IUPAC_name = "N"-methyl-"N"- [3- [3-(thiophene-2-carbonyl)
pyrazolo [5,1-b] pyrimidin-7-yl] phenyl] acetamide
width = 120
CAS_number = 325715-02-4
PubChem = 6450813
C=20 | H=16 | N=4 | O=2 | S=1
molecular_weight = 376.0993
legal_US = Rx only
routes_of_administration = Oral
Indiplon (INN and USAN) is a
nonbenzodiazepine, hypnotic sedativebeing developed in 2 formulations - an immediate release product for sleep onset and a modified-release version for sleep maintenance.
Mode of action
Indiplon is said to work by enhancing the action of the inhibitory neurotransmitter
GABA, like most other nonbenzodiazepine sedatives. It primarily binds to the α1 subunits of the GABAA receptors in the brain.
Indiplon was originally scheduled for release to doctors and pharmacies sometime in
2007, most likely in the springtime of that year, which is when Sanofi-Aventis' popular sleep aid, zolpidem, lost its patent rights in the United States and thus became available to patients as a much less expensive generic. Neurocrine Bioscienceshad planned to comarket indiplon in the US with Pfizer. However, following the issuing of a nonapprovable letter for the modified-release 15mg formulation and an approvable letter (with stipulations) for the 5mg and 10mg immediate-release version by the FDA ( May 2006), Pfizerdecided to end its relationship with Neurocrine.Fact|date=December 2007
December 13, 2007, Neurocrine announced that the FDA deemed their new drug application(NDA) 'approvable'.cite press release
title = Neurocrine Receives Approvable Letter for Indiplon Capsules with Additional Safety and Efficacy Data Required by FDA
publisher = Neurocrine Biosciences, Inc.
url = http://www.drugs.com/nda/indiplon_071213.html
accessdate = 2007-12-13] The 2007 Approvable Letter does not reference the setbacks seen previously in the
May 2006Approvable Letter, bringing the availability of indiplon one step closer to the consumer.
The planned brand name has not yet been revealed to the public. The NDA was initially approved by the FDA in 1998,Fact|date=December 2007 and since then, Neurocrine has been conducting clinical trials, with purportedly satisfactory results.Fact|date=December 2007
A recent analysis of
FDAand clinical trial data shows that nonbenzodiazepineZ-drugs cause cancerin humans. The data shows that trial subjects receiving hypnotic drugshad an increased the risk of developing cancer and malignancies. There have been 15 epidemiologicstudies which have shown that hypnoticdrugs cause increased mortality, mainly due to increased cancer deaths. The cancers included cancer of the brain, lung, bowel, breast, and bladder, and neoplasms. Initially FDA reviewers did not want to approve the drugs due to concerns of cancer but ultimately changed their mind and approved the drugs despite the concerns. FDA data has shown that zolpidem, zaleplon and eszopiclone are clastogenicand cause cancer in rodents. Benzodiazepine agonists are associated with an increased risk of ovarian cancerin humans. Zopiclonewas reportedly refused a product license by the FDAdue to indications that zopiclone caused cancer.Development of a malignant neoplasm has been associated with zolpidemusage but the rate of incidence of neoplasm in zolpidem users is as yet unknown. The rates, in clinical trials for the nonbenzodiazepine Z drugs, of malignancies and neoplasms are significantly higher in hypnotic groups than in placebo groups. Also the analysis of clinical trials and FDA data showed that eszopiclone, zaleplon, and zolpidemappeared to have an adverse effect on the immune systemcausing an increased rate of infections and colds in hypnotic users. Suppression of immune function might be the cause of the increased rate of cancer in nonbenzodiazepine hypnotic users. Indiplon has also shown an increased rate of cancers in clinical trials.The review author concluded saying; "the likelihood of cancer causation is sufficiently strong now that physiciansand patientsshould be warned that hypnoticspossibly place patients at higher risk for cancer". [cite journal | last = Kripke | first = Daniel F | year = 2008 | title = Evidence That New Hypnotics Cause Cancer | journal = Department of Psychiatry, UCSD | publisher = University of California | url = http://repositories.cdlib.org/cgi/viewcontent.cgi?article=1002&context=ucsdpsych | format = PDF | quote = the likelihood of cancer causation is sufficiently strong now that physicians and patients should be warned that hypnotics possibly place patients at higher risk for cancer. ]
* [http://www.neurocrine.com/html/clin_insomnia.html Neurocrine's Indiplon page]
* [http://www.drugs.com/NDA/indiplon_041019.html 2004 press release announcing Neurocrine's new product, Indiplon]
* [http://www.pfizer.com/ Pfizer]
* [http://www.genome.jp/dbget-bin/www_bget?dr+D02640 GenomeNet Entry: D02640]
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