Clinical Trials

LY2874455 has been evaluated in several completed Phase I clinical trials investigating its safety, pharmacokinetics, pharmacodynamics, and therapeutic activity as both monotherapy and combination therapy with merestinib. These studies targeted patients with advanced solid tumors, relapsed or refractory adult acute myeloid leukemia, and other hematologic malignancies. Sponsorship was provided by pharmaceutical entities, including Eli Lilly and Company, alongside academic institutions such as the Dana-Farber Cancer Institute.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03125239 COMPLETED
Relapsed Adult Acute Myeloid Leukemia; Refractory Adult Acute Myeloid Leukemia
Jacqueline Garcia, MD
2017-08-10 PHASE1
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
NCT01212107 COMPLETED
Advanced Cancer
Eli Lilly and Company
2010-12 PHASE1
NCT01212107 Completed
Advanced Cancer
Eli Lilly and Company
2010-12 Phase 1

(data from https://clinicaltrials.gov, updated on 2020-06-30)

Check the LY2874455 product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

LY2874455 functions as a potent pan-fibroblast growth factor receptor (FGFR1–4) and vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor that binds the kinase ATP-binding pocket to block downstream Ras-MAPK and PI3K-AKT intracellular signaling pathways, thereby suppressing cell proliferation and tumor angiogenesis. This multi-target kinase inhibition disrupts essential oncogenic survival signals, providing a rational biological basis for its clinical evaluation in advanced solid malignancies and relapsed or refractory 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>).

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