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A Phase 1, Open-Label Study to Assess the Relative Bioavailability, Effect of Food, and Gastric pH Modification on the Pharmacokinetics of TAK-931 in Patients with Advanced Solid Tumors

Completed
Conditions
advanced cancer
Advanced solid tumors
10027655
Registration Number
NL-OMON45823
Lead Sponsor
Millenium Pharmaceuticals
Brief Summary

Not available

Detailed Description

Not available

Recruitment & Eligibility

Status
Completed
Sex
Not specified
Target Recruitment
44
Inclusion Criteria

1. Adult patients with histologically or cytologically confirmed metastatic or locally advanced or metastatic solid tumors for whom there is no available standard treatment with proven survival benefit, this therapy is not indicated, or it is refused by the patient.
2. Eastern Cooperative Oncology Group performance status of 0 to 1.
3. Adequate bone marrow reserve and renal and hepatic function based on the following laboratory parameters:
* Absolute neutrophil count *1.5 × 109/L, platelet count *75.0 × 109/L, and hemoglobin *85 g/L.
* Total bilirubin *1.5 times the institutional upper limit of the normal range (ULN) or total bilirubin <3.0 times ULN in patients with well documented Gilbert*s Syndrome.
* Serum alanine aminotransferase or aspartate aminotransferase *3.0 times the ULN (<5 times ULN if liver enzyme elevations are due to hepatocellular cancer, biliary tract cancer, or metastatic disease in the liver).
* Creatinine <1.5 times the institutional ULN or estimated creatinine clearance using the Cockcroft-Gault formula *30 mL/min for patients with serum creatinine concentrations above institutional limits.
4. Left ventricular ejection fraction *50% as measured by echocardiogram or multiple gated acquisition scan within 4 weeks before receiving the first dose of study drug.
5. Recovered to Grade 1 or baseline from all toxic effects of previous therapy (except alopecia or neuropathy).

Exclusion Criteria

1. Patients who require continuous use of PPIs or histamine-2 receptor antagonists and patients who are taking PPIs within 5 days before the first dose of study drug.
2. Treatment with clinically significant enzyme inducers, such as phenytoin, carbamazepine, enzalutamide, mitotane, ritonavir, rifampin, or St John's wort within 14 days before the first dose of study drug.
3. Treatment with systemic anticancer treatments or any investigational products within 28 days before the first dose of study drug or 5 half-lives, whichever is shorter.
4. Patients with hypertension that is unstable or not controlled despite appropriate medical therapy.
5. Patients with treated brain metastases are eligible if there is no evidence of progression for at least 4 weeks after central nervous system-directed treatment, as ascertained by clinical examination and brain imaging (magnetic resonance imaging or computed tomography) during the screening period.
6. Known history of HIV infection.
7. Known hepatitis B (HBV) surface antigen seropositive or detectable hepatitis C infection viral load. Note: Patients who have positive hepatitis B core antibody or hepatitis B surface antigen antibody can be enrolled but must have an undetectable hepatitis B viral load.
8. Known gastrointestinal (GI) disease or GI procedure that could interfere with the GI absorption of study drug, such as total gastrectomy or GI conditions that could substantially modify gastric pH or GI transit.

Study & Design

Study Type
Interventional
Study Design
Not specified
Primary Outcome Measures
NameTimeMethod
<p>Part 1<br /><br><br /><br>* Ratio of geometric mean of the following PK parameters for TAK-931 tablets in<br /><br>reference to PIC and<br /><br>associated 90% CIs:<br /><br>* Maximum observed concentration (Cmax).<br /><br>* AUC from time 0 to time of the last quantifiable concentration (AUClast).<br /><br>* AUC from time 0 to infinity (AUC*).<br /><br><br /><br>Part 2<br /><br><br /><br>* Ratio of geometric mean of the following PK parameters for TAK-931 tablets<br /><br>under fed and fasted conditions and associated 90% CIs:<br /><br>* Cmax.<br /><br>* AUClast.<br /><br>* AUC*.<br /><br>* Ratio of geometric mean of the following PK parameters for TAK-931 tablets in<br /><br>the presence and absence of esomeprazole and associated 90% CIs:<br /><br>* Cmax.<br /><br>* AUClast.<br /><br>* AUC*.<br /><br>* Summary statistics of the following PK parameters for TAK-931:<br /><br>* Cmax.<br /><br>* AUClast.<br /><br>* AUC*.</p><br>
Secondary Outcome Measures
NameTimeMethod
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