Safety, pharmacokinetics, and pharmacodynamics of Gln-1062, a prodrug of galantamine.

ABSTRACT:

Introduction

Gln-1062 (MEMOGAIN) is an intranasally administered lipophilic prodrug of galantamine. Based on high brain-to-blood concentrations observed in pre-clinical studies, Gln-1062 is expected to have superior cognitive efficacy compared to oral galantamine.

Methods

Forty-eight healthy elderly subjects were randomized 12:4 to Gln-1062 (5.5, 11, or 22 mg, b.i.d., for 7 days) or placebo. Safety, tolerability, pharmacokinetics, and pharmacodynamics were assessed repeatedly. Pharmacokinetics were compared with 16 mg oral galantamine.

Results

Gln-1062 up to 22 mg, b.i.d., was well tolerated. Gln-1062 plasma concentrations increased immediately following dosing (median T_max of 0.5 hour [range 0.5-1.0]). C_max and AUC_0-last increased in

SUBMITTER: Bakker C 

PROVIDER: S-EPMC7551138 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature