NCT01432951

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

Completed Phase 1 Results posted Last updated 14 September 2020

What this trial tests

Phase 1 trial testing Enzastaurin in Solid Tumor in 26 participants. Completed in 5 January 2018.

Timeline

1 November 2011

Primary endpoint
11 January 2013

5 January 2018

Quick facts

Lead sponsor	Eli Lilly and Company
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	na
Design	single group
Masking	none
Primary purpose	other
Enrollment	26
Start date	1 November 2011
Primary completion	11 January 2013
Estimated completion	5 January 2018
Sites	3 locations across China

Drugs / interventions tested

• Enzastaurin — full drug profile →

Conditions studied

• Solid Tumor — all drugs for Solid Tumor →
• Lymphoma, Malignant — all drugs for Lymphoma, Malignant →

Sponsor

Eli Lilly and Company — full company profile →

Who can join

18 and older, any sex, with Solid Tumor or Lymphoma, Malignant. Patients with the condition only — healthy volunteers not accepted.

What's being measured

Primary outcomes are the specific endpoints the trial is designed to prove or disprove.

• 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
  Time frame: Day 14: Predose and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose
  PK (AUCt,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported.
• PK: Maximum Observed Drug Concentration at Steady State (Cmax,ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma
  Time frame: Day 14: Predose and and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose
  PK (Cmax,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported.
• PK: Time of Maximal Plasma Concentration at Steady State (Tmax, ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma
  Time frame: Day 14: Predose and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose
  PK (tmax,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported.
• PK: Average Concentration During a Dosing Interval at Steady State (Cav,ss) of Enzastaurin, It's Metabolites and Total Analytes in Plasma
  Time frame: Day 14: Predose and and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose
  PK (Cav,ss) of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported.
• PK: Terminal Elimination Half-Life of Enzastaurin, It's Metabolites and Total Analytes in Plasma
  Time frame: Day 14: Predose and 1, 2, 4, 6, 8, 10, 24, 48, 72, and 96 hours post dose
  PK terminal elimination half-life of Enzastaurin, its metabolites (LSN326020, LSN485912, and LSN2406799), and total analyte in plasma (enzastaurin + LSN326020 + LSN485912 + LSN2406799) were reported.

Sponsor's own description

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.

Publications & conference data

4 peer-reviewed publications reference this trial (live from Europe PMC):

1. Activators and Inhibitors of NRF2: A Review of Their Potential for Clinical Development.
   Robledinos-Antón N, Fernández-Ginés R, Manda G, Cuadrado A. · · 2019 · cited 443× · PMID 31396308 · DOI 10.1155/2019/9372182
2. Oxidative stress in cancer: from tumor and microenvironment remodeling to therapeutic frontiers.
   Liang X, Weng J, You Z, Wang Y, et al · · 2025 · cited 50× · PMID 40847302 · DOI 10.1186/s12943-025-02375-x
3. Current trends in clinical trials and the development of small molecule epigenetic inhibitors as cancer therapeutics.
   Zohourian N, Brown JA. · · 2024 · cited 5× · PMID 38639711 · DOI 10.2217/epi-2023-0443
4. A pharmacokinetic and safety study of a fixed oral dose of enzastaurin HCl in native Chinese patients with refractory solid tumors and lymphoma.
   Li X, Fang X, Li S, Zhang W, et al · · 2016 · cited 4× · PMID 26942463 · DOI 10.18632/oncotarget.7875