Clinical trial NCT02648672 (phase 1, status: completed)
Conditions: alzheimer's disease
ICD codes: G30.8, G30.9, G30.0, G30.1
Drugs: bpn14770, placebo
SMILES: CN1C(=O)C=C(N2CCC[C@@H](N)C2)N(CC2=C(C=CC=C2)C#N)C1=O
Eligibility criteria:

        Inclusion Criteria:

          1. Healthy male or female. Female subjects must not be pregnant or breastfeeding.

          2. Subject must be between 18 and 55 years of age (inclusive).

          3. Subject's body mass index (BMI) must be between 18 and 32 kg/m2 (inclusive), and
             subject must weigh a minimum of 50 kg (110 lbs).

          4. Female subjects must be surgically sterile (bilateral tubal ligation, hysterectomy, or
             bilateral oophorectomy at least 6 months prior to dosing) or at least 2 years
             postmenopausal. Menopausal status will be verified by a follicle-stimulating hormone
             (FSH) test at screening. In addition, all females must have a negative pregnancy test
             result within 48 hours before study drug administration regardless of childbearing
             potential.

          5. Male subjects must be willing to inform female partners of their participation in the
             study and to use adequate contraceptive methods (must have had vasectomy at least 6
             months prior to dosing or use at least one barrier method of birth control).

          6. Subject must understand the study procedures, voluntarily consent to participate in
             this study, and provide their written informed consent prior to start of any
             study-specific procedures.

          7. Subject is willing and able to remain in the study unit for the entire duration of the
             confinement period and return for outpatient visits.

        Exclusion Criteria:

          1. Clinically significant abnormality in the investigator's opinion indicated from the
             current hematology, biochemistry, or urinalysis tests, or from medical history, social
             history, vital signs, or physical examination.

          2. Positive serology results for hepatitis B surface antigen (HbsAg), hepatitis C virus
             (HCV), or human immunodeficiency virus (HIV).

          3. Marked hypotension (systolic blood pressure [BP] ˂90 mmHg or diastolic BP ˂50 mmHg) or
             hypertension (systolic BP ˃160 mmHg or diastolic BP ˃100 mmHg) based on supine and
             sitting values at screening or predose. Out-of-range vital signs may be repeated once.

          4. Marked bradycardia (heart rate ˂45 beats per minute [bpm]) or tachycardia (heart rate
             ˃110 bpm) based on supine, sitting, and ECG values at screening or predose.
             Out-of-range vital signs may be repeated once.

          5. Current or past history of cardiovascular, cerebrovascular, pulmonary, renal, or liver
             disease.

          6. History of hematological disorders (e.g., thrombocytopenia) in the immediate family
             (i.e, parents and siblings).

          7. Clinically important or significant conduction abnormalities on average of triplicate
             ECGs (including QTc intervals ˃450 msec); evidence or history of long QT syndrome.
             This exclusion applies to the ECGs taken at screening, Day -1, and Day 1 predose.

          8. Current or past history of gastric or duodenal ulcers or other diseases of the
             gastrointestinal tract that could interfere with absorption of study drug. Note:
             Subject with history of appendectomy or cholecystectomy may be enrolled.

          9. Active acute or chronic infectious diseases.

         10. Unable to discontinue any over the counter (OTC) medication utilized on a regular
             basis or has taken any prescription medication within 14 days prior to admission to
             the study on Day -2.

         11. Regular (daily) consumption of alcohol exceeding two servings of beer or the
             equivalent amount of other forms of alcohol (1 serving = 12 oz beer, 5.0 oz wine, or
             1.5 oz distilled spirits).

         12. Any history of alcohol or drug abuse within the previous year prior to the Screening
             Visit (per the current edition of the Diagnostic and Statistical Manual of Mental
             Disorders, 5th Edition: DSM-5).

         13. Any use of alcohol within 48 hours of admission into the study on Day -2.

         14. Active smokers or tobacco users (e.g., chew and snuff) who are unable to discontinue
             tobacco use at least 6 months prior to admission to the study on Day -2 and refrain
             from using tobacco during the study treatment and evaluation period.

         15. Inability or unwillingness to comply with the protocol or rules of the clinical
             research unit, or likely inability to complete the study.

         16. Participation in other clinical studies involving investigational drug within the
             previous 30 days prior to the Screening Visit.

         17. Donation of blood or blood products (including plasma) during the 8 weeks before the
             first administration of study drug on Day 1.

         18. Positive screen for drugs of abuse.

         19. History of allergy to penicillin or sulfonamides, or any other clinically significant
             drug allergy that includes symptoms such as shortness of breath, rash, or edema.