VBY-036 may treat or prevent nerve pain. This study aims to find the highest safe and tolerable dose of VBY-036 in healthy volunteers. Volunteers will be randomly selected to receive either a placebo or VBY-036 (30, 100, 300, 600 or 900 mg) once daily for seven days in a row.
Inclusion Criteria:
* Male or female, 18-60 years old
* Screening body mass index between 18-32 kg/m2
* Good health, no clinically significant findings in medical history, 12-lead ECG, \& vital signs;
* Clinical lab evaluations (Chem panel \[fasted at least 8 hrs\], CBC, HbA1c \& UA in reference range for test lab (unless deemed not clinically significant);
* Negative test for drugs of abuse at Screening \& at Check-in (includes alcohol);
* Negative hepatitis, HIV \& TB screens;
* Females non-pregnant, non-lactating, \& either postmenopausal for at least 1 year, surgically sterile for at least 90 days prior to Check-in, or agree to use from the time of consent until 90 days after Study Completion an effective form of contraception. For all females, a pregnancy test result must be negative at Screening \& Check-in.
* Males will be sterile or agree to use from Check-in until 90 days following discharge an effective method of contraception.
* Able to comprehend \& willing to sign Informed Consent Form
Exclusion Criteria:
* Females pregnant or nursing, or childbearing potential but unwilling to use contraception.
* History of renal or hepatic impairment; stomach or intestinal surgery or resection, malabsorption syndrome, cholecystectomy, or gastro-intestinal dysfunction that would alter absorption \&/or excretion of orally administered drugs (appendectomy or hernia repair allowed);
* Anemia (hemoglobin \<11.5 g/dL for females; \< 13 g/dL for males) or blood donation within 8 weeks of Check-in;
* Plasma donation within 4 weeks of Check-in;
* History of alcoholism or drug addiction within 6 months to Check-in;
* Use of drugs of abuse or prescription drugs for recreational use 6 months prior to Check-in;
* Use of any tobacco-containing or nicotine-containing products 6 months prior to Check-in \& during study;
* Participation in another drug trial 30 days of Check-in (within 8 weeks if previous investigational drug has immunomodulary effects, other than cathepsin S inhibition);
* History or clinical manifestations of metabolic, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, urological, neurological, or psychiatric disorders
* History of hypersensitivity or allergies to any drug compound
* History or presence of abnormal ECG
* Laboratory abnormality deemed clinically significant;
* Use of or inability to discontinue any prescription medications/products 14 days prior to Check-in \& during study;
* Use of certain over-the-counter, non-prescription preparations are permitted up to 3 days before first dose;
* Use of alcohol-containing, grapefruit-containing, star fruit containing foods or beverages or "energy drinks" 72 hours to Check-in \& during study;
* Poor peripheral venous access;
* Receipt of blood products 6 months to Check-in
* Subjects with history of Gilbert's Syndrome;
* Strenuous activities 48 hours to Check-in
* Illness 5 days to drug administration
* Any acute or chronic condition
Locations (1)
Covance Evansville
Evansville, Indiana, United States
Outcomes
Primary Outcomes
Highest safe and tolerated VBY-036 dose
Single dose of VBY-036 given daily for 7-days in a row for each cohort in an ascending manner.
Cohort B1 with 30 mg dose or placebo; Cohort B2 with 100 mg dose or placebo; Cohort B3 with 300 mg dose or placebo; Cohort B4 with 600 mg dose or placebo; Cohort B5 with 900 mg dose or placebo
Time frame: 7 days of dosing
Secondary Outcomes
Confirmation of cathepsin-S inhibition
Based on the accumulation of Iip 10 and/or cathepsin S protein levels