A Comparison Study of the Bioavailability of a Capsule Formulation of LGD-6972 to an Oral Solution Formulation

NCT02672839 | Completed Phase 1

• 1 other identifier: L6972-03
• Study Type: interventional
• Target: 12
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to compare relative oral bioavailability of a capsule formulation of LGD-6972 to a solution formulation of LGD-6972.

Conditions

Type 2 Diabetes Mellitus (T2DM)

Outcome Measures

Primary Outcomes (2)

• Pharmacokinetics Analysis- Area Under the Concentration Curve (AUC)

  AUC: ratio: medium test form to reference form

  Pre-dose, 1,2,4,6,8,10,12,16,24,36,48,72 hrs, 7 and 14 days post dose

• Pharmacokinetics Analysis- Maximum Concentration (Cmax)

  Cmax: ratio: medium test form to reference form

  Pre-dose, 1,2,4,6,8,10,12,16,24,36,48,72 hrs, 7 and 14 days post dose

Secondary Outcomes (1)

• Severity of all Adverse Events graded according to the Common Terminology Criteria for Adverse Events (CTCAE)

  Day -1, 24, 48, 72hrs, and 7day and 14day post dose

Study Arms (4)

Period 1 Treatment A

EXPERIMENTAL

Healthy subjects will receive a single dose orally of LGD-6972 capsules fasted

Drug: LGD-6972 Capsules

Period 1 Treatment B

EXPERIMENTAL

Healthy subjects will receive a single dose orally of LGD-6972 solution fasted

Drug: LGD-6972 Solution

Period 2 Treatment A

EXPERIMENTAL

Healthy subjects will receive a single dose orally of LGD-6972 capsules fasted

Drug: LGD-6972 Capsules

Period 2 Treatment B

EXPERIMENTAL

Healthy subjects will receive a single dose orally of LGD-6972 solution fasted

Drug: LGD-6972 Solution

Interventions

LGD-6972 Solution DRUG

15 mg of LGD-6972

Also known as: LGD-6972 Sodium Salt in Captisol ® (betadex [β-cyclodextrin] sulfobutylether sodium, NF)

Period 1 Treatment B; Period 2 Treatment B

LGD-6972 Capsules DRUG

15 mg LGD-6972

Also known as: LGD-6972 Sodium Salt Capsules

Period 1 Treatment A; Period 2 Treatment A

Eligibility Criteria

• Age: 21 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Healthy, adult man or woman, 21 to 65 years of age. If the subject is a woman, she must be surgically sterile (hysterectomy or bilateral oophorectomy or bilateral tubal ligation), or naturally post menopausal for at least 12 months and with a follicle stimulating hormone (FSH) level in the post-menopausal range (if not taking hormone replacement therapy) to be considered for enrollment
• Willing and able to provide written informed consent
• Not diabetic and has a fasting blood glucose between 70 and 105 mg/dL, inclusive
• In good health with no significant concomitant pathology based on medical history, physical examination, ECG, routine laboratory tests (chemistry, hematology, lipid profile, and urinalysis), and vital signs
• Has a body mass index (BMI) between 18.5 kg/m2 and 30 kg/m2, inclusive, and must weigh more than 45 kg
• Male subjects must either have a vasectomy or agree that they and any female partners will use 2 acceptable forms of contraception, one of which must be a condom, until 30 days after the last dose of study drug. Other acceptable forms of contraception include hormonal contraceptives, intrauterine device, Depo Provera®, Norplant® System Implants, bilateral tubal ligation, bilateral oophorectomy, hysterectomy, and contraceptive sponge, foam, or jelly.

You may not qualify if:

• History of drug and/or alcohol abuse within 2 years prior to screening
• Unwilling to comply with tobacco, nicotine, alcohol, and caffeine restrictions outlined in the protocol
• Unwilling to comply with restrictions on strenuous exercise as specified in the protocol
• Has a history of clinically significant cardiovascular, pulmonary, renal, endocrine, hepatic, neurologic, psychiatric, immunologic, hematologic, gastrointestinal (including pancreatitis), or metabolic disease requiring medical treatment or has any medical problems that pose an increased risk during the study or that may compromise the integrity of the study data
• Has liver transaminase levels (aspartate aminotransferase \[AST\] or alanine aminotransferase \[ALT\]) 10% of the upper limit of normal (ULN), or has creatine kinase (CK) levels 2 × ULN at screening or admission to site (Day 1). Abnormal values at screening may be retested once
• Has a serum triglyceride level 400 mg/dL at screening. If the triglyceride level is between 400 mg/dL and 500 mg/dL, one retest is permitted
• Recent history of uncontrolled high blood pressure or has systolic blood pressure 90 mmHg or 140 mmHg or diastolic blood pressure 50 mmHg or 90 mmHg at screening. One or more retests of blood pressure within a reasonable period of time are permissible at the discretion of the Investigator
• Is taking prescription or non-prescription drugs other than those outlined in the protocol
• Has a positive screening for hepatitis B virus (HBV), hepatitis C virus (HCV), and/or human immunodeficiency virus (HIV)
• Woman of childbearing potential
• Lactating or has a positive pregnancy test
• Has donated 450 mL of blood within 56 days of admission to the investigational site or has donated blood products within 30 days of admission.

Sponsors & Collaborators

• Ligand Pharmaceuticals: lead
• Medpace, Inc.: collaborator

Study Sites (1)

Medpace, Inc

Cincinnati, Ohio, 45227, United States

Location

MeSH Terms

Conditions

Diabetes Mellitus, Type 2

Interventions

SBE4-beta-cyclodextrin; betadex; RVT-1502

Condition Hierarchy (Ancestors)

Diabetes Mellitus; Glucose Metabolism Disorders; Metabolic Diseases; Nutritional and Metabolic Diseases; Endocrine System Diseases

Study Officials

• Lukasz Biernat, M.D.

  Medpace Clinical Pharmacology

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: January 27, 2016
• First Posted: February 3, 2016
• Study Start: February 1, 2016
• Primary Completion: May 1, 2016
• Study Completion: May 1, 2016
• Last Updated: May 18, 2016

Record last verified: 2016-03

Data Sharing

• IPD Sharing: Will share

Locations

US (1)