Mass Balance Recovery, Metabolite Profile and Metabolite Identification of [14C]NXL104

NCT01448395 | Completed Phase 1

• 1 other identifier: D4280C00008
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

A study to look at how radiolabelled NXL104 is taken up, broken down and removed by the body when given as an injection into the blood stream.

Conditions

Healthy

Keywords

Mass Balance; Metabolite Identification and Profiling; Metabolite profile and Identification of [14C]NXL104; Mass Balance Recovery

Outcome Measures

Primary Outcomes (5)

• Mass balance after a single intravenous (IV) dose of [14C]NXL104 as generated from recovery of total radioactivity excreted in urine

  168 hours

• Routes of [14C]NXL104 metabolism and excretion measured through total radioactivity concentrations in urine

  168 hours

• Whole blood and plasma partitioning of total radioactivity through measurement of total radioactivy levels in blood

  168 hours

• Mass balance after a single intravenous (IV) dose of [14C]NXL104 as generated from recovery of total radioactivity excreted in faeces

  168 hours

• Routes of [14C]NXL104 metabolism and excretion measured through total radioactivity concentrations in faeces

  168 hours

Secondary Outcomes (3)

• IV pharmacokinetics (PK) of [14C]NXL104 through calculation of Cmax, Tmax, AUC0-infinity, T1/2, MRT, terminal elimination rate constant, amount of NXL104 (Ae), % excreted, will be calculated from NXL104 concentrations in urine and faeces

  Predose, 0.25, 0.5, 1,1.25,1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120, 144, 168 hours

• Metabolites of [14C]NXL104 in plasma, whole blood, urine and faeces calculated from plasma,urine and faces concentration levels.Identification of major metabolites in plasma,urine and faeces where possible

  Whole blood:Predose, 0.25, 0.5, 1,1.25,1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120, 144, 168 hoursUrine and Faeces samples Predose-144 hours

• Safety and tolerability of NXL104 as number of patients with adverse events and assessment of Electrocardiogram (ECG) and vital signs results

  Electrocardiogram (ECG) recordings at Screening Pre-dose, 1 ,24 and 168 hoursContinuous ECG monitoring 0-1 hourVital signs measurements screening pre-dose, 0.5, 1, 2, 24 and 168 hours

Study Arms (1)

1

EXPERIMENTAL

Drug: [14C]NXL104

Interventions

[14C]NXL104 DRUG

500mg/100mL intravenous solution

1

Eligibility Criteria

• Age: 30 Years - 65 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Provision of informed consent prior to any study specific procedures.
• Healthy male subjects aged 30-65 years inclusive.
• Male subjects should be willing to use an adequate method of contraception (as defined in Section 5.1) from the day of dosing until 3 months after dosing with the investigational product.
• 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.
• Clinically normal physical examination and laboratory findings as judged by the investigator, including negative test results for drug abuse, alcohol, CO breath test and negative test results for Hepatitis B surface antigen, antibodies to Hepatitis C.

You may not qualify if:

• Any clinically significant disease or disorder (e.g. cardiovascular, pulmonary, gastrointestinal, liver, renal, neurological, musculoskeletal, endocrine, metabolic, malignant, psychiatric, major physical impairment).
• Any clinically relevant abnormal findings in physical examination, vital signs, clinical chemistry, haematology, urinalysis, which, in the opinion of the investigator, may put the subject at risk because of his participation in the study.
• QTc \> 450 ms or QT \> 500 ms or other ECG abnormality making interpretation more difficult, as judged by the investigator, or a history of additional risk factors for Torsades de Points (eg heart failure, hypokalemia, family history of long QT syndrome).
• Radiation exposure from clinical studies, including that from the present study, excluding background radiation but including diagnostic X-rays and other medical exposures, exceeding 5 mSv in the last twelve months or 10 mSv in the last five years.
• Participation in another clinical study with an investigational product during the last 3 months.

Sponsors & Collaborators

• Pfizer: lead

Study Sites (1)

Study site

Ruddington, Nottingham, United Kingdom

Location

Related Links

• Redacted CSP

Study Officials

• Paul Newell, MD

  AstraZeneca

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: September 30, 2011
• First Posted: October 7, 2011
• Study Start: October 1, 2011
• Primary Completion: November 1, 2011
• Study Completion: November 1, 2011
• Last Updated: September 1, 2017

Record last verified: 2017-08

Locations

GB (1)