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A Phase 1, Multi-Center, Open-Label, Dose-Escalation, Safety, Pharmacokinetic, and Pharmacodynamic Study of CX-4945 Administered Orally to Patients With Advanced Solid Tumors, Castleman's Disease or Multiple Myeloma

Phase 1
18 Years
Open (Enrolling)
Advanced Solid Tumors, Breast Cancer, Inflammatory Breast Cancer, Castleman's Disease, Multiple Myeloma

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Trial Information

A Phase 1, Multi-Center, Open-Label, Dose-Escalation, Safety, Pharmacokinetic, and Pharmacodynamic Study of CX-4945 Administered Orally to Patients With Advanced Solid Tumors, Castleman's Disease or Multiple Myeloma

Elevated CK2 activity has been associated with malignant transformation and aggressive tumor
growth and overexpression of CK2 has been documented in multiple types of cancer. CK2 has
emerged as a potential anticancer target and inhibition of CK2 represents a potential
therapeutic strategy to target a specific molecular defect perpetuating many cancers.
CX-4945 has demonstrated potent inhibition of CK2 enzymatic activity. This study will
evaluate the safety, pharmacokinetics (PK), and pharmacodynamic (PD) effects of CX-4945
administered to patients with malignancies or lymphoproliferative disorders known to
overexpress CK2 including advanced solid tumors, Multiple Myeloma and Castleman's Disease.

Inclusion Criteria:

- Histologically or cytologically confirmed malignancy or lymphoproliferative disorder
known to over express CK2 which has failed standard therapies (surgery, radiotherapy,
endocrine therapy, chemotherapy) or for which effective therapy is not available,
including the following types: (examples)

- Lung cancer

- Renal cell cancer

- Breast cancer

- Inflammatory breast cancer

- Head and neck cancer - squamous cell

- Prostate cancer

- Colorectal cancer

- Castleman's disease (multi-centric disease)

- Multiple myeloma (Eligible patients must have quantifiable M-protein levels
present in serum and/or urine)

- At least 18 years of age.

- One or more tumors measurable on radiograph or CT scan, or evaluable disease defined
as non-measurable lesions per RECIST or detection of protein M in serum and/or urine
of patients with Multiple Myeloma (serum ≥ 10 gm/L and urine ≥ 200 mg/24 hr).

- Laboratory data as specified below:

- Hematology: ANC >1500 cells/mm3, platelet count >100,000 cells/mm3 and Hemoglobin >
9 gm/L

- Hepatic: bilirubin <1.5 X ULN; alanine aminotransferase (ALT) or aspartate
aminotransferase (AST) < 2.5 X ULN. Patients with known liver metastases or liver
neoplasms: alanine aminotransferase (ALT) or aspartate aminotransferase (AST) < 5.0

- Renal: serum creatinine within normal limits (WNL), defined as within 10% of the
institution's stated reference range, or a calculated creatinine clearance >60
mL/min/1.73 m2 for patients with abnormal, increased, creatinine levels. Patients
with Multiple Myeloma (only): serum creatinine ≤ 2.5 the institutional upper limit
of the normal range and a calculated creatinine clearance > 40 mL/min/1.73 m2.

- Coagulation: INR < 1.5 times normal, aPTT < 1.5 times normal. Patients receiving
therapeutic doses of anticoagulant therapy may be considered eligible for the trial
if INR and aPTT are within the acceptable therapeutic limits for the institution.

- A negative pregnancy test (if female of childbearing potential).

- Estimated life expectancy of at least 3 months

- Karnofsky Performance Status ≥ 70%

- For men and women of child-producing potential, use of effective contraceptive
methods during the study

- Ability to understand the requirements of the study, provide written informed

Exclusion Criteria:

- Pregnant or nursing women.

- Seizure disorders requiring anticonvulsant therapy.

- Known brain metastases (unless previously treated and well controlled for a period of
> or = 3 months).

- Major surgery, other than diagnostic surgery, within 4 weeks prior to the first dose
of test drug.

- Treatment with radiation therapy or surgery within one month prior to study entry

- Treatment with chemotherapy or investigational drugs within 21 days prior to the
screening visit. Acute toxicities from prior therapy must have resolved to Grade ≤ 1
above baseline.

- Patients with a history of a second malignancy within 3 years of the baseline visit
excluding cutaneous carcinomas and in-situ carcinoma.

- Concurrent severe or uncontrolled medical disease.

- Active symptomatic fungal, bacterial and/or viral infection including active HIV or
viral hepatitis.

- Difficulty with swallowing or an active malabsorption syndrome

- Chronic diarrhea

- Gastrointestinal diseases including gastritis, ulcerative colitis, Crohn's disease,
or hemorrhagic coloproctitis

- History of gastric or small bowel surgery involving any extent of gastric or small
bowel resection.

- Clinically significant bleeding event within the last 3 months, unrelated to trauma,
or underlying condition that would be expected to result in a bleeding diathesis

- Patients who have exhibited allergic reactions to a similar structural compound or to
a formulation component.

- Concomitant use of warfarin and HMG-CoA reductase inhibitors (statins)

Type of Study:


Study Design:

Allocation: Non-Randomized, Endpoint Classification: Safety Study, Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Treatment

Outcome Measure:

Safety (Dose limiting toxicities, maximum tolerated dose)

Outcome Time Frame:

One year (Assessed at Cycle 1)

Safety Issue:


Principal Investigator

Study Director

Investigator Role:

Study Director

Investigator Affiliation:

Cylene Pharmaceuticals


United States: Food and Drug Administration

Study ID:




Start Date:

February 2009

Completion Date:

December 2011

Related Keywords:

  • Advanced Solid Tumors
  • Breast Cancer
  • Inflammatory Breast Cancer
  • Castleman's Disease
  • Multiple Myeloma
  • Inflammatory breast cancer
  • Castleman's Disease
  • Multiple Myeloma
  • Breast cancer
  • Solid tumors
  • CK2 inhibitor
  • Breast Neoplasms
  • Giant Lymph Node Hyperplasia
  • Multiple Myeloma
  • Neoplasms, Plasma Cell
  • Inflammatory Breast Neoplasms
  • Neoplasms



Front Range Cancer Specialists Fort Collins, Colorado  80528
Mayo Clinic Arizona Scottsdale, Arizona  85259
U T M D Anderson Cancer Center Houston, Texas  77030