Clinical Trials

Numerous Phase 1, Phase 2, and Phase 1/2 clinical trials evaluate prexasertib monotherapy and combination regimens for indications including advanced solid tumors, platinum-resistant ovarian cancer, small cell lung cancer, pediatric brain tumors such as medulloblastoma, and acute myeloid leukemia. Sponsored by Eli Lilly and Company alongside major academic centers including Dana-Farber Cancer Institute, Memorial Sloan Kettering Cancer Center, and St. Jude Children's Research Hospital, these studies encompass completed, active non-recruiting, and terminated recruitment statuses.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04095221 COMPLETED
Desmoplastic Small Round Cell Tumor; Rhabdomyosarcoma
Memorial Sloan Kettering Cancer Center
 2019-09-17 PHASE1; PHASE2
NCT04023669 COMPLETED
Brain Tumor; Brain Tumor, Recurrent; Brain Tumor, Refractory; Brain Tumor, Pediatric; Medulloblastoma; Medulloblastoma Recurrent; Medulloblastoma, Non-WNT/Non-SHH; Medulloblastoma, Non-WNT/Non-SHH, Group 3; Medulloblastoma, Non-WNT/Non-SHH, Group 4; Brain Cancer; CNS Cancer; CNS Tumor; CNS Neoplasm
St. Jude Children's Research Hospital
 2019-08-08 PHASE1
NCT02649764 COMPLETED
Chronic Myelomonocytic Leukemia; Recurrent Acute Myeloid Leukemia; Recurrent High Risk Myelodysplastic Syndrome; Refractory Acute Myeloid Leukemia; Refractory High Risk Myelodysplastic Syndrome
M.D. Anderson Cancer Center
 2016-05-04 PHASE1
NCT04032080 COMPLETED
Triple Negative Breast Cancer
Baylor Research Institute
 2019-09-05 PHASE2
NCT02203513 TERMINATED
Ovarian Cancer; Breast Cancer; Prostate Cancer
National Cancer Institute (NCI)
 2015-01-20 PHASE2
NCT03495323 COMPLETED
Cancer
Dana-Farber Cancer Institute
 2018-05-16 PHASE1
NCT02873975 COMPLETED
Advanced Cancers
Dana-Farber Cancer Institute
 2016-10-12 PHASE2
NCT03057145 COMPLETED
Solid Tumor
Geoffrey Shapiro, MD, PhD
 2017-03-10 PHASE1
NCT02124148 COMPLETED
Neoplasm Metastasis; Colorectal Neoplasms; Breast Cancer
Eli Lilly and Company
 2014-06-18 PHASE1
NCT02808650 COMPLETED
Childhood Solid Neoplasm; Recurrent Malignant Solid Neoplasm; Recurrent Primary Central Nervous System Neoplasm; Refractory Malignant Solid Neoplasm; Refractory Primary Central Nervous System Neoplasm
Children's Oncology Group
 2017-02-27 PHASE1
NCT04095221 Active not recruiting
Desmoplastic Small Round Cell Tumor|Rhabdomyosarcoma
Memorial Sloan Kettering Cancer Center
 2019-09-17 Phase 1|Phase 2
NCT03414047 COMPLETED
Ovarian Cancer
Eli Lilly and Company
 2018-04-10 PHASE2
NCT03735446 TERMINATED
Acute Myeloid Leukemia; Myelodysplastic Syndromes
Dana-Farber Cancer Institute
 2019-01-18 PHASE1
NCT02555644 COMPLETED
Head and Neck Neoplasms
Eli Lilly and Company
 2016-02-24 PHASE1
NCT03495323 Completed
Cancer
Dana-Farber Cancer Institute|Eli Lilly and Company
 2018-05-16 Phase 1
NCT03414047 Completed
Ovarian Cancer
Eli Lilly and Company
 2018-04-10 Phase 2
NCT02735980 COMPLETED
Small Cell Lung Cancer
Eli Lilly and Company
 2016-05-11 PHASE2
NCT02860780 COMPLETED
Advanced Cancer; Metastatic Cancer; Colorectal Cancer; Non-small Cell Lung Cancer
Eli Lilly and Company
 2016-08-10 PHASE1
NCT02778126 COMPLETED
Advanced Cancer
Eli Lilly and Company
 2016-09-22 PHASE1
NCT02514603 COMPLETED
Neoplasm
Eli Lilly and Company
 2015-10 PHASE1
NCT03057145 Completed
Solid Tumor
Geoffrey Shapiro MD PhD|Eli Lilly and Company|AstraZeneca|Dana-Farber Cancer Institute
 2017-03-10 Phase 1
NCT01115790 COMPLETED
Advanced Cancer; Squamous Cell Carcinoma; Carcinoma, Squamous Cell of Head and Neck; Lung Squamous Cell Carcinoma Stage IV; Anal Squamous Cell Carcinoma; Carcinoma, Non-Small-Cell Lung
Eli Lilly and Company
 2010-02 PHASE1

(data from https://clinicaltrials.gov, updated on 2025-02-20)

Check the Prexasertib (LY2606368) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Prexasertib functions as a potent, ATP-competitive inhibitor of checkpoint kinases 1 and 2 (Chk1/2), which abrogates DNA damage-induced cell cycle arrest and disrupts DNA repair pathways. This checkpoint failure leads to persistent double-strand DNA breaks, premature mitotic entry, and apoptosis, driving therapeutic efficacy in clinical evaluations against advanced solid tumors, small cell lung cancer, and platinum-resistant ovarian cancer.

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.