Effects of Gastric pH on the Pharmacokinetics of Dasatinib

Effects of Gastric pH on the Pharmacokinetics of Dasatinib in Healthy Volunteers

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01398046

Enrollment

Registered

2011-07-20

Start date

2011-08-31

Completion date

2014-02-28

Last updated

2015-04-28

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

Conditions

Healthy

Keywords

dasatinib, betaine, betaine hydrochloride, pharmacokinetics, healthy volunteer

Brief summary

The goal of this study is to evaluate the ability of a natural supplement (betaine hydrochloride) to affect the absorption of dasatinib in healthy volunteers. The investigators predict that betaine hydrochloride will increase the absorption of dasatinib, in volunteers pre-treated with proton-pump inhibitors (PPIs).

Interventions

DRUGDasatinib

dasatinib (100mg) PO x1

DRUGDasatinib plus Rabeprazole

Rabeprazole (20mg) PO twice daily (Days 1-3); Dasatinib (100mg) PO x1 (Day 4)

DRUGDasatinib plus Rabeprazole AND Betaine Hydrochloride

Rabeprazole (20mg) PO twice daily (Days 1-3); Betaine Hydrochloride (1500mg) PO x1 AND Dasatinib (100mg) PO x1 on Day 4

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 59 Years

Healthy volunteers

Yes

Inclusion criteria

* Male or female 18-59 years of age * Healthy adult with no active medical problems or significant chronic diseases as determined by the study doctor based on history, physical exam and laboratory evaluations * BMI between 18.5-30 kg/m2 * Taking no medications 2 weeks before and during the study enrollment, including drugs of abuse, prescription or over-the-counter (OTC) medications (except acetaminophen) * Subjects able to maintain adequate birth control during the study independent of hormonal contraceptive use * Be able to provide written informed consent and comply with requirements of the study * Avoid eating grapefruit and drinking grapefruit juice from 7 days before the first study day until the completion of the entire study * Abstinence from alcoholic beverages, caffeinated beverages and orange juice from 3pm the night before a study day until completion of that study day * Fast from food and beverages at least 8 hours prior to medication dosing * Be able to read, speak, and understand English

Exclusion criteria

* Subjects with a history of gastrointestinal disease including gastroesophageal reflux disease, gastritis, peptic ulcer disease, or dyspepsia * Subjects with a fasting gastric pH of \> 4 (i.e. hypochlorhydria) * Subjects with a history of dysphagia, achalasia, or difficulty swallowing capsules, tablets, or pills * Subjects on prescription or chronic over-the-counter (OTC) medications (including hormonal contraceptives) * Subjects with known allergies to rabeprazole or any other proton pump inhibitors (PPI's) or betaine hydrochloride * Subjects who smoke tobacco * Subjects with ongoing alcohol or illegal drug use * Subjects who are pregnant, lactating, or attempting to conceive * Subjects unable to maintain adequate birth control during the study

Design outcomes

Primary

Measure	Time frame	Description
Area-Under-the Concentration Curve from zero-to-twenty two hours (AUC,0-22) of Dasatinib	Day 4	The primary outcome measure will be dasatinib area-under-the-concentration curve (AUC) values from zero-to-twenty two (0-22) hours. Values from Experiemntal Arms of the study (Dasatinib plus Rabeprazole; Dasatinib plus Rabeprazole AND Betaine Hydrochloride) will be compared against the active comparator (dasatinib alone) and tested for statistical significance.
Area-Under-the Concentration Curve from zero-to-infinity (AUC,0-inf) of Dasatinib	Day 4	The primary outcome measure will be dasatinib area-under-the-concentration curve (AUC) values from zero-to-infinite time (0-inf). Values from Experiemntal Arms of the study (Dasatinib plus Rabeprazole; Dasatinib plus Rabeprazole AND Betaine Hydrochloride) will be compared against the active comparator (dasatinib alone) and tested for statistical significance.

Secondary

Measure	Time frame	Description
Maximum Concentration of Dasatinib	Day 4	The maximum plasma concentration (Cmax) will also be measured. Values from Experiemntal Arms of the study (Dasatinib plus Rabeprazole; Dasatinib plus Rabeprazole AND Betaine Hydrochloride) will be compared against the active comparator (Dasatinib alone) and tested for statistical significance.

Countries

United States

Outcome results

None listed

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