Absorption, Distribution, Metabolism and Excretion (ADME) Study of TKI258 in Patients With Advanced Solid Malignancies

An Open-Label, Non-Randomized, Single-Center, Phase I Study to Determine the Absorption, Distribution, Metabolism and Excretion (ADME) of TKI258 After a Single Oral Administration of TKI258 500mg and to Assess the Preliminary Safety of TK258 400mg Once Daily in Patients With Advanced Solid Malignancies

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT00669097

Enrollment

Registered

2008-04-29

Start date

2008-04-30

Completion date

Unknown

Last updated

2020-12-21

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

Conditions

Advanced Solid Malignancies

Keywords

ADME, TKI258, RTKs inhibitor, PDGRF inhibitor, VEGFER inhibitor

Brief summary

This is a phase l study to examine Absorption, Distribution, Metabolism and Excretion of TKI258. There are 2 cohorts. Cohort 1 (4 patients) will receive single radio-labeled 500mg dose of TKI258 followed after 15 days by daily dosing of 400mg TKI258. Cohort 2 (9 patients) will receive 400mg TKI258.

Interventions

DRUGTKI258

Study design

Allocation

Intervention model

SINGLE_GROUP

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to No maximum

Healthy volunteers

Inclusion criteria

1. Aged ≥ 18 years 2. Patients with histologically confirmed solid tumor or lymphoma who are resistant/refractory to approved therapies or for whom no appropriate therapies are available. 3. WHO performance status ≤ 2 4. All previous treatment (including surgery and radiotherapy) must have been completed at least four weeks prior to study entry and any acute toxicities must have been resolved 5. Written informed consent to participate in the study

Exclusion criteria

1. Primary Brain Tumors or symptomatic leptomeningeal metastases 2. Clinically significant cardiac impairment or unstable ischemic heart disease including a myocardial infarction within six months of study start 3. Fertile males not willing to use contraception or whose female partners are not using adequate contraceptive protection Pregnant or lactating women (all women of childbearing potential must have a negative pregnancy test (\> 5 mIU/ml) before inclusion in the study; post-menopausal women must be amenorrheic for at least 12 months). Female patients must use adequate contraceptive protection 4. Centrally located or squamous cell carcinoma of the lung 5. Proteinuria \> 1+ on dipstick testing 6. History of gastrointestinal malabsorption Surgery involving intestinal anastomosis within four weeks of study start. Other protocol-defined inclusion/

Design outcomes

Primary

Measure	Time frame
Cohort1: Find out about the routes and rates of excretion of TKI258 and its metabolites	Day 15
Cohort 2: Safety and Tolerability of TKI258	Time to patient withdrawal due to disease progression or tolerability issues

Secondary

Measure	Time frame
Cohort 1: Safety and tolerability of TKI258	Time to patient withdrawal due to disease progression or tolerability issues
Cohort 1: Preliminary anti-tumor activity of TKI258	Time to tumor progression
Preliminary Anti-tumor activity of TKI258	Time to tumor progression

Countries

Netherlands

Outcome results

None listed

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