Clinical Trials

PF-04691502 has been evaluated in multiple clinical trials sponsored by Pfizer to assess its safety and therapeutic efficacy across Phase 1 and Phase 2 settings. These studies primarily focused on advanced solid cancers, endometrial neoplasms, and hormone receptor-positive breast cancers, including a completed foundational dose-escalation trial evaluating safety and pharmacodynamics in advanced cancer. Further trials investigating PF-04691502 in combination with endocrine agents such as exemestane or letrozole for breast and recurrent endometrial cancers were predominantly terminated or withdrawn.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01347866 TERMINATED
Advanced Cancer
Pfizer
 2011-10 PHASE1
NCT01658176 WITHDRAWN
Breast Neoplasms
Pfizer
 2013-01 PHASE2
NCT01420081 TERMINATED
Endometrial Neoplasms
Pfizer
 2012-01-19 PHASE2
NCT01658176 Withdrawn
Breast Neoplasms
Pfizer
 2013-01 Phase 2
NCT01430585 TERMINATED
Early Breast Cancer (Phase 2); Advanced Breast Cancer (Phase 1b)
Pfizer
 2012-03 PHASE2
NCT01420081 Terminated
Endometrial Neoplasms
Pfizer
 2012-01-19 Phase 2
NCT01347866 Terminated
Advanced Cancer
Pfizer
 2011-10 Phase 1
NCT00927823 COMPLETED
Cancer
Pfizer
 2009-12 PHASE1

(data from https://clinicaltrials.gov, updated on 2018-10-29)

Check the PF-04691502 product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

PF-04691502 functions as an ATP-competitive dual inhibitor that potently binds class I PI3K isoforms and mTOR, thereby blocking downstream phosphorylation of AKT at T308 and S473 as well as effectors like p70S6K and 4EBP1. This pathway suppression leads to G1 phase cell cycle arrest and induction of apoptosis, suppressing tumor cell proliferation in PI3K- and mTOR-driven malignancies such as breast and endometrial cancers.

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.