A Study to Learn About the Study Medication, Zavegepant, in Healthy Volunteers

NCT06137703 | Completed Phase 1 Results FDA Drug

• 2 other identifiers: BHV3500-113C5301003
• Study Type: interventional
• Target: 52
• Locations: 1 country
• Sites: 1

Brief Summary

This trial is designed to compare the rate and extent of absorption of four different formulations of zavegepant. 52 healthy male and female volunteers will receive a single dose of each formulation at least 7 days apart over a period of about 7 weeks and the amount of drug in their blood will be assessed over the 24 hour period after each dose.

Conditions

Biological Availability

Outcome Measures

Primary Outcomes (3)

• Area Under the Concentration-Time Curve From Time 0 to Infinity (AUCinf) of Zavegepant

  AUCinf was calculated as AUClast+(Clast\*/kel), where AUClast is the area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration, Clast\* is the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, and kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve. AUClast was calculated using Linear/Log trapezoidal method.

  Pre-dose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours post dose

• Maximum Observed Concentration (Cmax) of Zavegepant

  Cmax was observed directly from data.

  Pre-dose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours post dose

• AUClast of Zavegepant

  AUClast was calculated using linear/log trapezoidal method.

  Pre-dose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours post dose

Secondary Outcomes (15)

• Time to Reach Cmax (Tmax) of Zavegepant

  Pre-dose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours post dose

• Terminal Phase Half-Life (t1/2) of Zavegepant

  Pre-dose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours post dose

• Apparent Clearance (CL/F) of Zavegepant From Plasma

  Pre-dose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours post-dose

• Apparent Volume of Distribution (Vz/F) of Zavegepant

  Pre-dose, and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours post dose

• Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

  Baseline up to study exit (approximately 6.5 weeks)

Study Arms (4)

Sequence 1

EXPERIMENTAL

Period 1 - Single zavegepant 100mg non-enteric coated soft gel capsule (Treatment A) followed by at least 7 days washout; Period 2 - Two zavegepant 100mg immediate release tablets (Treatment C) followed by at least 7 days washout; Period 3 - Single zavegepant 100mg immediate release tablet (Treatment B) followed by at least 7 days washout; Period 4 - Four zavegepant 25mg enteric coated soft gel capsule (Treatment D).

Drug: Zavegepant 100mg non-enteric coated soft gel capsule; Drug: Zavegepant 100mg immediate release tablet; Drug: Zavegepant 2 x 100mg immediate release tablets; Drug: Zavegepant 4 x 25mg enteric coated soft gel capsule

Sequence 2

EXPERIMENTAL

Period 1 - Two zavegepant 100mg immediate release tablets (Treatment C) followed by at least 7 days washout; Period 2 - Four zavegepant 25mg enteric coated soft gel capsule (Treatment D) followed by at least 7 days washout; Period 3 - Single zavegepant 100mg non-enteric coated soft gel capsule (Treatment A) followed by at least 7 days washout; Period 4 - Single zavegepant 100mg immediate release tablet (Treatment B).

Drug: Zavegepant 100mg non-enteric coated soft gel capsule; Drug: Zavegepant 100mg immediate release tablet; Drug: Zavegepant 2 x 100mg immediate release tablets; Drug: Zavegepant 4 x 25mg enteric coated soft gel capsule

Sequence 3

EXPERIMENTAL

Period 1 - Single zavegepant 100mg immediate release tablet (Treatment B) followed by at least 7 days washout; Period 2 - Single zavegepant 100mg non-enteric coated soft gel capsule (Treatment A) followed by at least 7 days washout; Period 3 - Four zavegepant 25mg enteric coated soft gel capsule (Treatment D) followed by at least 7 days washout; Period 4 - Two zavegepant 100mg immediate release tablets (Treatment C).

Drug: Zavegepant 100mg non-enteric coated soft gel capsule; Drug: Zavegepant 100mg immediate release tablet; Drug: Zavegepant 2 x 100mg immediate release tablets; Drug: Zavegepant 4 x 25mg enteric coated soft gel capsule

Sequence 4

EXPERIMENTAL

Period 1 - Four zavegepant 25mg enteric coated soft gel capsule (Treatment D) followed by at least 7 days washout; Period 2 - Single zavegepant 100mg immediate release tablet (Treatment B) followed by at least 7 days washout; Period 3 - Two zavegepant 100mg immediate release tablets (Treatment C) followed by at least 7 days washout; Period 4 - Single zavegepant 100mg non-enteric coated soft gel capsule (Treatment A).

Drug: Zavegepant 100mg non-enteric coated soft gel capsule; Drug: Zavegepant 100mg immediate release tablet; Drug: Zavegepant 2 x 100mg immediate release tablets; Drug: Zavegepant 4 x 25mg enteric coated soft gel capsule

Interventions

Zavegepant 100mg non-enteric coated soft gel capsule DRUG

Zavegepant (PF-07930207/BHV3500) 100mg non-enteric coated soft gel capsule

Also known as: Treatment A

Sequence 1; Sequence 2; Sequence 3; Sequence 4

Zavegepant 100mg immediate release tablet DRUG

Zavegepant (PF-07930207/BHV3500) 100mg dodecylmaltoside dosage form immediate release tablet

Also known as: Treatment B

Sequence 1; Sequence 2; Sequence 3; Sequence 4

Zavegepant 2 x 100mg immediate release tablets DRUG

2 x Zavegepant (PF-07930207/BHV3500) 100mg dodecylmaltoside dosage form immediate release tablets - total dose 200mg

Also known as: Treatment C

Sequence 1; Sequence 2; Sequence 3; Sequence 4

Zavegepant 4 x 25mg enteric coated soft gel capsule DRUG

Zavegepant (PF-07930207/BHV3500) 25 mg enteric coated soft gel capsules - total dose 100mg

Also known as: Treatment D

Sequence 1; Sequence 2; Sequence 3; Sequence 4

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participants must provide Informed Consent Form (ICF) obtained prior to the conduct of any study activities.
• Healthy Male or female participants at least 18 and less than 56 years of age,
• Participants must be Non-smokers and not have used any nicotine-containing products for 3 months prior to screening.
• Body Mass Index (BMI) \>18.5 and \<30.0kg/m2 and body weight ≥ 50.0kg for males and ≥ 45.0kg for females.
• All females participants must not be breastfeeding and have a negative urine pregnancy test at Screening.
• Females of childbearing potential must be willing to use acceptable contraceptive methods throughout the study and for 30 days after the last study drug administration.
• Male participants with a female partner of childbearing potential must be willing to use acceptable contraceptive methods from the first study drug administration until at least 90 days after the last study drug administration.

You may not qualify if:

• Current diagnosis of viral hepatitis or a history of liver disease.
• Any history of seizure disorder (e.g., epilepsy) other than a single childhood febrile seizure.
• Current or recent (within 3 months of the first study drug administration) gastrointestinal disease that may interfere with drug absorption.
• Prior gastrointestinal surgery that interferes with absorption and motility (e.g., gastric bypass, duodenectomy or gastric banding).
• History of drug or alcohol abuse.
• History of anaphylaxis, a documented hypersensitivity reaction, or a clinically significant reaction to any drug or to any of the excipient supporting the zavegepant formulations.
• Donation of plasma within 7 days prior to dosing, or 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 dosing.
• Participation in a clinical research study involving the administration of an investigational or marketed drug or device within 30 days prior to the dosing, extended to 90 days for biological products.
• Inability or difficulty to swallow tablets or capsules.
• Subjects with any clinically significant abnormality or significant abnormal laboratory test results found during medical screening or Day-1. Positive test for human immunodeficiency virus (HIV), hepatitis B surface antigen (HBsAg), or hepatitis C virus (HCV) antibody during screening.
• Inadequate renal function - estimated glomerular filtration rate (eGFR) according to the Modification of Diet in Renal Disease (MDRD) study equation ≤ 60 mL/min/1.73 m2 at Screening.
• Any of the following laboratory parameters greater than the upper limit of normal (ULN) values at Screening or Baseline (Day -1): alkaline phosphatase (ALP) aspartate aminotransferase (AST), alanine aminotransferase (ALT), total bilirubin, direct bilirubin, and indirect bilirubin, and alkaline phosphatase.
• Any clinically significant abnormalities on 12-lead ECG or blood pressure (BP) at Screening or Baseline (Day -1) visits.
• Any clinically significant abnormal haematological laboratory test values at Screening or Baseline (Day -1) visits.
• Positive test for COVID-19 performed on Day -1 of each period.

Sponsors & Collaborators

• Pfizer: lead

Study Sites (1)

Syneos Health Clinical Research Services, Llc

Miami, Florida, 33136, United States

Location

Related Links

• To obtain contact information for a study center near you, click here.

Results Point of Contact

• Title: Pfizer ClinicalTrials.gov Call Center
• Organization: Pfizer Inc.

ClinicalTrials.gov_Inquiries@pfizer.com

1-800-718-1021

Study Officials

• Pfizer CT.gov Call Center

  Pfizer

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Masking Details: All investigators, Sponsor personnel, clinical monitors, independent PK analyst, and participants in the study will be unblinded to the treatment allocation as the primary and secondary endpoints are based on objective criteria of laboratory findings.
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: Randomized, open-label, single dose, 4-period cross-over, comparative bioavailability study in healthy volunteer participants.

Study Record Dates

• First Submitted: November 14, 2023
• First Posted: November 18, 2023
• Study Start: August 24, 2022
• Primary Completion: December 7, 2022
• Study Completion: December 7, 2022
• Last Updated: October 1, 2024
• Results First Posted: October 1, 2024

Record last verified: 2024-06

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)