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Study Summary
No. 2005-0838:.......Melanoma......Kevin B. Kim......Melanoma Medical Oncology
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Study Summary Title
Study Summary
Number:
2005-0838
Study Title:A Phase I/II Dose Escalating Study to Evaluate the Safety, Pharmacokinetics, and Pharmacodynamics and Efficacy of TKI258 (CHIR-258) in Patients with Locally Advanced or Metastatic Melanoma
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Physician New Patient Referral
Name:Kevin B. KimPatients Call:800-392-1611 (in U.S.A.) 713-792-6161 (outside U.S.A.)
Dept:Melanoma Medical OncologyReferring MD
Call:
800-392-1611 (in U.S.A.) 713-792-6161 (outside U.S.A.)
Phone:713-792-2921
Contact us about clinical trials
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General Information
Disease Group:MelanomaSupported By:N/A
Phase of Study:Phase I/Phase IIReturn
Visit:
On day 1, 2, 15, 16 and one visit between 26-28 (or day 1 of cycle 2) of cycle
1.
On day 1, 15 and one visit between 26-28 (or day 1 of subsequent cycles) after
cycle 1
Treatment
Agents:
CHIR-258Home Care:N/A
Treatment Loc:Independent Multicenter Arrangements
Estimated
Length of Stay
in Houston:
N/A
Description/
Intervention:
The goal of this clinical research study is to find the highest tolerable dose
of TKI258 that can be given to patients with melanoma. TKI258 is designed to
prevent or slow the growth of cancer cells by blocking certain proteins
necessary for tumor cell growth. Researchers want to study how long TKI258
stays in the body and what effects, good and bad, TKI258 has on patients and
the disease. Researchers will also look at how different people with melanoma
respond in different ways after taking TKI258.
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Study Objectives / Outcomes
Primary objectives for dose escalation

1. To determine the maximum tolerated dose (MTD) based on dose limiting toxicity (DLT) of TKI258
2. To determine the plasma and whole blood pharmacokinetics (PK) of orally administered TKI258

Primary objectives for dose expansion

1. To assess tumor response according to Response Evaluation Criteria in Solid Tumors (RECIST)
as measured by response rate (RR) and lack of early progressive disease (.2 months) in a
multinomial two-stage design

Secondary objectives (escalation and expansion phases)

1. To assess the safety profile of TKI258 in this patient population

2. To assess the effect of TKI258 on biomarkers in the blood

To evaluate levels of circulating growth factors, soluble receptors and melanomarelated
markers
To evaluate effects of TKI258 on serum LDH/LDH isoenzymes and apoptotic markers
To evaluate effects of TKI258 on circulating endothelial cells
To evaluate effect of TKI258 on gene expression levels in blood cells

3. To assess biomarker changes in tumor/nevi biopsies and archival tumor tissues where
accessible and available, respectively
To measure the activity of target inhibition (e.g., FGFR and VEGFR2) on tumor cells
To evaluate PD as measured by modulation of signaling molecules, proliferation,
microvessel density and apoptosis
To assess status of gene mutations related to melanoma and target pathways

4. To assess changes in tumor glucose metabolism/cell viability between pre- and posttreatment
using [18F]-FDG-PET imaging in patients with at least one tumor .2 cm

5. To assess the anti-angiogenic effects of TKI258 using dynamic contrast enhanced
magnetic resonance imaging (DCE-MRI) in patients with liver metastases .3 cm

6. To explore the relationship between the PK profile and PD activities

7. To assess preliminary anti-tumor activity

Exploratory objectives
1. To explore genetic polymorphisms that may affect TKI258 metabolism and response
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Study Status Information
Study Activation / Registration Date:
IRB Review and Approval Date:04/05/2006
Study Type:Phase I
Recruitment Status:Terminated
Projected Accrual:36
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Enrollment Eligibility
If you do not meet the enrollment eligibility, there may be other treatment options for you. Please Contact the Referral Office for more information.

Inclusion Criteria:1) Diagnosis of histologically or cytologically documented, locally advanced or metastatic melanoma (AJCC stage IIIB, IIIC or IV) that is relapsed or refractory to standard therapy or for which no curative standard therapy exists.

2) For escalation phase patients: at least one measurable or non-measurable lesion as defined by RECIST; for expansion phase patients: at least one measurable lesion as defined by RECIST.

3) Patients must have at least one measurable liver lesion .3 cm in diameter to be eligible for DCEMRI. Patients with no liver involvement will not be evaluated by DCE-MRI but are still eligible for study entry.

4) Patients must have at least one measurable lesion .2 cm in diameter, be able to lay down for ~1 hour and have a blood glucose level .180 mg/dL prior to [18F]-FDG PET imaging. Patients not meeting these criteria will not be evaluated by PET imaging but are still eligible for study entry.

5) Age at least 18 years.

6) ECOG performance status 0 or 1.

7) All adults of reproductive potential must agree to use effective contraception or must be sterile. Barrier contraceptives must be used throughout the study in both sexes. Oral, implantable, or injectable contraceptives may be affected by cytochrome P450 interactions, and are therefore not considered effective for this study. Women of child-bearing potential must have a negative pregnancy test (serum) within 48 hours prior to the start of study treatment.

8) Required baseline laboratory data include: 1) Absolute neutrophil count (ANC) greater than or equal to 1,500/mm3 [SI units 1.5 x 109/L]; 2) Platelets greater than or equal to 75,000/mm3 [SI units 75 x 109/L]; 3) Hemoglobin greater than or equal to 8.0 gm/dL [SI units 80 gm/L]; 4) Serum creatinine less than or equal to 1.5 x upper limit of normal (ULN); 5) Bilirubin less than or equal to 1.5 x ULN; 6) AST (SGOT) and ALT (SGPT) less than or equal to 2.5 x ULN, except for subjects with tumor involvement of the liver who must have AST and ALT less than or equal to 5 x ULN;

9) Contd. #8) Amylase, Lipase less than or equal to ULN; 8) Electrolyte levels greater than or equal to LLN or correctable with supplements (ie.,potassium, total calcium, magnesium,phosphorus). 9) Urine dipstick reading Negative for proteinuria or, if documentation of +1 results for protein on dipstick reading, then total urinary protein less than or equal to 500 mg and measured creatinine clearance greater than or equal to 50 mL/min/1.73m2 from a 24-hour urine collection

10) Signed, witnessed informed consent obtained prior to any screening procedures.

Exclusion Criteria:1) Concurrent therapy with any other investigational agent.

2) Known uncontrolled CNS metastases.

3) Impaired cardiac function or clinically significant cardiac disease, including any one of the following: • LVEF < 45% as determined by MUGA scan or echocardiogram • Complete left bundle branch block • Obligate use of a cardiac pacemaker • Congenital long QT syndrome • History or presence of ventricular tachyarrhythmia • Presence of unstable atrial fibrillation (ventricular response > 100 bpm). Patients with stable atrial fibrillation are eligible, provided they do not meet any of the other cardiac exclusion criteria.

4) Cont. # 3: . Clinically significant resting bradycardia (less than 50 bpm), QTc > 480 msec on screening ECG • Right bundle branch block + left anterior hemiblock (bifasicular block) • Angina pectoris less than or equal to 3 months prior to starting study drug • Acute MI less than or equal to 3 months prior to starting study drug, Other clinically significant heart disease (e.g., CHF, uncontrolled hypertension, history of labile hypertension, or history of poor compliance with an antihypertensive regimen)

5) Currently receiving treatment with any of the medications that have a relative risk of prolonging the QT interval or inducing Torsades de Points (Table 9-4) and the treatment cannot be discontinued or switched to a different medication prior to starting study drug.

6) Received chemotherapy, targeted therapy or monoclonal antibody therapy less than or equal to 4 weeks prior to starting study drug (6 weeks in the case of nitrosoureas and Mitomycin C) or has not recovered from the side effects of such therapy.

7) Received biological therapy or immunotherapy (therapeutic or diagnostic) less than or equal to 2 weeks prior to starting study drug or has not recovered from the side effects of such therapy [see 5 for monoclonal antibody therapy].

8) Received an investigational agent (therapeutic or diagnostic) less than or equal to 4 weeks prior to starting study drug or has not recovered from the side effects of such therapy [see 5 for monoclonal antibody therapy].

9) Received wide-field radiotherapy less than or equal to 4 weeks or limited-field radiation for palliation less than or equal to 2 weeks prior to starting study drug or has not recovered from side effects of such therapy. The site of radiotherapy should not be the only site of measurable disease unless there is evidence of disease progression at this site prior to entry into this study.

10) Received any hematopoietic colony-stimulating factor (e.g., G-CSF, GM-CSF) less than or equal to 2 weeks prior to starting study drug. Erythropoietin is allowed.

11) Has undergone major surgery ≤ 2 weeks prior to starting study drug or has not recovered from side effects of such surgery.

12) Malabsorption syndrome or uncontrolled gastrointestinal toxicities (nausea, diarrhea, vomiting) with toxicity greater than NCI CTCAE grade 2.

13) Pregnant or breastfeeding women.

14) History of another primary malignancy that is currently clinically significant or currently requires active intervention.

15) Chronic anticoagulation therapy with full strength ASA, Coumadin, or Heparin (low dose ASA less than or equal to 81mg, or low dose coumadin less than or equal to 1mg to maintain indwelling venous access device patency is allowed).

16) History of thromboembolic or cerebrovascular events within the last 12 months, including: TIA, CVA, DVT, PE.

17) History of melena, hematemesis, or hemoptysis within the last 3 months.

18) Known diagnosis of HIV infection (HIV testing is not mandatory)

19) Other severe, acute, or chronic medical or psychiatric condition or laboratory abnormality that may increase the risk associated with study participation or study-drug administration or may interfere with the interpretation of study results and, in the judgment of the investigator, make the patient inappropriate for this study.

20) The use of ketoconazole, erythromycin, carbamazapine, phenobarbital, phenytoin, rifampin, St. John's wort and quinidine is prohibited.

21) Patients with any of the following contraindications are excluded from MRI:Cardiac pacemaker • Ferromagnetic metal implants other than those approved as safe for use in the MRI scanner, ie., some types of aneurysm clips, shrapnel) • Claustrophobia• Obesity (exceeding the equipment limits)

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Links
Registration Number: NCT00303251
Study Information on Clinical Trials Registry (clinicaltrials.gov)

Other Links:
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Results


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