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| Routes of administration | Oral |
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| Eliminationhalf-life | 1.5–1.8 hours |
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| ECHA InfoCard | 100.133.676 |
| Chemical and physical data | |
| Formula | C20H16N4O2S |
| Molar mass | 376.43 g·mol−1 |
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Indiplon (INN andUSAN) is a unmarketednonbenzodiazepine,hypnoticsedative that was developed in two formulations—an immediate-release formulation for sleep onset, and a modified-release (also called controlled-release or extended-release) version for sleep maintenance.
Indiplon works by enhancing the action of the inhibitory neurotransmitterGABA, like most other nonbenzodiazepine sedatives. It primarily binds to benzodiazepine sites on α1 subunit-containingGABAA receptors in the brain.[1]
Indiplon has a short elimination half-life of 1.5 to 1.8 hours in young and elderly subjects, respectively.[2]
Indiplon is apyrazolopyrimidine related to thenonbenzodiazepine hypnoticzaleplon.[3]
Indiplon was discovered atLederle Laboratories (which was later acquired byWyeth) in the 1980s and was called CL 285,489.[4]: 454 In 1998 Lederle licensed it, along with other early stage drug candidates, toDOV Pharmaceutical, a startup formed by former Lederle employees, and Dov exclusively sublicensed its rights in the drug toNeurocrine Biosciences in that same year.[4] In 2002, Neurocrine entered into an agreement with Pfizer to develop the drug.[4]
Indiplon was originally scheduled for release in 2007, whenSanofi-Aventis' popular hypnoticzolpidem lost its patent rights in the United States and thus became available as a much less expensive generic. In 2002,Neurocrine Biosciences had entered into an agreement withPfizer to co-market indiplon in the US, in a deal worth a potential $400mn.[5] However, following the issuing of anon-approvable letter for the modified-release 15 mg formulation and anapprovable letter with stipulations for the 5 mg and 10 mg immediate-release version by the FDA in May 2006,[6]Pfizer ended its relationship with Neurocrine.[7] Neurocrine's stock price dropped 60% on the news.[8]
Following a resubmission, theFDA in December 2007 deemed Neurocrine'snew drug application (NDA) 'approvable' in the 5 and 10 mg formulations,[9] but requested new studies as a prerequisite to approval, including a clinical trial in the elderly, a safety study comparing adverse effects to those of similarly marketed drugs, and a preclinical study examining indiplon's safety in the third trimester of pregnancy.[10]
Following the 2007 FDA letter, Neurocrine decided to discontinue all clinical and marketing development of Indiplon in the United States.[9][10]