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The Effect Of NS-0200 Versus Placebo On Hepatic Fat Content In Patients With Non Alcoholic Fatty Liver Disease

N

NuSirt Biopharma

Status and phase

Completed
Phase 2

Conditions

NAFLD

Treatments

Drug: Placebo
Drug: Leu-Met-Sil 1.0
Drug: Leu-Met-Sil 0.5

Study type

Interventional

Funder types

Industry

Identifiers

NCT02546609
NS-0200-01

Details and patient eligibility

About

The goal of this study is to determine if NS-0200 can reduce the amount of liver fat in patients diagnosed with non-alcoholic fatty liver disease (NAFLD). This study will compare two doses of NS-0200 to placebo in NAFLD patients.

Full description

This is a randomized, 16-week, placebo-controlled, double-blind study to evaluate the effect of two fixed-dose combinations of leucine, metformin and sildenafil, NS-0200 compared to placebo, on the reduction of liver fat in patients diagnosed with non-alcoholic fatty liver disease (NAFLD). Subjects meeting all the inclusion criteria and no exclusion criteria will be randomized to one of three study arms.

The primary objective of this study is to evaluate the change in hepatic fat content assessed by proton-density-fat-fraction (PDFF) employing magnetic resonance imaging (MRI) in subjects from : Screening/Visit 2 (Day-7/Week-1) to Study Termination/Visit 8 (Day 112/Week 16) receiving two fixed-dose combinations of leucine, metformin and sildenafil compared to placebo. Secondary objectives will also assess changes in serum alanine aminotransferase (ALT) activity, change in circulating cytokeratin 18, a surrogate marker of necro-inflammation, change in HbA1c, change in fasting glucose, insulin and insulin sensitivity, change in blood lipids such as cholesterol, LDL, HDL, triglycerides, and changes in in C-reactive protein. In addition this study will evaluate the safety and tolerability of NS-0200.

Patients will have two screening visits, the first to determine their eligibility based on lab tests and the second based on the percentage of hepatic fat assessed by MRI imaging. Once qualified, patients will be randomly assigned to either one of the treatment groups or the placebo control group and monitored for a total of 16 weeks. Patients will return to the clinic each month for lab tests, and routine examinations. At the conclusion of the treatment period patients will again undergo an MRI scan to examine the percentage of hepatic fat.

Enrollment

91 patients

Sex

All

Ages

18 to 75 years old

Volunteers

No Healthy Volunteers

Inclusion criteria

  1. Age 18-75 at study entry.

  2. Is male, or female and, if female, meets all of the following criteria:

    1. Not breastfeeding
    2. Post-menopausal or negative serum pregnancy test result (human chorionic gonadotropin, beta subunit [β-hCG]) at Screening /Visit 1 (Day-14/Week-2) (not required for hysterectomized females)
    3. If of childbearing potential (including peri-menopausal women who have had a menstrual period within one year) must practice and be willing to continue to practice appropriate birth control (defined as a method which results in a low failure rate, i.e., less than 1% per year, when used consistently and correctly, such as double barrier methods [male condom with spermicide, with or without cervical cap or diaphragm], implants, injectables, oral contraceptives [must have been using for at least the last 3 months], some intrauterine contraceptive devices, tubal ligation, or in an established relationship with a vasectomized partner) during the entire duration of the study.
  3. Has been diagnosed with NAFLD via CT (positive for excess liver fat), ultrasound (positive for excess liver fat), MRI (PDFF showing > 15% liver fat) or via biopsy (showing >33% fat) within the past six months. If diagnosis was between 3 and 6 months prior to Screening, an ultrasound (positive for excess liver fat) is required prior to the Screening /Visit 1 (Day-14/Week-2) MRI.

  4. Has liver fat (as measured by PDFF via MRI) greater than 15% at Screening/Visit 2 (Day-7/Week-1)

  5. Has had ALT levels >30 U/L for men, >19 U/L for women measured within 8 weeks of enrollment

  6. Has an HbA1c equal to or less than 9% at Screening /Visit 1 (Day-14/Week-2)

  7. Has a BMI between 25kg/m2 and 40 kg/m2

  8. Otherwise stable health for preceding twelve weeks

  9. Clinical laboratory tests (hematology, clinical chemistry, and urinalysis) either normal or with abnormalities consistent with NAFLD.

  10. Is able to read, understand, and sign the informed consent forms (ICF) and, when applicable, an authorization to use and disclose protected health information form (consistent with Health Insurance Portability and Accountability Act of 1996 [HIPAA] legislation), communicate with the investigator, and understand and comply with protocol requirements.

Exclusion criteria

  1. Clinically significant renal dysfunction defined as a serum creatinine concentration >1.4 mg/dL (females) or >1.6 mg/dL (males) or a blood urea nitrogen concentration >45 mg/dL at screening.

  2. Use of any of the following medications:

    1. Metformin

    2. Combination drugs that include Metformin

    3. Sildenafil

    4. Tadalafil

    5. Vardenafil

    6. Pioglitazone

    7. Rosiglitazone

    8. Short acting insulins

    9. An alpha blocker

    10. Oral nitrates

    11. Medications associated with increased hepatic steatosis

    12. Insulins

    13. OCT2/MATE inhibitors (e.g. cimetidine, quinidine, and pyrimethamine)

      • Methotrexate
      • Tamoxifen
      • Corticosteroids (Nasal steroids are allowed if the subject has been on a stable dose for the past 12 weeks and the dose employed does not exceed the maximal recommended dose.)
      • Estrogens
      • Amiodarone
      • Valproic acid
      • Coumadin
      • Isoniazide
      • Nucleoside analogues used for the treatment of HIV infections
    14. Any dietary supplement other than multi-vitamins

  3. Evidence of significant alcohol consumption (defined as >7 drinks/week for females and >14 drinks/week for males) within 6 months prior to randomization or presence or suspicion of other forms of chronic liver disease (e.g., cirrhosis, autoimmune hepatitis (>1:160 ANA), Wilson's disease, Hemochromatosis (Ferritin >1000 ug/L and percent iron saturation >45%), hepatitis A, B or C)

  4. Has a clinically significant medical condition that could potentially affect study participation and/or personal well-being, as judged by the investigator, including but not limited to the following conditions:

    1. Unable to undergo MRI or contraindications for MRI procedure
    2. History of cardio- or cerebro-vascular disease event within the previous 6 months
    3. Requires anti-coagulation therapy
    4. Gastrointestinal disorders including, but not limited to, the following: pancreatitis, inflammatory bowel disease, or other diseases associated with malabsorption or persistent abdominal discomfort
    5. Endocrine disorders other than type 2 diabetes and hypothyroidism on stable replacement therapy
    6. Chronic infection (e.g., tuberculosis, human immunodeficiency virus infection, hepatitis A virus, hepatitis B virus, or hepatitis C virus)
    7. Neurological or psychiatric diseases that preclude valid execution of informed consent or may interfere with the subject's compliance with study procedures (e.g., major depressive disorder within the last 2 years, a history of suicidal behavior in the last 3 months)
    8. History of other psychiatric disorders including schizophrenia and bipolar disorder)
  5. Participation in a weight loss program within the past 3 months.

  6. Weight change ≥5% during the past month.

  7. History of substance abuse (including alcohol abuse as defined above) in the past 3 months or a positive screen for drugs of abuse or alcohol at screening.

  8. Has received any investigational drug within 3 months of Screening.

  9. Has donated blood within 3 months before Screening or is planning to donate blood during the study.

  10. Has had a serious infection, such as pneumonia in the previous 12 weeks

  11. Has known allergies or hypersensitivity to metformin, sildenafil or leucine

  12. Is an immediate family member (spouse, parent, child, or sibling; biological or legally adopted) of personnel directly affiliated with the study at the clinical study site, or NuSirt Biopharma.

  13. Is employed by NuSirt Biopharma (defined as an employee, temporary contract worker, or designee responsible for the conduct of the study).

Trial design

Primary purpose

Treatment

Allocation

Randomized

Interventional model

Parallel Assignment

Masking

Quadruple Blind

91 participants in 3 patient groups, including a placebo group

Leu Met Sil 0.5mg
Experimental group
Description:
Leu-Met-Sil 0.5: 3 capsules BID consisting of 2 capsules containing 550 mg L-leucine each and 1 capsule containing 500 mg metformin and 0.5 mg of sildenafil.
Treatment:
Drug: Leu-Met-Sil 1.0
Leu Met Sil 1.0mg
Experimental group
Description:
Leu-Met-Sil 1.0: 3 capsules BID consisting of 2 capsules containing 550 mg L-leucine each and 1 capsule containing 500 mg metformin and 1.0 mg of sildenafil.
Treatment:
Drug: Leu-Met-Sil 0.5
Drug: Leu-Met-Sil 1.0
Placebo
Placebo Comparator group
Description:
Placebo: 3 capsules BID containing 99% Avicel PH302 and 1% magnesium stearate (w/w)
Treatment:
Drug: Placebo

Trial contacts and locations

13

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Data sourced from clinicaltrials.gov

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