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OpenTrials
Active, Not Recruiting

NCT Number: NCT00463814

AZD6244 (ARRY-142886) Solid Oral Dosage Formulation in Participants With Advanced Solid Malignancies

The primary purpose of the study is to assess the safety, tolerability and pharmacokinetics of a capsule of AZD6244 in participants with advanced solid malignancies.

Active, Not Recruiting

This study is active but is not currently recruiting participants.

Key information

Conditions

Tumor Cancer Neoplasms

Age range

18 year–99 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Research Site, Nijmegen, Netherlands

Loading trial locations.

Who can participate

Healthy volunteers accepted: No

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • cancer which is refractory to standard therapies
  • World Health Organization (WHO) performance status 0 to 2
  • evidence of post-menopausal status or negative pregnancy test

Exclusion criteria

  • Radiotherapy/chemotherapy within 21 days prior to entry
  • brain metastases/spinal cord compression unless stable off steroids/anticonvulsants
  • evidence of severe/uncontrolled systemic disease
  • participated in an investigational drug study within 30 days

Treatment and study plan

AZD6244

Drug

Participants will receive single oral dose of AZD6244 as described in arm description.

Other names: ARRY-142886

Primary outcomes

  1. Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Treatment-emergent Serious Adverse Events (TESAEs) in Part A and Part B

    Time frame: Day 1 through 11.8 months (maximum observed duration)

    An adverse event (AE) is any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. A serious adverse event (SAE) is an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. The TEAEs are defined as events present at baseline that worsened in intensity after administration of study drug or events absent at baseline that emerged after administration of study drug.

  2. Number of Participants With Abnormal Clinical Laboratory Parameters Reported as TEAEs in Part A and Part B

    Time frame: Day 1 through 11.8 months (maximum observed duration)

    Number of participants with abnormal clinical laboratory parameters reported as TEAEs are reported. Abnormal clinical laboratory parameters defined as any abnormal finding during analysis of hematology, clinical chemistry, and urinalysis.

  3. Number of Participants With Abnormal Vital Signs Reported as TEAEs in Part A and Part B

    Time frame: Day 1 through 11.8 months (maximum observed duration)

    Number of participants with abnormal vital signs reported as TEAEs are reported. Abnormal vital signs are defined as any abnormal finding in the vital sign parameters (blood pressure, oxygen saturation, weight, and pulse rate).

  4. Number of Participants With Abnormal Echocardiogram (ECHO) Parameters Reported as TEAEs in Part A and Part B

    Time frame: Day 1 through 11.8 months (maximum observed duration)

    Number of participants with abnormal ECHO parameters reported as TEAEs are reported.

  5. Number of Participants With Abnormal Electrocardiogram (ECG) Parameters Reported as TEAEs in Part A and Part B

    Time frame: Day 1 through 11.8 months (maximum observed duration)

    Number of participants with abnormal ECG parameters reported as TEAEs are reported.

Secondary outcomes

  1. Maximum Plasma Concentration (Cmax) of AZD6244 (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose; Day 8: Pre-dose (within 10 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, and 12 hours post-dose

    The Cmax of AZD6244 in Part A is reported.

  2. Cmax of AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The Cmax of AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  3. Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUC) of AZD6244 (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The AUC of AZD6244 in Part A is reported.

  4. Area Under the Plasma Concentration-time Curve From Time Zero to 12 Hours Post Dose (AUC[0-12]) of AZD6244 (Part A)

    Time frame: Day 8: Pre-dose (within 10 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, and 12 hours post-dose

    The AUC(0-12) of AZD6244 in Part A is reported.

  5. AUC of AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The AUC of AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  6. Area Under the Plasma Concentration-time Curve From Time Zero to 24 Hours Post Dose (AUC[0-24]) of AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The AUC(0-24) of AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  7. Time to Reach Maximum Plasma Concentration (Tmax) of AZD6244 (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose; Day 8: Pre-dose (within 10 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, and 12 hours post-dose

    The Tmax of AZD6244 in Part A is reported.

  8. Tmax of AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The Tmax of AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  9. Half-life (t1/2) of AZD6244 (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The t1/2 of AZD6244 in Part A is reported.

  10. t1/2 of AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The t1/2 of AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  11. Total Apparent Drug Clearance (CL/F) of AZD6244 (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose; Day 8: Pre-dose (within 10 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, and 12 hours post-dose

    The CL/F of AZD6244 in Part A is reported.

  12. CL/F of AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The CL/F of AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  13. Volume of Distribution at Steady State (Vss/F) of AZD6244 (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The Vss/F of AZD6244 in Part A is reported.

  14. Vss/F of AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The Vss/F of AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  15. Cmax of N-desmethyl AZD6244 (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose; Day 8: Pre-dose (within 10 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, and 12 hours post-dose

    The Cmax of N-desmethyl AZD6244 in Part A is reported.

  16. Cmax of N-desmethyl AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The Cmax of N-desmethyl AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  17. AUC of N-desmethyl AZD6244 (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The AUC of N-desmethyl AZD6244 in Part A is reported.

  18. AUC(0-12) of N-desmethyl AZD6244 (Part A)

    Time frame: Day 8: Pre-dose (within 10 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, and 12 hours post-dose

    The AUC(0-12) of N-desmethyl AZD6244 in Part A is reported.

  19. AUC of N-desmethyl AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The AUC of N-desmethyl AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  20. AUC(0-24) of N-desmethyl AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The AUC(0-24) of N-desmethyl AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  21. Tmax of N-desmethyl AZD6244 (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose; Day 8: Pre-dose (within 10 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, and 12 hours post-dose

    The Tmax of N-desmethyl AZD6244 in Part A is reported.

  22. Tmax of N-desmethyl AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The Tmax of N-desmethyl AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  23. t1/2 of N-desmethyl AZD6244 (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The t1/2 of N-desmethyl AZD6244 in Part A is reported.

  24. t1/2 of N-desmethyl AZD6244 (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The t1/2 of N-desmethyl AZD6244 in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  25. Cmax of AZD6244 Amide (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose; Day 8: Pre-dose (within 10 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, and 12 hours post-dose

    The Cmax of AZD6244 amide in Part A is reported.

  26. Cmax of AZD6244 Amide (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The Cmax of AZD6244 amide in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  27. AUC(0-12) of AZD6244 Amide (Part A)

    Time frame: Day 8: Pre-dose (within 10 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, and 12 hours post-dose

    The AUC(0-12) of AZD6244 amide in Part A is reported.

  28. Area Under the Plasma Concentration-time Curve From Time Zero to 4 Hours Post Dose (AUC[0-4]) of AZD6244 Amide (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The AUC(0-4) of AZD6244 amide in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  29. AUC(0-24) of AZD6244 Amide (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The AUC(0-24) of AZD6244 amide in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  30. Tmax of AZD6244 Amide (Part A)

    Time frame: Day 1: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose; Day 8: Pre-dose (within 10 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, and 12 hours post-dose

    The Tmax of AZD6244 amide in Part A is reported.

  31. Tmax of AZD6244 Amide (Part B Single Dose)

    Time frame: Days 1 and 8: Pre-dose (within 30 minutes of dosing); 5, 15, and 30 minutes, 1, 1.5, 2, 4, 8, 12, and 24 hours post-dose

    The Tmax of AZD6244 amide in Part B is reported. Day 1 and Day 8 in Part B are the first days of two periods in crossover bioavailability assessment of two AZD6244 formulations: capsule versus the free-base suspension.

  32. Cmax of AZD6244 (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The Cmax of AZD6244 in Part B is reported.

  33. Tmax of AZD6244 (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The Tmax of AZD6244 in Part B is reported.

  34. AUC(0-4) of AZD6244 (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The AUC(0-4) of AZD6244 in Part B is reported.

  35. Area Under the Plasma Concentration-time Curve From Time Zero to Time of the Last Quantifiable Concentration (AUC[0-t]) of AZD6244 (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The AUC(0-t) of AZD6244 in Part B is reported.

  36. Cmax of N-desmethyl AZD6244 (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The Cmax of N-desmethyl AZD6244 in Part B is reported.

  37. Tmax of N-desmethyl AZD6244 (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The Tmax of N-desmethyl AZD6244 in Part B is reported.

  38. AUC(0-4) of N-desmethyl AZD6244 (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The AUC(0-4) of N-desmethyl AZD6244 in Part B is reported.

  39. AUC(0-t) of N-desmethyl AZD6244 (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The AUC(0-t) of N-desmethyl AZD6244 in Part B is reported.

  40. Cmax of AZD6244 Amide (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The Cmax of AZD6244 amide in Part B is reported.

  41. Tmax of AZD6244 Amide (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The Tmax of AZD6244 amide in Part B is reported.

  42. AUC(0-4) of AZD6244 Amide (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The AUC(0-4) of AZD6244 amide in Part B is reported.

  43. AUC(0-t) of AZD6244 Amide (Part B Multiple Doses)

    Time frame: Days 15 and 22: Pre-dose (within 10 minutes of dosing); 1, 2, and 4 hours post-dose

    The AUC(0-t) of AZD6244 amide in Part B is reported.

  44. Percentage Inhibition of Extracellular Signal-regulated Kinase (ERK) Phosphorylation

    Time frame: 1, 4, 8, and 24 hours post-dose on Day 1 (Part A and Part B) and Day 8 (Part B)

    Percentage inhibition of ERK phosphorylation is reported.

Sponsors and collaborators

Lead sponsor

AstraZeneca

Industry

Registry information

Official study title

A Phase I, Open-Label, Multi-centre Study to Assess the Safety, Tolerability and Pharmacokinetics of a Solid Oral Dosage Formulation (Capsule) of AZD6244 in Patients With Advanced Solid Malignancies

Important dates

Study start
2007
Primary completion
2008
Study completion
2027
First posted
Apr 20, 2007
Registry last updated
May 29, 2026

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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