Purpose

The goal of this clinical trial is to evaluate the safety and efficacy of TOS-358 in women with HR+ HER2- metastatic breast cancer whose tumors have a mutation in PIK3CA and who meet all other study enrollment criteria. The main questions it aims to answer are: 1. Phase 1a: what is the maximum tolerated dose and recommended dose for phase 2? 2. Phase 1a: how safe and tolerable is TOS-358 at different dose levels when taken orally once or twice per day? 3. Phase 1b: how safe and effective is TOS-358 when given with standard of care medicines for HR+HER2- metastatic breast cancer (fulvestrant and CDK4/6i)

Condition

Eligibility

Eligible Ages
Over 18 Years
Eligible Sex
Female
Accepts Healthy Volunteers
No

Inclusion Criteria

  • Locally advanced, recurrent, or metastatic HR +/HER2- breast cancer - Up to 3 prior lines of therapy for metastatic disease - Willing and able to provide written informed consent for this study - Adults ≥ 18 years old at time of consent - Known PIK3CA mutations or amplifications as determined at a CAP/CLIA-certified or equivalently accredited diagnostic laboratory using a validated test - Measurable or evaluable disease by RECIST 1.1 - Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1 - Life expectancy ≥ 6 months, as determined by the investigator - Adequate bone marrow, liver, and kidney function within 14 days prior to first dose of investigational product - Fasting plasma glucose <= 140 mg/dL AND hemoglobin A1c (HbA1c) <= 7.0% - Available archived or fresh tumor tissue sample for detection of PIK3CA mutation by central laboratory test

Exclusion Criteria

  • Has an established diagnosis of diabetes mellitus type 1 or has uncontrolled diabetes mellitus type 2 - Known active central nervous system (CNS) metastases - PTEN mutations

Study Design

Phase
Phase 1
Study Type
Interventional
Allocation
Non-Randomized
Intervention Model
Parallel Assignment
Intervention Model Description
TOS-358 Single Agent Arm: Part 1 (multiple ascending doses, QD or BID): locally advanced, recurrent or metastatic HR+ breast, endometrial, urothelial or squamous cell carcinoma of the head and neck, with PIK3CA mutation per local assessment; Part 2 Patients with locally advanced, recurrent or metastatic HR+ HER2- breast cancer with PIK3CA mutation per local assessment will be enrolled in protocol defined groups in combination with fulvestrant +/- CDK4/6i.
Primary Purpose
Treatment
Masking
None (Open Label)

Arm Groups

ArmDescriptionAssigned Intervention
Experimental
TOS-358 + fulvestrant
TOS-358 + fulvestrant at standard dosing
  • Drug: TOS-358
    Covalent Phosphoinositide-3-Kinase (PI3K)-alpha Inhibitor
  • Drug: Fulvestrant
    Intramuscular SERD at standard doses
  • Drug: Palbociclib
    CDK4/6 inhibitor at standard doses
  • Drug: Ribociclib
    CDK4/6 inhibitor at standard doses
Experimental
TOS-358 + fulvestrant + CDK4/6i
TOS-358 + fulvestrant + CDK4/6i
  • Drug: TOS-358
    Covalent Phosphoinositide-3-Kinase (PI3K)-alpha Inhibitor
  • Drug: Fulvestrant
    Intramuscular SERD at standard doses
  • Drug: Palbociclib
    CDK4/6 inhibitor at standard doses
  • Drug: Ribociclib
    CDK4/6 inhibitor at standard doses
Experimental
TOS-358
PIK3CA covalent inhibitor
  • Drug: TOS-358
    Covalent Phosphoinositide-3-Kinase (PI3K)-alpha Inhibitor
  • Drug: Palbociclib
    CDK4/6 inhibitor at standard doses
  • Drug: Ribociclib
    CDK4/6 inhibitor at standard doses

Recruiting Locations

Vanderbilt-Ingram Cancer Center
Nashville, Tennessee 37232
Contact:
Jordan Berlin, MD
1-800-811-8480
CIP@VUMC.ORG

More Details

Status
Recruiting
Sponsor
Totus Medicines

Study Contact

Clinical Trials
Please e-mail
clinicaltrials@totusmedicines.com

Detailed Description

This study will be conducted in two parts: a dose finding portion to determine the maximum tolerated dose and recommended phase 2 dose (RP2D) of TOS-358 administered orally on once a day (QD) and twice daily (BID) schedules, and a dose expansion portion to evaluate safety and tolerability in tumor-specific cohorts administered TOS-358 at the recommended phase 2 dose and schedule. Women with histologically confirmed diagnosis of hormone receptor-positive (HR+), human epidermal growth factor receptor 2 (HER2) negative breast cancer with known PIK3CA mutations or amplifications and who meet all of the eligibility criteria will be enrolled in the study. In the dose finding portion of the study, TOS-358 will be evaluated as a single-agent at multiple dose levels administered orally until disease progression, unacceptable toxicity, or until meeting any other reason for discontinuation as specified in the protocol. In the Phase 1b portion, TOS-358 will be combined with fulvestrant +/- CDK4/6i.

Notice

Study information shown on this site is derived from ClinicalTrials.gov (a public registry operated by the National Institutes of Health). The listing of studies provided is not certain to be all studies for which you might be eligible. Furthermore, study eligibility requirements can be difficult to understand and may change over time, so it is wise to speak with your medical care provider and individual research study teams when making decisions related to participation.