Tozasertib (VX-680, MK-0457) Clinical Trials

Size	Price	Qty
25mg	USD 147
250mg	USD 470

Clinical Trials

Merck Sharp & Dohme LLC sponsored several clinical trials evaluating tozasertib across Phase 1 and Phase 2 protocols for advanced solid tumors, including non-small-cell lung carcinoma and colorectal cancer, and hematologic malignancies, such as chronic myelogenous leukemia, acute B-cell lymphocytic leukemia, and myelodysplastic syndromes. While dose-escalation assessments were successfully completed in leukemic cohorts, investigations evaluating continuous infusion regimens in solid tumors were prematurely terminated.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00099346	TERMINATED	Colorectal Cancer; Advanced Solid Tumors	Merck Sharp & Dohme LLC	2005-01	PHASE1
NCT00290550	Terminated	Carcinoma Non-Small-Cell Lung	Merck Sharp & Dohme LLC	2006-06	Phase 2
NCT00111683	Completed	Chronic Myelogenous Leukemia in Blast Crisis\|Lymphocytic Leukemia B Cell Acute\|Myelodysplastic Syndromes\|Myelogenous Leukemia Chronic	Merck Sharp & Dohme LLC	2005-06	Phase 1

(data from https://clinicaltrials.gov, updated on 2015-06-17)

Check the Tozasertib (VX-680, MK-0457) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Tozasertib functions as a potent pan-Aurora kinase inhibitor that competitively binds the ATP-binding site of Aurora A, B, and C kinases, thereby blocking key downstream mitotic phosphorylation events required for spindle assembly and centrosome maturation. This enzymatic inhibition induces G2/M cell-cycle arrest, accumulation of cells with 4N DNA content, and subsequent apoptosis, providing the biological rationale for inhibiting tumor progression in clinical conditions like non-small-cell lung cancer, colorectal carcinoma, and chronic myelogenous 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>).