A Study to Evaluate the Safety,Tolerability, Pharmacokinetics and Clinical Activity of Mocertatug Rezetecan for Injection in Participants With Advanced Solid Tumors (BEHOLD-1)

Last updated: June 23, 2026
Sponsor: GlaxoSmithKline
Overall Status: Active - Recruiting

Phase

1

Condition

Neoplasms

Solid Tumors

Treatment

GSK5733584

Mocertatug rezetecan

Clinical Study ID

NCT06431594
222730
2024-513860-25
  • Ages > 18
  • All Genders

Study Summary

The goal of this study is to assess the safety and tolerability of Mocertatug Rezetecan . The study will also see how the levels of Mo-Rez change over time at different dose amount

Eligibility Criteria

Inclusion

Inclusion Criteria:

  • Males or females aged 18 years or older (≥18 years).

  • Participants with pathologically confirmed advanced solid tumor (who have failed orare intolerant to standard of care.

  • PROC cohort

  1. Histologically documented, advanced (metastatic and/or unresectable) high-gradeserous/endometrioid ovarian, primary peritoneal, or fallopian tube cancer.

  2. Must have received or are intolerant to 1 but no more than 4 lines of priorsystemic therapy.

  3. Platinum-resistant disease, defined as progression or relapse within 6 monthsafter the completion of platinum-based therapy.

  4. Must have had prior bevacizumab , unless there is a documented contraindicationor intolerance.

  5. Participants with known Folate receptor-α (FR-α) expressing tumors must havereceived mirvetuximab soravtansine if the regimen is locally available, unlessthere is a documented contraindication or intolerance.

Participants with known Breast cancer susceptibility gene (BRCA) mutated tumors should have received a Poly adenosine diphosphate-ribose polymerase (PARP) inhibitor if the regimen is locally available, unless there is a documented contraindication or intolerance.

  • Endometrial cancer cohort
  1. Histologically documented, advanced (metastatic and/or unresectable) orrecurrent endometrial cancer.

  2. Must have received or are intolerant to 1 but no more than 4 lines of priorsystemic therapy.

  3. Must have had prior platinum and PD(L)-1 inhibitor (in same regimen or inseparate regimens), if the regimen is locally available, unless there is adocumented contradiction or intolerance

  4. All epithelial histologies are permitted including carcinosarcoma.

  • Participants have at least one target lesion as assessed per the RECIST 1.1

  • Tumor tissue from a newly obtained biopsy or archival tumor tissue is required forretrospective detection of B7 homolog 4 (B7-H4) expression by IHC in centrallaboratory and other biomarker analysis. Tissue from a newly obtained biopsy ispreferred. If a newly obtained biopsy is not feasible, archival tumor tissue within 2 years prior to the first dose of study drug is acceptable.

  • Eastern Cooperative Oncology Group Performance Status (ECOG PS) score of 0 to 2 andno deterioration within 2 weeks before the first dose.

  • Have a life expectancy of at least 12 weeks.

Exclusion

Exclusion Criteria:

  • Have received any B7-H4-targeted therapy

  • Have received any of cytotoxic chemotherapy drugs, anti-tumor traditional Chinesemedicines or other anti-tumor drugs within 28 days prior to the first dose of studydrug; or need to continue these drugs during the study.

  • Have received locoregional radiation therapy within 2 weeks prior to the first doseof study drug; more than 30% of bone marrow irradiation or wide-field radiationtherapy within 4 weeks prior to the first dose of study treatment.

  • Presence of pleural/abdominal effusion/ascites requiring clinical intervention;presence of pericardial effusion

  • Major surgery within 28 days prior to the first dose of study treatment.

  • Evidence of brain metastasis unless asymptomatic;

  • Has inadequate bone marrow reserve or hepatic/renal functions .

  • Mean Fridericia-corrected QT interval (QTcF) QTcF >450 msec or QTcF >480 msec forparticipants with bundle branch blocK;

  • Evidence of current clinically significant arrhythmias or ECG abnormalities

  • Left ventricular ejection fraction (LVEF) < 50%.

  • Have severe, uncontrolled or active cardiovascular disorders, serious or poorlycontrolled hypertension, clinically significant bleeding symptoms or seriousarteriovenous thromboembolic events

  • Has current active pneumonitis/ILD or any history of ILD, any history of pneumonitisrequiring steroids or immunomodulatory treatment within 90 days of plannedrandomization/enrollment or any history of drug-induced pneumonitis/ILD.Havereceived prior therapy with topoisomerase inhibitors or topoisomerase inhibitorAntibody-drug conjugate (ADCs)

  • PROC

  1. Primary platinum refractory disease defined as those who have progressed on orwithin 12 weeks of last dose of first line platinum therapy not permitted.

  2. Non-epithelial carcinoma, clear-cell, mucinous, germ-cell, low-grade serous, orlow-grade endometrioid carcinoma not permitted.

  • Endometrial cancer a. Mesenchymal tumors of the uterus (uterine sarcomas) notpermitted.

Study Design

Total Participants: 675
Treatment Group(s): 2
Primary Treatment: GSK5733584
Phase: 1
Study Start date:
July 02, 2024
Estimated Completion Date:
December 31, 2029

Connect with a study center

  • GSK Investigational Site

    Cipoletti Rio Negro, R8324CVE
    Argentina

    Active - Recruiting

  • GSK Investigational Site

    Ciudad de Buenos Aires, 1118
    Argentina

    Active - Recruiting

  • GSK Investigational Site

    La Plata, B1900AVG
    Argentina

    Active - Recruiting

  • GSK Investigational Site

    Rosario, S2002
    Argentina

    Active - Recruiting

  • GSK Investigational Site

    Blacktown, New South Wales 2148
    Australia

    Active - Recruiting

  • GSK Investigational Site

    Macquarie University, New South Wales 2109
    Australia

    Active - Recruiting

  • GSK Investigational Site

    Leuven, 3000
    Belgium

    Active - Recruiting

  • GSK Investigational Site

    Barretos, 14784-400
    Brazil

    Active - Recruiting

  • GSK Investigational Site

    Goiânia, 74605-070
    Brazil

    Active - Recruiting

  • GSK Investigational Site

    Rio de Janeiro, 20220-410
    Brazil

    Active - Recruiting

  • GSK Investigational Site

    Ottawa, Ontario K1H 8L6
    Canada

    Active - Recruiting

  • GSK Investigational Site

    Toronto, Ontario M4N 3M5
    Canada

    Active - Recruiting

  • GSK Investigational Site

    Montreal, Quebec H2X 0A9
    Canada

    Active - Recruiting

  • GSK Investigational Site

    Helsinki, 00180
    Finland

    Active - Recruiting

  • GSK Investigational Site

    Tampere, 33520
    Finland

    Active - Recruiting

  • GSK Investigational Site

    Lyon, 69373
    France

    Active - Recruiting

  • GSK Investigational Site

    Saint-Herblain, 44805
    France

    Active - Recruiting

  • GSK Investigational Site

    Villejuif, 94805
    France

    Active - Recruiting

  • GSK Investigational Site

    Aviano PN, 33081
    Italy

    Active - Recruiting

  • GSK Investigational Site

    Milan, 20141
    Italy

    Active - Recruiting

  • GSK Investigational Site

    Naples, 80131
    Italy

    Active - Recruiting

  • GSK Investigational Site

    Roma, 00168
    Italy

    Active - Recruiting

  • GSK Investigational Site

    Saitama, 350-1298
    Japan

    Active - Recruiting

  • GSK Investigational Site

    Shizuoka, 411-8777
    Japan

    Active - Recruiting

  • GSK Investigational Site

    Tokyo, 135-8550
    Japan

    Active - Recruiting

  • GSK Investigational Site

    Gyeonggi-do, 10408
    Korea, Republic of

    Active - Recruiting

  • GSK Investigational Site

    Seoul, 03080
    Korea, Republic of

    Active - Recruiting

  • GSK Investigational Site

    Amsterdam, 1066 CX
    Netherlands

    Active - Recruiting

  • GSK Investigational Site

    Gyeonggi-do, 10408
    South Korea

    Active - Recruiting

  • GSK Investigational Site

    Seoul, 03722
    South Korea

    Active - Recruiting

  • GSK Investigational Site

    Barcelona, 08035
    Spain

    Active - Recruiting

  • GSK Investigational Site

    Córdoba, 14004
    Spain

    Active - Recruiting

  • GSK Investigational Site

    Girona, 17007
    Spain

    Active - Recruiting

  • GSK Investigational Site

    Madrid, 28046
    Spain

    Active - Recruiting

  • GSK Investigational Site

    Pozuelo de AlarcOn Madr, 28223
    Spain

    Active - Recruiting

  • GSK Investigational Site

    Stockholm, 17164
    Sweden

    Active - Recruiting

  • GSK Investigational Site

    Uppsala, SE-751 85
    Sweden

    Active - Recruiting

  • GSK Investigational Site

    Cambridge, CB2 0QQ
    United Kingdom

    Active - Recruiting

  • GSK Investigational Site

    London, W1G 6AD
    United Kingdom

    Active - Recruiting

  • GSK Investigational Site

    Birmingham, Alabama 35294
    United States

    Active - Recruiting

  • GSK Investigational Site

    Fountain Valley, California 92708
    United States

    Active - Recruiting

  • GSK Investigational Site

    Santa Rosa, California 95403
    United States

    Active - Recruiting

  • GSK Investigational Site

    Lake Mary, Florida 32746
    United States

    Completed

  • GSK Investigational Site

    Orlando, Florida 32827
    United States

    Active - Recruiting

  • GSK Investigational Site

    Fairway, Kansas 66205
    United States

    Active - Recruiting

  • GSK Investigational Site

    Boston, Massachusetts 02114
    United States

    Active - Recruiting

  • GSK Investigational Site

    Detroit, Michigan 48201
    United States

    Active - Recruiting

  • GSK Investigational Site

    Grand Rapids, Michigan 49546
    United States

    Active - Recruiting

  • GSK Investigational Site

    Minneapolis, Minnesota 55455
    United States

    Active - Recruiting

  • GSK Investigational Site

    Mineola, New York 11501
    United States

    Active - Recruiting

  • GSK Investigational Site

    New York, New York 10016
    United States

    Active - Recruiting

  • GSK Investigational Site

    Portland, Oregon 97213
    United States

    Active - Recruiting

  • GSK Investigational Site

    Nashville, Tennessee 37203
    United States

    Active - Recruiting

  • GSK Investigational Site

    Dallas, Texas 75230
    United States

    Active - Recruiting

  • GSK Investigational Site

    West Valley City, Utah 84119
    United States

    Active - Recruiting

  • GSK Investigational Site

    Seattle, Washington 98104
    United States

    Active - Recruiting

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