Table 1.
Histamine H3 receptor ligands in clinical evaluation
| Disorder | Compound | Condition | Phase | Study identifiera |
|---|---|---|---|---|
| Narcolepsy | BF2.649 | EDS | III | NCT01067222 |
| BF2.649 | Cataplexy (add on Modafinil) | III | NCT01067235 | |
| GSK‐189254 | IIc | NCT00366080 | ||
| JNJ‐17216498 | IIb | NCT00424931 | ||
| PF‐03654746 | EDS | II | NCT01006122 | |
| ADHD | MK‐0249 | IIb | NCT00475735 | |
| PF‐03654746 | IIb | NCT00531752 | ||
| Alzheimer's disease | GSK‐239512 | (mild to moderate) | II | NCT01009255 |
| MK‐0249 | Cognitive function | Ic | NCT00874939 | |
| MK‐0249 | IIb | NCT00420420 | ||
| PF‐03654746 | (mild to moderate) | I | NCT01028911 | |
| Schizophrenia | BF2.649 | Cognitive function | II | NCT00690274 |
| GSK‐239512 | Cognitive function | II | NCT01009060 | |
| MK‐0249 | Cognitive function | IIb | NCT00506077 | |
| Parkinson's disease | BF2.649 | EDS | IIb | NCT00642928 |
| BF2.649 | EDS | III | NCT01036139 | |
| Neuropathic Pain | GSK‐189254 | Hyperalgesia | Ib | NCT00387413 |
ADHD, attention deficit hyperactivity disorder; EDS, excessive daytime sleepiness; BF2.649, tiprolisant, [1‐{3‐[3‐(4‐chlorophenyl)propoxy]propyl}piperidine hydrochloride][46,47]; GSK‐189254, 6‐[(3‐cyclobutyl‐2,3,4,5‐tetrahydro‐1H‐3‐benzazepin‐7‐yl)oxy]‐N‐methyl‐3‐pyridinecarboxamide hydrochloride [54].
awww.clinicaltrials.gov.
bCompleted.
cTerminated.