Valemetostat tosylate: Administered orally once daily
T-DXd: One IV infusion Q3W on Day 1 of each 21-day cycle
Dato-DXd: One IV infusion Q3W on Day 1 of each 21-day cycle.
Study summary
This study will evaluate the safety, tolerability, and efficacy of valemetostat tosylate in combination with DXd antibody-drug conjugates (ADC) in participants with advanced solid tumors.
Eligibility
Sex
ALL
Min age
18 Years
Max age
—
Healthy volunteers
No
Key Inclusion Criteria
All participants must meet all of the following criteria, as well as all criteria from the relevant sub-protocol to be eligible for enrollment:
* At least 18 years or the minimum legal adult age (whichever is greater) at the time the informed consent form (ICF) is signed.
* Has at least 1 measurable lesion based on investigator imaging assessment (computed tomography or magnetic resonance imaging) using RECIST v 1.1 at Screening.
* Is willing to provide an adequate tumor sample.
* Eastern Cooperative Oncology Group performance status (ECOG PS) of 0 or 1 at Screening.
Additional Key Inclusion for Sub-Protocol A:
* Diagnosed with pathologically documented breast cancer that:
1. Is unresectable or metastatic.
2. Has progressed on and would no longer benefit from endocrine therapy in hormone receptor-positive subjects in the opinion of the investigator.
3. Has been treated with at least 1 and at most 2 prior lines of chemotherapy in the recurrent or metastatic setting.
4. Has a history of low HER2 expression, defined as immunohistochemistry (IHC) 2+ /in situ hybridization (ISH)-negative or IHC 1+ (ISH-negative or untested), as classified by the American Society of Clinical Oncology/College of American Pathologists 2023 HER2 testing guidelines.
5. Was never previously HER2-positive (IHC 3+ or IHC 2+/ISH+) on prior pathology testing (per American Society of Clinical Oncology/College of American Pathologists guidelines
Additional Key Inclusion for Sub-Protocol B:
• Gastric or gastro-esophageal junction (GEJ) adenocarcinoma that is (a) unresectable or metastatic (b) has progressed on HER2-directed monoclonal antibody (mAb) containing therapy, such as trastuzumab or approved trastuzumab biosimilar-containing regimen.
Additional Key Inclusion for Sub-Protocol C:
* Pathologically documented Stage IIIB, IIIC, or IV non-squamous NSCLC with or without actionable genomic alterations (AGA) at the time of enrollment.
* Must meet prior therapy requirements:
* Participants without AGA: (a) received platinum-based chemotherapy in combination with α-PD-1/α -PD-L1 mAb as the only prior line of therapy or (b) received platinum-based chemotherapy and α -PD-1/ α -PD-L1 mAb (in either order) sequentially as the only 2 prior lines of therapy.
* Participants with AGA: (a) has been treated with 1 or 2 prior lines of applicable targeted therapy that is locally approved for participant's genomic alteration at the time of Screening, (b) participants who have received platinum-based chemotherapy as the only prior line of cytotoxic therapy, (c) may have received α -PD-1/α -PD-L1 mAb alone or in combination with a cytotoxic agent
Key Exclusion Criteria
* Has previously been treated with any enhancer of zeste homolog inhibitors.
* Uncontrolled or significant cardiovascular disease.
* Has spinal cord compression or clinically active central nervous system metastases, defined as untreated and symptomatic, or requiring therapy with corticosteroids or anticonvulsants to control associated symptoms.
* Has leptomeningeal carcinomatosis or metastasis.
* Clinically severe pulmonary compromise resulting from intercurrent pulmonary illnesses.
* Current use of moderate or strong cytochrome P450 (CYP)3A inducers.
* Systemic treatment with corticosteroids (\>10 mg daily prednisone equivalents).
* History of severe hypersensitivity reactions to other monoclonal antibodies (mAbs).
* Evidence of ongoing uncontrolled systemic bacterial, fungal, or viral infection requiring treatment with intravenous (IV) antibiotics, antivirals, or antifungals.
* Female who is pregnant or breastfeeding or intends to become pregnant during the study.
* Psychological, social, familial, or geographical factors that would prevent regular follow-up.
Additional Key Exclusion for Sub-Protocol A:
* Has previously received any anti-HER2 therapy in the metastatic setting.
* Has received prior treatment with an antibody-drug conjugate that consists of an exatecan derivative that is a topoisomerase I inhibitor, including either as part of prior treatment history or within prior participation in a clinical study.
Additional Key Exclusion for Sub-Protocol B:
\* Participants who have received an antibody-drug conjugate consisting of an exatecan derivative that is a topoisomerase I inhibitor.
Additional Key Exclusion for Sub-Protocol C:
\* Has received any agent, including an ADC, containing a chemotherapeutic agent targeting topoisomerase I or TROP2-targeted therapy including Dato-DXD
Primary outcome measure(s)
Number of Participants Reporting Dose-limiting Toxicities (Part 1 Dose Escalation) — Cycle 1 Day 1 up to Day 21 (each cycle is 21 days)
Number of Participants Reporting Treatment-emergent Adverse Events (Part 1 Dose Escalation) — Screening up to 40 days after last dose, up to approximately 5 years
Objective Response Rate Based on Investigator Assessment (Part 2 Dose Expansion) — Baseline (Screening), at every 6 weeks from Cycle 1 Day 1 in the first year, and every 12 weeks thereafter until disease progression or until the start of a new anticancer treatment, up to approximately 5 years
Trial sites (35)
Facility
City
Region
Status
City of Hope At Orange County Lennar Foundation Cancer Center
Irvine
California
Sharp Memorial Hospital
San Diego
California
Brcr Medical Center, Inc Dba Boca Raton Clinical Research
Plantation
Florida
University of Hawaii At Manoa
Honolulu
Hawaii
University of Chicago Medical Center
Chicago
Illinois
Dana-Farber Cancer Institute
Boston
Massachusetts
Memorial Sloan-Kettering Cancer Center (Mskcc) - New York
New York
New York
Clinical Research Alliance
Westbury
New York
Unc Hospitals
Chapel Hill
North Carolina
The Cleveland Clinic Foundation
Cleveland
Ohio
Providence Portland Medical Center
Portland
Oregon
Mary Crowley Cancer Research Centers
Dallas
Texas
Ut Southwestern Medical Center
Dallas
Texas
University of Texas M. D. Anderson Cancer Center
Houston
Texas
Next Virginia
Fairfax
Virginia
Fred Hutchinson Cancer Center
Seattle
Washington
Medical College of Wisconsin
Milwaukee
Wisconsin
Peking University Third Hospital
Beijing
China
Sun Yat-Sen University, Cancer Center
Guangzhou
China
SunYat-Sen University Cancer Center
Guangzhou
China
Harbin Medical Univeristy Cancer Hospital
Heilongjiang
China
Hunan Cancer Hospital
Hunan
China
Jilin Cancer Hospital
Jilin City
China
Jinana Center Hosptial
Shandong
China
IRCCS Istituto Scientifico Romagnolo Per
Cesena
Italy
National Cancer Center Hospital
Chūōku
Japan
National Hospital Org-Kyushu Cancer Center
Fukuoka
Japan
National Cancer Center Hospital East
Kashiwa
Japan
The Cancer Institute Hospital of Jfcr
Kōtoku
Japan
Aichi Cancer Center Hospital
Nagoya
Japan
Osaka International Cancer Institute
Osaka
Japan
Kindai University Hospital
Ōsaka-sayama
Japan
Shizuoka Cancer Center
Shizuoka
Japan
Osaka University Hospital
Suita
Japan
Kanagawa Cancer Center
Yokohama
Japan
Official registry record
This page summarises publicly available registry data for informational purposes — not medical advice. Eligibility is determined by each study team; patients should discuss participation with their clinician.
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