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Study of the Safety, Pharmacokinetics and Efficacy of Tinostamustine in Patients With Advanced Solid Tumors.

Registration Number
NCT03345485
Lead Sponsor
Mundipharma Research Limited
Brief Summary

Tinostamustine (EDO-S101) is a first-in-class alkylating deacetylase inhibitor designed to improve drug access to deoxyribonucleic acid (DNA) strands, induce DNA damage and counteract its repair in cancer cells. The main purpose of this study is to assess the safety, tolerability and efficacy of Tinostamustine in subjects with advanced solid tumours. Subjects will be given Tinostamustine via intravenous infusion on Days 1 and 15 of a 4-week cycle, the dose and infusion time will vary depending on the phase of the study.

Detailed Description

The study consists of 2 phases and 2 sub-studies:

This study is a multi-centre, open-label phase 1/2 study of single agent EDO-S101 in subjects with advanced solid tumours.

Phase 1 part of the study is designed to determine the safety, tolerability, maximum tolerated dose (MTD), recommended phase 2 dose (RP2D) and the Pharmacokinetic (PK) of EDO-S101 as a single agent in patients with solid tumours who have progressed after at least one (1) line of therapy and for whom no other standard therapy with proven clinical benefit is available.

Phase 2 part of the study is designed to evaluate the overall response rate (ORR) of the RP2D, plus the rate of patients with stable disease (SD) at 4 or 6 months, depending on the type of solid tumour. The RP2D was determined after phase 1 to be 80 mg/m2 of EDO-S101 administered over 1 hour on Day 1 and Day 15 of each 4-week treatment cycle.

In addition, two sub-studies are designed to better characterize the effect of EDO-S101: one at a dose of 60 mg/m2 administered over 60 minutes and the second at a dose of 80 mg/m2 administered over 80 minutes on cardiac repolarization (QTc) and other ECG parameters in the subjects with solid tumours.

Subjects were eligible for these studies if they had a histologically confirmed solid tumour, signed informed consent and met the inclusion/exclusion criteria. After providing informed consent, subjects were screened, and all procedures were performed as per protocol.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
71
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Tinostamustine (EDO-S101) - Phase 1 - 80mg/m2 (60 min) cohort 5Tinostamustine 80mg/m2 over 60min-
Tinostamustine (EDO-S101) - Phase 1 - 100mg/m2 (30 min) cohort 3Tinostamustine 100mg/m2 over 30min-
Tinostamustine (EDO-S101) - Phase 1 - 60mg/m2 (60 min) cohort 4Tinostamustine 60mg/m2 over 60min-
Tinostamustine (EDO-S101) - Phase 1 - 60mg/m2 (30 min) cohort 1Tinostamustine 60mg/m2 over 30min-
Tinostamustine (EDO-S101) - Phase 1 - 100mg/m2 (60 min) cohort 6Tinostamustine 100mg/m2 over 60min-
Tinostamustine (EDO-S101) - Phase 1 - 80mg/m2 (30 min) cohort 2Tinostamustine 80mg/m2 over 30min-
Tinostamustine (EDO-S101) - Phase 2 Relapsed/refractory Small Cell Lung Cancer (SCLC) cohortTinostamustine 80mg/m2 over 60min-
Tinostamustine (EDO-S101) - Phase 2 Relapsed/refractory Soft Tissue Sarcoma (STS) cohortTinostamustine 80mg/m2 over 60min-
Tinostamustine (EDO-S101) - Phase 2 Relapsed/refractory Triple Negative breast Cancer (TNBC) cohortTinostamustine 80mg/m2 over 60min-
Tinostamustine (EDO-S101) - Phase 2 Relapsed/refractory Ovarian Cancer (OC) cohortTinostamustine 80mg/m2 over 60min-
Tinostamustine (EDO-S101) - Phase 2 Relapsed/refractory Endometrial Cancer (EC) cohortTinostamustine 80mg/m2 over 60min-
Tinostamustine (EDO-S101) - Sub study 1 (SS1)Tinostamustine 60mg/m2 over 60min-
Tinostamustine (EDO-S101) - Sub study 2 (SS2)Tinostamustine 80mg/m2 over 80min-
Primary Outcome Measures
NameTimeMethod
Number of Participants With Treatment-related Adverse Events as Assessed by CTCAE V4.03 on Phase 1From each patient's time of first dose administration to discontinuation of study drug (at any time or D28 of the last treatment cycle), up to 6 months.

All TEAEs was reported from the first dose of study drug through the time of study drug discontinuation (at any time or Day 28 of the last treatment Cycle). All treatment-related TEAEs was followed until resolution or stabilization. For the purpose of regulatory reporting requirements, causal relationships of definite, probable, and possible was considered treatment-related.

Number of patients experiencing treatment-related adverse events (TEAE) as assessed by CTCAE v4.03. (June 2010).

Clinical Benefit Response Rate in Selected Solid Tumor Cohorts on Phase 2From start treatment and assessed after every 2 cycles until determination of stable disease and follow up for up to 84 days.

The Clinical Benefit Response Rate is calculated as the number of patients with Clinical Benefit Response divided by number of patients in the FAS (in the respective cohort). Clinical Benefit Response is defined as patients achieving stable disease with a duration of at least 12 weeks (84 days).

Summary subjects analysed were 36.

Highest Change From Baseline in QTcF in Sub-studiesFrom cycle 1 and at every cycle on treatment days D1 and D15, assessed pre-dose and post-start of infusion at 30 and 80mins (Substudy 2 - up to 6 months) and 30, 60, 90, 120 and 180mins (substudy 1 - up to 6 months).

QTcF: corrected QT interval \[QTc\] using Fridericia's formula) and other electrocardiogram (ECG) parameters in subjects with solid tumours who have progressed after at least 1 line of therapy and for whom no other standard therapy with proven clinical benefit is available.

Within each cycle a Change from baseline (CfB) is calculated for QTcF relative to the baseline value of day 1 of the cycle. QTcF CfB= QTcF Post-dose value - QTcF pre-dose value of D1 ECG Parameters: 4-hours ECG holter monitoring in C1 and ECGs during EDO-S101 administration.

Continuous variables the mean and standard deviation are presented together with the total number of observations and the number of missing and non-missing values.

Secondary Outcome Measures
NameTimeMethod
Treatment-related Adverse Events on Phase 2 and Sub StudiesFrom each patient's time of informed consent to discontinuation of study drug (at any time or D28 of the last treatment cycle), up to 8 months

Number of patients experiencing treatment-related adverse events (TEAE) as assessed by CTCAE v4.03, June 2010, with the exception that assessment of QTc prolongations constituting adverse events (AEs) of special interest were based on NCI CTCAE version 5.0, November 2017.

All subjects who received at least 1 dose of study treatment were included in the Safety Population. Safety analyses were performed on data from all subjects in the Safety Population.

Adverse events are reported on a patient basis. The percentages are calculated using the number of patients in the Safety Analysis Set as the denominator.

Progression Free Survival (PFS) Time for Phase 2 and Sub StudiesFrom patient's first dose until first documented progression/start of subsequent anti-cancer therapy/death from any cause, whichever came first, up to 26 months.

PFS was defined as the number of days between the date of the first dose of treatment of a patient and the first date of disease progression, start of a subsequent anti-cancer therapy, or death of the patient.

Overall Survival (OS) Time for Phase 2 and Sub StudiesFrom patient's first dose until first documented progression/start of subsequent anti-cancer therapy/death from any cause, whichever came first, up to 42 months.

Overall survival is defined as the number days between the date of the first dose of treatment and the date of death. If no date of death is recorded the Overall Survival time is censored at the Last available visit date.

Phase 2: To determine the overall survival (OS) time for subjects with solid tumours.

SS1:To determine the overall survival (OS) time for subjects who received 60 mg/m2 of EDO-S101 during a 60-minute Infusion.

SS2: To determine the overall survival (OS) time for subjects who received 80 mg/m2 of EDO-S101 during a 80-minute Infusion.

Maximum Duration of Response (DoR) Time for Phase 2 and Sub StudiesFrom patient's first overall response of CR or PR, until disease progression/subsequent anti-cancer therapy/death from any cause, up to 24 months.

The duration of objective response is measured from the date of the first tumor response assessment with an Investigator's Overall Response of CR or PR (whichever status is recorded first) until the date of progression or death. DoR is presented by subject.

Objective Response Rate (ORR) and the Clinical Benefit Rate (CBR) That Persists for at Least Four (4) Months in Selected Solid Tumor Cohorts on Sub StudiesFrom start of treatment, assessed every 2 cycles, until first documented complete CR, PR or SD, up to 6 months. If SD, assessment continued every 2 cycles until CR/PR/death (up to 6 months)

To determine the objective response rate (ORR) and the clinical benefit rate (CBR \[Complete Response (CR), Partial Response (PR) plus durable Stable Disease (SD)\]) in Sub Studies.

SD was regarded as durable if, after observing SD, the first observation of PD was at least 84 days after the start of study treatment.

Number of Participants With Duration of Stable Disease (SD) That Persists for at Least 4 Months in Selected Solid Tumor Cohorts in Sub Studies.From start of treatment, assessed every 2 cycles, until first documented complete CR, PR or SD, up to 6 months. If SD, assessment continued every 2 cycles until CR/PR/death (up to 6 months).

Duration of SD, was defined as the number of days between the date of the first dose of treatment and the first date of disease progression or death.

SD was regarded as durable if, after observing SD, the first observation of progression disease was at least 84 days after the start of study treatment.

Maximum Plasma Concentration (Cmax) in Phase 2 and Sub StudiesBlood samples were collected over a period of 24hr (phase 2 and sub-study 1) and 30hr (sub-study 2) on Cycle 1 Day 1 and Day 15.
Area Under the Curve [AUC(0-t)] in Phase 2 and Sub Studies.Blood samples were collected over a period of 24hr (phase 2 and sub-study 1) and 30hr (sub-study 2) on Cycle 1 Day 1 and Day 15.
Summary of Tmax in in Phase 2 and Sub Studies.Blood samples were collected over a period of 24hr (phase 2 and sub-study 1) and 30hr (sub-study 2) on Cycle 1 Day 1 and Day 15.
Clearance of Tinostamustine and Metabolites in Phase 2 and SubstudiesBlood samples were collected over a period of 24hr (phase 2 and sub-study 1) and 30hr (sub-study 2) on Cycle 1 Day 1 and Day 15.
Summary of Half-life of Tinostamustine in Phase 2 and Substudies.Blood samples were collected over a period of 24hr (phase 2 and sub-study 1) and 30hr (sub-study 2) on Cycle 1 Day 1 and Day 15.

Trial Locations

Locations (13)

New York University

🇺🇸

New York, New York, United States

Juravinski Cancer Centre

🇨🇦

Hamilton, Ontario, ON, Canada

BC Cancer-Vancouver

🇨🇦

Vancouver, Vancouver, BC, Canada

Fondazione IRCCS Istituto Nazionale dei Tumori

🇮🇹

Milan, Italy

Istituto Europeo di Oncologia

🇮🇹

Milan, Italy

Erasmus MC Kanker Instituut

🇳🇱

Rotterdam, Netherlands

Hospital Universitario La Paz

🇪🇸

Madrid, Fuencarral-El Pardo, Spain

Hospital Universitari Vall d'Hebron

🇪🇸

Barcelona, Horta-Guinardó, Spain

Cedars-Sinai Medical Center

🇺🇸

Los Angeles, California, United States

Stanford University Medical Center

🇺🇸

Palo Alto, California, United States

University of Michigan

🇺🇸

Ann Arbor, Michigan, United States

Mary Crowley Cancer Research

🇺🇸

Dallas, Texas, United States

McGill University

🇨🇦

Montréal, Quebec, Canada

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