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Safety and Tolerability Study of Oral LGD-6972 for Type 2 Diabetes Mellitus

Phase 1
Completed
Conditions
Type 2 Diabetes Mellitus
Interventions
Drug: Placebo (Captisol ®)
Registration Number
NCT02250222
Lead Sponsor
Ligand Pharmaceuticals
Brief Summary

Ligand Pharmaceuticals Incorporated is developing LGD-6972, a novel, orally-bioavailable addition to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. The mechanism of action of LGD-6972 is to reduce the excess liver glucose production characteristic of type 2 diabetes mellitus that is a major contributor to hyperglycemia. This clinical trial will evaluate the safety and tolerability of escalating doses LGD-6972 administered daily over 2 weeks in both healthy subjects and subjects with type 2 diabetes mellitus.

Detailed Description

This is to be a randomized, double-blind, placebo-controlled, sequential, multiple oral dose study conducted in normoglycemic healthy subjects (NHS) (Part 1) and subjects with type 2 diabetes mellitus (T2DM) who are treated with monotherapy metformin (a stable dose at randomization) along with diet and exercise (Part 2). Subjects with T2DM who are not on a stable dose of metformin but meet all other entry criteria may be enrolled in the study at the discretion of the Investigator, but must undergo a stabilization period of at least 12 weeks before determining eligibility for the study. In Part 1, a single group of healthy subjects will be dosed with repeated oral doses of 15 mg of LGD-6972 or placebo once daily (QD) for 14 days. In Part 2, a maximum of 3 groups of subjects with T2DM will be dosed with 3 sequential, increasing doses of LGD-6972 (5 mg, 10 mg or 15 mg) or placebo QD for 14 days.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
48
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Part 1: LGD-6972 15 mgLGD-697215 mg LGD-6972 administered once daily (QD) for 14 days.
Part 1: Placebo (Captisol ®)Placebo (Captisol ®)Placebo administered once daily (QD) for 14 days.
Part 2: LGD-6972 10 mgLGD-697210 mg LGD-6972 administered orally QD for 14 days.
Part 2: Placebo (Captisol ®)Placebo (Captisol ®)Placebo administered orally QD for 14 days.
Part 2: LGD-6972 5 mgLGD-69725 mg LGD-6972 administered orally QD for 14 days.
Part 2: LGD-6972 15 mgLGD-697215 mg LGD-6972 administered orally QD for 14 days.
Primary Outcome Measures
NameTimeMethod
Number of participants with one or more drug related adverse events or serious adverse eventsAt least 14 days after last dose

Safety and tolerability of repeat (14 days for normoglycemic healthy subjects (NHS) and 14 days for type 2 diabetes mellitus (T2DM) subjects) and sequential increasing oral doses of LGD-6972 in NHS and subjects withT2DM will be compared to NHS and T2DM subjects receiving placebo.

Secondary Outcome Measures
NameTimeMethod
Pharmacokinetic (PK) profile (area under the concentration curve (AUC) of LGD-6972 after repeat oral doses in NHS and in subjects with T2DM14 days

Steady state PK profile (AUC) of LGD-6972 in NHS and in subjects with T2DM will be characterized and compared.

Change from baseline in fasting plasma glucose measured 24 hours after first dose and pre-dose Day 14 of treatment with LGD-6972 in NHS14 days
Change from baseline in fasting plasma glucagon measured 24 hours after first dose and pre-dose Day 14 of treatment with LGD-6972 in NHS14 days
Change from baseline in active and total glucagon-like-peptide (GLP-1) in fasting plasma measured 24 hours after first dose and pre-dose Day 14 of treatment with LGD-6972 in NHS14 days
Change from baseline in fasting plasma glucose measured 24 hours after first dose and at Day 14 of treatment with LGD-6972 in subjects with T2DM14 days
Change from baseline in fasting plasma glucagon measured 24 hours after first dose and at Day 14 of treatment with LGD-6972 in subjects with T2DM14 days
Change from baseline in fasting plasma insulin measured 24 hours after first dose and at Day 14 of treatment with LGD-6972 in subjects with T2DM14 days
Change from baseline in fasting plasma active and total GLP-1 measured 24 hours after first dose and at Day 14 of treatment with LGD-6972 in subjects with T2DM14 days
Change from baseline in 7-point weighted mean glucose during 14 days of treatment with different doses of LGD-6972 in subjects with T2DM14 days
Hemoglobin A1c response during 14 days of treatment with different dosages of LGD-6972 in subjects with T2DM14 days
PK profile (maximum concentration (Cmax) of LGD-6972 after repeat oral doses in NHS and in subjects with T2DM14 days

Steady state PK profile (Cmax) of LGD-6972 in NHS and in subjects with T2DM will be characterized and compared.

Trial Locations

Locations (3)

Medpace Clinical Pharmacology

🇺🇸

Cincinnati, Ohio, United States

Clinical Pharmacology of Miami, Inc

🇺🇸

Miami, Florida, United States

Celerion, Inc

🇺🇸

Tempe, Arizona, United States

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