A Phase I, Open-Label, Dose-Escalation Study Evaluating the Safety, Tolerability, and Pharmacokinetics of GDC-0077 as a Single Agent in Patients With Locally Advanced or Metastatic PIK3CA-Mutant Solid Tumors and in Combination With Endocrine and Targeted Therapies in Patients With Locally Advanced or Metastatic PIK3CA-Mutant Breast Cancer

  • days left to enroll
  • participants needed
  • sponsor
    Genentech, Inc.
Updated on 21 September 2022
measurable disease
breast cancer
growth factor
epidermal growth factor receptor
epidermal growth factor
her2/neu-positive breast cancer
breast cancer staging
her2/neu-negative breast cancer


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)).

Condition Breast Cancer, Solid Tumor
Treatment Metformin, Trastuzumab, Letrozole, fulvestrant, Pertuzumab, Palbociclib, GDC-0077, Inavolisib
Clinical Study IdentifierNCT03006172
SponsorGenentech, Inc.
Last Modified on21 September 2022


Yes No Not Sure

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
Stages I and II
Stage II Arm G
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
Female participants with locally advanced or metastatic PIK3CA-mutant HER2+ breast cancer
Left ventricular ejection fraction 50% or greater

Exclusion Criteria

History of leptomeningeal disease
Type 1 or 2 diabetes requiring anti-hyperglycemic medication
Metaplastic breast cancer
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
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
Any active infection that could impact patient safety or serious infection requiring intravenous antibiotics
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
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