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Name: PF-05212377
Synonyms: PF-5212377, WYE-103760, SAM-760
Therapy Type: Small Molecule (timeline)
Target Type: Other Neurotransmitters (timeline)
Condition(s): Alzheimer's Disease
U.S. FDA Status: Alzheimer's Disease (Phase 2)
Company: Pfizer


SAM-760 is an orally available antagonist of the serotonin 6 receptor (5-HT6). By modulating serotonin levels in the brain, 5-HT6 antagonists are thought to lead to secondary increases in the levels of the neurotransmitters acetylcholine and glutamate, benefitting learning and memory.  Wyeth originally developed PF 5212377 as WYE 103760, also known as as SAM 760, before becoming a subsidiary of Pfizer in 2009.


Between 2009 and 2011, Wyeth and then Pfizer conducted four Phase 1 trials of PF-05212377 in about 230 healthy volunteers. One trial, conducted in France, evaluated the effect of a single  dose of PF 5212377 on scopolamine-induced cognitive impairments for its ability to improve performance in the Groton Maze Learning Task. Also in France, a multiple ascending-dose study assessed safety, tolerability, and pharmacokinetics of once-daily dosing for 14 days, and a similar study evaluated ascending single doses of PF 5212377. A U.S. trial using Positron Emission Tomography (PET) correlated plasma drug levels and 5-HT6 receptor binding in the brain follwing a single dose.

In November 2012, Pfizer initiated a Phase 2 clinical trial to assess the efficacy of PF 5212377 in mild to moderate Alzheimer's disease patients with neuropsychiatric symptoms on a stable dose of donepezil (NCT01712074). This trial is intended to enroll approximately 342 patients from the United States.

Clinical Trial Timeline

  • Phase 2
  • Study completed / Planned end date
  • Planned end date unavailable
  • Study aborted
Sponsor Clinical Trial 2010 2011 2012 2013 2014 2015 2016 2017 2018 2019 2020 2021 2022 2023 2024 2025
Pfizer NCT01712074


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External Citations

  1. NCT01712074

Further Reading

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