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Phase I/II Trial of Valproic Acid and Karenitecin for Melanoma

Phase 1
Terminated
Conditions
Malignant Melanoma
Interventions
Registration Number
NCT00358319
Lead Sponsor
H. Lee Moffitt Cancer Center and Research Institute
Brief Summary

This is a Phase I study looking at the combination of Valproic Acid (VPA) and Karenitecin to treat patients with metastatic malignant melanoma. We will find the dose-limiting toxicity (DLT) and the highest dose (maximum tolerated dose) of this combination treatment that has acceptable side effects and recommend a Phase II dose level.

There will be seven escalating doses of Valproic acid and one dose escalation step of Karenitecin. Each patient shall receive one cycle of Karenitecin alone (cycle 1 days 1 - 5) followed by the same dose of Karenitecin given in combination with VPA (cycle 2 days 1-7). Patients will receive oral VPA in divided doses for 5 days and Karenitecin starting on the 3rd day every 3 weeks (a treatment cycle).

Treatment will continue until progression of disease or an unacceptable level of toxicity. After 2 cycles of treatment there will be the first efficacy evaluation or restaging of the disease. In the absence of disease progression and if there is continued safety and tolerability, treatment may continue.

Detailed Description

Treatment cycles are every 3 weeks and there are 17 study visits in all.

During Phase I subjects will receive one cycle of Karenitecin alone (cycle 1 days 1-5) and then combination therapy with VPA + Karenitecin (cycle 2 days 1-7)followed by oral VPA in divided doses for 5 days and Karenitecin starting the third day (days 3-7) every 3 weeks. After 2 cycles of treatment there will be the first efficacy evaluation or restaging of the disease.

Dose escalations will continue until unacceptable dose limiting toxicity (DLT) occurs, then dose escalation will be stopped and the previous dose level will be explored. In each dose level, participants will undergo pharmacokinetic (PK) sampling to determine blood levels. The melanoma skin lesions will also be biopsied to measure the effect of the combination therapy.

All patients enrolled in the Phase II will be treated with VPA and Karenitecin using the dosing schedule determined to be the MTD in Phase I. In the absence of disease progression and if there is continued safety and tolerability, treatment may continue in consecutive 3 week cycles.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
42
Inclusion Criteria

Same for Phase I & II

  • Cytologically/histologically-documented metastatic (stage IV) malignant melanoma
  • Age greater than or equal to 18 years old
  • ECOG performance status 0-2
  • Subjects must be able to give informed consent and be able to follow the guidelines given in the study
  • The subject has no major impairment of hematological function, as defined by the following laboratory parameters: WBC > 3.0x109/L; ANC > 1.5 x 109/L; Hgb > 9.0g/dL; PLT >100x109/L. Red blood cell transfusions and repeat evaluations for study entry are allowed
  • All subjects of reproductive potential must use an effective method of contraception during the study and three months following termination of treatment (Not applicable to patients with bilateral oophorectomy and/or hysterectomy or to those patients who are postmenopausal.)
  • Subjects with biopsiable disease are preferred but not mandatory; subjects with biopsiable disease will be encouraged to undergo biopsy.
Exclusion Criteria

Phase I:

  • Subjects must not have evidence of significant active infection (e.g., pneumonia, cellulitis, wound abscess, etc.) at time of study entry.
  • Subjects must have adequate renal and normal hepatic function (creatinine < 1.5 x upper limit of normal (ULN), bilirubin and SGOT (AST) < 1.5 X ULN) obtained within 4 weeks prior to registration.
  • Pregnant women are excluded from the study because VPA is known to cause birth defects. Nursing mothers are excluded from this trial as effects on newborns and excretion of either drug in milk is unknown.
  • Women of childbearing age must have a negative pregnancy test and be willing to use a highly effective method of contraception. Men who are sexually active must also be willing to use an accepted and effective method of contraception.
  • Subjects with uncontrolled CNS metastasis or a history of seizures are excluded. Subjects with stable CNS metastasis (either surgically resected, treated with the gamma knife or stable for 3 months following whole brain radiotherapy are eligible)

Phase II:

  • Subjects must not have evidence of significant active infection (e.g., pneumonia, cellulitis, wound abscess, etc.) at time of study entry.
  • Subjects must have adequate renal and normal hepatic function (creatinine < 1.5 x upper limit of normal (ULN), bilirubin and SGOT (AST) < 1.5 X ULN) obtained within 4 weeks prior to registration.
  • Pregnant women are excluded from the study because VPA is known to cause birth defects. Nursing mothers are excluded from this trial as effects on newborns and excretion of either drug in milk is unknown.
  • Women of childbearing age must have a negative pregnancy test and be willing to use a highly effective method of contraception. Men who are sexually active must also be willing to use an accepted and effective method of contraception.
  • Subjects with uncontrolled CNS metastasis or a history of seizures are excluded. Subjects with stable CNS metastasis (either surgically resected, treated with the gamma knife or stable for 3 months following whole brain radiotherapy are eligible)
  • Subjects who have been previously treated with more than 2 prior chemotherapy regimens. Any previous immunotherapy regimens are allowed.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Phase IKarenitecinDose escalation phase
Phase IValproic AcidDose escalation phase
Phase IIValproic AcidAll patients enrolled in the Phase II will be treated with Valproic Acid (VPA) and Karenitecin using the dosing schedule determined to be the Maximum Tolerated Dose (MTD) in Phase I.
Phase IIKarenitecinAll patients enrolled in the Phase II will be treated with Valproic Acid (VPA) and Karenitecin using the dosing schedule determined to be the Maximum Tolerated Dose (MTD) in Phase I.
Primary Outcome Measures
NameTimeMethod
Maximum tolerated dose (MTD) of Valproic Acid and KarenitecinAverage of 6 months
Time to progression (TTP)Average of 6 months
Safety profile of Valproic Acid (VPA) and KarenitecinAverage of 6 months
Response rateAverage of 6 months
Overall survival (OS)Average of 6 months
Secondary Outcome Measures
NameTimeMethod
Pharmacokinetic parameters of VPA and KarenitecinAverage of 6 months
Relationship between topo I expression, location and DNA strand breakageAverage of 6 months
Patient response to this drug combinationAverage of 6 months

Trial Locations

Locations (1)

H. Lee Moffitt Cancer Center & Research Institute

🇺🇸

Tampa, Florida, United States

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