
* Subjects with a history of noncompliance to medical regimens.
* Subjects with impairment of gastrointestinal (GI) function or GI disease that could significantly alter the absorption of the study drugs based on investigator discretion.
* Subjects with documented pneumonitis/interstitial lung disease which was active and requiring treatment.
* Subjects concurrently using other anticancer therapy. All anticancer therapy had to be discontinued prior to Day 1 of study treatment.
* Subjects who had major surgery within 14 days prior to starting treatment with alpelisib, or did not recover from major side effects.
* Subjects with significant cardiac abnormalities.
* History of acute pancreatitis within 1 year of screening or past medical history of chronic pancreatitis.
* Subjects who did not use highly effective contraception while on alpelisib and through the duration after the final dose of alpelisib (not applicable to postmenopausal women).
* Subjects with unresolved osteonecrosis of the jaw.
Minimum Eligible Age

18 Years

Maximum Eligible Age

99 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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Novartis Pharmaceuticals

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Novartis Pharmaceuticals

Role: STUDY_DIRECTOR

Novartis Pharmaceuticals

Locations

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Banner MD Anderson Cancer Center

Gilbert, Arizona, United States

Site Status

Mayo Clinic Arizona

Phoenix, Arizona, United States

Site Status

Kaiser Permanente Medical Group

Anaheim, California, United States

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Beverly Hills Cancer Center

Beverly Hills, California, United States

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University of Calif Irvine Med Cntr

Irvine, California, United States

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Kaiser Permanent Southern Californi

San Diego, California, United States

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UCSF

San Francisco, California, United States

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Yale University Yale Cancer Center

New Haven, Connecticut, United States

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Advent Health Cancer Institute

Orlando, Florida, United States

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University of Kansas Cancer Center

Kansas City, Kansas, United States

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University of Louisville James Graham Brown Cancer Center

Louisville, Kentucky, United States

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Mercy Medical Center

Baltimore, Maryland, United States

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Greater Baltimore Med Center Cancer Center

Baltimore, Maryland, United States

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Massachusetts General Hospital

Boston, Massachusetts, United States

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Lahey Clinic

Burlington, Massachusetts, United States

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Josephine Ford Cancer Center

Detroit, Michigan, United States

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St Vincent Frontier Cancer Center

Billings, Montana, United States

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New Mexico Cancer Care Alliance

Albuquerque, New Mexico, United States

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Memorial Sloane Ketterin Cancer Ctr

New York, New York, United States

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Uni Hosp of Cleveland Cancer Center

Cleveland, Ohio, United States

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Texas Oncology

Dallas, Texas, United States

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Cancer Care Centers of South Texas HOAST

San Antonio, Texas, United States

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UT Health San Antonio

San Antonio, Texas, United States

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Virginia Oncology Associates

Norfolk, Virginia, United States

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Northwest Medical Specialists

Tacoma, Washington, United States

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Novartis Investigative Site

CABA, Buenos Aires, Argentina

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CABA, Buenos Aires, Argentina

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CABA, Buenos Aires, Argentina

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Rosario, Santa Fe Province, Argentina

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Rosario, Sante Fe, Argentina

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La Rioja, , Argentina

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Leuven, , Belgium

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Liège, , Belgium

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Vancouver, British Columbia, Canada

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Halifax, Nova Scotia, Canada

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Kitchener, Ontario, Canada

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Toronto, Ontario, Canada

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Temuco, Región de la Araucanía, Chile

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Santiago, , Chile

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Santiago, , Chile

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Odense C, , Denmark

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Vejle, , Denmark

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Nice, Alpes Maritimes, France

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Saint-Cloud, Hauts De Seine, France

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Bordeaux, , France

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Caen, , France

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Lille, , France

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Lyon, , France

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Montpellier, , France

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Saint-Herblain, , France

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Strasbourg, , France

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Toulouse, , France

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Dresden, Saxony, Germany

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Augsburg, , Germany

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Berlin, , Germany

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Erlangen, , Germany

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Essen, , Germany

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Heidelberg, , Germany

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Ulm, , Germany

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Delhi, , India

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Petah Tikva, , Israel

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Ramat Gan, , Israel

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Rehovot, , Israel

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Tel Aviv, , Israel

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Ancona, AN, Italy

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Bergamo, BG, Italy

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Bologna, BO, Italy

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Genova, GE, Italy

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Milan, MI, Italy

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Milan, MI, Italy

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Roma, RM, Italy

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Napoli, , Italy

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Osaka, Osaka, Japan

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Jalisco, , Mexico

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Maastricht, Limburg, Netherlands

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Singapore, , Singapore

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Singapore, , Singapore

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Seoul, Korea, South Korea

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Seoul, , South Korea

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L'Hospitalet de Llobregat, Barcelona, Spain

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Salamanca, Castille and León, Spain

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Barcelona, Catalonia, Spain

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Barcelona, , Spain

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Castellon, , Spain

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Madrid, , Spain

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Seville, , Spain

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Tainan, , Taiwan

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Taipei, , Taiwan

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Taipei, , Taiwan

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Edinburgh, Scotland, United Kingdom

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Sutton, Surrey, United Kingdom

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Leicester, , United Kingdom

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London, , United Kingdom

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Nottingham, , United Kingdom

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Countries

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United States Argentina Belgium Canada Chile Denmark France Germany India Israel Italy Japan Mexico Netherlands Singapore South Korea Spain Taiwan United Kingdom

References

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Rugo HS, Lerebours F, Ciruelos E, Drullinsky P, Ruiz-Borrego M, Neven P, Park YH, Prat A, Bachelot T, Juric D, Turner N, Sophos N, Zarate JP, Arce C, Shen YM, Turner S, Kanakamedala H, Hsu WC, Chia S. Alpelisib plus fulvestrant in PIK3CA-mutated, hormone receptor-positive advanced breast cancer after a CDK4/6 inhibitor (BYLieve): one cohort of a phase 2, multicentre, open-label, non-comparative study. Lancet Oncol. 2024 Dec;25(12):e629-e638. doi: 10.1016/S1470-2045(24)00673-9.

Reference Type DERIVED
PMID: 39637900 (View on PubMed)

Borrego MR, Lu YS, Reyes-Cosmelli F, Park YH, Yamashita T, Chiu J, Airoldi M, Turner N, Fein L, Ghaznawi F, Singh J, Pantoja K, Schnell C, Akdere M, Chia S. SGLT2 inhibition improves PI3Kalpha inhibitor-induced hyperglycemia: findings from preclinical animal models and from patients in the BYLieve and SOLAR-1 trials. Breast Cancer Res Treat. 2024 Nov;208(1):111-121. doi: 10.1007/s10549-024-07405-8. Epub 2024 Aug 23.

Reference Type DERIVED
PMID: 39177931 (View on PubMed)

Rodon J, Demanse D, Rugo HS, Burris HA, Simo R, Farooki A, Wellons MF, Andre F, Hu H, Vuina D, Quadt C, Juric D. A risk analysis of alpelisib-induced hyperglycemia in patients with advanced solid tumors and breast cancer. Breast Cancer Res. 2024 Mar 4;26(1):36. doi: 10.1186/s13058-024-01773-1.

Reference Type DERIVED
PMID: 38439079 (View on PubMed)

Rugo HS, Lerebours F, Ciruelos E, Drullinsky P, Ruiz-Borrego M, Neven P, Park YH, Prat A, Bachelot T, Juric D, Turner N, Sophos N, Zarate JP, Arce C, Shen YM, Turner S, Kanakamedala H, Hsu WC, Chia S. Alpelisib plus fulvestrant in PIK3CA-mutated, hormone receptor-positive advanced breast cancer after a CDK4/6 inhibitor (BYLieve): one cohort of a phase 2, multicentre, open-label, non-comparative study. Lancet Oncol. 2021 Apr;22(4):489-498. doi: 10.1016/S1470-2045(21)00034-6. Erratum In: Lancet Oncol. 2021 May;22(5):e184. doi: 10.1016/S1470-2045(21)00194-7.

Reference Type DERIVED
PMID: 33794206 (View on PubMed)

Provided Documents

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Document Type: Study Protocol

View Document

Document Type: Statistical Analysis Plan

View Document

Related Links

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https://www.novctrd.com/ctrdweb/patientsummary/patientsummaries?patientSummaryId=3006

A Plain Language Trial Summary is available on www.novctrd.com

Other Identifiers

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2023-509167-24-00

Identifier Type: REGISTRY

Identifier Source: secondary_id

CBYL719X2402

Identifier Type: -

Identifier Source: org_study_id

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