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Study to Evaluate Safety/Duration in Stomach of Extended Release Capsules Containing Memantine Hydrochloride in Healthy Adults

Early Phase 1
Completed
Conditions
Healthy
Alzheimer Disease
Gastric Retention
Interventions
Drug: LYN-057
Procedure: Imaging Assessment (MRI)
Procedure: Imaging Assessment (U/S)
Registration Number
NCT03711825
Lead Sponsor
Lyndra Inc.
Brief Summary

To assess how long memantine hydrochloride (HCl) (50 mg) extended release capsules stay in the stomach as determined by imaging assessment (MRI or abdominal ultrasound).

To evaluate the safety of a memantine HCl extended release capsule formulation

Detailed Description

This is a single centre, open label, single dose study in healthy adult subjects.

Eligible individuals will be admitted to an inpatient unit in two or more cohorts. Enough eligible individuals will be admitted allowing for the enrollment of the Sentinel (n= 2) and Main Group (total of n=8 in Main), and an optional Supplemental Group (n= 6), if required.

All enrolled subjects will be dosed with a single administration of an extended release capsule containing memantine hydrochloride (LYN-057), 50 mg. Dosing will be conducted in an inpatient clinical unit, with access to an acute care facility. Subjects will remain in the inpatient unit for 7 days after dosing. During this time, subjects will undergo intermittent imaging assessments for gastric retention \[magnetic resonance imaging (MRI) and abdominal ultrasound (U/S)\], safety assessments, blood sampling for evaluation of memantine pharmacokinetics (PK), and faecal collections for assessments of formulation components and bowel movement characteristics.

Subjects will return to the clinic for PK sampling and safety assessments on Days 10, 15, 22 and Day 29 (End of Study Visit). In addition, some subjects may continue to perform faecal collection and/or may undergo imaging assessments on Day 10 based on clinical criteria. On Day 29 (End of Study Visit), subjects will undergo final safety and PK assessments and will be discharged from the study.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
8
Inclusion Criteria
  1. Healthy male and female subjects
  2. Body mass index of 18.0 to 30.0 kg/meters-squared
  3. Suitable scores for two swallowing questionnaires
  4. Demonstrate normal swallowing and gastrointestinal passage for capsule, as assessed while undergoing imaging studies
  5. Must provide written informed consent
Exclusion Criteria
  1. Participants who have previously been enrolled in this study
  2. History of any drug or alcohol abuse in the past 2 years
  3. Current smokers and those who have smoked within the past 12 months
  4. Individuals with clinically significant medical history relating to the gastrointestinal tract and potential complications, thereof
  5. Individuals with a positive test for HIV, hepatitis B or hepatitis C
  6. Individuals who are contraindicated based on memantine HCl
  7. Serious adverse reaction or serious hypersensitivity to components of the study formulation or patency capsule
  8. Individuals who have received any experimental agent within 30 days (or 5 half-lives), whichever is longer, prior to the date of dosing
  9. Individuals with contraindication to MRI imaging
  10. Individuals with functional constipation, irritable bowel, or functional diarrhea, as evaluated by standardized questionnaire
  11. Individuals with contraindications to elective X-ray based on known or expected radiation exposure

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Sentinel/MainImaging Assessment (MRI)Sentinel dosing of two subjects in clinic of LYN-057 (50 mg), followed by Main, i.e. remaining 6 subjects, for total of 8 subjects doses; followed by imaging assessment (MRI/abdominal U/S)
Sentinel/MainImaging Assessment (U/S)Sentinel dosing of two subjects in clinic of LYN-057 (50 mg), followed by Main, i.e. remaining 6 subjects, for total of 8 subjects doses; followed by imaging assessment (MRI/abdominal U/S)
Sentinel/MainLYN-057Sentinel dosing of two subjects in clinic of LYN-057 (50 mg), followed by Main, i.e. remaining 6 subjects, for total of 8 subjects doses; followed by imaging assessment (MRI/abdominal U/S)
Primary Outcome Measures
NameTimeMethod
Safety and tolerability of a single dose of LYN-057 extended release capsuleThrough study completion, up to 3 months

Safety collected from a combination of the following: Adverse Event (AE) reporting and examinations specified per protocol

Gastric retention by imaging assessment by MRIUp to 9 days post-dosing

Visualization of formulation/formulation components in stomach by MRI

Gastric retention by imaging assessment by abdominal U/SUp to 9 days post-dosing

Visualization of formulation/formulation components in stomach by abdominal U/S

Secondary Outcome Measures
NameTimeMethod
Memantine HCl pharmacokinetics - Area Under the Curve (AUC)Pre-dose, on day of dosing at 2, 4, 6, 8 and 12 hours post-dosing, thereafter daily during inpatient stay through Day 8. After Day 8, PK sampling on Day 10, 15, 22 and 29.

Memantine HCl pharmacokinetics - AUC by validated assay

Memantine HCl pharmacokinetics - Maximum Plasma Concentration (Cmax)Pre-dose, on day of dosing at 2, 4, 6, 8 and 12 hours post-dosing, thereafter daily during inpatient stay through Day 8. After Day 8, PK sampling on Day 10, 15, 22 and 29.

Memantine HCl pharmacokinetics - Cmax by validated assay

Physical features of recovered formulation componentsThrough study completion, up to 29 days

Recording of the descriptive physical features, e.g. number of polymeric arms (if separate) or attached to the core, of formulation components recovered from collected fecal specimens

Memantine HCl pharmacokinetics - Time after administration of maximum plasma concentration (Tmax)Pre-dose, on day of dosing at 2, 4, 6, 8 and 12 hours post-dosing, thereafter daily during inpatient stay through Day 8. After Day 8, PK sampling on Day 10, 15, 22 and 29.

Memantine HCl pharmacokinetics - Tmax by validated assay

Trial Locations

Locations (1)

CMAX

🇦🇺

Adelaide, South Australia, Australia

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