Clinical Trials

Multiple Phase 1 and Phase 2 clinical trials evaluate the pharmacological profile and therapeutic application of merestinib as monotherapy or combination therapy in healthy volunteers and across oncological indications, including relapsed or refractory acute myeloid leukemia, biliary tract carcinoma, colorectal cancer, non-small-cell lung carcinoma, and advanced solid tumors. Sponsored by Eli Lilly and Company in collaboration with academic centers such as the Dana-Farber Cancer Institute and the University of Utah, these studies encompass active, completed, and terminated recruitment statuses.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02920996 TERMINATED
Carcinoma, Non-Small-Cell Lung; Solid Tumor
Dana-Farber Cancer Institute
 2016-11-11 PHASE2
NCT03125239 COMPLETED
Relapsed Adult Acute Myeloid Leukemia; Refractory Adult Acute Myeloid Leukemia
Jacqueline Garcia, MD
 2017-08-10 PHASE1
NCT02791334 COMPLETED
Solid Tumor; Microsatellite Instability-High (MSI-H) Solid Tumors; Cutaneous Melanoma; Pancreatic Cancer; Breast Cancer (HR+HER2-)
Eli Lilly and Company
 2016-06-29 PHASE1
NCT03292536 TERMINATED
Bone Metastases; Breast Cancer
University of Utah
 2018-01-11 PHASE1
NCT03027284 COMPLETED
Advanced Cancer; Metastatic Cancer; Biliary Tract Carcinoma; Cholangiocarcinoma; Gall Bladder Carcinoma; Solid Tumor; Non-Hodgkin's Lymphoma
Eli Lilly and Company
 2017-02-03 PHASE1
NCT02745769 COMPLETED
Advanced Cancer; Colorectal Cancer; Mantle Cell Lymphoma
Eli Lilly and Company
 2016-10-21 PHASE1
NCT02711553 ACTIVE_NOT_RECRUITING
Biliary Tract Cancer; Metastatic Cancer; Advanced Cancer
Eli Lilly and Company
 2016-05-19 PHASE2
NCT03125239 Completed
Relapsed Adult Acute Myeloid Leukemia|Refractory Adult Acute Myeloid Leukemia
Jacqueline Garcia MD|Eli Lilly and Company|Dana-Farber Cancer Institute
 2017-08-10 Phase 1
NCT01285037 COMPLETED
Cancer
Eli Lilly and Company
 2009-09-09 PHASE1
NCT03027284 Completed
Advanced Cancer|Metastatic Cancer|Biliary Tract Carcinoma|Cholangiocarcinoma|Gall Bladder Carcinoma|Solid Tumor|Non-Hodgkin''s Lymphoma
Eli Lilly and Company
 2017-02-03 Phase 1
NCT02745769 Completed
Advanced Cancer|Colorectal Cancer|Mantle Cell Lymphoma
Eli Lilly and Company
 2016-10-21 Phase 1
NCT02779738 COMPLETED
Healthy
Eli Lilly and Company
 2016-05 PHASE1
NCT02779738 Completed
Healthy
Eli Lilly and Company
 2016-05 Phase 1
NCT02370485 COMPLETED
Healthy
Eli Lilly and Company
 2015-02 PHASE1
NCT01981408 COMPLETED
Healthy Volunteers
Eli Lilly and Company
 2013-11 PHASE1

(data from https://clinicaltrials.gov, updated on 2024-04-11)

Check the Merestinib (LY2801653) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Merestinib (LY2801653) functions as a type-II ATP-competitive inhibitor targeting c-Met tyrosine kinase alongside related kinases such as MST1R, AXL, ROS1, and FLT3, effectively blocking receptor autophosphorylation and downstream oncogenic signal transduction. This targeted pathway inhibition suppresses tumor cell proliferation, survival, and invasive potential, providing a strong mechanistic rationale for its clinical evaluation in advanced solid tumors, biliary tract carcinomas, and relapsed acute myeloid leukemia.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.