Safety, Biodistribution, Radiation Dosimetry and Pharmacokinetics Study of BAY88-8223 in Japanese Patients

This study has been completed.
Information provided by (Responsible Party):
Bayer Identifier:
First received: March 1, 2012
Last updated: May 20, 2016
Last verified: May 2016
This is an uncontrolled, open-label, non-randomized Phase I study to investigate safety, biodistribution, radiation dosimetry and pharmacokinetics of a single dose of BAY88-8223 in Japanese patients with castration-resistant prostate cancer and bone metastases.

Condition Intervention Phase
Prostatic Neoplasms
Drug: Radium-223 dichloride (Xofigo, BAY88-8223)
Phase 1

Study Type: Interventional
Study Design: Allocation: Non-Randomized
Endpoint Classification: Safety Study
Intervention Model: Parallel Assignment
Masking: Open Label
Primary Purpose: Treatment
Official Title: Uncontrolled, Open-label, Non-randomized Phase I Study to Investigate Safety, Biodistribution, Radiation Dosimetry and Pharmacokinetics of a Single Dose of BAY88-8223 in Japanese Patients With Castration-resistant Prostate Cancer and Bone Metastases

Resource links provided by NLM:

Further study details as provided by Bayer:

Primary Outcome Measures:
  • Number of participants with Critical toxicities [ Time Frame: Up to day 28 ] [ Designated as safety issue: Yes ]
    Critical toxicities (using National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) version 4.0) will be defined as the occurrence of one or more of the following drug-related toxicities: 1) ≥Grade 3 non-hematologic toxicity, 2) Grade 3 neutropenia with fever, 3) Grade 4 neutropenia that failed to recover to grade 2 or less after treatment with Granulocyte colony-stimulating factor (GCSF) within 2 weeks, 4) Grade 4 thrombocytopenia

  • Maximum drug concentration in blood after single dose administration (Cmax) of BAY88-8223 for blood samples [ Time Frame: up to 72 hours ] [ Designated as safety issue: No ]
  • Area under the concentration - time curve (AUC) of BAY88-8223 for blood samples [ Time Frame: up to 72 hours ] [ Designated as safety issue: No ]

Secondary Outcome Measures:
  • Changes in prostate specific antigen (PSA) [ Time Frame: baseline, up to 12 weeks ] [ Designated as safety issue: No ]
  • Overall Survival [ Time Frame: Up to 36 months ] [ Designated as safety issue: No ]

Enrollment: 19
Study Start Date: March 2012
Study Completion Date: April 2016
Primary Completion Date: October 2012 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: Radium-223 dichloride [50 kBq/kg] Drug: Radium-223 dichloride (Xofigo, BAY88-8223)
Radium-223 dichloride (Xofigo, BAY88-8223) 50 kBq/kg
Experimental: Radium-223 dichloride [100 kBq/kg] Drug: Radium-223 dichloride (Xofigo, BAY88-8223)
Radium-223 dichloride (Xofigo, BAY88-8223) 100 kBq/kg
Experimental: Radium-223 dichloride [expansion] Drug: Radium-223 dichloride (Xofigo, BAY88-8223)
Expansion arm: Radium-223 dichloride (Xofigo, BAY88-8223) 50 kBq/kg


Ages Eligible for Study:   20 Years and older
Genders Eligible for Study:   Male
Accepts Healthy Volunteers:   No

Inclusion Criteria:

  • Male ≥ 20 years of age
  • Histologically or cytologically confirmed adenocarcinoma of the prostate
  • Presents with at least 2 bone metastases, confirmed by scintigraphic imaging within the previous 4 weeks
  • Patients who has failed initial hormonal therapy using either an orchiectomy or a Gonadotropin releasing hormone (GnRH) agonist in combination with an antiandrogen must first progress through antiandrogen withdrawal prior to being eligible. The minimum timeframe to document failure of anti-androgen withdrawal will be four weeks
  • Progressive castration resistant metastatic disease
  • Castrate level of testosterone (<50 ng/dL), treatment to maintain castrate levels of testosterone must be continued

Exclusion Criteria:

  • Has received an investigational drug in the 4 weeks before or is scheduled to receiving one during or in the 8 weeks after study drug administration.
  • Has received chemo-, immuno-, or radiotherapy within the last 4 weeks prior to entry in the study, or has not recovered from acute adverse events as a result of such therapy
  • Has received prior hemibody external radiotherapy
  • Has a need for immediate external radiotherapy
  • Has received systemic radiotherapy with radium-223, strontium-89, samarium-153, rhenium-186 or rhenium-188 for the treatment of bony metastases within the last 24 weeks prior to administration of study drug
  • When receiving bisphosphonates, has changed the dose within 4 weeks before administration of study drug
  Contacts and Locations
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its identifier: NCT01565746

Kashiwa, Chiba, Japan, 277-8577
Yokohama, Kanagawa, Japan, 236-0004
Osakasayama, Osaka, Japan, 589-8511
Sponsors and Collaborators
Study Director: Bayer Study Director Bayer
  More Information

Additional Information:
Responsible Party: Bayer Identifier: NCT01565746     History of Changes
Other Study ID Numbers: 15354 
Study First Received: March 1, 2012
Last Updated: May 20, 2016
Health Authority: Japan: Pharmaceuticals and Medical Devices Agency

Keywords provided by Bayer:
radium-223 dichloride
prostate cancer

Additional relevant MeSH terms:
Prostatic Neoplasms
Genital Diseases, Male
Genital Neoplasms, Male
Neoplasms by Site
Prostatic Diseases
Urogenital Neoplasms
Radium Ra 223 dichloride
Antineoplastic Agents
Neuromuscular Agents
Neuromuscular Blocking Agents
Neuromuscular Depolarizing Agents
Peripheral Nervous System Agents
Physiological Effects of Drugs processed this record on May 25, 2016