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A Clinical Safety and Efficacy Study of Mebendazole on GI Cancer or Cancer of Unknown Origin.

Phase 1
Terminated
Conditions
Cancer of the Gastrointestinal Tract
Cancer of Unknown Origin
Interventions
Drug: ReposMBZ
Registration Number
NCT03628079
Lead Sponsor
Repos Pharma
Brief Summary

This study will evaluate the safety and efficacy of mebendazole (ReposMBZ) in patient with advanced gastrointestinal cancer or cancer of unknown origin. All patients will be given ReposMBZ for 16 weeks continuous treatment, individually dosed based on the serum concentration of mebendazole.

Detailed Description

Mebendazole has been used extensively during long time for local gut helminthic infections at low dose but also at considerably higher doses during months to years against invasive echinococcus infections. Recent research has now clearly indicated that mebendazole has anticancer effect. Given these observations and the experience of excellent tolerance to mebendazole the current clinical trial protocol is based on the repositioning strategy to more extensively investigate whether mebendazole could be developed into a useful anticancer drug.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
11
Inclusion Criteria
  1. At least 18 years of age.

  2. Histologically confirmed diagnosis of squamous cell cancer or adenocarcinoma, including primary cancer of the liver, of the gastrointestinal tract or cancer of unknown origin.

  3. Measurable disease according to RECIST 1.1.

  4. Defined time to tumour progression on the standard/experimental treatment preceding the trial treatment.

  5. Locally advanced or metastatic disease not amenable to standard treatment, i.e. progress on standard therapy or observed/expected intolerance to standard therapy.

    • (removed via Amendment 1)
  6. Pharmacological treatment attempt considered reasonable.

  7. Females of childbearing potential should use adequate contraception throughout the study;

    1. Combined (estrogen and progestogen containing) hormonal contraception associated with inhibition of ovulation (oral, intravaginal or transdermal)
    2. Progestogen-only hormonal contraception associated with inhibition of ovulation (oral, injectable or implantable)
    3. Intrauterine device (IUD)
    4. Intrauterine hormone-releasing system (IUS)
    5. Bilateral tubal occlusion
    6. Vasectomized partner
    7. Sexual abstinence
  8. Signed informed consent.

Exclusion Criteria
  1. Anti-tumour therapy within 3 weeks prior to study drug administration day

  2. Ongoing infection or other major recent or ongoing disease that, according to the investigator, poses an unacceptable risk to the patient.

  3. WHO performance status ≥ 2.

  4. Child-Pugh B or C liver function status if hepatocellular carcinoma.

  5. Inadequate laboratory parameters reflecting major organ function i.e.:

    1. neutrophils ≤ 1,3 x 109/l
    2. platelets ≤ 100 x 109/l
    3. bilirubin > 1.5 x upper limit of normal (ULN)
    4. Alanine aminotransferase (ALAT) > 5 x ULN
    5. Glomerular filtration rate (GFR) <50 ml/min (calculated from P-creatinine)
    6. Prothrombin complex/INR outside normal range
  6. Current active participation in any other interventional clinical study.

  7. Contraindications to the investigational product, e.g. known or suspected hypersensitivity or inability to oral drug administration.

  8. Pregnancy or lactation.

  9. Lack of suitability for participation in the study, e g expected difficulties to follow the protocol procedures, as judged by the Investigator.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Single arm studyReposMBZReposMBZ 100 mg capsule by mouth followed by 8h PK sampling to decide the initial daily dose. Treatment: Repos MBZ capsules by mouth twice daily for 16 weeks, daily dose 50mg-4g, based on the serum level of mebendazole.
Primary Outcome Measures
NameTimeMethod
Changes in body temperature over time.From date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Body temperature (Celsius degrees)

Incidence of adverse events (AEs) probably or possibly related to ReposMBZFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

AEs graded according to CTCAE 4.03.

Changes in plasma Albumin over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Blood Chemistry (plasma): Albumin (g/L)

Changes in plasma Sodium, Potassium, Calcium and Glucose over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Blood chemistry (plasma): Sodium, Potassium, Calcium, Glucose (mmol/L)

Changes in red, white and platelet blood cell count over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Haematology: RBC (red blood cell count), White blood cells with differential count and platelets (absolute count/L)

Tumour response: CT/MRI assessed according to RECIST 1.1From date of first dose ReposMBZ until the date of first documented progression or date of death from any cause, whichever comes first, assessed up to 24 months (end of study).

Best overall radiological response Time to tumour progression (TTP) compared with TTP on the treatment just preceding this protocol.

Changes in C-reactive protein (CRP) over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Blood chemistry (plasma): CRP (mg/L)

Changes in plasma Bilirubin over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Blood chemistry (plasma): Bilirubin (µmol/L)

Changes in plasma ALAT (alanine aminotransferase), ASAT (aspartate aminotransferase), LDH (lactate dehydrogenase), ALP (alkaline phosphatase) over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Blood chemistry (plasma): ALAT, ASAT, LDH, ALP (µkat/L)

Changes in Haemoglobin over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Haematology: Haemoglobin (g/L)

Changes in Activated Partial Thromboplastin Time (APTT) over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Coagulation (plasma): APTT (s)

Changes in blood pressure over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Systolic and diastolic blood pressure (mmHg) Weight (kg)

Changes in Prothrombin complex (PK/INR) over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Coagulation (plasma): Prothrombin complex (INR)

Changes in heart rate over timeFrom date of first dose, up to 30 days after last dose of ReposMBZ or start of new treatment, whatever comes first, assessed up to 20 weeks after start of treatment phase.

Supine heart rate (beats per minute)

Secondary Outcome Measures
NameTimeMethod
Change in tumour load and TTP according to irRECISTFrom date of first dose ReposMBZ until the date of first documented progression or date of death from any cause, whichever comes first, assessed up to 24 months (end of study).

Best over all radiological response according to irRECIST 1.1.

Area under the serum concentration versus time curve (AUC) for ReposMBZPre-dose, 30 minutes, 60 minutes, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours.

Analysis of serum concentration after single dose administration of ReposMBZ.

The Cmax serum concentration of ReposMBZ after repeated dose administration.Pre-dose, 30 minutes, 60 minutes, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours (only up to the time point for Cmax after single dose), assessed up to 16 weeks after start of treatment phase.

Cmax will be used to adjust the dose until target S-mebendazole level is reached and to show the individual variation of S-mebendazole concentration over time

The peak serum concentration (Cmax) of ReposMBZ after single dose administration.Pre-dose, 30 minutes, 60 minutes, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours.

Cmax will be used to decide the starting dose in the treatment phase.

Target S-mebendazole concentration after repeated dose administration.From first dose in treatment phase and assessed up to 16 weeks after start of treatment phase.

Number of patients that reach the steady state S-mebendazole target concentration.

Time to reach the steady state S-mebendazole target concentration after repeated dose administration..From first dose in treatment phase and assessed up to 16 weeks after start of treatment phase.

Time from first dose in treatment phase until target S-mebendazole concentration is reached

Systemic immune activation.From baseline up to 20 weeks after start of treatment phase, assessed up to 24 months (end of study).

Change of cytokine levels in blood, evaluated by cytokine array.

Immune cell activation.From baseline and up to 20 weeks after start of treatment phase, assessed up to 24 months (end of study).

Up-regulation of activation markers compared to baseline, evaluated by flow cytometry.

Overall survival.From date of first dose ReposMBZ to date of death, assessed up to 24 months (end of study).

Months of survival from first dose until death of any cause.

Trial Locations

Locations (1)

Dept of oncology, University Hospital

🇸🇪

Uppsala, Sweden

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