MedPath

A Study of TAK-981 Given With Rituximab in Adults With Relapsed or Refractory CD20-Positive Non-Hodgkin Lymphoma

Phase 1
Terminated
Conditions
Lymphoma, Non-Hodgkin
Interventions
Drug: TAK-981
Drug: Rituximab
Registration Number
NCT04074330
Lead Sponsor
Takeda
Brief Summary

This study is about a medicine called TAK-981 given with rituximab, used to treat adults with relapsed or refractory CD20-positive non-Hodgkin lymphoma.

This study has 2 parts.

The main aims of the study are:

* To check for side effects from treatment with TAK-981 given with rituximab.

* To check how much TAK-981 participants can tolerate.

* To check if participants with diffuse large B-cell lymphoma or follicular lymphoma respond well to treatment.

Participants will receive TAK-981 and rituximab in 21-day cycles. They will continue treatment for about 12 months unless their condition gets worse (disease progression), they cannot tolerate the treatment, or they leave the study for certain reasons.

Detailed Description

The drug being tested in this study is called TAK-981 in combination with rituximab. The study will include a dose escalation phase (Phase 1) and an expansion phase in select non-Hodgkin lymphoma (NHL) indications (Phase 2).

The study will enroll approximately 180 participants, approximately 35 participants in Phase 1 and approximately 145 participants in Phase 2. The participants with indolent or aggressive relapsed or refractory (r/r) NHL in Phase 1 will identify the maximum tolerated dose (MTD) and/or pharmacologically active dose (PAD). PAD can be defined retrospectively once MTD is reached and it can below MTD or coincide with it. In the dose escalation phase, the starting dose of TAK-981 will be 10 mg. The RP2D will be determined based on the available safety, preliminary pharmacokinetic (PK), pharmacodynamic information data, and after any early antitumor activity observed along with the statistical inference from the Bayesian logistic regression modeling (BLRM).

Participants in the Phase 2 will be enrolled once the Phase 1 of the study is completed, and MTD and/or PAD is determined. Phase 2 will explore the efficacy and safety of TAK-981 in combination with rituximab in participants with select NHL types and indications. Participants in Phase 2 will be enrolled in one of the three treatment arms based on Cohorts:

* Phase 2, Cohort A r/r DLBCL Progressed after CAR T-cell therapy:TAK-981+Rituximab

* Phase 2, Cohort B:r/r DLBCL;no CAR T-cell Therapy;2-3 Prior Lines: Two Dose Levels of TAK-981+Rituximab

* Phase 2, Cohort C:r/r FL;no CAR T-cell Therapy;2-3 Prior Lines: Two Dose Levels of TAK-981+Rituximab

This multi-center trial will be conducted worldwide. The overall time to participate in this study is approximately 72 months. Participants will make multiple visits to the clinic, and will attend the end of treatment (EOT) visit 30 days after receiving their last dose of drug or before the start of subsequent systemic anticancer therapy, whichever occurs first for a follow-up assessment.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
38
Inclusion Criteria

Each participant must meet all the following inclusion criteria to be enrolled in the study:

  1. Participant Population:

    o. For Phase 1 Dose Escalation: o. aNHL including mantle cell lymphoma and DLBCL histologies such as transformed DLBCL from low-grade lymphoma (follicular or others), DLBCL associated with small-cell infiltration in bone marrow, B-cell lymphoma with intermediate features between DLBCL and Burkitt's lymphoma or with intermediate features between DLBCL and Hodgkin lymphoma, FL grade 3B, and aggressive B-cell lymphoma unclassifiable who must have previously received rituximab, cyclophosphamide, doxorubicin (hydroxydaunorubicin), vincristine, (Oncovin) and prednisone (R-CHOP) (or equivalent anti-CD20 containing therapy) and 1 additional line of therapy in the r/r setting.

    o. iNHL (including FL of grades 1-3A and marginal zone lymphoma) refractory to rituximab or to any other anti-CD20 monoclonal antibodies, who have received at least 1 prior systemic therapy for r/r iNHL.

    o. Rituximab or anti-CD20 refractoriness is defined as failure to respond to, or progression during, any previous rituximab/anti-CD20-containing regimen (monotherapy or combined with chemotherapy), or progression within 6 months of the last rituximab or anti-CD20 dose.

    Note: The minimum qualifying rituximab/anti-CD20 dose is 1 full cycle (that is, weekly*4 doses monotherapy or 1 complete dose if combined with chemotherapy). Prior anti-CD20 antibody or cytotoxic drugs may have been administered as single agents or as components of combination therapies. Each repeated course of the same single-agent or combination is considered an independent regimen.

    o. For Phase 2, the following confirmed CD20+: o. r/r DLBCL progressed or relapsed after a prior CAR T-cells therapy that has received approval by a health authority for the treatment of DLBCL (Cohort A).

    o. r/r DLBCL that has progressed or relapsed after at least 2 but no more than 3 prior lines of systemic therapy and has not I prior cellular therapy. At least one prior line of therapy must have included a CD20-targeted therapy (Cohort B).

    o. r/r FL that has progressed or relapsed after at least 2 but no more than 3 prior lines of systemic therapy. At least 1 prior line of therapy must have included a CD20-targeted therapy (Cohort C).

  2. Must be considered ineligible in the opinion of the investigator, or refused autologous stem-cell transplantation (ASCT).

  3. Eastern Cooperative Oncology Group (ECOG) performance score of less than or equal to (<=) 2.

  4. Adequate bone marrow function per local laboratory reference range at screening as follows:

    o Platelet count greater than or equal to (>=) 75.0*10^9/L, Grade 2 thrombocytopenia (platelet count >=50.0*10^9 per liter [/L]) is allowed if it is clearly due to marrow involvement with no evidence of myelodysplastic syndrome or hypoplastic bone marrow if found. Absolute neutrophil count (ANC) >=1.0*10^9/L. Hemoglobin >=85 gram per liter (g/L) (red blood cell [RBC] transfusion allowed >=14 days before assessment).

  5. Adequate renal and hepatic function, per local laboratory reference range at screening as follows:

    • Calculated creatinine clearance >=30 milliliter per minute (mL/min) calculated with Cockcroft-Gault formula.
    • Potassium levels >=lower limit of normal (LLN). For potassium >upper limit of normal (ULN) discussion with Takeda medical monitor (MM)/designee recommended.
    • Aspartate aminotransferase and alanine aminotransferase <=3.0*the ULN of the institution's normal range; bilirubin <=1.5*ULN. Participants with Gilbert's syndrome may have a bilirubin level >1.5*ULN, per discussion between the investigator and the medical monitor.
  6. Left ventricular ejection fraction (LVEF) >=40 percent (%); as measured by echocardiogram or multiple gated acquisition (MUGA) scan.

  7. Suitable venous access for safe drug administration and the study-required PK and pharmacodynamic sampling.

  8. Have at least 1 bidimensionally measurable lesion per Lugano Classification by computed tomography (CT). Tumor lesions situated in a previously irradiated area are considered measurable if progression has been demonstrated in such lesions.

  9. Willing to consent to 1 mandatory pretreatment and 1 on-treatment skin biopsy during Phase 1. The skin biopsy entry requirement may be discontinued by the sponsor once there is enough pharmacodynamic evidence of target engagement.

  10. For participants enrolled in Phase 2, if available, mandatory submission of archival tumor tissue acquired ≤12 months prior to screening.

  11. Recovered to Grade 1, baseline or established as sequela, from all toxic effects of previous therapy (except alopecia, neuropathy, autoimmune endocrinopathies with stable endocrine replacement therapy, neurotoxicity [Grade 1 or 2 permitted], or bone marrow parameters [any of Grade 1, 2, permitted if directly related to bone marrow involvement]).

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Exclusion Criteria

Participants meeting any of the following exclusion criteria are not to be enrolled in the study:

  1. Central nervous system lymphoma; active brain or leptomeningeal metastases, as indicated by positive cytology from lumbar puncture or CT scan/magnetic resonance imaging (MRI).
  2. History of Grade >=3 infusion-related reaction (IRR) that lead to permanent discontinuation of previous rituximab treatment.
  3. Post transplantation lymphoproliferative disease except relapsed NHL after ASCT.
  4. Undergone ASCT or treatment with cellular therapy including CAR T within <=12 weeks of TAK-981 dosing.
  5. Prior allogeneic hematopoietic stem-cell transplantation.
  6. Lymphomas with leukemic expression.
  7. Prior anticancer therapy including chemotherapy, hormonal therapy, or investigational agents within 2 weeks or within at least 5 half-lives before TAK-981 dosing, whichever is shorter. Low dose steroids (oral prednisone or equivalent <=20 mg per day), hormonal therapy for prostate cancer or breast cancer (in adjuvant situation), and treatment with bisphosphonates and receptor activator of nuclear factor kappa-B ligand (RANKL) inhibitors are allowed.
  8. Major surgery within 14 days before the first dose of study drug and not recovered fully from any complications from surgery.
  9. Significant medical diseases or conditions, as assessed by the Investigators and sponsor that would substantially increase the risk-benefit ratio of participating in the study. This includes but is not limited to acute myocardial infarction or unstable angina within the last 6 months; uncontrolled diabetes mellitus; significant active bacterial, viral, or fungal infections; severely immunocompromised state; severe non-compensated hypertension and congestive heart failure New York Heart Association Class III or IV; ongoing symptomatic cardiac arrhythmias of >Grade 2, pulmonary embolism, or symptomatic cerebrovascular events; or any other serious cardiac condition (example, pericardial effusion or restrictive cardiomyopathy). Chronic atrial fibrillation on stable anticoagulant therapy is allowed.
  10. Known chronic hepatitis C and/or positive serology (unless due to vaccination or passive immunization due to immunoglobulin [Ig] therapy) for chronic hepatitis B. Known Human Immunodeficiency Virus (HIV) infection.
  11. Second malignancy within the previous 3 years, except treated basal cell or localized squamous skin carcinomas, localized prostate cancer, cervical carcinoma in situ, resected colorectal adenomatous polyps, breast cancer in situ, or other malignancy for which the participant is not on active anticancer therapy.
  12. Receipt of any live vaccine within 4 weeks of initiation of study treatment.
  13. Active, uncontrolled autoimmune disease requiring >20 mg of prednisone or equivalent, cytotoxics or biologicals.
  14. Corticosteroid use within 1 week before the first dose of study drug, except as indicated for other medical conditions such as inhaled steroid for asthma, topical steroid use, or as premedication for administration of study drug or contrast. Participants requiring steroids at daily doses >20 mg prednisone equivalent systemic exposure daily, or those who are administered steroids for lymphoma control or white blood cell count lowering are not eligible.
  15. With baseline prolongation of the QT interval with Fridericia correction method (QTcF) (example, >470 milliseconds (ms) for women and >450 ms for men and a history of congenital long QT syndrome, or torsades de pointes).
  16. Receiving or requiring the continued use of medications that are known to be strong or moderate inhibitors and inducers of Cytochrome P450 3A4/5 (CYP3A4/5) and strong P-glycoprotein (Pgp) inhibitors. To participate in this study, such participants should discontinue use of such agents for at least 2 weeks (1 week for CYP3A4/5 and Pgp inhibitors) before receiving a dose of TAK-981.
  17. Participants in Germany who are committed to an institution by virtue of an order issued either by judicial or administrative authorities as per German law.
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Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Phase 1: TAK-981 10mg QWTAK-981Participants with indolent or aggressive non-Hodgkin lymphoma (NHL) received TAK-981 10 mg, infusion, intravenously (IV), once weekly (QW) on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 milligram per square meter (mg/m\^2), infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or disease progression (PD) or unacceptable toxicity.
Phase 1: TAK-981 40mg QWTAK-981Participants with indolent or aggressive NHL received TAK-981 40 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: TAK-981 60mg QWTAK-981Participants with indolent or aggressive NHL received TAK-981 60 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: TAK-981 90mg QWTAK-981Participants with indolent or aggressive NHL received TAK-981 90 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: TAK-981 90mg BIWTAK-981Participants with indolent or aggressive NHL received TAK-981 90 mg, infusion, IV, BIW on Days 1, 4, 8, and 11 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: TAK-981 120mg QWTAK-981Participants with indolent or aggressive NHL received TAK-981 120 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: Japan Lead-in: TAK-981 60mg QWTAK-981Japanese participants with indolent or aggressive NHL received TAK-981 60 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: Japan Lead-in: TAK-981 60mg BIWTAK-981Japanese participants with indolent or aggressive NHL received TAK-981 60 mg, infusion, IV, BIW on Days 1, 4, 8, and 11 every 21 days in each 21-day treatment cycle for up to 12 months or PD or unacceptable toxicity.
Phase 2 (A): TAK-981 120 mgTAK-981Participants with relapsed or refractory (r/r) diffuse large B-cell lymphoma (DLBCL) received TAK-981 120 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab infusion, intravenously, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 2 (C): TAK-981 120 mgTAK-981Participants with follicular lymphoma (FL) received TAK-981 120 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab infusion, intravenously, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: TAK-981 10mg QWRituximabParticipants with indolent or aggressive non-Hodgkin lymphoma (NHL) received TAK-981 10 mg, infusion, intravenously (IV), once weekly (QW) on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 milligram per square meter (mg/m\^2), infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or disease progression (PD) or unacceptable toxicity.
Phase 1: TAK-981 40mg QWRituximabParticipants with indolent or aggressive NHL received TAK-981 40 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: TAK-981 60mg QWRituximabParticipants with indolent or aggressive NHL received TAK-981 60 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: TAK-981 90mg QWRituximabParticipants with indolent or aggressive NHL received TAK-981 90 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: TAK-981 90mg BIWRituximabParticipants with indolent or aggressive NHL received TAK-981 90 mg, infusion, IV, BIW on Days 1, 4, 8, and 11 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: TAK-981 120mg QWRituximabParticipants with indolent or aggressive NHL received TAK-981 120 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 1: Japan Lead-in: TAK-981 60mg QWRituximabJapanese participants with indolent or aggressive NHL received TAK-981 60 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab 375 mg/m\^2, infusion, IV, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 2 (A): TAK-981 120 mgRituximabParticipants with relapsed or refractory (r/r) diffuse large B-cell lymphoma (DLBCL) received TAK-981 120 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab infusion, intravenously, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Phase 2 (C): TAK-981 120 mgRituximabParticipants with follicular lymphoma (FL) received TAK-981 120 mg, infusion, IV, QW on Days 1 and 8 every 21 days in each 21-day treatment cycle in combination with rituximab infusion, intravenously, once on Days 1, 8, and 15 of Cycle 1 and then on Day 1 of each 21-day treatment cycle from Cycle 2 for up to 12 months or PD or unacceptable toxicity.
Primary Outcome Measures
NameTimeMethod
Phase 1: Number of Participants With Dose Limiting Toxicities (DLTs) Per Dose LevelUp to 42 months

DLTs were evaluated according to NCI CTCAE, Version 5.0.

Phase 2: Overall Response Rate (ORR)Up to 42 months

ORR was defined as the percentage of participants who achieved complete response (CR) and partial response (PR), as defined by the investigator according to Lugano classification for lymphomas during the study.

Phase 1: Number of Participants With One or More Treatment-Emergent Adverse Events (TEAEs)From the first dose of study drug through 30 days after the last dose of study drug (up to 42 months)

Adverse event (AE) means any untoward medical occurrence in a participant administered a pharmaceutical product. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product. A TEAE was defined as an adverse event which occurred on or after the first dose of study drug and no more than 30 days after the last dose of study drug.

Phase 1: Number of Participants With Grade 3 or Higher TEAEsFrom the first dose of study drug through 30 days after the last dose of study drug (up to 42 months)

AE means any untoward medical occurrence in a participant administered a pharmaceutical product. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product whether or not it is related to the medicinal product. A TEAE was defined as an adverse event which occurred on or after the first dose of study drug and no more than 30 days after the last dose of study drug. A severity grade was evaluated as per the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) Version 5.0, except for Cytokine Release Syndrome (CRS), which was assessed by American Society for Transplantation and Cellular Therapy (ASTCT) consensus grading criteria.

Phase 1: Duration of TEAEsFrom the first dose of study drug through 30 days after the last dose of study drug (up to 42 months)

AE means any untoward medical occurrence in a participant administered a pharmaceutical product. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product whether or not it is related to the medicinal product. A TEAE was defined as an adverse event which occurred on or after the first dose of study drug and no more than 30 days after the last dose of study drug. As per planned analysis, data for this outcome measure were collected and analyzed for the combined population (Phase 1: TAK-981 60mg QW+Japan Lead-in: TAK-981 60mg QW) based on regimen in which same dose groups in Phase 1 irrespective of nationality were pooled.

Secondary Outcome Measures
NameTimeMethod
Phase 1: Progression-Free Survival (PFS)Up to 42 months

PFS is defined as the time from the date of the first dose administration to the date of first documentation of PD or death due to any cause, whichever occurs first. PD was determined by Response Evaluation Criteria in Lymphoma. PFS was assessed by the investigator according to Lugano classification for lymphoma during the study.

Cmax: Maximum Observed Plasma Concentration for TAK-981Cycle 1: Days 1 and 8, pre-infusion and at multiple timepoints (Up to 24 hours) post end of infusion (cycle length=21 days)

As per planned analysis, data for this outcome measure were collected and analyzed for the combined population (Phase 1: TAK-981 60mg QW+Japan Lead-in: TAK-981 60mg QW) based on regimen in which same dose groups in Phase 1 irrespective of nationality were pooled. This outcome measure was planned to be analyzed for Phase 1 only.

Tmax: Time of First Occurrence of the Maximum Plasma Concentration (Cmax) for TAK-981Cycle 1: Days 1 and 8, pre-infusion and at multiple timepoints (Up to 24 hours) post end of infusion (cycle length=21 days)

As per planned analysis, data for this outcome measure were collected and analyzed for the combined population (Phase 1: TAK-981 60mg QW+Japan Lead-in: TAK-981 60mg QW) based on regimen in which same dose groups in Phase 1 irrespective of nationality were pooled. This outcome measure was planned to be analyzed for Phase 1 only.

Phase 1: Disease Control Rate (DCR)Up to 42 months

DCR is defined as the percentage of participants who achieved CR, PR, and stable disease (SD) as defined by the investigator according to Lugano classification for Lymphomas during the study.

Phase 1: Duration of Response (DOR)Up to 42 months

DOR is the time from the date of first documentation of a PR or better to the date of first documentation of PD for responders (PR or better). DOR was assessed by the investigator according to Lugano classification for lymphoma during the study.

Phase 1: Time to Progression (TTP)Up to 42 months

TTP is defined as the time from the date of first study drug administration to the date of first documented disease progression. TTP was assessed by the investigator according to Lugano classification for lymphoma during the study.

Phase 1: Fold Change From Baseline in Levels of TAK-981-Small Ubiquitin-like Modifier (TAK-981-SUMO) Adduct Formation in Blood as Assessed by Flow Cytometry During Phase 1Cycle 1 Day 1 (1 hour, 4 hours, 8 hours) and Day 8 (Pre-dose, 1 hour, 4 hours and 8 hours) (Cycle length = 21 days)

The level of TAK-981-SUMO adduct formation was evaluated as the percentage of adduct formed in blood. Positive change denotes improvement.

Phase 1: Levels of TAK-981-Small Ubiquitin-like Modifier (TAK-981-SUMO) Adduct Formation in Skin as Assessed by Immunohistochemistry (IHC) During Phase 1Cycle 1 Days 1 and 8 (Cycle length = 21 days)

The level of TAK-981-SUMO adduct formation was evaluated as the percentage of adduct formed in skin.

Phase 1: Fold Change From Baseline in SUMO Pathway Inhibition in Blood as Assessed by Flow Cytometry During Phase 1Cycle 1 Day 1 (1 hour, 4 hours, 8 hours) and Day 8 (Pre-dose, 1 hour, 4 hours and 8 hours) (Cycle length = 21 days)

SUMO pathway inhibition in blood was evaluated by flow cytometry with an antibody recognizing SUMO2/3 chains.

Phase 1: SUMO Pathway Inhibition in Skin as Assessed by Immunohistochemistry (IHC) During Phase 1Cycle 1 Days 1 and 8 (Cycle length = 21 days)

SUMO pathway inhibition in skin was evaluated with skin tissue biopsies by IHC.

Phase 2: Number of Participants With One or More Treatment-Emergent Adverse Events (TEAEs)From the first dose of study drug through 30 days after the last dose of study drug (up to 42 months)

Adverse event (AE) means any untoward medical occurrence in a participant administered a pharmaceutical product. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product. A TEAE was defined as an adverse event which occurred on or after the first dose of study drug and no more than 30 days after the last dose of study drug.

Phase 2: Number of Participants With Grade 3 or Higher TEAEsFrom the first dose of study drug through 30 days after the last dose of study drug (up to 42 months)

AE means any untoward medical occurrence in a participant administered a pharmaceutical product. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product whether or not it is related to the medicinal product. A TEAE was defined as an adverse event which occurred on or after the first dose of study drug and no more than 30 days after the last dose of study drug. A severity grade was evaluated as per the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) Version 5.0, except for Cytokine Release Syndrome (CRS), which was assessed by American Society for Transplantation and Cellular Therapy (ASTCT) consensus grading criteria.

Phase 2: Duration of TEAEsFrom the first dose of study drug through 30 days after the last dose of study drug (up to 42 months)

AE means any untoward medical occurrence in a participant administered a pharmaceutical product. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product whether or not it is related to the medicinal product. A TEAE was defined as an adverse event which occurred on or after the first dose of study drug and no more than 30 days after the last dose of study drug.

Phase 2: Disease Control Rate (DCR)Up to 42 months

CR is defined as the percentage of participants who achieved CR, PR, and SD as defined by the investigator according to Lugano classification for Lymphomas during the study.

Phase 2: Duration of Response (DOR)Up to 42 months

DOR is the time from the date of first documentation of a PR or better to the date of first documentation of PD for responders (PR or better). DOR was assessed by the investigator according to Lugano classification for lymphoma during the study.

AUC0-t: Area Under the Plasma Concentration-time Curve From Time 0 to Time t Over the Dosing Interval for TAK-981Cycle 1: Days 1 and 8, pre-infusion and at multiple timepoints (Up to 24 hours) post end of infusion (cycle length=21 days)

As per planned analysis, data for this outcome measure were collected and analyzed for the combined population (Phase 1: TAK-981 60mg QW+Japan Lead-in: TAK-981 60mg QW) based on regimen in which same dose groups in Phase 1 irrespective of nationality were pooled. This outcome measure was planned to be analyzed for Phase 1 only.

AUC0-∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-981Cycle 1: Days 1 and 8, pre-infusion and at multiple timepoints (Up to 24 hours) post end of infusion (cycle length=21 days)

As per planned analysis, data for this outcome measure were collected and analyzed for the combined population (Phase 1: TAK-981 60mg QW+Japan Lead-in: TAK-981 60mg QW) based on regimen in which same dose groups in Phase 1 irrespective of nationality were pooled. This outcome measure was planned to be analyzed for Phase 1 only.

t1/2z: Terminal Disposition Phase Half-life for TAK-981Cycle 1: Days 1 and 8, pre-infusion and at multiple timepoints (Up to 24 hours) post end of infusion (cycle length=21 days)

As per planned analysis, data for this outcome measure were collected and analyzed for the combined population (Phase 1: TAK-981 60mg QW+Japan Lead-in: TAK-981 60mg QW) based on regimen in which same dose groups in Phase 1 irrespective of nationality were pooled. This outcome measure was planned to be analyzed for Phase 1 only.

CL: Total Clearance After Intravenous Administration for TAK-981Cycle 1: Days 1 and 8, pre-infusion and at multiple timepoints (Up to 24 hours) post end of infusion (cycle length=21 days)

As per planned analysis, data for this outcome measure were collected and analyzed for the combined population (Phase 1: TAK-981 60mg QW+Japan Lead-in: TAK-981 60mg QW) based on regimen in which same dose groups in Phase 1 irrespective of nationality were pooled. This outcome measure was planned to be analyzed for Phase 1 only.

Vss: Volume of Distribution at Steady State After Intravenous Administration for TAK-981Cycle 1: Days 1 and 8, pre-infusion and at multiple timepoints (Up to 24 hours) post end of infusion (cycle length=21 days)

As per planned analysis, data for this outcome measure were collected and analyzed for the combined population (Phase 1: TAK-981 60mg QW+Japan Lead-in: TAK-981 60mg QW) based on regimen in which same dose groups in Phase 1 irrespective of nationality were pooled. This outcome measure was planned to be analyzed for Phase 1 only.

Phase 1: Overall Response Rate (ORR)Up to 42 months

ORR is defined as the percentage of participants who achieved CR and PR, as defined by the investigator according to Lugano classification for lymphomas during the study.

Phase 2: Time to Progression (TTP)Up to 42 months

TTP is defined as the time from the date of first study drug administration to the date of first documented disease progression. TTP was assessed by the investigator according to Lugano classification for lymphoma during the study.

Phase 2: Progression-Free Survival (PFS)Up to 42 months

PFS is defined as the time from the date of the first dose administration to the date of first documentation of PD or death due to any cause, whichever occurs first. PD was determined by Response Evaluation Criteria in Lymphoma. PFS was assessed by the investigator according to Lugano classification for lymphoma during the study.

Trial Locations

Locations (59)

East Carolina University

🇺🇸

Greenville, North Carolina, United States

Ohio State University Wexner Medical Center

🇺🇸

Columbus, Ohio, United States

University Hospitals Cleveland Medical Center

🇺🇸

Cleveland, Ohio, United States

Derriford Hospital

🇬🇧

Plymouth, Devon, United Kingdom

Texas Oncology (Medical City) - USOR

🇺🇸

Dallas, Texas, United States

Western Pennsylvania Hospital

🇺🇸

Pittsburgh, Pennsylvania, United States

Oxford University Hospitals NHS Trust

🇬🇧

Oxford, Oxfordshire, United Kingdom

Azienda Ospedaliera Cardinale G Panico

🇮🇹

Tricase, Puglia, Italy

Hospital Universitario La Paz - PPDS

🇪🇸

Madrid, Spain

Royal Marsden Hospital - Downs Road

🇬🇧

London, London, City Of, United Kingdom

Charite - Universitatsmedizin Berlin

🇩🇪

Berlin, Germany

Hospital de La Santa Creu i Sant Pau

🇪🇸

Barcelona, Spain

Hotel Dieu - Nantes

🇫🇷

Nantes, Loire-Atlantique, France

The Cancer Institute Hospital of Japanese Foundation For Cancer Research

🇯🇵

Koto-Ku, Tokyo, Japan

Levine Cancer Institute - Charlotte

🇺🇸

Chapel Hill, North Carolina, United States

National Hospital Organization Nagoya Medical Center

🇯🇵

Nagoya-Shi, Aiti, Japan

Centre Hospitalier de l'Universite de Montreal

🇨🇦

Montreal, Quebec, Canada

University Hospital Birmingham

🇬🇧

Birmingham, United Kingdom

A.O.U. Maggiore della Carita

🇮🇹

Novara, Piemonte, Italy

Fondazione IRCCS Policlinico San Matteo di Pavia

🇮🇹

Pavia, Italy

Fondazione IRCCS Ca Granda Ospedale Maggiore Policlinico

🇮🇹

Milano, Lombardia, Italy

Istituto Nazionale Dei Tumori

🇮🇹

Milano, Lombardia, Italy

Hopital Francois Mitterand

🇫🇷

Dijon, Cote-d'Or, France

Universitatsklinikum Essen

🇩🇪

Essen, Nordrhein-Westfalen, Germany

National Cancer Center Hospital East

🇯🇵

Kashiwa, Tiba, Japan

CHU Montpellier - Hopital St Eloi

🇫🇷

Montpellier, Herault, France

Institut Paoli Calmettes

🇫🇷

Marseille, Bouches-du-Rhone, France

Azienda Ospedaliera San Camillo Forlanini

🇮🇹

Roma, Lazio, Italy

Hopital Saint Antoine

🇫🇷

Paris, France

Complejo Asistencial Universitario de Salamanca H. Clinico

🇪🇸

Salamanca, Spain

Hospital del Mar

🇪🇸

Barcelona, Spain

National University Corporation Tohoku University Tohoku University Hospital

🇯🇵

Sendai-Shi, Miyagi, Japan

Universitatsklinikum Wurzburg

🇩🇪

Wurzburg, Bayern, Germany

Universitatsklinikum Leipzig

🇩🇪

Leipzig, Sachsen, Germany

University College London

🇬🇧

London, London, City Of, United Kingdom

Sir Mortimer B Davis Jewish General Hospital

🇨🇦

Pointe-Claire, Quebec, Canada

Hopital Universitaire Pitie Salpetriere

🇫🇷

Paris, France

Azienda Ospedaliera Citta della Salute e della Scienza di Torino

🇮🇹

Torino, Piemonte, Italy

Klinikum rechts der Isa der Technischen Universitaet Muenchen

🇩🇪

Munchen, Bayern, Germany

Hospital Universitario Ramon y Cajal

🇪🇸

Madrid, Spain

Beatson West of Scotland Cancer Centre - PPDS

🇬🇧

Glasgow, Lanarkshire, United Kingdom

Beijing Cancer Hospital

🇨🇳

Beijing, Beijing, China

Shanghai East Hospital

🇨🇳

Shanghai, Shanghai, China

University of Alabama at Birmingham

🇺🇸

Birmingham, Alabama, United States

Mayo Clinic - Cancer Center - Rochester - PPDS

🇺🇸

Rochester, Minnesota, United States

University of Cincinnati

🇺🇸

Cincinnati, Ohio, United States

City of Hope - Comprehensive Cancer Center (CCC)

🇺🇸

Portland, Oregon, United States

Hospital Universitario Virgen del Rocio - PPDS

🇪🇸

Sevilla, Spain

Otto-von-Guericke-Universitat Magdeburg

🇩🇪

Magdeburg, Sachsen-Anhalt, Germany

University of Michigan Comprehensive Cancer Center

🇺🇸

Ann Arbor, Michigan, United States

Texas Oncology (Tyler) - USOR

🇺🇸

Tyler, Texas, United States

Centre Henri Becquerel

🇫🇷

Rouen, Seine-Maritime, France

Universitatsklinikum Tubingen

🇩🇪

Tubingen, Baden-Wurttemberg, Germany

Azienda Sanitaria Locale di Ravenna

🇮🇹

Ravenna, Emilia-Romagna, Italy

Universitatsklinikum Freiburg

🇩🇪

Freiburg, Baden-Wurttemberg, Germany

ASST Grande Ospedale Metropolitano Niguarda - Presidio Ospedaliero Ospedale Niguarda

🇮🇹

Milano, Lombardia, Italy

Kindai University Hospital

🇯🇵

Osakasayama-Shi, Osaka, Japan

Hospital Clinic de Barcelona

🇪🇸

Barcelona, Spain

Hopital Prive Sevigne

🇫🇷

Rennes, Ille-et-Vilaine, France

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