CompletedPhase 1ACTRN12620000213943

A Phase 1 study to evaluate Safety, Tolerability and Pharmacokinetics of Ultramicronized-Palmitoylethanolamide (PEA) in Healthy Subjects.

A Phase 1, randomized, Double-Blind, Placebo-Controlled study to evaluate the Safety, Tolerability and Pharmacokinetics of single and multiple ascending doses of Ultramicronized PEA in normal healthy volunteers.

Sponsor

FSD Pharma Inc.

Enrollment

48 participants

Start Date

Apr 7, 2020

Study Type

Interventional

Conditions

Chronic Pain Inflammation

Summary

This study of ultramicronized PEA (particle size between 0.6 and 10 µm) will investigate the safety, tolerability, PK of single and multiple ascending doses of ultramicronized PEA compared to placebo in healthy subjects. The effect of food on the absorption of the ultramicronized PEA will also be assessed..

Eligibility

Sex: Both males and femalesMin Age: 18 YearssMax Age: 65 Yearss

Inclusion Criteria15

Male or female, light smoker (no more than 9 cigarettes or equivalent daily) or non-smoker, healthy subjects, aged 18 to 65 years inclusive.
Healthy is defined as
a) the absence of clinically significant illness and surgery within 4 weeks prior to study drug administration.
b) the absence of clinically significant history of neurological, endocrine, cardiovascular, respiratory, hematological, immunological, psychiatric, gastrointestinal, renal, hepatic, and metabolic disease.
Body mass index of >18.5 to <32.0 kg/m2.
Females of childbearing potential who are sexually active with a non-sterile male partner (sterile male partners are defined as men vasectomized since at least 6 months) must be willing to use one of the following acceptable contraceptive methods throughout the study and for 30 days after (the last) study drug administration:
a) simultaneous use of intra-uterine contraceptive device, placed at least 4 weeks prior to (the first) study drug administration, and condom for the male partner.
b) simultaneous use of hormonal contraceptives, started at least 4 weeks prior to (the first) study drug administration and must agree to use the same hormonal contraceptive throughout the study, and condom for the male partner.
c) simultaneous use of diaphragm or cervical cap and male condom for the male partner, started at least 21 days prior to (the first) study drug administration.
Male subjects who are not vasectomized for at least 6 months, and who are sexually active with a female partner of childbearing potential (childbearing potential females are defined as women that are neither post-menopausal nor surgically sterile) must be willing to use one of the following acceptable contraceptive methods from (the first) study drug administration and for 90 days after (the last) study drug administration:
a) simultaneous use of a male condom and, for the female partner, intra-uterine contraceptive device or hormonal contraceptives used since at least 4 weeks.
b) simultaneous use of a male condom and, for the female partner, a diaphragm or cervical cap.
Male subjects (including men who have had a vasectomy) with a pregnant partner must agree to use a condom from (the first) study drug administration and for 90 days after (the last) study drug administration.
Male subjects must be willing not to donate sperm for 90 days following (the last) study drug administration.
Capable of consent.

Exclusion Criteria16

Any clinically significant abnormality at physical examination.
Any laboratory test results deemed clinically significant by the Investigator or positive test for HIV, HBsAg, or HCV found during medical screening.
Positive pregnancy test at screening or Day 1.
Positive urine drug screen or alcohol breath test at screening or Day 1.
History of allergic reactions to PEA or other related drugs, or to any excipient in the formulation.
Clinically significant ECG abnormalities or vital sign abnormalities (systolic BP lower than 90 or over 140 mmHg, diastolic BP lower than 40 or over 90 mmHg, HR less than 40 or over 100 bpm, or RR less than 10 or over 22 bpm) at screening.
History of significant drug abuse within 1 year prior to screening or use of soft drugs (such as marijuana) within 1 month prior to the screening or hard drugs (such as cocaine, phencyclidine [PCP], crack, opioid derivatives including heroin, and amphetamine derivatives) within 3 months prior to screening.
History of significant alcohol abuse within 1 year prior to screening or regular use of alcohol within 6 months prior to the screening visit (more than 14 units of alcohol per week [1 unit equals to 150 mL of wine, 360 mL of beer, or 45 mL of 40% alcohol]).
Participation in a clinical research study involving the administration of an investigational or marketed drug or device within 30 days prior to the first dosing, administration of a biological product in the context of a clinical research study within 90 days prior to the first dosing, or concomitant participation in an investigational study involving no drug or device administration.
Use of medications for the timeframes specified below, with the exception of hormonal contraceptives and medications exempted by the Investigator on a case-by-case basis because they are judged unlikely to affect the PK profile of the study drug or subject safety (e.g., topical drug products without significant systemic absorption):
a) prescription medications within 14 days prior to (the first) dosing;
b) over-the-counter products and natural health products (including herbal remedies such as St. John’s wort, homeopathic and traditional medicines, probiotics, food supplements such as vitamins, minerals, amino acids, essential fatty acids, and protein supplements used in sports) within 7 days prior to (the first) dosing, with the exception of the occasional use of acetaminophen (up to 2 g daily);
c) depot injection or implant of any drug (other than hormonal contraceptives) within 3 months prior to (the first) dosing;
Donation of plasma within 7 days prior to dosing. Donation or loss of blood (excluding volume drawn at screening) of 50 mL to 499 mL of blood within 30 days, or more than 499 mL within 56 days prior to the first dosing.
Breast-feeding subject.
Any reason which, in the opinion of the Investigator, would prevent the subject from participating in the study.

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Interventions

Subjects will be administered Ultramicronized PEA or matching placebo tablets in Cohort 1-6 via oral route as below. Cohort 1- Single dose of 600mg Ultramicronized PEA tablet i.e 1 tablet (n=6) or m

Subjects will be administered Ultramicronized PEA or matching placebo tablets in Cohort 1-6 via oral route as below. Cohort 1- Single dose of 600mg Ultramicronized PEA tablet i.e 1 tablet (n=6) or matching placebo (n=2); Cohort 2 - Single dose of 1200mg Ultramicronized PEA tablet i.e 2 tablets (under fasting and fed conditions) (n=6) or matching placebo (n=2); For cohorts dosed under fasting conditions, no food will be allowed from at least 10 hours before until at least 4 hours after dosing. Except for water given with the study drug, no fluids will be allowed from 1 hour before until 1 hour after dosing. There will be a washout period of at least 7 days between dosing of the fasting and the fed periods. For the fed period of Cohort 2, after a supervised fast of at least 10 hours, subjects will be served a high-fat, high-calorie meal of approximately 800 to 1000 calories (approximately 50% of total caloric content of the meal derived from fat). This meal should derive approximately 150, 250, and 500-600 calories from protein, carbohydrate, and fat, respectively. Drug administration will occur approximately 30 minutes after the meal has been started. Except for fluids provided with the breakfast and water given with the study drug, no fluids will be allowed from 1 hour before until 1 hour after dosing. Cohort 3 - Single dose of 1800mg Ultramicronized PEA tablet i.e 3 tablets (n=6) or matching placebo (n=2); Cohort 4 - Single dose of 2400mg Ultramicronized PEA tablet i.e 4 tablets (n=6) or matching placebo (n=2); Cohort 5 - Twice daily dose of 600mg Ultramicronized PEA tablet i.e 1 tablet from Day 1 to Day 6 and once in the morning of Day 7 (n=6) or matching placebo (n=2); Cohort 6 - Twice daily dose of 1200mg Ultramicronized PEA tablet i.e 2 tablets from Day 1 to Day 6 and once in the morning of Day 7 (n=6) or matching placebo (n=2); Subjects cannot be enrolled in more than one cohort. For Part A (Cohort 1-4) Study medication will be administered to each subject with 240 mL of water and a mouth check will be performed to ensure consumption of the medication. In the event that subjects cannot swallow all tablets with 240 mL of water, additional water may be allowed up to a maximum total volume of 400 mL. For Cohort 2, the total volume of water administered for dosing in the fasting period will be recorded and the same volume will be used for dosing in the fed period. Time of dosing will be set equal to the time when the (first) tablet is administered to the subject. The dosing procedure must be completed within 2 minutes. For Part B (Cohort 5-6), each study drug administration will be separated by approximately 12 hours and should be done at approximately the same time every day.