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Also known as PF-05212377 (SAM-760), SAM-760
PF-05212377 · 5 trials · 1 indication
| Arm | Type | Description |
|---|---|---|
| PF-05212377 70 mg | EXPERIMENTAL | - |
| PF-05212377 20 mg | EXPERIMENTAL | - |
| PF-05212377 10 mg | EXPERIMENTAL | - |
| Placebo | EXPERIMENTAL | placebo, plus scopolamine 0.5 mg |
| PF-05212377 5 mg, plus scopolamine 0.5 mg; | EXPERIMENTAL | - |
| PF-05212377 20 mg, plus scopolamine 0.5 mg; | EXPERIMENTAL | - |
| PF-05212377 60 mg, plus scopolamine 0.5 mg; | EXPERIMENTAL | - |
| donepezil 10 mg, plus scopolamine 0.5 mg. | ACTIVE_COMPARATOR | - |
| PF-05212377 | EXPERIMENTAL | - |
| Active | EXPERIMENTAL | - |
| 1 | EXPERIMENTAL | active arm/healthy young |
| 2 | PLACEBO_COMPARATOR | placebo arm |
| 3 | OTHER | ketoconazole interaction evaluation |
| Name | Type | Description |
|---|---|---|
| PF-05212377 | DRUG | Single, oral dose administration of 70 mg PF-0521377 using a capsule formulation. |
| Placebo | DRUG | Capsule, single dose, oral, 1 day |
| Scopolamine | DRUG | injectable subcutaneous formulation, single dose, 1 day |
| Donepezil | DRUG | Tablet, 10mg, single dose, 1 day |
| PF-05212377 (SAM-760) | DRUG | Oral capsule, once daily for 14 days 1.5 mg, 5 mg, 15 mg, 30 mg and 50 mg |
| SAM-760 | DRUG | SAM-760 capsule, 0.25, 0.75, 2.25, 5, 10, 15, 20, 25, 35 and 45mg, single dose, 1 day |
| Placebo of SAM-760 | DRUG | SAM-760 matching placebo capsule, single dose, 1 day, |
| ketoconazole | DRUG | Ketoconazole oral tablets, 200 mg bid, 14 days |
Inclusion Criteria: * Males and females must be at least 18 years of age and no older than 55 years of age with a Body Mass Index (BMI) must be between 17.5 and 30.5. * Subjects must sign a consent form and comply with all scheduled visits, treatment plan, lab tests and other study procedures. Exc...
PF-05212377 is an investigational small molecule developed by Pfizer, Inc. It is a selective antagonist of the HTR6 receptor, also known as the 5-HT6 serotonin receptor. The compound has been studied in Phase 1 clinical trials involving healthy volunteers, and its clinical development has focused on early-stage safety, tolerability, and brain distribution assessments.
PF-05212377 targets HTR6, the serotonin 5-HT6 receptor, and acts as an antagonist at this site. By blocking HTR6, the compound was designed to modulate serotonin signaling in the brain. Preclinical and clinical work characterized its receptor binding and brain penetration using positron emission tomography imaging in healthy volunteers.
PF-05212377 is developed by Pfizer, Inc., which trades on the New York Stock Exchange under the ticker PFE. Pfizer sponsored the Phase 1 clinical program for the compound, including studies conducted in the United States and France. The molecule is also referenced in the literature and trial records as SAM-760.
PF-05212377 is in Phase 1 clinical development. All four recorded trials for the compound are Phase 1 studies, and all four are completed. The program enrolled a total of 114 participants across these trials, which were randomized, double-blind, and controlled, and involved healthy volunteers rather than patients with a disclosed disease.
PF-05212377 has been evaluated in four completed Phase 1 trials. These include NCT02005991, a PET study of brain distribution; NCT01258751, which examined plasma drug levels and brain receptor binding; NCT01213355, a scopolamine challenge study; and NCT01159496, a multiple ascending dose study of safety, tolerability, and pharmacokinetics. Enrollment ranged from 4 to 60 participants.
Yes, PF-05212377 is also known as SAM-760. Both names refer to the same Pfizer small molecule, an HTR6 antagonist studied in Phase 1 trials. Trial records for NCT01159496 list the compound under both designations, so searches using either name point to the same investigational asset and clinical program.