Clinical Trials

Multiple completed Phase 1 clinical trials sponsored by Pfizer evaluated the investigational compound PF-04995274 in healthy volunteers to characterize its initial safety, tolerability, pharmacokinetics, and pharmacodynamics. These studies encompassed a first-in-human dose-escalation design, central biomarker assessments, and positron emission tomography imaging to measure 5-HT4 receptor occupancy.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01193062 Completed
Healthy
Pfizer
 2010-09 Phase 1
NCT01173757 Completed
Healthy
Pfizer
 2010-08 Phase 1
NCT01091272 Completed
Healthy
Pfizer
 2010-04 Phase 1

(data from https://clinicaltrials.gov, updated on 2024-05-22)

Check the PF-04995274 product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

PF-04995274 selectively binds to and acts as a potent partial agonist of the serotonin 4 receptor (5-HT4R), stimulating intracellular G protein-coupled signaling pathways to promote neurotransmitter release and synaptic efficacy. By crossing the blood-brain barrier to engage central 5-HT4 receptors, this molecular mechanism modulates key neurochemical processes, establishing the rationale for its Phase 1 clinical evaluation assessing safety, pharmacodynamics, and receptor occupancy in healthy human volunteers.

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.