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| ID | Type | Description | Link |
|---|---|---|---|
| H6Q-FW-JCCC | Other Identifier | Eli Lilly and Company |
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The purpose of this study is to assess the pharmacokinetics (PK) of enzastaurin and its metabolites in native Chinese participants with advanced and/or metastatic solid tumors or lymphoma. Information about any side effects that may occur will also be collected. Treatment of disease is not the main purpose of the study.
This is a Phase 1 study of enzastaurin in native Chinese participants with advanced and/or metastatic solid tumors or lymphoma. Participants will receive daily doses of enzastaurin for 14 days, stop dosing for 3 days during PK sampling, and resume dosing on Day 18. Participants may be allowed to receive enzastaurin for approximately 2 to 4 weeks after day 18 to provide an opportunity for a participant's oncologist to assess the potential benefit of the participant continuing to receive enzastaurin in the safety extension phase. There is no planned duration for the extension phase; participants are allowed to continue receiving enzastaurin until disease progression or other reason for discontinuation as per the investigator's assessment.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Enzastaurin | Experimental | Enzastaurin 500 mg, four 125-mg tablets administered orally once daily for 14 days. Dosing is held for 3 days, and resumes on Day 18. Participants may continue receiving optional enzastaurin for an additional 2 to 4 weeks. Safety Extension: Participants had the option to continue receiving enzastaurin until disease progression or discontinuation criteria are met, as per the investigator's assessment. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Enzastaurin | Drug | Administered orally |
|
|
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics (PK): Area Under the Concentration -Time Curve Over a Dosing Interval at Steady State (AUCt,ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma | PK (AUCt,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported. | Day 14: Predose and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose |
| PK: Maximum Observed Drug Concentration at Steady State (Cmax,ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma | PK (Cmax,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported. | Day 14: Predose and and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose |
| PK: Time of Maximal Plasma Concentration at Steady State (Tmax, ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma | PK (tmax,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported. | Day 14: Predose and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose |
| PK: Average Concentration During a Dosing Interval at Steady State (Cav,ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma | PK (Cav,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported. | Day 14: Predose and and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose |
| PK: Terminal Elimination Half-Life of Enzastaurin, It's Metabolites and Total Analytes in Plasma | PK terminal elimination half-life of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported. |
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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: participants with glioblastoma, and other hematologic malignancies [except lymphoma] are excluded from this study.)
Male and female participants 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 participants have hormone-refractory prostate cancer, the study doctor will discuss with the participants what drugs they would be allowed to continue to receive during the study
Have adequate organ function, including:
Electrolytes: Participants may be entered into the study if, in the investigator's opinion, any electrolyte disorders, including potassium less than 3.4 milliequivalents/liter (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 participant will be discontinued from the study. Participants with hypercalcemia are excluded.
Have an estimated life expectancy, in the judgment of the investigator, that will permit the participant to complete the PK phase and at least 1 cycle of the safety extension phase (if the participant were to participate in the safety extension phase)
Exclusion Criteria:
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.
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| Name | Affiliation | Role |
|---|---|---|
| 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) | Eli Lilly and Company | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. | Beijing | 100071 |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 26942463 | Derived | Li X, Fang X, Li S, Zhang W, Yang N, Cui Y, Huang H, Cai R, Lin X, Fu X, Hong H, Lin T. A pharmacokinetic and safety study of a fixed oral dose of enzastaurin HCl in native Chinese patients with refractory solid tumors and lymphoma. Oncotarget. 2016 Apr 5;7(14):18585-93. doi: 10.18632/oncotarget.7875. |
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Participants who were considered to have completed the study who received at least 1 dose of study drug and from whom a valid assay result was obtained.
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| ID | Title | Description |
|---|---|---|
| FG000 | Enzastaurin | Enzastaurin 500 mg, four 125-mg tablets was administered orally once daily for 14 days. Dosing is held for 3 days, and resumes on Day 18. Participants may continue receiving optional enzastaurin treatment for up to 30 days. Safety Extension: Participants had the option to continue receiving enzastaurin treatment until disease progression or discontinuation criteria are met, as per the investigator's assessment. |
| Title | Milestones | Reasons Not Completed | |||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Treatment Phase (Day 1 to 30) |
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| |||||||||||||||||||||||||||
| Safety Extension Day 30 to End of Study |
|
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| ID | Title | Description |
|---|---|---|
| BG000 | Enzastaurin | Enzastaurin 500 mg, four 125-mg tablets was administered orally once daily for 14 days. Dosing is held for 3 days, and resumes on Day 18. Participants may continue receiving optional enzastaurin treatment for up to 30 days. |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | Mean |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | |||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Pharmacokinetics (PK): Area Under the Concentration -Time Curve Over a Dosing Interval at Steady State (AUCt,ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma | PK (AUCt,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported. | All participants who received at least one dose of study drug had evaluable PK data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanomole*hour/Liter (nmol*h/L) | Day 14: Predose and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose |
|
From Baseline to Study Completion (Up to 6 years and 1 month)
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | Enzastaurin | Enzastaurin 500 mg, four 125-mg tablets was administered orally once daily for 14 days. Dosing is held for 3 days, and resumes on Day 18. Participants may continue receiving optional enzastaurin treatment for up to 30 days. |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Leukopenia | Blood and lymphatic system disorders | MedDRA 14.0 | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Chief Medical Officer | Eli Lilly and Company | 800-545-5979 | ClinicalTrials.gov@lilly.com |
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| ID | Term |
|---|---|
| D008223 | Lymphoma |
| ID | Term |
|---|---|
| D009370 | Neoplasms by Histologic Type |
| D009369 | Neoplasms |
| D008232 | Lymphoproliferative Disorders |
| D008206 | Lymphatic Diseases |
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| ID | Term |
|---|---|
| C504878 | enzastaurin |
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| Day 14: Predose and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose |
| China |
| For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. | Changsha | 410013 | China |
| For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. | Guangzhou | 510060 | China |
| years |
|
| Sex: Female, Male | Count of Participants | Participants | No |
|
| Ethnicity (NIH/OMB) | Count of Participants | Participants | No |
|
| Race (NIH/OMB) | Count of Participants | Participants | No |
|
| Region of Enrollment | Number | participants |
|
|
|
| Primary | PK: Maximum Observed Drug Concentration at Steady State (Cmax,ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma | PK (Cmax,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported. | All participants who received at least one dose of study drug had evaluable PK data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanomole/liter (nmol/L) | Day 14: Predose and and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose |
|
|
|
| Primary | PK: Time of Maximal Plasma Concentration at Steady State (Tmax, ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma | PK (tmax,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported. | All participants who received at least one dose of study drug had evaluable PK data. | Posted | Median | Full Range | Hour (h) | Day 14: Predose and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose |
|
|
|
| Primary | PK: Average Concentration During a Dosing Interval at Steady State (Cav,ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma | PK (Cav,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported. | All participants who received at least one dose of study drug had evaluable PK data. | Posted | Geometric Mean | Geometric Coefficient of Variation | nmol/L | Day 14: Predose and and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose |
|
|
|
| Primary | PK: Terminal Elimination Half-Life of Enzastaurin, It's Metabolites and Total Analytes in Plasma | PK terminal elimination half-life of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported. | All participants who received at least one dose of study drug had evaluable PK data. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hour (h) | Day 14: Predose and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose |
|
|
|
| 0 |
| 25 |
| 19 |
| 25 |
| EG001 | Enzastaurin Safety Extension | Participants had the option to continue receiving enzastaurin 500 mg, orally once daily until disease progression or discontinuation criteria are met, as per the investigator's assessment. | 0 | 15 | 9 | 15 |
| Neutropenia | Blood and lymphatic system disorders | MedDRA 14.0 | Systematic Assessment |
|
| Sinus tachycardia | Cardiac disorders | MedDRA 14.0 | Systematic Assessment |
|
| Abdominal distension | Gastrointestinal disorders | MedDRA 14.0 | Systematic Assessment |
|
| Abdominal pain | Gastrointestinal disorders | MedDRA 14.0 | Systematic Assessment |
|
| Diarrhoea | Gastrointestinal disorders | MedDRA 14.0 | Systematic Assessment |
|
| Faeces hard | Gastrointestinal disorders | MedDRA 14.0 | Systematic Assessment |
|
| Gastritis | Gastrointestinal disorders | MedDRA 14.0 | Systematic Assessment |
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| Gingival swelling | Gastrointestinal disorders | MedDRA 14.0 | Systematic Assessment |
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| Reflux oesophagitis | Gastrointestinal disorders | MedDRA 14.0 | Systematic Assessment |
|
| Fatigue | General disorders | MedDRA 14.0 | Systematic Assessment |
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| Oedema | General disorders | MedDRA 14.0 | Systematic Assessment |
|
| Pain | General disorders | MedDRA 14.0 | Systematic Assessment |
|
| Furuncle | Infections and infestations | MedDRA 14.0 | Systematic Assessment |
|
| Lung infection | Infections and infestations | MedDRA 14.0 | Systematic Assessment |
|
| Nasopharyngitis | Infections and infestations | MedDRA 14.0 | Systematic Assessment |
|
| Upper respiratory tract infection | Infections and infestations | MedDRA 14.0 | Systematic Assessment |
|
| Alanine aminotransferase increased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Aspartate aminotransferase increased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Blood albumin decreased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Blood bilirubin | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Blood follicle stimulating hormone | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Blood luteinising hormone increased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Blood potassium decreased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Electrocardiogram qt prolonged | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Haemoglobin decreased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Lymphocyte count decreased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Lymphocyte count increased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Neutrophil count decreased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Platelet count decreased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Protein total decreased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| White blood cell count decreased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| White blood cell count increased | Investigations | MedDRA 14.0 | Systematic Assessment |
|
| Back pain | Musculoskeletal and connective tissue disorders | MedDRA 14.0 | Systematic Assessment |
|
| Pain in extremity | Musculoskeletal and connective tissue disorders | MedDRA 14.0 | Systematic Assessment |
|
| Insomnia | Psychiatric disorders | MedDRA 14.0 | Systematic Assessment |
|
| Chromaturia | Renal and urinary disorders | MedDRA 14.0 | Systematic Assessment |
|
| Dyspnoea | Respiratory, thoracic and mediastinal disorders | MedDRA 14.0 | Systematic Assessment |
|
| Epistaxis | Respiratory, thoracic and mediastinal disorders | MedDRA 14.0 | Systematic Assessment |
|
| Dry skin | Skin and subcutaneous tissue disorders | MedDRA 14.0 | Systematic Assessment |
|
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| D006425 | Hemic and Lymphatic Diseases |
| D007160 | Immunoproliferative Disorders |
| D007154 | Immune System Diseases |
| Title | Measurements |
|---|---|
|
| LSN2406799 |
|
| Total Analytes |
|
| Title | Measurements |
|---|---|
|
| LSN2406799 |
|
| Total Analytes |
|
| Title | Measurements |
|---|---|
|
| LSN2406799 |
|
| Total Analytes |
|
| Title | Measurements |
|---|---|
|
| LSN2406799 |
|
| Total Analytes |
|