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Clinical Trial Details — Status: Completed

Administrative data

NCT number NCT03251092
Other study ID # PTI-808-01
Secondary ID
Status Completed
Phase Phase 1/Phase 2
First received
Last updated
Start date July 17, 2017
Est. completion date December 23, 2019

Study information

Verified date April 2020
Source Proteostasis Therapeutics, Inc.
Contact n/a
Is FDA regulated No
Health authority
Study type Interventional

Clinical Trial Summary

Part 1 of this trial will enroll healthy volunteers into a single ascending dose (SAD), multiple ascending dose (MAD), and Food Effect (FE) treatment groups.

The SAD treatment group is comprised of at least 3 ascending dose level cohorts where healthy adult subjects will be randomized to receive a single dose of either PTI-808 or placebo and will be followed for 7 days post dose. A safety review committee (SRC) will convene after the completion of each cohort to evaluate safety and pharmacokinetic (PK) data.

Following the conclusion of the respective SAD level dose groups and after sufficient review of study data and approval by the SRC, a second set of healthy adult subjects will participate in an assigned MAD treatment group. The MAD treatment group is comprised of 3 ascending dose level cohorts where subjects will be randomized to receive either PTI-808 or placebo daily for 7 days and will be followed for 7 days after receiving the last dose.

Also following the conclusion of the respective SAD level dose groups, healthy adult subjects will participate in the FE treatment group.

Part 2 of this will enroll healthy volunteers to assess the safety, tolerability, and PK of PTI 808 co administered with PTI 801 and PTI 428 to HVs with daily dosing for 7 consecutive days.

Part 3 will enroll adult subjects with cystic fibrosis (CF) into a MAD treatment group consisting of 2 cohorts. Subjects will receive PTI-808 co-administered with PTI-801 and PTI-428. PTI-808 will be administered daily for 7 consecutive days followed by PTI-808 + PTI-801 + PTI-428 administered daily for 14 consecutive days.

Part 4 will enroll adult subjects with cystic fibrosis (CF) into 28-day cohorts. Subjects will receive PTI-808 co-administered with PTI-801 with or without PTI-428 versus matching placebo.


Description:

Part 1 of this trial will enroll healthy volunteers into a single ascending dose (SAD), multiple ascending dose (MAD), and Food Effect (FE) treatment groups.

The SAD treatment group is comprised of at least 3 ascending dose level cohorts where healthy adult subjects will be randomized to receive a single dose of either PTI-808 or placebo and will be followed for 7 days post dose.

The MAD treatment group is comprised of 3 ascending dose level cohorts where subjects will be randomized to receive either PTI-808 or placebo daily for 7 days and will be followed for 7 days after receiving the last dose.

Following the conclusion of the respective SAD level dose groups the food effect portion of the study will be initiated and subjects will be randomized to receive an initial single dose of PTI-808 either after an overnight fast of at least 10 hours (fasted group) or after an overnight fast of at least 10 hours followed the consumption of a high fat high calorie meal (fed group). After a 10 day washout period, subjects will cross over to the opposite group and receive a second dose of PTI-808. Subjects will be followed for up to 7 days following dosing.

Part 2 of this will enroll healthy volunteers to assess the safety, tolerability, and PK of PTI 808 co administered with PTI 801 and PTI 428 to HVs with daily dosing for 7 consecutive days.

Part 3 - Part 3 will enroll adult subjects with CF to assess the safety, tolerability, and PK of multiple ascending doses of PTI-808 co-administered with PTI-801 and PTI-428. Subjects will receive 7 days of PTI-808 or placebo followed by 14 days of PTI-808 or placebo co-administered with PTI-801+PTI-428 or matching placebos.

Part 4 - Part 4 will assess the safety, tolerability, PK, and the effects of PTI-808 co-administered with PTI-801 with or without PTI-428 over a 28-day treatment period in CF subjects who are either homozygous for the F508del CFTR genotype or are heterozygous for the F508del CFTR genotype. Subjects will be randomized to receive treatment with PTI-808 co-administered with PTI-801 with or without PTI-428 versus matching placebo.


Recruitment information / eligibility

Status Completed
Enrollment 179
Est. completion date December 23, 2019
Est. primary completion date December 23, 2019
Accepts healthy volunteers Accepts Healthy Volunteers
Gender All
Age group 18 Years to 99 Years
Eligibility Part 1 and Part 2 Inclusion Criteria:

1. Adults aged 18 to 55 years old, inclusive, at the time of informed consent

2. Body mass index =18 and <30 kg/m2

3. Subject must be a non-smoker and non-tobacco user for a minimum of 30 days prior to screening and for the duration of the study.

4. Subject understands the full nature and purpose of the study, including possible risks and side effects, and is willing and able to comply with all compulsory study procedures and provides informed consent/permission prior to any study procedures being performed.

5. Females of childbearing potential and males capable of fathering a child must meet the contraception requirements

Part 1 & Part 2 Exclusion Criteria:

1. History or current evidence of any clinically significant cardiac, endocrinologic, hematologic, hepatobiliary, immunologic, metabolic, urologic, pulmonary, neurologic, dermatologic, psychiatric, renal, or other major disease, as determined by the investigator

2. Prolonged QT interval with Fridericia's correction >450 msec at screening

3. Abnormal liver function as defined by aspartate transaminase (AST), alanine transaminase (ALT), or bilirubin >1.5× the upper limit of the normal range

4. Abnormal renal function at screening defined as creatinine clearance <90 mL/min using the Cockroft-Gault equation

5. Clinically significant screening results that would exclude subject from the study (e.g., medical histories, PE, ECGs, vital signs, and laboratory profiles) as deemed by the investigator

6. Participation in another clinical study or treatment with an investigational agent within 30 days or five half-lives, whichever is longer, prior to Study Day 1

7. History of cancer within the past 5 years (excluding non-melanoma skin cancer)

8. History or current evidence of alcohol or drug abuse or dependence within 12 months of screening as determined by the investigator

9. Positive urine screen for prohibited drugs (cocaine, cannabinoids, nicotine [urine cotinine is the detection mechanism for nicotine], opiates, barbiturates, amphetamines, and benzodiazepines) or positive alcohol test at screening

10. Positive blood screen for human immunodeficiency virus (HIV), hepatitis B surface antigen (HBsAg), or hepatitis C virus antibody (HCVAb)

11. Clinically significant infection within 3 months of screening as determined by the investigator

12. Known or suspected hypersensitivity or idiosyncratic reaction to study medication or any components thereof

13. Has donated blood within 3 months of screening or plans to donate blood within 3 months of study completion

14. Pregnant or nursing women

15. Any conditions that, in the opinion of the investigator, would make the subject unsuitable for enrollment or could interfere with the subject's participation in or completion of the study

16. Use of prohibited medications within 14 days prior to dosing of study drug

Part 3 CF Inclusion Criteria:

1. Confirmed diagnosis of CF with the F508del/F508del genotype

2. Forced expiratory volume in 1 second (FEV1) 40-90% predicted, inclusive

3. Non-smoker and non-tobacco user for a minimum of 30 days prior to screening

Part 3 CF Exclusion Criteria:

1. Participation in another clinical trial or treatment with an investigational agent within 28 days or 5 half-lives, whichever is longer, prior to Study Day 1

2. History of cancer within the past 5 years (excluding cervical cancer in situ with curative therapy for at least one year prior to screening and non-melanoma skin cancer)

3. History of organ transplantation

4. Hospitalization, sinopulmonary infection, CF exacerbation, or other clinically significant infection or illness (as determined by the investigator) requiring an increase or addition of medication, such as antibiotics or corticosteroids, within 14 days of Day 1

5. Initiation of any new chronic therapy (e.g., ibuprofen, hypertonic saline, azithromycin, Pulmozyme®, Cayston®, TOBI®)) or any change in chronic therapy (excluding pancreatic enzyme replacement therapy) within 28 days prior to Day 1

6. History or current evidence of alcohol or drug abuse or dependence within 12 months of screening as determined by the investigator

7. Pregnant or nursing women

8. Currently taking or has taken a CFTR modulator within 30 days prior to initial dose of study drugs

Part 4 CF Inclusion Criteria:

1. Confirmed diagnosis of CF with either the F508del CFTR homozygous genotype on record or for heterozygote subjects, only one copy of the F508del CFTR mutation on record

2. Forced expiratory volume in 1 second (FEV1) 40-90% predicted, inclusive

3. Non-smoker and non-tobacco user for a minimum of 30 days prior to screening

Part 4 CF Exclusion Criteria:

1. Participation in another clinical trial or treatment with an investigational agent within 28 days or 5 half-lives, whichever is longer, prior to Study Day 1

2. History of cancer within the past 5 years (excluding cervical cancer in situ with curative therapy for at least one year prior to screening and non-melanoma skin cancer)

3. History of organ transplantation

4. Hospitalization, sinopulmonary infection, CF exacerbation, or other clinically significant infection or illness (as determined by the investigator) requiring an increase or addition of medication, such as antibiotics or corticosteroids, within 28 days of Day 1

5. Initiation of any new chronic therapy (e.g., ibuprofen, hypertonic saline, azithromycin, Pulmozyme®, Cayston®, TOBI®)) or any change in chronic therapy (excluding pancreatic enzyme replacement therapy) within 28 days of Day 1

6. History or current evidence of alcohol or drug abuse or dependence within 12 months of screening as determined by the investigator

7. Pregnant or nursing women

8. Currently taking or has taken a CFTR modulator within 14 days prior to the screening visit

Study Design


Intervention

Drug:
PTI-808
Active
Placebo
Placebo
PTI-428
Active
PTI-801
Active

Locations

Country Name City State
Australia John Hunter Hospital Lambton New South Wales
Belgium Universitair ziekenhuis Brussel Brussels
Belgium UZ Leuven Leuven
Canada Centre hospitalier de l'Université de Montréal (CHUM) Montréal Quebec
Canada McGill University Health Centre Montréal Quebec
Canada Institut universitaire de cardiologie et de pneumologie de Québec-Université Laval Québec
Canada St. Paul's Hospital Vancouver British Columbia
Denmark University of Copenhagen Rigshospitalet Copenhagen
France Hospices Civils de Lyon Lyon
France Hôpital Guillaume-et-René-Laennec Nantes Loire-Atlantique
France Hôpital Pasteur Nice Alpes-Maritimes
France Hôpital Cochin Paris
France Hôpital Haut Lévêque Pessac Gironde
France Hôpital Maison Blanche Maladies respiratoires et allergologie Reims Marne
Germany Charité Universitätsmedizin Berlin Berlin
Germany University Hospital Cologne Cologne
Germany Universitätsklinikum Essen Essen
Germany Klinikum der J.W. Goethe Universität Frankfurt
Germany Klinikum des Universität München München
New Zealand Auckland Clinical Studies Ltd. Grafton Auckland
United Kingdom Belfast City Hospital Belfast
United Kingdom Birmingham Heartlands Hospital Birmingham West Midlands
United Kingdom Western General Hospital Edinburgh Scotland
United Kingdom Royal Devon and Exeter Hospital Exeter Devon
United Kingdom King's College Hospital London
United Kingdom University Hospital Southampton Southampton
United States Central Florida Pulmonary Group Altamonte Springs Florida
United States Michigan Medicine, University of Michigan Ann Arbor Michigan
United States Emory Children's Center Atlanta Georgia
United States Johns Hopkins University Baltimore Maryland
United States Billings Clinic Billings Montana
United States Boston Children's Hospital Boston Massachusetts
United States Massachusetts General Hospital Boston Massachusetts
United States University of North Carolina at Chapel Hill Chapel Hill North Carolina
United States Medical University of South Carolina Charleston South Carolina
United States Northwestern Memorial Hospital Chicago Illinois
United States National Jewish Health Denver Colorado
United States Harper University Hospital Detroit Michigan
United States Children's Mercy Kansas City Missouri
United States Dartmouth Hitchcock Medical Center Lebanon New Hampshire
United States University of Minnesota Minneapolis Minnesota
United States University of Nebraska Medical Center Omaha Nebraska
United States Children's Hospital of Philadelphia Philadelphia Pennsylvania
United States University of Utah Salt Lake City Utah
United States ICON Early Phase Services San Antonio Texas
United States Stanford University Medical Center Stanford California
United States Banner University of Arizona Medical Center Tucson Arizona
United States New York Medical College Valhalla New York

Sponsors (1)

Lead Sponsor Collaborator
Proteostasis Therapeutics, Inc.

Countries where clinical trial is conducted

United States,  Australia,  Belgium,  Canada,  Denmark,  France,  Germany,  New Zealand,  United Kingdom, 

Outcome

Type Measure Description Time frame Safety issue
Other Part 2 Nasal biomarker change in nasal epithelial mRNA and protein over time Baseline up to 14 days
Other Part 3 CF Sweat Chloride Change in sweat chloride concentrations over time Baseline up to 28 days
Other Part 3 CF Nasal biomarker Change in nasal epithelial mRNA and protein expression over time Baseline up to 28 days
Other Part 4 CF Weight and BMI Change in weight and BMI over time Baseline up to 42 days
Other Part 4 CF Blood Glucose Change in blood glucose over time Baseline up to 42 days
Other Part 4 CF disease-specific health related quality of life Change in disease-specific health related quality of life over time Baseline up to 42 days
Other Part 4 CF Nasal biomarker Change in nasal epithelial mRNA and protein expression over time Baseline up to 42 days
Primary Part 1 SAD and MAD: Adverse Events Safety and tolerability measure by number of subjects who experience adverse events Baseline to up to 14 days
Primary Part 1 SAD and MAD: Physical Exams Safety and tolerability measure by number of subjects who experience potential clinically significant changes in physical examinations Baseline to up to 14 days
Primary Part 1 SAD and MAD: The number of subjects who experience potential clinically significant changes in vital signs Safety and tolerability measure by number of subjects who experience potential clinically significant changes in vital signs Baseline to up to 14 days
Primary Part 1 SAD and MAD: ECGs Safety and tolerability measure by number of subjects who experience potential clinically significant changes in ECGs Baseline to up to 14 days
Primary Part 1 SAD and MAD: The number of subjects who experience potential clinically significant changes in safety labs Safety and tolerability measure by number of subjects who experience potential clinically significant changes in safety labs Baseline to up to 14 days
Primary Part 1 SAD and FE: terminal half life Apparent terminal half-life (t1/2) of single oral dose Through 72 hours post dose
Primary Part 1 SAD and FE : Tmax Time to reach maximum plasma concentration (Tmax) of single oral dose Through 72 hours post dose
Primary Part 1 SAD and FE: Cmax Maximum plasma concentration (Cmax) of single oral dose Through 72 hours post dose
Primary Part 1 SAD : AUC Area under the concentration-time curve from time 0 to 24 hours post dose (AUC 0-24) of single oral dose Through 24 hours post dose
Primary Part 1 SAD and FE: AUC0 AUC from time 0 to time of last measurable concentration (AUC0-last) of single oral dose Through 72 hours post dose
Primary Part 1 SAD and FE: AUC0-inf AUC from time 0 to infinity (AUC0-inf) of single dose Through 72 hours post dose
Primary Part 1 MAD: t1/2 t1/2 of multiple oral dose Through 72 hours post dose
Primary Part 1 MAD: Tmax Tmax of multiple oral doses Through 72 hours post dose
Primary Part 1 MAD: Cmax Cmax of multiple oral doses Through 72 hours post last dose
Primary Part 1 MAD: AUC0-24 AUC0-24 of multiple oral dose Through 24 hours post last dose
Primary Part 1 MAD: AUC0-last AUC0-last of multiple oral doses Through 72 hours post last dose
Primary Part 1 MAD: Urine Cumulative amount of PTI-808 excreted unchanged in urine (Ae) as appropriate of multiple oral doses Through 24 hours post last dose
Primary Part 1 MAD: CLR Renal clearance (CLR) of multiple oral doses Through 24 hours post dose
Primary Part 2: Physical Exams Safety and tolerability measure by number of subjects who experience potential clinically significant changes in physical examinations Baseline up to 14 days
Primary Part 2: ECGs Safety and tolerability measure by number of subjects who experience potential clinically significant changes in ECGs Baseline up to 14 days
Primary Part 2: Safety Labs Safety and tolerability measure by number of subjects who experience potential clinically significant changes in safety labs Baseline up to 14 days
Primary Part 2: Vitals Signs Measure by number of subjects who experience potential clinically significant changes in vital signs Baseline up to 14 days
Primary Part 3 CF: Physical Exams Safety and tolerability measured by number of subjects who experience potential clinically significant changes in physical examinations Baseline up to 28 days
Primary Part 3 CF: ECGs Safety and tolerability measured by number of subjects who experience potential clinically significant changes in ECGs Baseline up to 28 days
Primary Part 3 CF: Safety Labs Safety and tolerability measured by number of subjects who experience potential clinically significant changes in safety labs Baseline up to 28 days
Primary Part 3 CF: Vital Signs Measured by number of subjects who experience potential clinically significant changes in vital signs Baseline up to 28 days
Primary Part 4 CF: Physical Exams Safety and tolerability measured by number of subjects who experience potential clinically significant changes in physical examinations Baseline up to 42 days
Primary Part 4 CF: ECGs Safety and tolerability measured by number of subjects who experience potential clinically significant changes in ECGs Baseline up to 42 days
Primary Part 4 CF: Safety Labs Safety and tolerability measured by number of subjects who experience potential clinically significant changes in safety labs Baseline up to 42 days
Primary Part 4 CF: Vital Signs Safety and tolerability measured by number of subjects who experience potential clinically significant changes in physical examinations Baseline up to 42 days
Secondary Part 2: Apparent terminal half life (t1/2) of multiple oral doses PTI 808 is co administered with PTI 801 and PTI 428 Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 is co administered with PTI 801 and PTI 428 in healthy adults Day 1 through Day 10
Secondary Part 2: Maximum plasma concentration (Cmax) of multiple oral doses PTI 808 is co administered with PTI 801 and PTI 428 Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 is co administered with PTI 801 and PTI 428 in healthy adults Day 1 through Day 10
Secondary Part 2: Time to reach maximum plasma concentration (Tmax) of multiple oral doses PTI 808 is co administered with PTI 801 and PTI 428 Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 is co administered with PTI 801 and PTI 428 in healthy adults Day 1 through Day 10
Secondary Part 2: AUC0-last of multiple oral doses when PTI 808 is co administered with PTI 801 and PTI 428 Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 is co administered with PTI 801 and PTI 428 in healthy adults Day 1 through Day 10
Secondary Part 2: AUC from time 0 to infinity (AUC0-inf) of multiple oral doses when PTI 808 is co administered with PTI 801 and PTI 428 Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 is co administered with PTI 801 and PTI 428 in healthy adults Day 1 through Day 10
Secondary Part 3 CF: Time to reach maximum plasma concentration (Tmax) of multiple oral doses PTI 808 is co administered with PTI 801 and PTI 428 Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 is co administered with PTI 801 and PTI 428 in adults with CF Day 1 through Day 22
Secondary Part 3 CF: Maximum plasma concentration (Cmax) of multiple oral doses PTI 808 is co administered with PTI 801 and PTI 428 Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 is co administered with PTI 801 and PTI 428 in adults with CF Day 1 through Day 22
Secondary Part 3 CF: AUC0-last of multiple oral doses when PTI 808 is co administered with PTI 801 and PTI 428 Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 is co administered with PTI 801 and PTI 428 in adults with CF Day 1 through Day 22
Secondary Part 3 CF: FEV1 Change in forced expiratory volume in one second (FEV1) over time Baseline through Day 28
Secondary Part 4 CF: Time to reach maximum plasma concentration (Tmax) of multiple oral doses of PTI 808 + PTI 801 co-administered with or without PTI 428 Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 + PTI 801 is co administered with or with out PTI 428 in adults with CF Day 1 through Day 28
Secondary Part 4 CF: Maximum plasma concentration (Cmax) of multiple oral doses of PTI 808 + PTI 801 co-administered with or without PTI 428 Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 + PTI 801 is co administered with or with out PTI 428 in adults with CF Day 1 through 28
Secondary Part 4 CF: AUC0-last of multiple oral doses when PTI 808 + PTI 801 is coadministered with or without PTI 428 in adults with CF Evaluate the PK profile of PTI 808, PTI 801, and PTI 428 when PTI 808 + PTI 801 is co administered with or without PTI 428 in adults with CF Day 1 through 28
Secondary Part 4 CF: FEV1 Change in forced expiratory volume in one second (FEV1) over time Baseline through Day 42
Secondary Part 4 CF Sweat Chloride Change in sweat chloride concentrations over time Baseline through Day 42

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