Evaluating the Effects of Omeprazole on the Pharmacokinetics of XS004 (Dasatinib) Tablets in Healthy Adult Subjects Under Fasting Conditions

NCT05433896 | Completed Phase 1 FDA Drug

• 1 other identifier: XS004-09
• Study Type: interventional
• Target: 17
• Locations: 1 country
• Sites: 1

Brief Summary

In this open label, single-sequence study, subjects received one dose of XS004 Dasatinib Amorphous Solid Dispersion Film-Coated Tablet, 90 mg Test Formulation at the start of study on Day 1 and Day 6. Omeprazole 40 mg was administered on Day 2, 3, 4, 5 and 6. The study was conducted in two groups.

Conditions

Pharmacokinetics; Drug Interactions

Outcome Measures

Primary Outcomes (3)

• Maximum Observed Plasma Concentration of Dasatinib (Cmax)

  Pharmacokinetic parameters (Cmax) for plasma dasatinib on Day 1 (Dasatinib alone) and on Day 6 (Dasatinib + Omeprazole) calculated for each subject using drug concentration-time data by non-compartmental methods.

  Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.

• Area Under the Plasma Concentration-Time Curve from Zero to 24h

  Pharmacokinetic parameters (AUC 0-24) for plasma dasatinib on Day 1 (Dasatinib alone) and on Day 6 (Dasatinib + Omeprazole) calculated for each subject using drug concentration-time data by non-compartmental methods.

  Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.

• Area Under the Plasma Concentration-Time Curve from Zero Extrapolated to Infinity

  Pharmacokinetic parameters (AUC 0-INF) for plasma dasatinib on Day 1 (Dasatinib alone) and on Day 6 (Dasatinib + Omeprazole) calculated for each subject using drug concentration-time data by non-compartmental methods.

  Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.

Secondary Outcomes (4)

• Area Under the Plasma Concentration-Time Curve (Percent Extrapolation)

  Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.

• Time of Maximum Observed Plasma Concentration of Dasatinib (Tmax)

  Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.

• Elimination Rate Constant (Kel)

  Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.

• Terminal Half-Life (T1/2)

  Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.

Study Arms (2)

Dasatinib ASD alone

EXPERIMENTAL

At the clinic, participants were administered a single oral dose of 90 mg Dasatinib (Amorphous Solid Dispersion Film-Coated Tablet) on Day 1 after an overnight fast of at least 9 hours. Dasatinib was given with approximately 240 mL of room temperature water. Fasting continued for at least 4 hours following drug administration, after which a standardized lunch was served.

Drug: Dasatinib ASD

Dasatinib ASD + Omeprazole

OTHER

At the clinic, on Day 2 to Day 6, participants were administered a single oral dose of Omeprazole 40 mg × 1 Delayed Release Capsule once before meals in the evening with approximately 150 mL of room temperature water. No food was allowed two hours before and one hour after administration of Omeprazole. In addition, participants were administered a single oral dose of 90 mg Dasatinib (Amorphous Solid Dispersion Film-Coated Tablet) on Day 6 after an overnight fast of at least 9 hours. Dasatinib was given with approximately 240 mL of room temperature water. Fasting continued for at least 4 hours following drug administration, after which a standardized lunch was served.

Drug: Dasatinib ASD; Drug: Omeprazole 40 MG

Interventions

Dasatinib ASD DRUG

XS004 Dasatinib Amorphous Solid Dispersion Film-Coated Tablet, 90 mg Test Formulation

Dasatinib ASD + Omeprazole; Dasatinib ASD alone

Omeprazole 40 MG DRUG

Omeprazole Delayed Release Capsules, USP 40 mg

Dasatinib ASD + Omeprazole

Eligibility Criteria

• Age: 18 Years - 60 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Age: 18-60 years
• Sex: Healthy adult males (sterile or using contraception) and females of non-childbearing potential
• Clinical laboratory values should be within the laboratory's stated normal range. If not within this range, they must be without clinical significance, as determined by the Investigator
• No clinically significant diseases captured in the medical history or evidence of clinically significant findings on the physical examination (including vital signs) and/or ECG, as determined by the Investigator
• Any abnormalities/deviations from the acceptable range of medical history, laboratory values, ECG, and vital signs that might be considered clinically relevant by the study physician or Investigator will be evaluated as individual cases
• Able to comply with study procedures, in the opinion of the Investigator(s)
• Willing to give written consent, pregnancy outcome consent, and adhere to all the requirements of this protocol

You may not qualify if:

• Any major illness in the last three months or any significant ongoing chronic medical illness
• Does not agree to consume the provided meals
• Participation in any clinical trial 30 days prior to dosing
• Positive results for drugs of abuse or alcohol breath analysis prior to dosing
• Positive screening results to HIV Ag/Ab Combo, Hepatitis B surface Antigen, Hepatitis C Virus, or anti-HBc tests
• Females currently breastfeeding, demonstrating a positive pregnancy screen, or using hormone replacement therapy within three months prior to dosing

Sponsors & Collaborators

• Xspray Pharma AB: lead
• Axis Clinicals Limited: collaborator

Study Sites (1)

AXIS Clinicals

Dilworth, Minnesota, 56529-1342, United States

Location

MeSH Terms

Interventions

Omeprazole

Intervention Hierarchy (Ancestors)

2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring

Study Officials

• Per Andersson, PhD

  Xspray Pharma AB

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: June 21, 2022
• First Posted: June 27, 2022
• Study Start: November 1, 2020
• Primary Completion: December 19, 2020
• Study Completion: December 19, 2020
• Last Updated: June 27, 2022

Record last verified: 2022-06

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)