Comparative Bioavailability of XS004 (Dasatinib) Formulation G and SPRYCEL® (Dasatinib) in Healthy, Adult Subjects Under Fasting Conditions

An Open Label, Balanced, Randomized, Two-Treatment, Two-Sequence, Four-Period, Full Replicate, Crossover, Single Dose, Oral Comparative Bioavailability Study of XS004 (Dasatinib) 100 mg Film-Coated Tablets, Formulation G of Xspray Pharma AB, Sweden, and SPRYCEL® (Dasatinib) 140 mg Film-Coated Tablets of Bristol-Myers Squibb Company, Princeton, NJ 08543 USA in Healthy, Adult Subjects Under Fasting Conditions

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT05439408

Enrollment

110

Registered

2022-06-30

Start date

2021-06-07

Completion date

2021-06-25

Last updated

2022-06-30

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Biological Availability

Brief summary

An open label, single-center, balanced, randomized, two-treatment, two-sequence, four-period, full replicate, crossover, single dose, Phase I, oral comparative bioavailability study in healthy, adult participants (male subjects and female subjects of non-childbearing potential) under fasting conditions with a screening period of 21 days prior to enrollment. In each study period, 21 blood samples were collected from each participant to analyze the pharmacokinetic profile of the test as well as the reference drug.

Interventions

DRUGDasatinib ASD 100 mg

XS004 Dasatinib Amorphous Solid Dispersion Film-Coated Tablet, 100 mg Test Formulation

DRUGDasatinib 140 MG [Sprycel]

SPRYCEL® (dasatinib) 140 mg Film-Coated Tablets

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

OTHER

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

* Healthy males (sterile or using contraception) or females of non-childbearing potential 18 and 55 years of age * Acceptable medical history, physical examination, laboratory investigations within 21 days prior to enrollment * Clinical laboratory values were within the laboratory's stated normal range. If not within this range, they must be without clinical significance, as determined by the Investigator * The subject is able to communicate meaningfully with study personnel and is anticipated to be able to comply fully with study procedures

Exclusion criteria

* Any history of impairment of cardiovascular, pulmonary, hepatic, renal, gastrointestinal, endocrine, immunological, dermatological, neurological, psychiatric disease or disorder * Participated in any other clinical study or donated blood in last 90 days * Positive screens for serum hepatitis B surface antigen (HbsAg), hepatitis C antibody (HepC) or human immunodeficiency virus (HIV) * Female subjects demonstrating a positive pregnancy screen, currently breastfeeding or using hormone replacement therapy within three months prior to dosing of test product

Design outcomes

Primary

Measure	Time frame	Description
Maximum Observed Plasma Concentration (Cmax) of XS004 and SPRYCEL®	For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.	The pharmacokinetic parameters (Cmax) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods.
Area Under the Plasma Concentration-Time Curve from Zero to the Last Measurable Concentration (AUC0-t) of XS004 and SPRYCEL®	For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.	The pharmacokinetic parameters (AUC 0-t) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods.
Area Under the Plasma Concentration-Time Curve from Zero Extrapolated to Infinity (AUC0-inf) of XS004 and SPRYCEL®	For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.	The pharmacokinetic parameters (AUC 0-inf) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods.

Secondary

Measure	Time frame	Description
Elimination Rate Constant (Kel) of XS004 and SPRYCEL®	For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.	The pharmacokinetic parameters (Kel) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods. Apparent first-order terminal elimination rate constant calculated from a semi-log plot of the plasma concentration versus time curve.
Area Under the Plasma Concentration-Time Curve (Percent Extrapolation) of XS004 and SPRYCEL®	For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.	The pharmacokinetic parameters (AUC %Extrap) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods.
Upper Limit on Time for Elimination Rate Constant (Kel_upper) of XS004 and SPRYCEL®	For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.	The pharmacokinetic parameters (Kel\_upper) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods. Apparent first-order terminal elimination rate constant calculated from a semi-log plot of the plasma concentration versus time curve. Kel\_upper is the upper limit on time for the elimination rate constant.
Lower Limit on Time for Elimination Rate Constant (Kel_lower) of XS004 and SPRYCEL®	For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.	The pharmacokinetic parameters (Kel\_lower) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods. Apparent first-order terminal elimination rate constant calculated from a semi-log plot of the plasma concentration versus time curve. Kel\_lower is the lower limit on time for the elimination rate constant.
Time of Maximum Observed Plasma Concentration (Tmax) of XS004 and SPRYCEL®	For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.	The pharmacokinetic parameters (Tmax) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods.
Terminal Half-Life (T1/2) of XS004 and SPRYCEL®	For each study period, blood samples were drawn at pre-dose (0.00) and at 0.25, 0.33, 0.50, 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, 2.50, 3.00, 4.00, 5.00, 6.00, 8.00, 12.00, 16.00, 20.00, 24.00, and 30.00 hours post-dose.	The pharmacokinetic parameters (T1/2) were determined for the test and reference products (XS004 and SPRYCEL®, respectively) for each subject using non-compartmental methods.

Countries

India

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026