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

NCT ID: NCT05646862

Last Updated: 2026-02-05

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

ACTIVE_NOT_RECRUITING

Clinical Phase

PHASE3

Total Enrollment

420 participants

Study Classification

INTERVENTIONAL

Study Start Date

2023-06-07

Study Completion Date

2029-03-30

Brief Summary

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This is a Phase III, multicenter, randomized, open-label, global study designed to evaluate the efficacy and safety of inavolisib plus fulvestrant compared with alpelisib plus fulvestrant in patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2) -negative, PIK3CA-mutated, locally advanced (LA) or metastatic breast cancer (mBC), who progressed during or after cyclin dependent kinase 4/6i (CDK4/6i)-based therapy.

Detailed Description

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The drug-drug interaction (DDI) substudy will evaluate the impact of repeat doses of inavolisib (coadministered with fulvestrant) on single-dose pharmacokinetics of sensitive CYP450 enzyme substrates (midazolam, omeprazole and bupropion) in participants with hormone receptor (HR)-positive, HER2-negative, PIK3CA-mutated, locally advanced (LA) or metastatic breast cancer (mBC), who progressed during or after CDK4/6 inhibitor (CDK4/6i) in combination with endocrine therapy (ET).

Conditions

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Breast Cancer

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

PARALLEL

Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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Sub-study: Inavolisib + Fulvestrant + CYP substrates

Participants will be administered the treatments as outlined in the interventions section.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will be administered a 9 milligram (mg) inavolisib tablet orally once a day (PO QD) on Days 1-28 of each 28-day cycle of main study and sub-study.

Fulvestrant

Intervention Type DRUG

Participants will be administered 500 mg of fulvestrant on Days 1 and 15 of Cycle 1 and then on Day 1 of each subsequent 28-day cycle of main study and sub-study.

Bupropion

Intervention Type DRUG

Participants will be administered bupropion PO on Day -3 and Day 12 of Cycle 1 of the sub-study.

Omeprazole

Intervention Type DRUG

Participants will be administered omerprazole PO on Day -4 and Day 11 of Cycle 1 of sub-study.

Midazolam

Intervention Type DRUG

Participants will be administered midazolam PO on Day -4 and Day 11 of Cycle 1 of sub-study.

Inavolisib + Fulvestrant

Participants will be administered the treatments as outlined in the interventions section.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will be administered a 9 milligram (mg) inavolisib tablet orally once a day (PO QD) on Days 1-28 of each 28-day cycle of main study and sub-study.

Fulvestrant

Intervention Type DRUG

Participants will be administered 500 mg of fulvestrant on Days 1 and 15 of Cycle 1 and then on Day 1 of each subsequent 28-day cycle of main study and sub-study.

Alpelisib + Fulvestrant

Participants will be administered the treatments as outlined in the interventions section.

Group Type ACTIVE_COMPARATOR

Fulvestrant

Intervention Type DRUG

Participants will be administered 500 mg of fulvestrant on Days 1 and 15 of Cycle 1 and then on Day 1 of each subsequent 28-day cycle of main study and sub-study.

Alpelisib

Intervention Type DRUG

Alpelisib will be administered to participants at the approved dose in combination with fulvestrant: 300 mg taken PO QD and on days 1-28 of each 28-day cycle.

Interventions

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Inavolisib

Participants will be administered a 9 milligram (mg) inavolisib tablet orally once a day (PO QD) on Days 1-28 of each 28-day cycle of main study and sub-study.

Intervention Type DRUG

Fulvestrant

Participants will be administered 500 mg of fulvestrant on Days 1 and 15 of Cycle 1 and then on Day 1 of each subsequent 28-day cycle of main study and sub-study.

Intervention Type DRUG

Alpelisib

Alpelisib will be administered to participants at the approved dose in combination with fulvestrant: 300 mg taken PO QD and on days 1-28 of each 28-day cycle.

Intervention Type DRUG

Bupropion

Participants will be administered bupropion PO on Day -3 and Day 12 of Cycle 1 of the sub-study.

Intervention Type DRUG

Omeprazole

Participants will be administered omerprazole PO on Day -4 and Day 11 of Cycle 1 of sub-study.

Intervention Type DRUG

Midazolam

Participants will be administered midazolam PO on Day -4 and Day 11 of Cycle 1 of sub-study.

Intervention Type DRUG

Eligibility Criteria

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Inclusion Criteria

* If pre/perimenopausal women and men treatment with luteinizing hormone-releasing hormone (LHRH) agonist therapy beginning at least 2 weeks prior to Day 1 of Cycle 1
* Histologically or cytologically confirmed adenocarcinoma of the breast that is locally advanced or metastatic and is not amenable to surgical or radiation therapy with curative intent
* Documented HR +/ HER2- tumor according to American Society of Clinical Oncology/College of American Pathologists (ASCO/CAP) guidelines
* Confirmation of biomarker eligibility: detection of specified mutation(s) of PIK3CA via specified test
* Disease progression after or during treatment with a combination of CDK4/6i and endocrine therapy: \<= 2 prior lines of systemic therapy in mBC setting; CDK4/6i based therapy does not need to be the last one received prior study entry; one line of chemotherapy in mBC setting allowed
* Measurable or evaluable disease per Response Evaluation Criteria in Solid Tumors version 1.1 (RECIST v1.1)
* Participants for whom endocrine-based therapy is recommended and treatment with cytotoxic chemotherapy is not indicated at time of entry into the study, as per national or local treatment guidelines
* Eastern Cooperative Oncology Group (ECOG) Performance Status of 0, 1, or 2
* Life expectancy of \> 6 months
* Adequate hematologic and organ function prior to initiation of study treatment

Exclusion Criteria

* Metaplastic breast cancer
* Prior treatment in locally advanced or metastatic setting with any PI3K, AKT, or mTOR inhibitor or any agent whose mechanism of action is to inhibit the PI3K/-AKT/-mTOR pathway
* Participant who relapsed with documented evidence of progression \> 12 months from completion of adjuvant CDK4/6i based therapy with no treatment for metastatic disease
* Type 2 diabetes requiring ongoing systemic treatment at the time of study entry; or any history of Type 1 diabetes
* Inability or unwillingness to swallow pills
* Malabsorption syndrome or other condition that would interfere with enteral absorption
* Any history of leptomeningeal disease or carcinomatous meningitis
* Known and untreated, or active central nervous system (CNS) metastases. Participants with a history of treated CNS metastases are eligible if they meet specific certain criteria
* Any concurrent ocular or intraocular condition that, in the opinion of the investigator, would require medical or surgical intervention during the study period to prevent or treat vision loss that might result from that condition
* Active inflammatory or infectious conditions in either eye or history of idiopathic or autoimmune-associated uveitis in either eye
* Requirement for daily supplemental oxygen
* Symptomatic active lung disease, including pneumonitis
* History of or active inflammatory bowel disease
* Any active bowel inflammation
* Clinically significant and active liver disease, including severe liver impairment, viral or other hepatitis, current alcohol abuse, or cirrhosis
* Participants with known human immunodeficiency virus infection that meet specific criteria
* History of other malignancy within 5 years prior to screening, except for cancers with very low risk of recurrence
* Chronic therapy of \>= 10 mg of prednisone per day or an equivalent dose of other anti-inflammatory corticosteroids or immunosuppressants for a chronic disease
* Active ongoing osteonecrosis of the jaw


* Pregnant, lactating, or breastfeeding, or intending to become pregnant during the study or at least 60 days after the final dose of study treatment
* Known active, systemic infection at study enrollment, or any major episode of infection requiring treatment with intravenous antibiotics or hospitalization within 7 days prior to Day 1 of Cycle 1
* Investigational drug(s) within 4 weeks before randomization or within 5 half-lives of the investigational drug(s), whichever is longer
* Allergy or hypersensitivity to components or excipients of the inavolisib, fulvestrant, or alpelisib formulations
* History of severe cutaneous reactions like Stevens-Johnson Syndrome, Erythema Multiforme, Toxic Epidermal Necrolysis, or Drug Reaction with Eosinphilia and Systemic Symptoms


* Pregnant, lactating, or breastfeeding, or intending to become pregnant during the substudy or within 2 weeks after the final dose of inavolisib and within 2 years after the final dose of fulvestrant, whichever is longer
* Known active, systemic infection at study enrollment, or any major episode of infection requiring treatment with intravenous antibiotics or hospitalization within 7 days prior to Day -4 of Cycle 1
* Investigational drug(s) within 4 weeks prior to Day -4 or within 5 half-lives of the investigational drug(s), whichever is longer
* Allergy or hypersensitivity to components or excipients of the inavolisib, fulvestrant formulations
* Treatment with mild, moderate, or strong inducers of CYP2B6, CYP3A4, and/or CYP2C19 (including St. John's Wort) within 14 days or 5 drug-elimination half-lives, whichever is longer, prior to initiation of study treatment on Day -4 until after the final PK sample has been collected on Day 15 of Cycle 1
* Treatment with mild, moderate, or strong inhibitors of CYP2B6, CYP3A4, and/or CYP2C19 (including grapefruit juice or supplements) within 14 days or 5 drug-elimination half-lives, whichever is longer, prior to initiation of study treatment on Day -4 until after the final PK sample has been collected on Day 15 of Cycle 1
Minimum Eligible Age

18 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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Hoffmann-La Roche

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Clinical Trials

Role: STUDY_DIRECTOR

Hoffmann-La Roche

Locations

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Cancer Blood and Specialty Clinic

Los Alamitos, California, United States

Site Status

Los Angeles Cancer Network

Los Angeles, California, United States

Site Status

UC Davis Comprehensive Cancer Center

Sacramento, California, United States

Site Status

Rocky Mountain Cancer Centers

Denver, Colorado, United States

Site Status

Cleveland Clinic Florida

Weston, Florida, United States

Site Status

Grady Health System

Atlanta, Georgia, United States

Site Status

Midtown West Medical

Atlanta, Georgia, United States

Site Status

Emory University Hospital

Atlanta, Georgia, United States

Site Status

Winship Cancer Institute at Emory Saint Joseph's Hospital

Atlanta, Georgia, United States

Site Status

Massachusetts General Hospital

Boston, Massachusetts, United States

Site Status

Cancer & Hematology Centers of Western Michigan

Grand Rapids, Michigan, United States

Site Status

Minnesota Oncology Hematology

Saint Paul, Minnesota, United States

Site Status

Asante Rogue Regional Medical Center

Medford, Oregon, United States

Site Status

Texas Oncology - Dallas Presbyterian Hospital

Dallas, Texas, United States

Site Status

Centro de Investigaciones Médicas y Desarrollo LC S.R.L

Buenos Aires, , Argentina

Site Status

Centro Oncologico Korben

Ciudad Autonoma Buenos Aires, , Argentina

Site Status

Fundacion CORI para la Investigacion y Prevencion del Cancer

La Rioja, , Argentina

Site Status

Instituto de Oncología de Rosario

Rosario, , Argentina

Site Status

Hosp Provincial D. Centenarios

Rosario, , Argentina

Site Status

CER San Juan Centro Polivalente de Asistencia e Investigacion Clinica

San Juan, , Argentina

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Clinica Viedma S.A.

Viedma, , Argentina

Site Status

Coffs Harbour Health Campus

Coffs Harbour, New South Wales, Australia

Site Status

Concord Repatriation General Hospital

Concord, New South Wales, Australia

Site Status

Kinghorn Cancer Centre

Darlinghurst, New South Wales, Australia

Site Status

Gosford Hospital

Gosford, New South Wales, Australia

Site Status

Icon Cancer Care Wesley

Auchenflower, Queensland, Australia

Site Status

Bendigo Cancer Centre

Bendigo, Victoria, Australia

Site Status

Sir Charles Gairdner Hospital

Perth, Western Australia, Australia

Site Status

Cliniques Universitaires St-Luc

Brussels, , Belgium

Site Status

GHdC Site Les Viviers

Charleroi, , Belgium

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UZ Antwerpen

Edegem, , Belgium

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UZ Gent

Ghent, , Belgium

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UZ Leuven Gasthuisberg

Leuven, , Belgium

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Clinique Ste-Elisabeth

Namur, , Belgium

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NUPEC

Belo Horizonte, Minas Gerais, Brazil

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Hospital Santa Cruz / Centro de Oncologia D'Or

Curitiba, Paraná, Brazil

Site Status

Hospital do Cancer de Pernambuco - HCP

Recife, Pernambuco, Brazil

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Instituto D?Or de Pesquisa e Ensino ? Hospital Esperança Recife

Recife, Pernambuco, Brazil

Site Status

Liga Norte Riograndense Contra O Câncer

Natal, Rio Grande do Norte, Brazil

Site Status

Santa Casa de Misericordia de Porto Alegre

Porto Alegre, Rio Grande do Sul, Brazil

Site Status

Hospital de Base de Sao Jose do Rio Preto

São José do Rio Preto, São Paulo, Brazil

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Hospital Sírio-Libanês

São Paulo, São Paulo, Brazil

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Arthur J.E. Child Comprehensive Cancer Center-Calgary

Calgary, Alberta, Canada

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Cross Cancer Institute

Edmonton, Alberta, Canada

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BC Cancer ? Vancouver

Vancouver, British Columbia, Canada

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The Moncton Hospital

Moncton, New Brunswick, Canada

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Juravinski Hospital

Hamilton, Ontario, Canada

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The Ottawa Hospital - General Campus

Ottawa, Ontario, Canada

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CIUSSS de l Est de l Ile de Montreal - Hopital Maisonneuve Rosemont

Montreal, Quebec, Canada

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Centre Hospitalier de l'Universite de Montreal (CHUM)

Montreal, Quebec, Canada

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Jewish General Hospital

Montreal, Quebec, Canada

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Hôpital du Sacré-Coeur de Montreal

Montreal, Quebec, Canada

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The First Hospital of Jilin University

Changchun, , China

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Sichuan Provincial Cancer Hospital

Chengdu, , China

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Sun yat-sen University Cancer Center

Guangzhou, , China

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Guangdong Provincial People's Hospital

Guangzhou, , China

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The Second Affiliated Hospital of Zhejiang University School of Medicine

Hangzhou, , China

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Sir Run Run Shaw Hospital Zhejiang University

Hangzhou, , China

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Harbin Medical University Tumor Hospital

Harbin, , China

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The Second Affiliated Hospital to Nanchang University

Nanchang, , China

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Jiangsu Cancer Hospital

Nanjing, , China

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Tianjin Cancer Hospital

Tianjin, , China

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Union Hospital Tongji Medical College Huazhong University of Science and Technology

Wuhan, , China

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Hubei Cancer Hospital

Wuhan, , China

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First Affiliated Hospital of Medical College of Xi'an Jiaotong University

Xi'an, , China

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Zhejiang Cancer Hospital

Zhejiang, , China

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Centre Hospitalier de La Cote Basque

Bayonne, , France

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Centre Leon Berard

Lyon, , France

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ICM

Montpellier, , France

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Centre Eugene Marquis

Rennes, , France

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IUCT Oncopole

Toulouse, , France

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Uniklinik RWTH Aachen Klinik für Gynäkologie und Geburtsmedizin

Aachen, , Germany

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Universitätsklinikum Essen

Essen, , Germany

Site Status

Praxis für Interdisziplinäre Onkologie und Hämatologie GbR

Freiburg im Breisgau, , Germany

Site Status

Universitätsmedizin Göttingen Georg-August-Universität

Göttingen, , Germany

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Mammazentrum Hamburg am Krankenhaus Jerusalem

Hamburg, , Germany

Site Status

Medizinische Hochschule Zentrum Frauenheilkunde Abt.Gynäkologische Onkologie

Hanover, , Germany

Site Status

Nationales Centrum für Tumorerkrankungen (NCT)

Heidelberg, , Germany

Site Status

Brustzentrum Rhein-Ruhr Servicegesellschaft mbH

Mönchengladbach, , Germany

Site Status

St. Vincenz-Krankenhaus GmbH Paderborn Frauen- und Kinderklinik St. Louise

Paderborn, , Germany

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A.O. S. Anna e San Sebastiano

Caserta, Campania, Italy

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IRST Istituto Scientifico Romagnolo Per Lo Studio E Cura Dei Tumori, Sede Meldola

Meldola, Emilia-Romagna, Italy

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Ospedale San Raffaele

Milan, Lombardy, Italy

Site Status

Ospedale Santa Chiara

Trento, Trentino-Alto Adige, Italy

Site Status

Panamerican Clinical Research S.A de C.V.

Guadalajara, Jalisco, Mexico

Site Status

RENATI INNOVATION S.A.P.I. de C.V

Guadalajara, Jalisco, Mexico

Site Status

COI Centro Oncologico Internacional Santa Fe

Mexico City, Mexico CITY (federal District), Mexico

Site Status

Health Pharma Professional Research

Mexico City, Mexico CITY (federal District), Mexico

Site Status

OncoMed

Mexico City, Mexico CITY (federal District), Mexico

Site Status

ARKE Estudios Clínicos S.A. de C.V.

Mexico City, Mexico CITY (federal District), Mexico

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Instituto Nacional de Cancerologia

Distrito Federal, , Mexico

Site Status

CENEIT Oncologicos

Mexico City, , Mexico

Site Status

Antiguo Hospital Civil de Guadalajara Fray Antonio Alcalde

Morelia, , Mexico

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Centrum Onkologii im. Prof. Franciszka ?ukaszczyka

Bydgoszcz, , Poland

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Narodowy Instytut Onkologii Odzia? w Gliwicach

Gliwice, , Poland

Site Status

Przychodnia Lekarska KOMED, Roman Karaszewski

Konin, , Poland

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Szpital Wojewódzki im. Miko?aja Kopernika

Koszalin, , Poland

Site Status

Szpital Uniwersytecki w Krakowie

Krakow, , Poland

Site Status

MRUKMED Lekarz Beata Madej-Mruk i Partner Spolka Partnerska Oddzial nr 1 w Rzeszowie

Rzeszów, , Poland

Site Status

Narodowy Instytut Onkologii im. M.Sklodowskiej-Curie

Warsaw, , Poland

Site Status

Medical Oncology Centre of Rosebank

Johannesburg, , South Africa

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Richards Bay Oncology Centre

KwaZulu Natal, , South Africa

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Kyungpook National University Chilgok Hospital

Daegu, , South Korea

Site Status

National Cancer Center

Goyang-si, , South Korea

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Inha University Hospital

Incheon, , South Korea

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Korea University Anam Hospital

Seoul, , South Korea

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Seoul National University Hospital

Seoul, , South Korea

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Severance Hospital, Yonsei University Health System

Seoul, , South Korea

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Asan Medical Center

Seoul, , South Korea

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Gangnam Severance Hospital

Seoul, , South Korea

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Samsung Medical Center

Seoul, , South Korea

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Seoul St Mary's Hospital

Seoul, , South Korea

Site Status

ICO L'Hospitalet

L'Hospitalet de Llobregat, Barcelona, Spain

Site Status

Hospital Universitario de Canarias

San Cristóbal de La Laguna, Tenerife, Spain

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Hospital San Pedro De Alcantara

Cáceres, , Spain

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Hospital General Universitario Gregorio Marañon

Madrid, , Spain

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Hospital Ramon y Cajal

Madrid, , Spain

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Hospital Universitario 12 de Octubre

Madrid, , Spain

Site Status

Hospital Regional Universitario Carlos Haya

Málaga, , Spain

Site Status

Hospital Universitario Virgen Macarena

Seville, , Spain

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China Medical University Hospital

Taichung, , Taiwan

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National Cheng Kung University Hospital

Tainan, , Taiwan

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Taipei Veterans General Hospital

Taipei, , Taiwan

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Chang Gung Memorial Hosipital at Linkou

Taoyuan, , Taiwan

Site Status

Veterans General Hospital - Taichung

Xitun Dist., , Taiwan

Site Status

National Taiwan University Hospital

Zhongzheng Dist., , Taiwan

Site Status

Gulhane Training and Applicaton Hospital

Ankara, , Turkey (Türkiye)

Site Status

Memorial Ankara Hastanesi

Ankara, , Turkey (Türkiye)

Site Status

Dicle University Faculty of Medicine

Diyarbakır, , Turkey (Türkiye)

Site Status

Trakya University Medical Faculty

Edirne, , Turkey (Türkiye)

Site Status

Medipol Mega Üniversite Hastanesi Göztepe

Istanbul, , Turkey (Türkiye)

Site Status

Marmara Uni Faculty of Medicine

Istanbul, , Turkey (Türkiye)

Site Status

Ege Uni Medical Faculty Hospital

Izmir, , Turkey (Türkiye)

Site Status

Katip Celebi University Ataturk Training and Research Hospital

Izmir, , Turkey (Türkiye)

Site Status

Goztepe Prof.Dr. Suleyman Yalcin City Hospital

Kadiköy, , Turkey (Türkiye)

Site Status

Hacettepe Uni Medical Faculty Hospital

Sihhiye/Ankara, , Turkey (Türkiye)

Site Status

Basingstoke and North Hampshire Hospital

Basingstoke, , United Kingdom

Site Status

Blackpool Victoria Hospital

Blackpool, , United Kingdom

Site Status

Western General Hospital

Edinburgh, , United Kingdom

Site Status

Princess Alexandra Hospital

Harlow, , United Kingdom

Site Status

St Bartholomew's Hospital

London, , United Kingdom

Site Status

Maidstone & Tonbridge Wells Hospital

Maidstone, , United Kingdom

Site Status

Mount Vernon & Watford Hospital Trust

Northwood, , United Kingdom

Site Status

Churchill Hospital

Oxford, , United Kingdom

Site Status

Royal Hampshire County Hospital

Winchester, , United Kingdom

Site Status

Countries

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United States Argentina Australia Belgium Brazil Canada China France Germany Italy Mexico Poland South Africa South Korea Spain Taiwan Turkey (Türkiye) United Kingdom

Other Identifiers

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WO43919

Identifier Type: -

Identifier Source: org_study_id

2022-502322-41-00

Identifier Type: REGISTRY

Identifier Source: secondary_id

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