Pharmacokinetic Analysis
Conditions
Keywords
deupirfenidone, pirfenidone, PK, pharmacokinetics, elderly
Brief summary
A three-part, randomized, double-blind study in healthy older adults to identify a dose of deupirfenidone for further clinical study.
Detailed description
A Phase 1 study to evaluate safety, tolerability, and PK in older healthy subjects of multiple twice daily (BID) or 3 times daily (TID) doses of deupirfenidone administered over 3 days compared to that of pirfenidone or placebo administered TID. The study also investigated the PK profile of deupirfenidone at steady state compared to that of pirfenidone at steady state and the effect of food on the PK profile of deupirfenidone and pirfenidone. The study was conducted in 3 parts. Part 1 was a randomized, double-blinded, two-period crossover study conducted in healthy older adults to evaluate the tolerability differentiation of BID dosing of deupirfenidone to pirfenidone. Part 2 was a randomized, double-blinded, two-period crossover study conducted in healthy older adults to evaluate the tolerability differentiation of TID dosing of deupirfenidone to pirfenidone. Part 3 was a randomized, double-blinded, parallel arm, placebo-controlled study conducted in healthy older adults to evaluate the safety and tolerability of two doses of deupirfenidone.
Interventions
Sponsors
PureTech
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
OTHER
Masking
QUADRUPLE (Subject, Caregiver, Investigator, Outcomes Assessor)
Masking description
Over-encapsulation of study drug
Intervention model description
The study was conducted in 3 parts. Part 1 was a randomized, double-blinded, two-period crossover study conducted in healthy older adults to evaluate the pharmacokinetics of BID dosing of deupirfenidone to pirfenidone. Part 2 was a randomized, double-blinded, two-period crossover study conducted in healthy older adults to evaluate the pharmacokinetics of TID dosing of deupirfenidone to pirfenidone. Part 3 was a randomized, double-blinded, parallel arm, placebo-controlled study conducted in healthy older adults to evaluate the pharmacokinetics of two doses of deupirfenidone.
Eligibility
Sex/Gender
ALL
Age
60 Years to 80 Years
Healthy volunteers
Yes
Inclusion criteria
* Male or female between 60 and 80 years old (inclusive) at the time of Screening. * In good general health at Screening, free from clinically significant laboratory values, or clinically significant unstable medical, surgical, or psychiatric illness, as determined by the Investigator. Subjects with mild, chronic, stable disease and on stable medication could be included if deemed medically prudent by the Investigator. * Has a body mass index (BMI) between ≥18.0 and ≤50.0 kg/m2 at Screening.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Part 1: Cmax of BID deupirfenidone versus TID pirfenidone | 14 days | To compare the Cmax of 850 mg BID dosing of deupirfenidone to 801 mg TID dosing of pirfenidone at steady state, in older healthy subjects, when administered in a two-period crossover design. |
| Part 2: Cmax of TID deupirfenidone versus TID pirfenidone | 14 days | To compare the Cmax of 550 mg TID deupirfenidone to 801 mg TID pirfenidone at steady state in older healthy subjects, when administered in a two-period crossover design. |
| Part 3: Cmax of TID deupirfenidone versus placebo | 6 days | To evaluate the Cmax of two doses of deupirfenidone. |
| Part 1: AUC of BID deupirfenidone versus TID pirfenidone | 14 Days | To compare the AUC of 850 mg BID dosing of deupirfenidone to 801 mg TID dosing of pirfenidone at steady state, in older healthy subjects, when administered in a two-period crossover design. |
| Part 1: Tmax of BID deupirfenidone versus TID pirfenidone | 14 Days | To compare the Tmax of 850 mg BID dosing of deupirfenidone to 801 mg TID dosing of pirfenidone at steady state, in older healthy subjects, when administered in a two-period crossover design. |
| Part 2: AUC of TID deupirfenidone versus TID pirfenidone | 14 Days | To compare the AUC of 550 mg TID deupirfenidone to 801 mg TID pirfenidone at steady state in older healthy subjects, when administered in a two-period crossover design. |
| Part 2: Tmax of TID deupirfenidone versus TID pirfenidone | 14 Days | To compare the Tmax of 550 mg TID deupirfenidone to 801 mg TID pirfenidone at steady state in older healthy subjects, when administered in a two-period crossover design. |
| Part 3: AUC of TID deupirfenidone versus placebo | 6 Days | To evaluate the AUC of two doses of deupirfenidone. |
| Part 3: PK profile of TID deupirfenidone versus placebo | 6 Days | To evaluate the Tmax of two doses of deupirfenidone. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Part 1: The effect of food on the Cmax of BID deupirfenidone versus TID pirfenidone | 1 day | To compare the Cmax of 850 mg BID dosing of deupirfenidone to 801 mg TID dosing of pirfenidone at steady state, in older healthy subjects, when administered with food on the last day of dosing prior to wash-out in a two-period crossover design. |
| Part 2: The effect of food on the Cmax of TID deupirfenidone versus TID pirfenidone | 1 day | To compare the Cmax of 550 mg TID deupirfenidone to 801 mg TID pirfenidone at steady state in older healthy subjects, when administered with food on the last day of dosing prior to wash-out in a two-period crossover design. |
| Part 1: The effect of food on the AUC of BID deupirfenidone versus TID pirfenidone | 6 Days | To compare the AUC of 850 mg BID dosing of deupirfenidone to 801 mg TID dosing of pirfenidone at steady state, in older healthy subjects, when administered with food on the last day of dosing prior to wash-out in a two-period crossover design. |
| Part 1: The effect of food on the Tmax of BID deupirfenidone versus TID pirfenidone | 1 Day | To compare the Tmax of 850 mg BID dosing of deupirfenidone to 801 mg TID dosing of pirfenidone at steady state, in older healthy subjects, when administered with food on the last day of dosing prior to wash-out in a two-period crossover design. |
| Part 2: The effect of food on the AUC of TID deupirfenidone versus TID pirfenidone | 1 Day | To compare the AUC of 550 mg TID deupirfenidone to 801 mg TID pirfenidone at steady state in older healthy subjects, when administered with food on the last day of dosing prior to wash-out in a two-period crossover design. |
| Part 2: The effect of food on the Tmax of TID deupirfenidone versus TID pirfenidone | 1 Day | To compare the Tmax of 550 mg TID deupirfenidone to 801 mg TID pirfenidone at steady state in older healthy subjects, when administered with food on the last day of dosing prior to wash-out in a two-period crossover design. |
Countries
United States
Contacts
PRINCIPAL_INVESTIGATORSteven H Reynolds, DO
Collaborative Neuroscience Network, LLC.
PRINCIPAL_INVESTIGATORMichael A Hassman, DO
Hassman Research
PRINCIPAL_INVESTIGATORBruce G Rankin, DO
Accel Research Sites
Outcome results
None listed