Solid Tumours
Conditions
Keywords
Pharmacokinetics, mass balance, AZD6244
Brief summary
To evaluate the absorption, distribution, metabolism and excretion (ADME) of single dose \[14C\] selumetinib in volunteers
Interventions
DRUG[C14] selumetinib (oral)
Single oral administration \[C14\] 75mg
Sponsors
AstraZeneca
Study design
Allocation
NON_RANDOMIZED
Intervention model
SINGLE_GROUP
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
50 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
* Provision of signed and dated, written informed consent prior to any study specific procedures. * Have a body mass index (BMI) between 18 and 32 kg/m2 inclusive and weigh at least 50 kg and no more than 100 kg, inclusive. * Regular bowel movements (ie, on average production of at least 1 stool per day).
Exclusion criteria
* Current or past history of central serous retinopathy or retinal vein thrombosis, intraocular pressure greater than 21 mmHg or uncontrolled glaucoma. * Exposure to radiation levels above background exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years. * History or presence of any clinically significant disease or disorder in the opinion of the investigator * Any clinically important abnormalities in clinical chemistry, haematology, or urinalysis results, vital signs or ECG at baseline in the opinion of the Investigator.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Concentration of total radioactivity in blood and plasma and percentage of radioactive dose in urine and faeces and total balance | Samples collected prior to treatment, during treatment and follow-up for a maximum of 14 days |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Metabolite profiling and identification in plasma and excreta | Samples collected prior to treatment, during treatment and follow-up for a maximum of 14 days. | — |
| Pharmacokinetic parameters of selumetinib | Samples collected prior to treatment, during treatment and follow-up for a maximum of 14 days. | Cmax, tmax, t½, AUC, CL/F, Vz/F, MRT, fe, Ae, CLR |
| Plasma concentrations of selumetinib | Samples collected prior to treatment, during treatment and follow-up for a maximum of 14 days | — |
| Safety | Assessments prior to treatment and after treatment including follow up. | Adverse events, vital signs, electrocardiogram, haematology, clinical chemistry, urinalysis, physical examination, left ventricular ejection fraction, and opthalmology assessments. |
Countries
United Kingdom
Outcome results
None listed