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

NCT05433896 — Phase 1, Completed, 17 participants, Xspray Pharma AB

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An Open Label, Non-Randomized, Two-Treatment, Single-Period, Single-Dose, Drug-Drug Interaction Study to Evaluate the Effects of Omeprazole on the Pharmacokinetics of XS004 (Dasatinib) 90 mg Film-Coated Tablets in Healthy Adult Subjects Under Fasting Conditions

Registry	NCT05433896
Status	Completed
Phase	Phase 1
Study type	Interventional; non randomized, sequential, masking: none, other
Enrollment	17 (Actual)
Sponsor	Xspray Pharma AB (Industry); collaborators: Axis Clinicals Limited
Conditions	Pharmacokinetics, Drug Interactions
Interventions	Dasatinib ASD, Omeprazole 40 MG (Drug)
Dates	start 2020-11-01, primary completion 2020-12-19, completion 2020-12-19, first posted 2022-06-27, last updated 2022-06-27
Locations	1 site in United States

-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.

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+Arms and interventions

Arm	Type	Interventions	Description
Dasatinib ASD alone	Experimental	Drug: Dasatinib ASD	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.
Dasatinib ASD + Omeprazole	Other	Drug: Dasatinib ASD; Drug: Omeprazole 40 MG	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.

Dasatinib ASD (Drug): XS004 Dasatinib Amorphous Solid Dispersion Film-Coated Tablet, 90 mg Test Formulation
Omeprazole 40 MG (Drug): Omeprazole Delayed Release Capsules, USP 40 mg

+Outcome measures

Primary outcomes

Maximum Observed Plasma Concentration of Dasatinib (Cmax) [Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.]: 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.
Area Under the Plasma Concentration-Time Curve from Zero to 24h [Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.]: 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.
Area Under the Plasma Concentration-Time Curve from Zero Extrapolated to Infinity [Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.]: 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.

Secondary outcomes

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.]: Pharmacokinetic parameters (AUC %Extrapolation) 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.
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.]: Pharmacokinetic parameters (Tmax) 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.
Elimination Rate Constant (Kel) [Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6.]: Pharmacokinetic parameters (Kel) 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. Apparent first order elimination rate constant calculated from a semi-log plot of plasma concentration versus time point.
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.]: Pharmacokinetic parameters (T1/2) 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.

+Eligibility

Sex: All, ages: 18 Years to 60 Years, accepts healthy volunteers

Inclusion Criteria:

* 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

Exclusion Criteria:

* 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

+Locations (1)

Facility	City	Country	Status
AXIS Clinicals	Dilworth, Minnesota	United States

+Investigators

Per Andersson, PhD, Study director, Xspray Pharma AB