Clinical Trials

PF-05251749 has been evaluated in several clinical trials sponsored by Biogen, all of which are completed Phase 1 studies involving healthy adult and elderly subjects. These investigations primarily assessed early-stage safety, tolerability, and pharmacokinetic profiling. The resulting data provided foundational safety and bioavailability profiles to support the compound's viability for targeting circadian rhythm disruptions in neurodegenerative disorders.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02691702 COMPLETED
Healthy Adult Subjects; Healthy Elderly Subjects
Biogen
 2016-03-28 PHASE1
NCT02443740 COMPLETED
Healthy
Biogen
 2015-05-31 PHASE1

(data from https://clinicaltrials.gov, updated on 2021-02-17)

Check the PF-05251749（CK1-IN-2） product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

PF-05251749 acts as a potent, brain-penetrant inhibitor that selectively binds Casein Kinase 1 delta (CK1δ) and epsilon (CK1ε), thereby blocking downstream serine/threonine phosphorylation of circadian regulatory proteins and altering cellular clock dynamics. By regulating central circadian molecular pathways, this targeted enzyme inhibition provides the mechanistic rationale for evaluating its safety, tolerability, and pharmacokinetic profiles in healthy adult and elderly subjects participating in early-phase clinical trials.

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.