This is a first-in-humans study of GSI-136, a drug being developed for the treatment of
Alzheimer Disease. The main purpose of this study is to determine whether GSI-136 is safe
and tolerable in healthy young and healthy elderly subjects. The amount of drug in the body
and the effects of the drug on the body will also be evaluated at certain timepoints.
1. Men or women of nonchildbearing potential (WONCBP) aged 18 to 50 years or greater
than 65 years, inclusive, at screening. WONCBP may be included if they are either
surgically sterile (hysterectomy and/or oophorectomy) or postmenopausal for greater
than 1 year (with follicle-stimulating hormone [FSH] level greater than 38 mIU/mL)
and must have a negative pregnancy test result within 48 hours before test article
administration. Women who are surgically sterile must provide documentation of the
procedure by an operative report or by ultrasound scan. Sexually active men must
agree to use a medically acceptable form of contraception during the study and
continue it for 12 weeks after test article administration.
2. Body mass index (BMI) in the range of 18.0 to 30.0 kg/m2 and body weight greater than
3) The elderly subjects must be generally healthy, but may be enrolled with a stable,
chronic illness, if it is well controlled and does not interfere with the primary
objective of the study. Subjects may be included with clinically important deviations
from normal limits in medical history, physical examination findings, vital sign
measurements, 12-lead ECGs, or clinical laboratory test results that are associated with
stable, chronic, and well-controlled medical conditions.
1. Any history or presence of chronic respiratory disorder or disease including but not
limited to asthma, sleep apnea, or chronic obstructive pulmonary disease (COPD).
2. Any significant cardiovascular, hepatic, renal, respiratory, gastrointestinal,
endocrine, immunologic, dermatologic, hematologic, neurologic, or psychiatric
3. Presence or history of thyroid disease, symptomatic vertigo, significant cardiac
valvular disease, congestive heart failure, angina pectoris, significant cardiac
arrhythmia, or seizures.