A Study to Assess 11 Beta-hydroxysteroid Dehydrogenase Type 1 Inhibition in Adipose Tissue by SPI-62

Sparrow Pharmaceuticals12 enrolled

Overview

This will be an exploratory, open-label study of 11β-hydroxysteroid dehydrogenase type 1 (HSD-1) inhibition by SPI-62 in obese subjects with type 2 diabetes mellitus (T2DM)

The main objective of the study is to characterize the relationship between SPI-62 plasma concentration and adipose tissue inhibition of HSD-1 in obese subjects with T2DM.Additional objectives of the study are to characterize the relationship between adipose SPI-62 concentration and HSD-1 inhibition, to characterize the relationship between SPI-62 plasma concentration and liver inhibition of HSD-1, and to monitor the safety and tolerability of SPI-62, in obese subjects with T2DM. This will be a Phase I, open-label study in male and non-menstruating female subjects. Potential subjects will be screened to assess their eligibility to enter the study within 28 days prior to the first dose administration. Subjects will receive SPI-62 daily for up to 14 days. Subjects will also receive cortisone-d8, a mass-labeled HSD-1 substrate, by infusion during one or two confined study visits during the period of SPI-62 administration. Subjects may also receive cortisone-d8 during one to four additional confined study visits after cessation of SPI-62. Subjects will receive a follow-up call approximately 30 days after the last dose of study drug (SPI-62 or cortisone-d8). Results of population pharmacokinetic-pharmacodynamic modeling of data from this trial combined with those of prior trials will be reported separately from the Clinical Study Report.

Study Type

INTERVENTIONAL

Allocation

Purpose

BASIC_SCIENCE

Masking

NONE

Enrollment

Conditions

Type 2 Diabetes Mellitus in Obese Obesity Type2Diabetes

Interventions

SPI-62DRUG

SPI-62 is supplied as 1 mg tablets for oral dosing.

Cortisone-d8DRUG

Cortisone-d8 is supplied as a 1 mcg/mL solution for infusion

Eligibility

Sex: ALLMin age: 18 YearsMax age: 65 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: * Male or non-menstruating female * 18 to 65 years of age * BMI 30.0 to 45.0 kg/m2 * Diagnosis of T2DM for at least 3 months prior to the first dose of study drug. Exclusion Criteria: * Uncontrolled T2DM with glycated hemoglobin ≥9.5%. * Any other current or prior medical condition expected to interfere with the conduct of the trial or the evaluation of its results. * Any clinically significant abnormal laboratory value which cannot be explained by a known and permitted clinical condition. * Positive urine drug screen (except tetrahydrocannabinol) or positive alcohol breath test result. * Participation in a clinical trial involving administration of an investigational drug (new chemical entity) in the past 30 days or 5 half-lives, whichever is longer, or 90 days for a biological, prior to the first dose of study drug. * Use of, or intent to use, any medications/products (prescription or over-the-counter) or herbal supplements within 4 weeks prior to the first dose of study drug, except those specifically allowed in the protocol.

Locations (1)

ProSciento

Chula Vista, California, United States

Outcomes

Primary Outcomes

Pharmacokinetics (Cmax)

Pharmacokinetics of SPI-62 and its major metabolite AS2570469 by assessment of Observed Maximum Plasma Concentration (Cmax)

Time frame: Days 1 through 14

Secondary Outcomes

Pharmacokinetics (tmax)

Pharmacokinetics of SPI-62 and its major metabolite AS2570469 by assessment of Time to Cmax (tmax)

Time frame: Days 1 through 14

Pharmacokinetics (AUC0-t)

Pharmacokinetics of SPI-62 and its major metabolite AS2570469 by assessment of Area Under the Curve over the dosing interval

Time frame: Days 1 through 14

Cortisone-d8 concentrations

individual values

Time frame: Days 1 through 14

Urinary HSD-1 Ratio

Individual values of the urinary HSD-1 ratio defined as (tetrahydrocortisol + allotetrahydrocortisol) / tetrahydrocortisone

Time frame: Days -1 to 15

Data from ClinicalTrials.gov

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