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Phase 1b Combo w/ Ribociclib, Alpelisib, or Everolimus

Phase 1
Recruiting
Conditions
Metastatic Breast Cancer
Advanced Breast Cancer
ER-positive Breast Cancer
HER2-negative Breast Cancer
Breast Cancer
Interventions
Registration Number
NCT05508906
Lead Sponsor
Olema Pharmaceuticals, Inc.
Brief Summary

This is a Phase 1b open-label, 2-part study in 3 treatment groups. The 3 treatment groups are as follows:

Treatment Group 1: OP-1250 in combination with ribociclib (KISQALI®, Novartis Pharmaceuticals Corporation).

Treatment Group 2: OP-1250 in combination with alpelisib (PIQRAY®, Novartis Pharmaceuticals Corporation).

Treatment Group 3: OP-1250 in combination with everolimus.

Detailed Description

Part 1 (Dose Escalation): This part will evaluate the safety and pharmacokinetics of a range of doses of OP-1250 administered orally (PO) daily to subjects in combination with 600 mg of ribociclib administered PO daily for 21 consecutive days followed by 7 days off treatment (Treatment Group 1) or with 300 mg or 250 mg of alpelisib administered PO daily (Treatment Group 2) or with everolimus 10 mg administered PO daily (Treatment Group 3) and determine the RP2D (Recommended Phase 2 Dose) for each treatment group.

Part 2 (Dose Expansion): This part of the study will further evaluate the safety and PK of OP-1250 at the RP2D in combination with ribociclib (Treatment Group 1), alpelisib (Treatment Group 2), or everolimus (Treatment Group 3) and provide an exploratory estimate of anti-tumor activity of the combinations. An additional group of OP-1250 at an alternate dose level in combination with ribociclib (Treatment Group 1b) will be explored to optimize the RP2D of OP-1250.

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
155
Inclusion Criteria
  • Female or male aged >18 years.
  • Willing and able to participate and comply with all study requirements.
  • Histologically- or cytologically-confirmed advanced or metastatic Breast Cancer (mBC).
  • ER+/HER2- disease, as determined in the most recently obtained archival tumor tissue sample from a metastatic site, using locally accepted criteria by the local pathology report.
  • Evaluable disease with one of the following: Measurable disease, ie, at least 1 measurable lesion as per RECIST 1.1 (a lesion at a previously irradiated site may only be counted as a target lesion if there is clear sign of progression since the irradiation) OR patients with predominantly bone disease (with or without other non-measurable lesions) are allowed if it is possible to evaluate on radiological examinations (eg. bone scan, PET/CT, CT, MRI) even if lesions are non-measurable according to RECIST 1.1.
  • Life expectancy ≥6 months, as judged by the investigator.
  • Eastern Cooperative Oncology Group (ECOG) performance status (PS) of 0 or 1.
  • Has received no more than 1 prior hormonal regimen (Treatment Group 1). Has received no more than 2 prior hormonal regimens (Treatment Group 2 and Treatment Group 3) for advanced or metastatic disease. Prior hormonal regimens in combination with CDK4/6 inhibitors are allowed in all treatment groups.
  • Has received no more than 1 prior chemotherapy (which includes antibody drug conjugates) for locally advanced or metastatic breast cancer.
Exclusion Criteria
  • Prior or concurrent malignancy whose natural history or treatment may interfere with the safety or efficacy assessment of the investigational regimen.
  • Clinically significant, uncontrolled heart disease and/or cardiac repolarization abnormality.
  • History of cerebral vascular disease within 6 months prior to the first administration of study drug dose.
  • History of a pulmonary embolism, or deep venous thrombosis within the last 6 months, or subject has an increased risk of thrombosis as determined by the investigator.
  • History of pneumonitis or interstitial lung disease.
  • Leptomeningeal disease or spinal cord compression.
  • Medical history or ongoing gastrointestinal disorders that could affect absorption of oral therapeutics.
  • Known human immunodeficiency virus infection.
  • Known clinically significant history of liver disease consistent with Child-Pugh Class B or C, including active viral or other hepatitis (eg, hepatitis B or hepatitis C virus), current alcohol abuse, or cirrhosis.
  • History of severe cutaneous reaction, such as Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis, or drug reaction with eosinophilia and systemic symptoms.
  • Has clinically significant co-morbidities, such as active infection, psychiatric disease, or any other condition that could impact the ability of the subject to participate in this study or otherwise has the potential to confound the study results.
  • Have received prior treatment with OP-1250.
  • Have received prior treatment with approved or investigational PI3K inhibitor (Treatment Group 2) or mTOR inhibitor (Treatment Group 3).

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
OP-1250 with RibociclibOP-1250Treatment Group 1: OP-1250 in combination with ribociclib (KISQALI®, Novartis Pharmaceuticals Corporation).
OP-1250 with RibociclibRibociclibTreatment Group 1: OP-1250 in combination with ribociclib (KISQALI®, Novartis Pharmaceuticals Corporation).
OP-1250 with AlpelisibOP-1250Treatment Group 2: OP-1250 in combination with alpelisib (PIQRAY®, Novartis Pharmaceuticals Corporation)
OP-1250 with AlpelisibAlpelisibTreatment Group 2: OP-1250 in combination with alpelisib (PIQRAY®, Novartis Pharmaceuticals Corporation)
OP-1250 with EverolimusOP-1250Treatment Group 3: OP-1250 in combination with everolimus
OP-1250 with EverolimusEverolimusTreatment Group 3: OP-1250 in combination with everolimus
Primary Outcome Measures
NameTimeMethod
Dose Limiting Toxicities (DLTs)The first 28 days of treatment

To determine the maximum tolerated dose (MTD) and/or recommended Phase 2 dose (RP2D) of OP-1250 when administered with ribociclib (Treatment Group 1), alpelisib (Treatment Group 2), or everolimus (Treatment Group 3). The incidence of DLTs will be assessed in the Dose Escalation part (Part 1) of the study.

Characterize the incidence, nature and severity of treatment emergent adverse events (TEAEs) and serious adverse events (SAEs) of OP-1250 when administered with ribociclib, alpelisib, or everolimusUp to 35 days after end of treatment

Characterize the incidence, nature and severity of TEAEs and SAEs of OP-1250 when administered with ribociclib (Treatment Group 1), alpelisib (Treatment Group 2), or everolimus (Treatment Group 3) according to NCI-CTCAE version 5.0.

Pharmacokinetics (PK) of OP-1250 when administered with ribociclib (Treatment Group 1) or alpelisib (Treatment Group 2), or everolimus (Treatment Group 3).Every 28 days

To assess the PK of OP-1250 in combination with ribociclib, alpelisib, or everolimus plasma levels of OP-1250 (and potential metabolites) and ribociclib (Treatment Group 1), plasma levels of OP-1250 (and potential metabolites) and alpelisib (Treatment Group 2), or plasma levels of OP-1250 (and potential metabolites) and everolimus (Treatment Group 3) will be assessed at predefined intervals to establish PK parameters (including: Cmax, Cmin, Tmax, AUC, and t1⁄2) and OP-1250 trough concentration at steady state).

Secondary Outcome Measures
NameTimeMethod
Preliminarily assess the anti-tumor activity (ORR) of OP-1250 when administered with ribociclib (Treatment Group 1), alpelisib (Treatment Group 2), or everolimus (Treatment Group 3), as assessed by the investigator using RECIST v1.1.Up to 1 year

Tumor response will be evaluated in patients with measurable or evaluable disease using RECISTv1.1 guidelines.

Evaluate clinical benefit rate (CBR) of OP-1250 when administered with ribociclib (Treatment Group 1), alpelisib (Treatment Group 2), or everolimus (Treatment Group 3)Up to 1 year

CBR will be assessed as proportion of subjects achieving complete response (CR), partial response (PR), or stable disease (SD) with duration of at least 24 weeks.

Evaluate duration of response (DoR) of OP-1250 when administered with ribociclib (Treatment Group 1), alpelisib (Treatment Group 2), or everolimus (Treatment Group 3)Up to 1 year

DoR will be calculated as the number of days from the start date of PR or CR (whichever response is achieved first) to the first date that progressive disease is documented.

Trial Locations

Locations (16)

Advent Health Hematology and Oncology

🇺🇸

Orlando, Florida, United States

University of Iowa

🇺🇸

Iowa City, Iowa, United States

Banner MD Anderson Cancer Center

🇺🇸

Gilbert, Arizona, United States

University of California San Francisco Health

🇺🇸

San Francisco, California, United States

University of Colorado Cancer Center

🇺🇸

Aurora, Colorado, United States

Dana Farber Cancer Institute

🇺🇸

Boston, Massachusetts, United States

Henry Ford Health

🇺🇸

Detroit, Michigan, United States

Regents of the University of Minnesota

🇺🇸

Minneapolis, Minnesota, United States

Washington University, School of Medicine

🇺🇸

Saint Louis, Missouri, United States

Ichan School of Medicine at Mount Sinai

🇺🇸

New York, New York, United States

Atrium Health Levine Cancer Institute

🇺🇸

Charlotte, North Carolina, United States

Henry-Joyce Cancer Clinic, The Vanderbilt Clinic

🇺🇸

Nashville, Tennessee, United States

MD Anderson Cancer Center

🇺🇸

Houston, Texas, United States

Northwest Medical Specialties

🇺🇸

Tacoma, Washington, United States

Macquarie Health

🇦🇺

Sydney, New South Wales, Australia

Breast Cancer Research Center- Western Australia

🇦🇺

Nedlands, Western Australia, Australia

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