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| Clinical data | |
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| Other names | NBI75043; NBI-1; "Compound 2a"[1] |
| Routes of administration | Oral[2][3] |
| Drug class | H1 receptor antagonist;Antihistamine;Sedative;Hypnotic |
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| Pharmacokinetic data | |
| Eliminationhalf-life | Oral: 6.7 hours[3] IVTooltip Intravenous injection: 9.1 hours[3] |
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| Chemical and physical data | |
| Formula | C19H22N2S |
| Molar mass | 310.46 g·mol−1 |
| 3D model (JSmol) | |
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NBI-75043 is apotent and highlyselectivehistamineH1 receptorantagonist orantihistamine which was under development for the treatment ofinsomnia but was never marketed.[2][4][5][1] It is takenorally.[2][3] The drug has been found to enhance bothslow wave sleep andREM sleep in rodents.[1] Itselimination half-life was found to be 6.7 hoursorally and 9.1 hours byintravenous injection in aclinical study.[3] For comparison,diphenhydramine had a half-life of 12 hours and 9.3 hours by these respectiveroutes in the same study.[3] Thechemical synthesis of NBI-75043 has been described.[1] NBI-75043 was under development byNeurocrine Biosciences.[2] It enteredphase 1clinical trials for insomnia in 2006 and completed a phase 1 trial the same year.[2][4] No further development was reported after that and its development was eventually discontinued.[2][4] Studies of NBI-75043 were published in 2009.[1][3]
This compound appears to be NBI-75043, which was reported to have entered Phase I trials in 2006 [128]. No further development activity has been disclosed.
NBI-75043 (22) is a highly selective and potent H1 receptor antagonist that was under evaluation for safety and efficacy in the treatment of insomnia.
