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Study of Itraconazole in Castrate-resistant Prostate Cancer (CRPC) Post-chemotherapy

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details.
ClinicalTrials.gov Identifier: NCT01450683
Recruitment Status : Terminated (Low accrual)
First Posted : October 12, 2011
Results First Posted : September 8, 2014
Last Update Posted : April 11, 2017
Information provided by (Responsible Party):
Sandy Srinivas, Stanford University

Brief Summary:
This study evaluates if itraconazole causes a reduction in the serum levels of prostate-specific antigen (PSA) in male subjects with castration-resistant prostate cancer (CRPC).

Condition or disease Intervention/treatment Phase
Prostate Cancer Prostatic Neoplasms Castrate-resistant Prostate Cancer (CRPC) Androgen-insensitive Prostate Cancer Hormone-refractory Prostate Cancer Metastatic Disease Drug: Itraconazole Phase 2

Detailed Description:

Castration-resistant prostate cancer (CRPC) is also known as "androgen-insensitive" or "hormone-refractory" prostate cancer. While numerous therapies impact biochemical response in the setting of CRPC, there remains unmet medical need, largely expressed as the lack of durable response. New therapies that extend survival of patients beyond that provided by chemotherapy are needed.

It is hypothesized that the triazole antifungal drug itraconazole, through its activity as a potent inhibitor of the Hedgehog (Hh) signaling pathway via the Smoothened (Smo) pathway, may provide clinical benefit in the treatment of prostate cancer. The Hh signaling pathway is a critical embryonic developmental pathway whose aberrant activity has been implicated in the growth and metastases of a variety of tumor types including prostate cancer. Itraconazole is structurally related to ketoconazole, demonstrated to reduce serum PSA by more than 50% in about 20 to 25% of treated prostate cancer subjects.

This study will assess efficacy on the basis of serum levels of PSA, an established surrogate endpoint for efficacy in prostate cancer.

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Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 4 participants
Allocation: N/A
Intervention Model: Single Group Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: A Phase 2 Study of Itraconazole in Castrate-resistant Prostate Cancer Post-chemotherapy
Study Start Date : September 2010
Actual Primary Completion Date : April 2011
Actual Study Completion Date : April 2011

Resource links provided by the National Library of Medicine

MedlinePlus related topics: Prostate Cancer

Arm Intervention/treatment
Experimental: Itraconazole
600 mg/day oral (PO)
Drug: Itraconazole

600 mg/day oral (PO)

IUPAC name: (2R,4S)-rel-1-(Butan-2-yl)-4-{4-[4-(4-{[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-4,5-dihydro-1H-1,2,4-triazol-5-one

Other Names:
  • Sporanox
  • R51211

Primary Outcome Measures :
  1. Reduction in Serum PSA [ Time Frame: 12 weeks treatment, with primary outcome assessed at 15 weeks ]
    Number of subjects with > 50% drop in serum PSA as compared to baseline, at 12 weeks and confirmed at 15 weeks

Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years and older   (Adult, Older Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   No


  • Male aged ≥ 18 years
  • Life expectancy ≥ 6 months
  • Histologically- or cytologically-confirmed adenocarcinoma of the prostate
  • Metastatic disease or prior history of metastases, as documented by positive bone scan or metastatic lesions on CT or MRI
  • Prostate cancer progression, as documented by PSA according to PCWG2 or radiographic progression according to RECIST criteria version 1.1
  • Progression must have been during or after docetaxel based chemotherapy.
  • Surgically or medically castrated, with testosterone levels of < 50 ng/dL (< 2.0 nM). If the patient is currently being treated with LHRH agonists (patient who have not undergone an orchiectomy), this therapy must have been initiated at least 4 weeks prior to Cycle 1 Day 1 and treatment must be continued throughout the study.
  • Eastern Cooperative Oncology Group (ECOG) Performance Status of ≤ 2
  • Hemoglobin ≥ 10.0 g/dL
  • Platelet count ≥100,000 microliters
  • Serum creatinine ≤ 2, OR a calculated creatinine clearance ≥ 40 mL/min
  • Serum bilirubin < 1.5 x ULN (except for patients Gilbert's disease)
  • AST or ALT < 2.5 x ULN
  • Able to swallow the study drug whole as a tablet
  • Willing and able to provide written informed consent


  • Known brain metastasis
  • Radiation therapy within 4 weeks of Cycle 1, Day 1
  • Prior systemic treatment with an azole drug (eg, fluconazole, ketoconazole) within 4 weeks of Cycle 1, Day 1
  • Prior flutamide (Eulexin) treatment within 4 weeks of Cycle 1, Day 1 (patients whose PSA did not decline for ≥ 3 months months in response to antiandrogen given as a 2nd line or later intervention will require only a 2-week washout prior to Cycle 1,Day 1)
  • Prior Bicalutamide (Casodex), nilutamide (Nilandron) treatment within 6 weeks of Cycle 1 Day 1 (patients whose PSA did not decline for ≥ 3 months in response to antiandrogen given as a 2nd line or later intervention will require only a 2-week washout prior to Cycle 1 Day 1)
  • Known active or symptomatic viral hepatitis or chronic liver disease
  • Clinically significant heart disease as evidenced by myocardial infarction or arterial thrombotic events in the past 6 months; severe or unstable angina
  • Other malignancy, except non-melanoma skin cancer, with a ≥ 30% probability of recurrence within 24 months
  • Administration of an investigational therapeutic within 30 days of Cycle 1, Day 1
  • Any condition which, in the opinion of the investigator, would preclude the patient's participation in this trial.
  • No more than 3 prior chemotherapy regimens.

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT01450683

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United States, California
Stanford University School of Medicine
Stanford, California, United States, 94305
Sponsors and Collaborators
Stanford University
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Principal Investigator: Dr. Sandy Srinivas Stanford University
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Responsible Party: Sandy Srinivas, Associate Professor of Medicine, Stanford University
ClinicalTrials.gov Identifier: NCT01450683    
Other Study ID Numbers: IRB-19413
SU-12032010-7271 ( Other Identifier: Stanford University )
PROS0037 ( Other Identifier: OnCore )
First Posted: October 12, 2011    Key Record Dates
Results First Posted: September 8, 2014
Last Update Posted: April 11, 2017
Last Verified: March 2017
Additional relevant MeSH terms:
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Prostatic Neoplasms
Neoplasm Metastasis
Genital Neoplasms, Male
Urogenital Neoplasms
Neoplasms by Site
Genital Diseases, Male
Genital Diseases
Urogenital Diseases
Prostatic Diseases
Male Urogenital Diseases
Neoplastic Processes
Pathologic Processes
Antifungal Agents
Anti-Infective Agents
14-alpha Demethylase Inhibitors
Cytochrome P-450 Enzyme Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Steroid Synthesis Inhibitors
Hormone Antagonists
Hormones, Hormone Substitutes, and Hormone Antagonists
Physiological Effects of Drugs
Cytochrome P-450 CYP3A Inhibitors