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Study Summary
No. 2009-0949:.......Melanoma; Phase I Studies; Solid Tumors......Kevin B. Kim......Melanoma Medical Oncology
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Study Summary Title
Study Summary
Number:
2009-0949
Study Title:An Open-Label, Dose-Escalation, Phase I/II Study to Investigate the Safety, Pharmacokinetics, Pharmacodynamics and Clinical Activity of the BRAF Inhibitor GSK2118436 in Combination with the MEK Inhibitor GSK1120212 in Subjects with BRAF Mutant 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:Melanoma
Phase I Studies
Solid Tumors
Supported By:GlaxoSmithKline
Phase of Study:Phase I/Phase IIReturn
Visit:
Part A: screening, Day 1, Day 15, Day 16, week 4, week 6, week 8, every 4
weeks, follow up
Part B: screening, Day 1, Day 8, Day 15, Day 21, every 4 weeks
Part C: screening, Day 1, Day 15, 6 weeks, every 4 weeks
Treatment
Agents:
GSK1120212
GSK2118436
Home Care:Study drug may be taken at home.
Treatment Loc:Both at MDACC & outside MDACC at one or more Collaborating Sites or Institutions
Estimated
Length of Stay
in Houston:
This protocol will be performed on an outpatient basis.
Description/
Intervention:
The goal of this clinical research study is to find the best dose of the drugs
dabrafenib and trametinib that can be given together or alone in patients with
advanced solid cancer that has a BRAF mutation. The effects of the study drugs
at different dose levels and the safety of the study drugs will also be
studied.
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Study Objectives / Outcomes
Part A
Primary: To determine the pharmacokinetics (PK) of single dose (Day 1) GSK2118436 (and its metabolite(s), including GSK2285403), alone and with repeat dose (Days 2 through 15) GSK1120212 dosed orally.

Secondary: To confirm steady-state exposure of GSK1120212.

Part B
Primary:
  • To determine the safety and tolerability of GSK2118436 and GSK1120212 dosed orally in combination in subjects with BRAF mutant metastatic melanoma or other BRAF-positive tumors.
  • To determine the range of tolerated doses of GSK2118436 and GSK1120212 dosed orally in combination in subjects with BRAF mutant metastatic melanoma or other BRAF-positive tumors.

Secondary:
  • To characterize the steady-state PK of GSK2118436 (and its metabolite(s) including GSK2285403), and GSK1120212.
  • To evaluate the clinical activity of GSK2118436 and GSK1120212 in subjects with BRAF mutant metastatic melanoma.]
  • To evaluate the pharmacodynamic response in BRAF mutant CRC-Pharmacodynamic cohort after treatment with GSK2118436 and GSK1120212.
  • To explore relationships between GSK2118436, GSK1120212 PK, MAPK signalling inhibition and clinical endpoints.


Part C
Primary:
  • To determine clinical activity of GSK2118436 and GSK1120212 in subjects with BRAF mutant metastatic melanoma. To determine the safety, tolerability and range of tolerated doses of GSK2118436 and GSK1120212 dosed orally in combination in subjects with BRAF mutant metastatic melanoma.

Secondary:
  • To characterize the population PK parameters of GSK2118436 and GSK1120212 when administered daily in subjects with BRAF mutant metastatic melanoma.
  • To characterize the overall survival of subjects with BRAF mutant meatastatic melanoma when administered GSK2118436 and GSK112012 in combination

    Note: Subjects with any BRAF mutation+ tumors will also be enrolled on this study.


Part D: Randomized GSK2118436 HPMC Cohorts
Primary:
  • To determine the single and stady-state PK of GSK2118436 HPMC capsules alone and in combination with GSK1120212 dosed orally.
  • To determine the safety and tolerability of GSK2118436 and GSK1120212 dosed orally in combination in subjects with BRAF mutant metastatic melanoma.

Secondary:
  • To determine the single dose and steady state PK of GSK2118436 metabolites using HPMC capsules.
  • To determine single dose and steady-state PK of GSK1120212.
  • To evaluate clinical activity of the combination in subjects with BRAF mutant metastatic melanoma.
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Study Status Information
Study Activation / Registration Date:03/26/2010
IRB Review and Approval Date:03/26/2010
Study Type:Phase I
Recruitment Status:Open
Projected Accrual:430
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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) Capable of giving written informed consent, which includes compliance with the requirements and restrictions listed in the consent form.

2) Male or female age >/= 18 years of age and able to swallow and retain oral medication

3) Tumor type criteria: i. BRAF mutation-positive melanoma (i.e., V600E, V600K, or V600D) as determined via relevant genetic testing (in Parts A and B, other BRAF mutation-positive tumor types may be enrolled with approval of the GSK medical monitor). Testing with the GSK BRAF mutation assay may be required for enrollment.

4) Part A: No archived tissue required, but must have known BRAF mutation (i.e., V600E, V600K or V600D); Part B: Must have archived tissue requested, must have BRAF mutation (i.e., V600E, V600K or V600D); Subjects in BRAF mutant CRC Pharmacodynamic cohort must be able to provide fresh tissue at Screening and Day 15 of the study. Part C: Archived tissue is required, need fresh biopsy if archived tissue is not available, must have BRAF mutation (must be V600E, V600K or V600D). Only melanoma patients can be enrolled. Part D: Archived tissue is required; need fresh biopsy if archived tissue is not available, must have documentation of BRAF mutation (must be V600E or V600K). Only melanoma patients can be enrolled.

5) Measurable disease per RECIST criteria (required for Part C and Part D enrollment).

6) ECOG Performance Status of 0 or 1.

7) A female subject is eligible to participate if she is of: Non-childbearing potential defined as pre-menopausal females witha documented tubal ligation or hysterectomy; or postmenopausal defined as 12 months of spontaneous amenorrhea [in questionable cases a blodo sample with simultaneous follicle stimulating homrone (FSH)> 40 MIU/mL and estradiol < 40 pg/mL (<140 pmol/L) is confirmatory] Females on hormone replacement therapy (HRT) and whose menopausal status is in doubt will be required to use one of the contraception methods if they wish to continue their HRT during the study, Otherwise, they must discontinue HRT to allow confirmation of post-menopausal status prior to study enrollment. For most forms of HRT, at least 2-4 weeks will elapse between the cessation fo therapy and the blood draw; this interval depends on the type and dosage of HRT. Following confirmation of their post-menopausal status, they can resume use of HRT during the study without use of a contraceptive method.

8) #7 Con't. Female subjects must have a negative serum pregnancy test within 14 days prior to the start of dosing and must agree to use contraception for 4 months after the last dose of study medication.

9) Calcium phosphate prodcut (CPP) </= 4.0mmol^2/L^2 (50 mg^2/dL^2)

10) 11) Adequate organ system function as defined: Hematologic: Absolute neutrophil count (ANC) >/= 1.2 x 10^9, hemoglobin >/=9 g/dL, platelets >/=75x10^9/L, PT/PTT/INR </=1.3 x upper limit of normal (ULN), Hepatic: Albumin >/= 2.5 g/dL, total bilirubin </=1.5 xULN, AST/ALT </=2.5 xULN, Renal: creatinine</=ULN OR calculated creatinine clearance >/=50 ml/min OR 24-hour urine creatinine clearance >/=50 ml/min, Cardiac: left ventricular ejection fraction (LVEF) >/=lower limit of normal (LLN) by ECHO or MUGA

Exclusion Criteria:1) Currently receiving cancer therapy (chemotherapy, radiation therapy, immunotherapy, or biologic therapy).

2) Part A and Part B: Prior exposure to BRAF or MEK inhibitors unless approved by the GSK medical monitor.

3) Part C: Prior exposure to BRAF or MEK inhibitors. Prior anti-cancer therapy in the metastatic setting, with the exception of up to one regimen of chemotherapy and/or interleukin-2 (IL-2).

4) Part D: Prior exposure to BRAF inhibitors. A washout period of 6 weeks is required for ipilimumab.

5) Received an investigational anti-cancer drug within four weeks or five half-lives (whichever is shorter) of the first dose of study drug administration. At least 14 days must have passed between the last dose of the prior investigational agent and the first dose of study drug. This washout period is not required for prior GSK2118436 or prior GSK1120212 administration. One week of washout is required for PLX4032.

6) Current use of a prohibited medication or requires any of these medications during treatment with study drug.

7) Known HIV, Hepatitis B or Hepatitis C infection. Subjects who have evidence of clearance of Hepatitis B infection can be enrolled with approval of the GSK medical monitor.

8) Current use of therapeutic warfarin. Low molecular weight heparin (LMWH) is permitted provided that subject's PT and PTT meet entry criteria. Subjects requiring therapeutic levels of LMWH must receive approval from GSK Medical Monitor and must be monitored appropriately as clinically indicated.

9) Any major surgery, radiotherapy, or immunotherapy within the last 4 weeks. Limited radiotherapy within the last 2 weeks.

10) Chemotherapy regimens with delayed toxicity within the last 3 weeks. Chemotherapy regimens given continuously or on a weekly basis with limited potential for delayed toxicity within the last 2 weeks.

11) Unresolved toxicity greater than NCI-CTCAE v4 Grade 1 from previous anti-cancer therapy except alopecia.

12) History of retinal vein occlusion (RVO) or central serous retinopathy (CSR), or predisposing factors to RVO or CSR (e.g. uncontrolled glaucoma or ocular hypertension, uncontrolled systemic disease such as hypertension, diabetes mellitus, or history of hyperviscosity or hypercoagulability syndromes).

13) Visible retinal pathology as assessed by ophthalmologic exam that is considered a risk factor for RVO or CSR such as: evidence of new optic disc cupping, evidence of new visiaul field defects, intraocular pressure >21 mm Hg as measured by tonography.

14) Presence of active gastrointestinal disease or other condition that will interfere significantly with the absorption, distribution, metabolism, or excretion of drugs.

15) Subjects with brain metastases are excluded, unless all known lesions must be previously treated with surgery or stereotactic radiosurgery, and brain lesion(s), if still present, must be confirmed stable (i.e. no increase in lesion size) for >/= 90 days prior to first dose on study (must be documented with two consecurive MRI or CT scans using contrast), and asymptomatic with no corticosteroids requirement for >/= 30 days prior to first dose on study, and no enzyme-inducing anticonfulsants for >/= 30 days prior to first dose on study.

16) Psychological, familial, sociological, or geographical conditions that do not permit compliance with the protocol.

17) Patients with a history of pneumonitis or interstitial lung disease.

18) History of acute coronary syndromes (including myocardial infarction and unstable angina), coronary angioplasty, or stenting within the past 6 months.

19) QTc interval >/= 480 msec (>/= 500 msec for subjects with Bundle Branch Block). Uncontrolled arrhythmias. Subjects with controlled atrial fibrillation for >1 month prior to study Day 1 were eligible.

20) Class II, III, or IV heart failure as defined by the New York Heart Association (NYHA) functional classification system. a. Abnormal cardiac valve morphology (subjects with minimal abnormalities, could be entered on study with approval from the GSK Medical Monitor).

21) Treatment refractory hypertension defined as a blood pressure of systolic> 140 mmHg and/or diastolic > 90 mm Hg which cannot be controlled by anti-hypertensive therapy

22) Patients with intra-cardiac defibrillators or permanent pacemakers

23) Cardiac metastases

24) Known immediate or delayed hypersensitivity reaction or idiosyncrasy to drugs chemically related to the study drugs, or excipients.

25) Pregnant or lactating female.

26) Unwillingness or inability to follow the procedures required in the protocol.

27) Uncontrolled diabetes, hypertension or other medical conditions that may interfere with assessment of toxicity

28) Subjects with known glucose 6 phosphate dehydrogenase (G6PD) deficiency

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Links
Registration Number: NCT01072175
Study Information on Clinical Trials Registry (clinicaltrials.gov)

Other Links:
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Results


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