Synonyms: BACE inhibitor
Therapy Type: Small Molecule (timeline)
Target Type: Amyloid-Related (timeline)
Condition(s): Alzheimer's Disease
U.S. FDA Status: Alzheimer's Disease (Discontinued)
Pfizer developed the BACE 1 inhibitor PF-06751979 for the treatment of Alzheimer's disease into Phase 1. No preclinical information on this compound was published. This drug was given as an oral suspension.
Between July 2015 and July 2016, Pfizer conducted a first-in-human, single- and multiple-ascending-dose trial of PF-06751979 in 55 healthy people in California. Doses ranged from 3 to 160 mg; treatment duration was up to two weeks. Primary outcome measures included a wide range of safety measures; secondary outcomes included plasma pharmacokinetics, as well as quantification of various CSF Aβ fragments at baseline and at two weeks.
In June 2016, a second trial started enrolling 46 elderly volunteers to evaluate single and multiple ascending doses ranging from 200 to 700 mg against placebo. Outcomes included numerous safety and pharmacokinetic and -dynamic measures, as well as measurement of these Aβ fragments: Aβ1-40, Aβ1-42, Aβ total, Aβx-40, Aβx 42, sAPPα, sAPPβ. This trial took place in Belgium. At the 2017 AAIC conference, Pfizer published results of these two trials as showing PF-06751979 to have been safe and well-tolerated, and to have reduced plasma and CSF Aβ in a dose-dependent fashion (podium presentation by Qiu et al., 2017).
In April 2017, a third trial evaluated the effect of this drug on the pharmacokinetics of midalozam in 12 healthy volunteers.
In January 2018, Pfizer announced it was ending its research and development in neurology, including this compound.
For all trials on this compound, see clinicaltrials.gov.
Last Updated: 02 Feb 2018
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