*A Two Part Phase I Study to Assess Safety, Tolerability, Systemic Exposure and Effect on Analgesia and Anaesthesia of Single and Multiple doses of TDT 077 in Healthy Older Subjects.*

Recruitment & Eligibility

Status: Completed

Sex: Not specified

Target Recruitment: 96

Inclusion Criteria

• Subjects must voluntarily sign a written informed consent agreement;
• Age 55-75 years except cohort 6B. Age 18-40 for cohort 6B;
• Female subjects should be of non-childbearing potential (surgically sterile or more than 1 year post-menopausal) or if of childbearing potential must be using a medically acceptable form of birth control for the duration of the study;
• Male subjects: you are not able to cause a pregnancy or uses a medically acceptable form of birth control for th duration of the study;
• Subjects must be in good health;
• Body Mass Index (BMI) between 18 and 30 (inclusive), with body weight greater than or equal to 60 kg and less than or equal to 100 kg;
• No clinically significant abnormalities at screening

Exclusion Criteria

• Subjects with a known hypersensitivity or allergy to bupivacaine, other local anaesthetics or to any of the excipients in TDT 077 (Part 1A and Part 2);
• Subjects with a known hypersensitivity or allergy to lidocaine and/or prilocain, other local anaesthetics or to any of the excipients in EMLA® hydrophilic cream (Part 1B);
• Subject has any skin irritation or disease that might interfere with absorption of study drug or skin irritation assessment, including eczema, psoriasis, melanoma;
• Subjects with active presence or history of alcoholism or drug addiction;
• Subject has a tattoo or other skin deformities that might interfere with skin irritation assessment;
• Subject has had a surgery within the last 3 months prior to dosing;
• Female subjects that are pregnant or lactating;
• Subjects who have used prescription medication within two weeks prior to the first dosing day, except for contraceptives or HRT;
• Subjects who have used over-the-counter medication (including homeopathic medicines and vitamins), within 96 hours prior to the dosing day;
• Subjects who have been treated with other local anaesthetic therapy within 3 weeks prior to dosing;
• Subjects who smoke more than 10 cigarettes per day and who are unable to abstain from smoking when at the study centre;
• Subjects who participated in an investigational drug study within 3 months prior to the dosing day;
• Subjects who have lost or donated >350 ml of blood within 12 weeks prior to the screening session;
• Subjects who test positive for HBsAg, Anti-HCV or HIV;
• Subjects with a relevant food or drug hypersensitivity or allergy;
• Subjects who are considered unsuitable to participate in the study for any reason in the opinion of the principal investigator.

Study & Design

Study Type: Interventional

Study Design: Not specified

Primary Outcome Measures

Name	Time	Method
<p>Part 1A:<br /><br>Primary objective is to evaluate the safety and tolerability of ascending<br /><br>single doses of TDT 077 in healthy older male and female subjects.<br /><br><br /><br>Part 1B:<br /><br>To validate the sensitivity of the clinical methods for the assessment of<br /><br>analgesia and anaesthesia.<br /><br><br /><br>Part 2:<br /><br>Primary objective is to evaluate the safety and tolerability of ascending<br /><br>multiple doses of TDT 077 in healthy older male and female subjects.</p><br>

Secondary Outcome Measures

Name	Time	Method
<p>Part 1A:<br /><br>Secondary objective is to evaluate the systemic exposure (PK) of ascending<br /><br>single doses of TDT 077 in healthy older male and female subjects. The third<br /><br>objective is to evaluate the magnitude and duration of effect (analgesia and<br /><br>anaesthesia) of ascending single doses of TDT 077 in older male and female<br /><br>subjects.<br /><br><br /><br>Part 1B:<br /><br>Not applicable<br /><br><br /><br>Part 2:<br /><br>Secondary objective is evaluate the systemic exposure (PK) of ascending<br /><br>multiple doses of TDT 077 in healthy older male and female subjects. Third<br /><br>objective is to evaluate the magnitude and duration of effect (analgesia and<br /><br>anaesthesia) of ascending multiple doses of TDT 077 in healthy older male and<br /><br>female subjects.</p><br>