Phase 1 Completed N=97 Randomized Triple-blind Basic Science

Study to Evaluate Safety and Tolerability of PF-07242813 in Healthy Participants and Participants With Atopic Dermatitis

Source: ClinicalTrials.gov NCT04668066 ↗

Enrolled (actual)

Serious AEs

2.5%

Results posted

Jun 2024

Primary outcomePrimary: Part 1: SAD Cohorts: Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Treatment Emergent Serious Adverse Events (TESAEs) — 0; 0; 0; 2 Participants

Summary

This is the first time PF-07242813 will be given to humans. The purpose of the study is to evaluate the safety, tolerability, and pharmacokinetics of escalating single and repeat doses of PF-07242813 in healthy participants and in participants with moderate to severe atopic dermatitis. An additional goal is to assess the pharmacodynamics of PF-07242813 in participants with moderate to severe AD, including potential effects on clinical signs and symptoms.

Outcome Measures

Outcome	Result	p-value
PRIMARY Part 1: SAD Cohorts: Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Treatment Emergent Serious Adverse Events (TESAEs)	0; 0; 0; 2; 0; 2	—
PRIMARY Part 1: MAD Cohorts: Number of Participants With TEAEs and TESAEs	3; 1; 4; 2; 2; 5	—
PRIMARY Part 2: Number of Participants With TEAEs and TESAEs	4; 5; 0; 1	—
PRIMARY Part 1: SAD Cohorts: Number of Participants With Clinically Significant Findings in Vital Signs	0; 0; 0; 0; 0; 0	—
PRIMARY Part 1: MAD Cohorts: Number of Participants With Clinically Significant Findings in Vital Signs	0; 0; 0; 0; 0; 0	—
PRIMARY Part 2: Number of Participants With Clinically Significant Findings in Vital Signs	0; 0	—
PRIMARY Part 1: SAD Cohorts: Number of Participants With Laboratory Test Abnormalities	1; 1; 1; 2; 2; 3	—
PRIMARY Part 1: MAD Cohorts: Number of Participants With Laboratory Test Abnormalities	3; 2; 5; 5; 4; 6	—
PRIMARY Part 2: Number of Participants With Laboratory Test Abnormalities	11; 9	—
PRIMARY Part 1: SAD Cohorts Only: Number of Participants With Cardiac Telemetry Abnormalities	0; 0; 0; 0; 0; 0	—
PRIMARY Part 1: SAD Cohorts: Number of Participants With Clinically Significant Findings in Electrocardiogram (ECG)	0; 0; 0; 0; 0; 0	—
PRIMARY Part 1: MAD Cohorts: Number of Participants With Clinically Significant Findings in ECG	0; 0; 0; 0; 0; 0	—
PRIMARY Part 2: Number of Participants With Clinically Significant Findings in ECG	0; 0	—
SECONDARY Part 1: SAD Cohorts: Area Under the Serum Concentration Time Profile From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) for PF-07242813	NA; NA; NA; 546200; 1834000; 9349000	—
SECONDARY Part 1: SAD Cohorts: Area Under the Serum Concentration Time Profile From Time Zero Extrapolated to Infinite Time (AUCinf) for PF-07242813	92700; 555100; 1912000; 9790000; 46510000; 153700000	—
SECONDARY Part 1: SAD Cohorts: Maximum Serum Concentration (Cmax) for PF-07242813	NA; NA; NA; 3271; 8397; 33250	—
SECONDARY Part 1: SAD Cohorts: Time to Reach Maximum Concentration (Tmax) for PF-07242813	NA; NA; NA; 2.00; 2.00; 1.61	—
SECONDARY Part 1: SAD Cohorts: Terminal Elimination Half Life (t1/2) for PF-07242813	NA; 138.0; 170.8; 256.0; 434.6; 557.8	—
SECONDARY Part 1: MAD Cohorts: Area Under the Serum Concentration Time Profile Over the Dosing Interval (AUCtau) for PF-07242813	296000; 981600; 5543000; 12560000; 27290000; 503400	—
SECONDARY Part 1: MAD Cohorts: Cmax for PF-07242813	1087; 3619; 21380; 48550; 163800; 1828	—
SECONDARY Part 1: MAD Cohorts: Tmax for PF-07242813	96.00; 216.05; 96.00; 72.00; 1.61; 168.00	—
SECONDARY Part 1: MAD Cohorts: Terminal Elimination Half Life (t1/2) for PF-07242813	111; 210.5; 352.8; 475.5; 474.0	—
SECONDARY Part 2: Percent Change From Baseline in Eczema Area and Severity Index (EASI) Total Score at Week 6	-38.2; -43.8	0.6343

Eligibility Criteria

Inclusion Criteria Part 1 (Healthy Volunteer Cohorts):

BMI of 17.5 to 30.5 kg/m2; and BW>50 kg (110 lbs)
Overtly healthy as determined by medical evaluation including medical history, physical examination, vital sign assessments, temperature, 12-lead ECGs, laboratory tests
Japanese cohort: healthy adults of Japanese descent, where parents and grandparents are Japanese
Capable of giving signed informed consent, which includes compliance with the requirements and restrictions listed in the ICD and in this protocol

Inclusion Criteria Part 2 (Atopic Dermatitis Cohort):

Have a clinical diagnosis of chronic atopic dermatitis (also known as atopic eczema) for approximately 1 year prior to Day 1 and have the diagnosis of AD confirmed (Hanifin and Rajka criteria of AD).
Either have had an inadequate response to treatment with topical medications (for at least 4 consecutive weeks within 1 year of the first dose of the study drug) OR Have a documented reason why topical treatments are considered medically inappropriate (eg, because of important side effects or safety risks) within the last year.
Have moderate to severe AD (defined as having an affected BSA (captured as part of EASI) ≥10%, IGA ≥3, and EASI ≥12 at both the screening and baseline visits).
Generally healthy adult, with no significant comorbidities.
Mild or moderate asthma that is well-controlled (not requiring high dose inhaled corticosteroids, systemic [oral or parenteral] corticosteroids, or biologic asthma treatments).
BMI of 17.5 to 40 kg/m2; and a total body weight >50 kg (110 lbs).

Exclusion Criteria Part 1 (Healthy Volunteer Cohorts):

Evidence of active, latent, or inadequately treated infection with TB; History of HIV, hepatitis B or C infection; positive testing for HIV, HepB, HepC except HepB vaccination
Medical or psychiatric condition that may increase the risk of study participation, or inappropriate for the study in investigator's judgement
History of any lymphoproliferative disorder, evidence or history of clinically significant diseases
History of systemic infection requiring hospitalization, parenteral antimicrobial therapy, or judged clinically significant by the investigator within 6 months
Known history of or evidence of current endocrine disease
Exposure to live or attenuated vaccines within 28 days of screening.
Have any malignancies or a history of malignancies except adequately treated or excised non-metastatic basal cell or squamous cell cancer of the skin, or cervical carcinoma in situ.
Allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing).
Have undergone significant trauma or major surgery within 1 month of 1st dose of study drug.
Use of prescription or nonprescription drugs, dietary or herbal supplements within 7 days or 5 half-lives (whichever is longer) prior to 1st dose of study drug.
Females taking hormone replacement therapy may be eligible to participate in this study if they are willing to discontinue therapy at least 28 days prior to the first dose of study treatment and remain off hormonal therapy for the duration of the study.
Positive urine drug test, alcohol intake more than 14 units per week or use of tobacco/nicotine containing products more than 5 cigarettes per day.
Treatment with an investigational drug within 28 days or 5 half-lives preceding the first dose of study treatment (whichever is longer).
Abnormal BP, ECG and lab tests including AST/ALT, total bilirubin and anterior pituitary hormones, at screenings and/or baseline, based on pre-specified criteria per protocol.
Unwilling or unable to comply with the Lifestyle guidance specified in this protocol (Lifestyle Considerations section).

Exclusion Criteria Part 2 (Atopic Dermatitis Cohort):

Evidence of active, latent, or inadequately treated TB.
History of or positive result for HIV or hepatitis infection. Positive Covid-19 test (if collected).
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Data sourced from ClinicalTrials.gov (NCT04668066). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.