Clinical trial NCT01931761: Study Evaluating Absorption, Distribution, Metabolism and Excretion (ADME) of Single Dose [14C] Selumetinib in Volunteers
Official title: A Phase I, Single-centre, Non-randomised, Open-label, Pharmacokinetic and Mass Balance Study of Orally Administered [14C]-Selumetinib in Healthy Male Volunteers
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Solid Tumours
Keywords: Pharmacokinetics, mass balance, AZD6244
Lead sponsor: AstraZeneca
Sponsor class: INDUSTRY
First posted: 2013-08-29
Enrollment: 6
Sex: MALE
Minimum age (years): 50
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: NON_RANDOMIZED
Intervention model: SINGLE_GROUP
Primary purpose: BASIC_SCIENCE

Brief summary: To evaluate the absorption, distribution, metabolism and excretion (ADME) of single dose \[14C\] selumetinib in volunteers


Eligibility criteria: 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.

Primary outcomes:
measure: Concentration of total radioactivity in blood and plasma and percentage of radioactive dose in urine and faeces and total balance
timeFrame: Samples collected prior to treatment, during treatment and follow-up for a maximum of 14 days
Secondary outcomes:
measure: Metabolite profiling and identification in plasma and excreta
timeFrame: Samples collected prior to treatment, during treatment and follow-up for a maximum of 14 days.
measure: Pharmacokinetic parameters of selumetinib
timeFrame: Samples collected prior to treatment, during treatment and follow-up for a maximum of 14 days.
measure: Plasma concentrations of selumetinib
timeFrame: Samples collected prior to treatment, during treatment and follow-up for a maximum of 14 days
measure: Safety
timeFrame: Assessments prior to treatment and after treatment including follow up.
Other outcomes:
Locations:
city: Ruddington
country: United Kingdom
facility: Research Site
Study officials:
affiliation: University of Aberdeen
name: Stuart Mair, MD
role: PRINCIPAL_INVESTIGATOR
References:
citation: Dymond AW, Howes C, Pattison C, So K, Mariani G, Savage M, Mair S, Ford G, Martin P. Metabolism, Excretion, and Pharmacokinetics of Selumetinib, an MEK1/2 inhibitor, in Healthy Adult Male Subjects. Clin Ther. 2016 Nov;38(11):2447-2458. doi: 10.1016/j.clinthera.2016.09.002. Epub 2016 Oct 15.