We updated the design of this site on December 18, 2017. Learn more.
ClinicalTrials.gov Menu

Phase I Study of Novel Estrogen Receptor(ER) a36 Modifier Icaritin in Advanced Breast Cancer Patients

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: NCT01278810
Recruitment Status : Unknown
Verified November 2010 by Chinese Academy of Medical Sciences.
Recruitment status was:  Recruiting
First Posted : January 19, 2011
Last Update Posted : January 28, 2011
Information provided by:

Study Description
Brief Summary:
To assess safety, tolerance and PK profile of different doses(50mg,100mg,200mg,300mg, 400mg, 500mg,QD)of Icaritin in advanced breast cancer Patients in China

Condition or disease Intervention/treatment Phase
Metastatic Breast Cancer Drug: Icaritin Phase 1

Detailed Description:

ERa36 predominantly localizes on the plasma membrane and in the cytoplasm and mediates a membrane-initiated "nongenomic" signaling pathway. Membrane-initiated estrogen signaling has been linked to rapid responses to estrogen and generally activates signaling pathways like MAPK/ERK, phosphatidylinositol-3-kinase, and protein kinase C pathways. Preclinical study demonstrated that ERa36 was expressed in tumor cells and might be the driving force of breast cancer cell proliferation. 40% of breast cancer tumors which used to be considered as ER negative also express ERa36. In the former study the investigators found that 40% of ERa66-positive breast cancer patients express high levels of ERa36 in their tumors, and this subset of patients are less likely to benefit from tamoxifen treatment compared with those with ERa66-positive/ERa36-negative tumors.

Icaritin is a newly discovered small molecular compound which is high selective ERa36 modulators and perhaps will be a very promising new drug to treat advanced breast cancer by targeting this nongenomic pathway. It was showed that it can inhibit the growth of breast cancer cells both in vitro and in vivo. The investigators have completed the preclinical PK&PD and toxicity studies in animals and now move on to test it in a FIM clinical trial.

Study Design

Study Type : Interventional  (Clinical Trial)
Estimated Enrollment : 30 participants
Allocation: Non-Randomized
Intervention Model: Single Group Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: A Phase I ,Single Center, Open-labeling, Single and Dose-escalating Study to Assess the Safety, Tolerability and Pharmacokinetic Profile of Oral Novel ERa36 Modifier Icaritin in Advanced Breast Patients
Study Start Date : November 2010
Estimated Primary Completion Date : November 2011
Estimated Study Completion Date : December 2011

Resource links provided by the National Library of Medicine

MedlinePlus related topics: Breast Cancer
U.S. FDA Resources

Arms and Interventions

Arm Intervention/treatment
Experimental: Icaritin Drug: Icaritin
50mg,100mg,200mg,300mg,400mg,500mg ascending-multiple oral dose, Qd, single dose and continuing dose 28 days, to assess the safety,tolerance and pharmacokinetics of icaritin
Other Name: IC-162

Outcome Measures

Primary Outcome Measures :
  1. To assess safety of icaritin in breast cancer patients [ Time Frame: 1-2 YEAR ]
    to find the dose-limiting toxicity(DLT)and maximal tolerated dose(MTD)of icaritin in breast cancer patients

Secondary Outcome Measures :
  1. To assess pharmacokinetic profile of icaritin in breast cancer patients [ Time Frame: 1 year ]

Eligibility Criteria

Information from the National Library of Medicine

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, Learn About Clinical Studies.

Ages Eligible for Study:   18 Years to 65 Years   (Adult)
Sexes Eligible for Study:   Female
Accepts Healthy Volunteers:   No

Inclusion Criteria:

  1. Female, age ≥ 18 years old and ≤ 65 years old
  2. The patients with advanced breast tumors who are confirmed through histologic or cytologic diagnosis with ER positive or investigator think that subjects will benefit from the trial
  3. The advanced breast cancer patients which relapse or failure from previous standard treatment
  4. 19 ≤ BMI index ≤ 30
  5. No serious heart, liver,lung and kidney diseases
  6. Received at least once anti-cancer treatment (including chemotherapy, radiotherapy, biological or endocrine treatment). And the last treatment must be at least four weeks before study enrollment or more than 5 times half life. The surgery treatment must be more than three months
  7. Life expectancy of at least 12 weeks
  8. Patients which can cooperate to observe AE and efficacy
  9. No any other concurrent anti-cancer treatment
  10. A signed informed consent must be obtained prior to performing any study specific procedures
  11. ECOG Performance Status of 0,1
  12. Female:Women with childbearing potential must have a negative pregnancy test performed

Exclusion Criteria:

  1. Have a known hypersensitivity to flavonoid drugs
  2. Hepatic:

    • ALB >limit if normal
    • TB> the upper limit of normal
    • ALT and AST > upper limit of Normal


    • Serum Creatinine > 1.5 times the upper limit of normal

    Bone marrow:

    • Absolute neutrophil count (ANC) < 1.5 × 109/L
    • Platelet count < 90 × 109/L
    • Hemoglobin < 9 g/dL
  3. PT/APTT > 1.25 times the upper limit of normal
  4. Suffered from thrombotic disease
  5. Serum Ca > the upper limit of normal
  6. Not recovered from toxic effects of previous anti-cancer treatments or surgery
  7. Any serious or uncontrollable concomitant systemic disorder (such as unstable respiratory disorders, cardiovascular, hepatic or kidney disorders.) or active infection which will influence the clinical trial
  8. CNS metastases or invade requiring treatment for unstable status or various psychiatric disorders
  9. No malabsorption or other disease which will affect the drug absorption,distribution,metabolism and excretion
  10. Concurrent other malignancies with the exception of cervical cancer in situ or squamous Cell Carcinoma of the Skin
Contacts and Locations

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): NCT01278810

China, Beijing
Cancer institute & hospital, chinese academy of medical sciences Recruiting
Beijing, Beijing, China, 100021
Contact: Ying Fan, MD    +86 010-87788120    fanying@csco.org.cn   
Sponsors and Collaborators
Chinese Academy of Medical Sciences
Beijing Shenogen Biomedical Co., Ltd
Principal Investigator: Binghe Xu, MD Cancer Institute and Hospital, Chinese Academy of Medical Sciences
Principal Investigator: Binghe Xu, MD Cancer institute & hospital
More Information

Responsible Party: xubinghe, Cancer institute & hospital, chinese academy of medical sciences
ClinicalTrials.gov Identifier: NCT01278810     History of Changes
Other Study ID Numbers: TG0929ICR
First Posted: January 19, 2011    Key Record Dates
Last Update Posted: January 28, 2011
Last Verified: November 2010

Keywords provided by Chinese Academy of Medical Sciences:

Additional relevant MeSH terms:
Breast Neoplasms
Neoplasms by Site
Breast Diseases
Skin Diseases