Evaluation of Safety, Efficacy and Thermogenesis-induction of RZL-012 in Overweight and Obese Volunteers

Raziel Therapeutics

Status and phase: Completed; Phase 2

Conditions: Weight Loss; Overweight and Obesity; Obesity

Treatments: Drug: RZL-012; Drug: Placebo

Study type: Interventional

Funder types: Other; Industry

Identifiers

NCT03171415

RZL-012-P2aUS-001

Details and patient eligibility

About

Obesity is a direct result of food-intake in excess of body energy expenditure. Thus, induction of increased energy expenditure via the activation of thermogenesis at targeted anatomical sites can counterbalance obesity. This trial aims to study RZL-012, a novel compound, in treating obesity by activating thermogenesis in subcutaneous fat.

Full description

Obesity is a direct result of food-intake in excess of body energy expenditure. Therefore, a feasible approach to combat obesity is via energy-consuming activities, such as physical exercise. Unfortunately, our modern society is moving in the other direction, spending more time in immobilized positions, at work and at home. An alternative strategy for the induction of increased energy expenditure is via the activation of thermogenic cells that utilize fat to produce heat.RZL-012 is a novel molecule that enables de-novo generation of thermogenic tissue at favorable anatomical sites. As a result, the extra fat accumulated in obese persons will be turned into heat. This is a double blind, randomized, placebo controlled, dose escalation Phase 2a clinical trial for the evaluation of safety, efficacy and thermogenesis-induction of RZL-012 in overweight and obese volunteers. This trial aims to study the ability of RZL-012 in treating obesity via the induction of thermogenic foci in subcutaneous fat.

Enrollment: 32 patients

Sex: Male

Ages: 20 to 60 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

1. Adult male subjects, 20-60 years old.
2. Subject is considered overweight and obese, with 27.5 < BMI ≤ 34.9.
3. Significant subcutaneous abdominal fat as defined by Waist to hip ratio (WHR) ≥ 0.9.
4. Subjects with stable weight in the last 3 months by medical history.
5. Not one of the following eating disorders by subject's declaration: anorexia nervosa, bulimia nervosa.
6. Generally considered healthy according to medical history, physical examination, electrocardiogram (ECG) and laboratory evaluation with a special emphasis on metabolic parameters (fasting glucose concentration < 100 mg, normal blood pressure).
7. Subject is willing to refrain from sexual activity or agrees to use a double-barrier contraceptive device (e.g., condom and spermicide) for 4 weeks after treatment with RZL 012.
8. Subjects must be able to adhere to the visit schedule and protocol requirements and be available to complete the study.
9. Subjects must sign an informed consent indicating that they are aware of the investigational nature of the study.

Exclusion criteria

1. Subjects weighing less than 75 kg.
2. Subjects who have reduced/gained weight more than 5% of their current body weight in the last 3 months.
3. Unable to tolerate subcutaneous injection.
4. Subjects with uncontrolled cardiac, hepatic, renal or neurologic/psychiatric disorders, that in the opinion of the investigator put the subject at significant risk, are not eligible.
5. Subjects who test positive to either Hepatitis B virus (HBV), Hepatitis C virus (HCV), or Human immunodeficiency virus (HIV) are not eligible.
6. Subjects with a clinical history of primary or secondary immunodeficiency, autoimmune disease or subjects taking immunosuppressive drugs such as corticosteroids are ineligible.
7. As a result of medical review, physical examination, the PI (or medically qualified nominee) considers the subject unfit for the study.
8. Medication use on regular basis.
9. Positive drug and alcohol tests.
10. Known sensitivity to components of the injection formulation.
11. Prior wound, tattoo or infection in the treated area.
12. Excessive growth of hair in the abdomen region.
13. Claustrophobia or MRI incompatible device or implant.

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Sequential Assignment

Masking: Triple Blind

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32 participants in 2 patient groups, including a placebo group

RZL-012

Experimental group

Description:

A single-time injection, multiple subcutaneous injections of RZL-012 administered into 8-36 sites (0.1mL per site): 1. 40mg RZL-012 -administered at 8 sites 2. 80mg RZL-012 - administered at 16 sites 3. 120mg RZL-012 - administered at 24 sites 4. 180mg RZL-012 - administered at 36 sited

Treatment:

Drug: RZL-012

Placebo

Placebo Comparator group

Description:

A single-time injection, multiple subcutaneous injections of Placebo administered into 8-36 sites (0.1mL per site)

Treatment:

Drug: Placebo