Clinical Trials

Multiple completed Phase 1, Phase 1/2, and Phase 2 clinical trials sponsored by Eli Lilly and Company have evaluated the therapeutic potential and pharmacokinetic profile of Rabusertib (LY2603618). These investigations primarily focused on indications including solid tumors, pancreatic neoplasms, and non-small cell lung cancer, testing Rabusertib both as a monotherapy and in combination with standard chemotherapeutics such as gemcitabine, pemetrexed, and cisplatin.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01341457 COMPLETED
Solid Tumors
Eli Lilly and Company
 2011-05 PHASE1
NCT01139775 COMPLETED
Non Small Cell Lung Cancer
Eli Lilly and Company
 2011-02 PHASE1; PHASE2
NCT00839332 COMPLETED
Pancreatic Neoplasms
Eli Lilly and Company
 2009-02 PHASE1; PHASE2
NCT00988858 COMPLETED
Non Small Cell Lung Cancer
Eli Lilly and Company
 2009-11 PHASE2
NCT01358968 COMPLETED
Cancer
Eli Lilly and Company
 2011-06 PHASE1
NCT01296568 COMPLETED
Advanced Cancer
Eli Lilly and Company
 2011-02 PHASE1
NCT01341457 Completed
Solid Tumors
Eli Lilly and Company
 2011-05 Phase 1
NCT01296568 Completed
Advanced Cancer
Eli Lilly and Company
 2011-02 Phase 1
NCT01139775 Completed
Non Small Cell Lung Cancer
Eli Lilly and Company
 2011-02 Phase 1|Phase 2
NCT00415636 COMPLETED
Cancer
Eli Lilly and Company
 2007-01 PHASE1
NCT00988858 Completed
Non Small Cell Lung Cancer
Eli Lilly and Company
 2009-11 Phase 2
NCT00839332 Completed
Pancreatic Neoplasms
Eli Lilly and Company
 2009-02 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2019-03-01)

Check the Rabusertib (LY2603618) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Rabusertib selectively binds to and inhibits checkpoint kinase 1 (Chk1), blocking ATP-dependent phosphorylation and disrupting the cellular DNA damage response checkpoint system. This target inhibition prevents DNA repair in replication-stressed malignant cells, inducing cell cycle arrest and apoptosis to potentiate anti-tumor activity in clinical settings such as solid tumors, non-small cell lung cancer, and pancreatic neoplasms.

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.