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Pharmacokinetics of Enzastaurin HCl in Native Chinese Patients With Advanced and/or Metastatic Solid Tumors or Lymphoma

Phase 1
18 Years
Open (Enrolling)
Solid Tumor, Lymphoma, Malignant

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Trial Information

Pharmacokinetics of Enzastaurin HCl in Native Chinese Patients With Advanced and/or Metastatic Solid Tumors or Lymphoma

Inclusion Criteria:

- Have given written informed consent

- Have a histologic or cytologic diagnosis of cancer (solid tumor or lymphoma) with
clinical or radiologic evidence of locally advanced and/or metastatic disease for
which no life-prolonging therapy exists. (Note: patients with glioblastoma, and other
hematologic malignancies [except lymphoma] are excluded from this study.)

- Male and female patients with reproductive potential must use an approved
contraceptive method, if appropriate (for example, intrauterine device, birth control
pills, or barrier device) during and for 3 months after discontinuation of study
treatment. Women with childbearing potential must have a negative serum pregnancy
test within 7 days prior to study enrollment.

- Have a performance status of 0 to 2 on the Eastern Cooperative Oncology Group (ECOG)
scale and, in the investigator's opinion, are suitable for participation in the study

- Have discontinued all previous therapies for cancer, including chemotherapy,
radiotherapy, anticancer hormone therapy, or other investigational therapy for at
least 30 days prior to study entry (6 weeks for mitomycin-C or nitrosoureas), and
have recovered from the acute effects of therapy

- If the patients have hormone-refractory prostate cancer, the study doctor will
discuss with the patients what drugs they would be allowed to continue to receive
during the study

- Have adequate organ function, including:

- Bone Marrow Reserve: absolute neutrophil count (ANC) greater than or equal to
1.5 × 10^9/L prior to treatment, platelets greater than or equal to 100 ×
10^9/L, and hemoglobin greater than or equal to 10 g/dL. Patients may receive
erythrocyte transfusions to achieve this hemoglobin level at the discretion of
the investigator. Patients may be allowed erythropoietin of choice as per
standard of care.

- Hepatic: bilirubin within 1.5 times the upper limit of normal (ULN), alanine
transaminase, and aspartate transaminase less than or equal to 2.5 times ULN or
less than or equal to 5 times ULN when liver metastases are known

- Renal: serum creatinine less than or equal to 1.5 mg/dL

- Electrolytes: Patients may be entered into the study if, in the investigator's
opinion, any electrolyte disorders, including potassium less than 3.4 mEq/L, calcium
less than 8.4 mg/dL, or magnesium less than 1.2 mEq/L, may be appropriately managed
and stabilized by the time of the laboratory evaluation on the lead-in day. If
electrolytes have not been stabilized during this time, the patient will be
discontinued from the study. Patients with hypercalcemia are excluded.

- Have an estimated life expectancy, in the judgment of the investigator, that will
permit the patient to complete the PK phase and at least 1 cycle of the safety
extension phase (if the patient were to participate in the safety extension phase)

Exclusion Criteria:

- Have received treatment within 28 days of the first dose of study drug with an
experimental agent for non cancer indications that has not received regulatory
approval for any indication

- Patients with glioblastoma or hematologic malignancies other than lymphoma are
excluded from this study. Patients who have central nervous system (CNS) metastases
(unless the patient has completed successful local therapy for CNS metastases and has
been off of corticosteroids for at least 4 weeks before starting study therapy) are
excluded. In the absence of a clinical suspicion of brain metastases, no screening
computed tomography (CT) or magnetic resonance imaging (MRI) scan before enrollment
is required.

- Serious concomitant systemic disorder, including active infection, that is
incompatible with the study (at the discretion of the investigator)

- Have a history of human immunodeficiency virus (HIV), hepatitis B, or hepatitis C

- Have a serious cardiac condition

- Have abnormal electrocardiogram (ECG) findings, at the discretion of the investigator

- Use medications that are known to cause certain changes in electrocardiogram (ECG)

- Have a history of unexplained syncope (fainting or passing out) within the last year,
or have a known family history of unexplained sudden death

- Have had a complete gastrectomy or other significant gastrointestinal diseases that,
in the investigator's opinion, may significantly impact drug absorption

- Are receiving total parenteral nutrition

- Are not able to swallow tablets

- Are a woman who is breast feeding, lactating, or pregnant

- Are allergic to enzastaurin

- Are receiving herbal regimens

- Drugs and herbal supplements that are known to be potent or moderate inhibitors or
inducers of cytochrome P450 (CYP)3A are specifically excluded. Foods that are known
to be potent or moderate inhibitors of CYP3A (for example, grapefruit, grapefruit
juice, Seville oranges, or Seville orange juice) are also specifically excluded
during the study. In addition, starfruit and starfruit juice are excluded during the
PK phase of the study.

- Drugs with narrow therapeutic windows that are also known substrates of CYP2C9,
CYP2C8, CYP2C19, and CYP3A are excluded

- Have an average weekly alcohol intake that exceeds 21 units per week (men) and 14
units per week (women) or are unwilling to stop alcohol consumption from the lead-in
day through the completion of collecting samples for study drug measurement (1 unit =
12 oz or 360 mL of beer; 5 oz or 150 mL of wine; 1.5 oz or 45 mL of distilled

- Use of drugs of abuse, as evidenced by history and/or positive findings on urinary
drug screening, unless prescribed by a physician (for example, narcotic pain

- The investigator thinks you should not participate for any reason

Type of Study:


Study Design:

Allocation: Non-Randomized, Endpoint Classification: Pharmacokinetics Study, Intervention Model: Single Group Assignment, Masking: Open Label

Outcome Measure:

Pharmacokinetics: area under the concentration-time curve over a dosing interval at steady state (AUCt,ss) of enzastaurin, its principle metabolites and total analyte

Outcome Time Frame:

Day 14 dose: Predose and up to 96 hours post dose

Safety Issue:


Principal Investigator

Call 1-877-CTLILLY (1-877-285-4559) or 1-317-615-4559 Mon - Fri 9 AM - 5 PM Eastern time (UTC/GMT - 5 hours, EST)

Investigator Role:

Study Director

Investigator Affiliation:

Eli Lilly and Company


China: Food and Drug Administration

Study ID:




Start Date:

November 2011

Completion Date:

June 2014

Related Keywords:

  • Solid Tumor
  • Lymphoma, Malignant
  • Lymphoma
  • Neoplasms