To Evaluate the Safety, Tolerability, and Pharmacokinetics of Inavolisib Single Agent in Participants With Solid Tumors and in Combination With Endocrine and Targeted Therapies in Participants With Breast Cancer

NCT ID: NCT03006172

Last Updated: 2025-12-18

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

PHASE1

Total Enrollment

200 participants

Study Classification

INTERVENTIONAL

Study Start Date

2016-12-13

Study Completion Date

2026-12-31

Brief Summary

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This is an open-label, multicenter, Phase I study designed to evaluate the safety, tolerability, and pharmacokinetics of inavolisib administered orally as a single agent in patients with locally advanced or metastatic PIK3CA-mutant solid tumors, including breast cancer, and in combination with standard-of-care endocrine and/or targeted therapies for the treatment of locally advanced or metastatic PIK3CA-mutant breast cancer. Participants will be enrolled in two stages: a dose-escalation stage (Stage I) and an expansion stage (Stage II). Participants will be assigned to one of seven regimens: inavolisib as a single agent (Arm A), inavolisib in combination with palbociclib and letrozole (Arm B), inavolisib in combination with letrozole (Arm C), inavolisib in combination with fulvestrant (Arm D), inavolisib in combination with palbociclib and fulvestrant (Arm E), inavolisib in combination with palbociclib, fulvestrant, and metformin (Arm F), and inavolisib in combination with trastuzumab and pertuzumab (and letrozole or fulvestrant, if applicable (Arm G)).

Detailed Description

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Conditions

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Breast Cancer Solid Tumor

Keywords

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PIK3CA mutant, Breast Cancer

Study Design

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Allocation Method

NON_RANDOMIZED

Intervention Model

SEQUENTIAL

Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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Stage I Arm A: Inavolisib Single Agent

Participants will receive inavolisib in escalating dose levels with starting dose of 6 milligrams (mg). Participants will receive single dose of inavolisib on Day 1 of Cycle 1 followed by once daily from Day 8 of Cycle 1. (Cycle length: 35 days for Cycle 1 and 28 days for all other cycles). Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will receive oral inavolisib once daily on Days 1-28 of each 28-day cycle (Arms A, B, C, D, E, F) or Days 1-21 of each 21-day cycle (Arm G).

Stage I Arm B: Inavolisib + Palbociclib + Letrozole

Participants will receive inavolisib in escalating dose levels (starting dose 3 mg) on Days 1-28, palbociclib on Days 1-21, and letrozole on Days 1-28 of each 28-day cycle. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will receive oral inavolisib once daily on Days 1-28 of each 28-day cycle (Arms A, B, C, D, E, F) or Days 1-21 of each 21-day cycle (Arm G).

Letrozole

Intervention Type DRUG

Participants will receive once daily oral doses of letrozole 2.5 mg on Days 1-28 of each cycle.

Palbociclib

Intervention Type DRUG

Participants will receive once daily oral doses of palbociclib 125 mg on Days 1-21 of each cycle.

Stage I Arm C: Inavolisib + Letrozole

Participants will receive inavolisib in escalating dose levels along with letrozole on Days 1-28 of each 28-day cycle. The starting dose of inavolisib will not exceed the starting dose in Stage I Arm A. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will receive oral inavolisib once daily on Days 1-28 of each 28-day cycle (Arms A, B, C, D, E, F) or Days 1-21 of each 21-day cycle (Arm G).

Letrozole

Intervention Type DRUG

Participants will receive once daily oral doses of letrozole 2.5 mg on Days 1-28 of each cycle.

Stage II Arm B: Inavolisib + Palbociclib + Letrozole

Participants will receive inavolisib on Days 1-28 in combination with palbociclib on Days 1-21 and letrozole on Days 1-28 of each 28-day cycle. Dose of inavolisib will be decided based on the results of Stage I Arm B. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will receive oral inavolisib once daily on Days 1-28 of each 28-day cycle (Arms A, B, C, D, E, F) or Days 1-21 of each 21-day cycle (Arm G).

Letrozole

Intervention Type DRUG

Participants will receive once daily oral doses of letrozole 2.5 mg on Days 1-28 of each cycle.

Palbociclib

Intervention Type DRUG

Participants will receive once daily oral doses of palbociclib 125 mg on Days 1-21 of each cycle.

Stage II Arm C: Inavolisib + Letrozole

Participants will receive inavolisib in combination with letrozole on Days 1-28 of each 28-day cycle. Dose of inavolisib will be decided based on the results of Stage I Arm C. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will receive oral inavolisib once daily on Days 1-28 of each 28-day cycle (Arms A, B, C, D, E, F) or Days 1-21 of each 21-day cycle (Arm G).

Letrozole

Intervention Type DRUG

Participants will receive once daily oral doses of letrozole 2.5 mg on Days 1-28 of each cycle.

Stage II Arm D: Inavolisib + Fulvestrant

Participants will receive inavolisib on Days 1-28 in combination with fulvestrant on Day 1 and 15 of Cycle 1 and then on Day 1 from Cycle 2 (cycle length: 28 days). Dose of inavolisib will be decided based on the results of Stage I Arm C. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will receive oral inavolisib once daily on Days 1-28 of each 28-day cycle (Arms A, B, C, D, E, F) or Days 1-21 of each 21-day cycle (Arm G).

Fulvestrant

Intervention Type DRUG

Participants will receive fulvestrant 500 mg, administered intramuscularly on Days 1 and 15 of Cycle 1. For subsequent cycles, participants will receive fulvestrant intramuscularly on Day 1 of each cycle.

Stage II Arm E: Inavolisib + Palbociclib + Fulvestrant

Participants will receive inavolisib (Days 1-28) in combination with palbociclib (Days 1-21) and fulvestrant (Days 1 and 15 of Cycle 1; Day 1 for subsequent cycles)(Cycle = 28 days). Dose of inavolisib will be determined from the results of Stage I Arm B. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will receive oral inavolisib once daily on Days 1-28 of each 28-day cycle (Arms A, B, C, D, E, F) or Days 1-21 of each 21-day cycle (Arm G).

Fulvestrant

Intervention Type DRUG

Participants will receive fulvestrant 500 mg, administered intramuscularly on Days 1 and 15 of Cycle 1. For subsequent cycles, participants will receive fulvestrant intramuscularly on Day 1 of each cycle.

Palbociclib

Intervention Type DRUG

Participants will receive once daily oral doses of palbociclib 125 mg on Days 1-21 of each cycle.

Stage II Arm F: Inavolisib + Palbociclib + Fulvestrant + Metformin

Participants will receive inavolisib (Days 1-28) in combination with palbociclib (Days 1-21), fulvestrant (Days 1 and 15 of Cycle 1; Day 1 for subsequent cycles) and metformin (Days 1-28)(Cycle = 28 days). Dose of inavolisib will be determined from the results of Stage I Arm B. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will receive oral inavolisib once daily on Days 1-28 of each 28-day cycle (Arms A, B, C, D, E, F) or Days 1-21 of each 21-day cycle (Arm G).

Fulvestrant

Intervention Type DRUG

Participants will receive fulvestrant 500 mg, administered intramuscularly on Days 1 and 15 of Cycle 1. For subsequent cycles, participants will receive fulvestrant intramuscularly on Day 1 of each cycle.

Palbociclib

Intervention Type DRUG

Participants will receive once daily oral doses of palbociclib 125 mg on Days 1-21 of each cycle.

Metformin

Intervention Type DRUG

Participants will receive oral metformin once daily, starting on Cycle 1, Day 1, as tolerated.

Stage II Arm G: Inavolisib + Trastuzumab + Pertuzumab

Participants will receive inavolisib in combination with trastuzumab and pertuzumab (Days 1-21). Dose of inavolisib will be determined from the results of Stage I Arm A. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.

Group Type EXPERIMENTAL

Inavolisib

Intervention Type DRUG

Participants will receive oral inavolisib once daily on Days 1-28 of each 28-day cycle (Arms A, B, C, D, E, F) or Days 1-21 of each 21-day cycle (Arm G).

Trastuzumab

Intervention Type DRUG

Participants will receive trastuzumab, administered by IV infusion on Day 1 of each 21-day cycle, at a loading dose of 8 mg/kg for Cycle 1 and a dose of 6 mg/kg for subsequent cycles, until disease progression or unacceptable toxicity.

Pertuzumab

Intervention Type DRUG

Participants will receive pertuzumab, administered by IV infusion on Day 1 of each 21-day cycle, at a loading dose of 840 mg for Cycle 1 and a dose of 420 mg for subsequent cycles, until disease progression or unacceptable toxicity.

Interventions

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Inavolisib

Participants will receive oral inavolisib once daily on Days 1-28 of each 28-day cycle (Arms A, B, C, D, E, F) or Days 1-21 of each 21-day cycle (Arm G).

Intervention Type DRUG

Fulvestrant

Participants will receive fulvestrant 500 mg, administered intramuscularly on Days 1 and 15 of Cycle 1. For subsequent cycles, participants will receive fulvestrant intramuscularly on Day 1 of each cycle.

Intervention Type DRUG

Letrozole

Participants will receive once daily oral doses of letrozole 2.5 mg on Days 1-28 of each cycle.

Intervention Type DRUG

Palbociclib

Participants will receive once daily oral doses of palbociclib 125 mg on Days 1-21 of each cycle.

Intervention Type DRUG

Metformin

Participants will receive oral metformin once daily, starting on Cycle 1, Day 1, as tolerated.

Intervention Type DRUG

Trastuzumab

Participants will receive trastuzumab, administered by IV infusion on Day 1 of each 21-day cycle, at a loading dose of 8 mg/kg for Cycle 1 and a dose of 6 mg/kg for subsequent cycles, until disease progression or unacceptable toxicity.

Intervention Type DRUG

Pertuzumab

Participants will receive pertuzumab, administered by IV infusion on Day 1 of each 21-day cycle, at a loading dose of 840 mg for Cycle 1 and a dose of 420 mg for subsequent cycles, until disease progression or unacceptable toxicity.

Intervention Type DRUG

Other Intervention Names

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RO7113755, GDC-0077

Eligibility Criteria

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Inclusion Criteria

* Evaluable or measurable disease per RECIST, Version 1.1 (measurable disease only for Arm D)
* Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1
* Life expectancy of greater than or equal to (\>=) 12 weeks
* Adequate hematologic and organ function, including blood counts, liver and kidney function

Stage I Arm A (Inavolisib):

\- Locally advanced, recurrent, or metastatic, PIK3CA mutant, incurable solid tumor malignancy, including breast cancer

Stages I and II, Arms B and C:

\- Postmenopausal female participants with locally advanced or metastatic PIK3CA-mutant HR+/HER2- breast cancer

Stage II, Arms D, E, or F:

\- Female participants with locally advanced or metastatic PIK3CA-mutant HR+/HER2- breast cancer

Stage II Arm D:

\- Prior treatment with CDK4/6 inhibitor

Stage II Arm G:

* Female participants with locally advanced or metastatic PIK3CA-mutant HER2+ breast cancer
* Left ventricular ejection fraction 50% or greater

Stages I and II:

\- All participants must provide tumor tissue from the primary or metastatic tumor site obtained from a prior or new biopsy or surgical procedure for detection of PIK3CA mutation by central laboratory test.

Exclusion Criteria

* Metaplastic breast cancer
* History of leptomeningeal disease
* Type 1 or 2 diabetes requiring anti-hyperglycemic medication
* Inability or unwillingness to swallow pills
* Malabsorption syndrome or other condition that would interfere with enteral absorption
* Known and untreated, or active central nervous system metastases
* Uncontrolled pleural effusion or ascites
* Any active infection that could impact patient safety or serious infection requiring intravenous antibiotics
* History of other malignancy within 5 years, except for treated carcinoma in situ of the cervix, non-melanoma skin carcinoma, or Stage I uterine cancer
* History of or active ventricular dysrhythmias or congestive heart failure requiring medication or symptomatic coronary heart disease
* Congenital long QT syndrome, prolonged QT interval, or family history of sudden unexplained death or long QT syndrome

Stage II Arms B, C, D, and E only:

* Prior treatment with \>1 chemotherapy regimen for metastatic disease
* Prior treatment with PI3K inhibitor
* History of significant toxicity related to mTOR inhibitor requiring treatment discontinuation

Stage II Arms B and E only:

\- Prior CDK4/6 inhibitor treatment

Stage II Arm G only:

* Current uncontrolled hypertension or unstable angina
* History of congestive heart failure, serious cardiac arrhythmia, or recent myocardial infarction
* Prior ejection fraction decrease on trastuzumab
* Prior cumulative doxorubicin greater than 360 mg/m2
* Symptomatic active lung disease
* History of significant toxicity related to trastuzumab and/or pertuzumab requiring discontinuation of treatment
Minimum Eligible Age

18 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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Genentech, Inc.

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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Dana Farber Cancer Institute

Boston, Massachusetts, United States

Site Status

Memorial Sloan Kettering Cancer Center

New York, New York, United States

Site Status

Columbia University Medical Center

New York, New York, United States

Site Status

SCRI Oncology Partners

Nashville, Tennessee, United States

Site Status

Princess Margaret Hospital

Toronto, Ontario, Canada

Site Status

Institut Bergonie

Bordeaux, , France

Site Status

Institut Gustave Roussy

Villejuif, , France

Site Status

Hospital Universitari Vall d'Hebron

Barcelona, , Spain

Site Status

Royal Marsden Hospital - Surrey

Surrey, Sutton, United Kingdom

Site Status

St Bartholomew's Hospital

London, , United Kingdom

Site Status

Royal Marsden Hospital - London

London, , United Kingdom

Site Status

Countries

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United States Canada France Spain United Kingdom

References

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Jhaveri KL, Accordino MK, Bedard PL, Cervantes A, Gambardella V, Hamilton E, Italiano A, Kalinsky K, Krop IE, Oliveira M, Schmid P, Saura C, Turner NC, Varga A, Cheeti S, Hilz S, Hutchinson KE, Jin Y, Royer-Joo S, Peters U, Shankar N, Schutzman JL, Juric D. Phase I/Ib Trial of Inavolisib Plus Palbociclib and Endocrine Therapy for PIK3CA-Mutated, Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced or Metastatic Breast Cancer. J Clin Oncol. 2024 Nov 20;42(33):3947-3956. doi: 10.1200/JCO.24.00110. Epub 2024 Sep 5.

Reference Type DERIVED
PMID: 39236276 (View on PubMed)

Other Identifiers

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GO39374

Identifier Type: -

Identifier Source: org_study_id

2016-003022-17

Identifier Type: EUDRACT_NUMBER

Identifier Source: secondary_id

2023-508124-36-00

Identifier Type: OTHER

Identifier Source: secondary_id