zaleplon
Trade name: sonata
Approved
Aug 13, 1999
Zaleplon is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. While Zaleplon is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Zaleplon also binds selectively to the CNS GABAA-receptor chloride ionophore complex at benzodiazepine(BZ) omega-1 (BZ1, ο1) receptors. Zaleplon exerts its action through subunit modulation of the GABABZ receptor chloride channel macromolecular complex. Zaleplon also binds selectively to the brain omega-1 receptor located on the alpha subunit of the GABA-A/chloride ion channel receptor complex and potentiates t-butyl-bicyclophosphorothionate (TBPS) binding. Zaleplon is marketed under the brand names Sonata, Starnoc, and Andante. — NCATS
Clinical trial activity
10 trials · 17 clinical orgs · 14 marketing orgs
Earliest trial started Jan 1, 2004 (NCT00694187)
Timeline
1990s
- Aug 13, 1999
American Home Products — Earliest FDA Approval
- Aug 13, 1999
Pfizer — NDA Secondary Org
- Aug 13, 1999
American Home Products — NDA Organization
2000s
- Jan 1, 2004
- Jun 6, 2008
Aurobindo Pharma — Marketing Organization
- Jun 6, 2008
Mylan — Marketing Organization
- Jun 6, 2008
Teva — Marketing Organization
- Jun 6, 2008
Unichem — Marketing Organization
- Jun 6, 2008
Upsher-Smith Laboratories — Marketing Organization
- Jun 6, 2008
West-Ward Pharmaceutical — Marketing Organization
- Jun 6, 2008
Natco Pharma — Marketing Organization
- Jun 20, 2008
Chartwell Pharmaceuticals — Marketing Organization
- Jun 20, 2008
Cipla — Marketing Organization
- Nov 25, 2008
Hikma — Marketing Organization
- Sep 17, 2009
Orbion Pharms — Marketing Organization
- Sep 17, 2009
Orchid Pharma — Marketing Organization
Indications
Studied for
Mechanism of action
- GABA A receptor alpha-1/beta-1/gamma-2POSITIVE ALLOSTERIC MODULATOR
GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator
Selective for the brain omega-1 receptor (i.e. BZ1-type, i.e. alpha1/beta1/gamma2-GABA receptor)
Approval history
- approvedAug 13, 1999
Chemistry & pharmacology
SMILES
CCN(C(C)=O)C1=CC(=CC=C1)C2=CC=NC3=C(C=NN23)C#N- Mol. weight
- 305.3339 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaZaleplon ↗
- NCATSS62U433RMH ↗
- ChEMBLCHEMBL1521 ↗
Also known as
- 3'-(3-cyanopyrazolo(1,5-alpha)pyrimidin-7-yl)-n-ethylacetanilide
- 3'-(3-cyanopyrazolo(1,5-a)pyrimidin-7-yl)-n-ethylacetanilide
- 3'-(3-cyanopyrazolo(1,5-a)pyrimidin-7-yl)-n-ethylacetanilide
- acetamide, n-(3-(3-cyanopyrazolo(1,5-a)pyrimidin-7-yl)phenyl)-n-ethyl-
- cl 284846
- cl 284,846
- cl 284,846
- cl-284846
- cl-284846
- cl-284846
- cl-284846
- cl284,846
- l846
- l846
- l 846
- l-846
- l-846
- l-846
- ljc 10846
- ljc 10846
- ljc-10846
- ljc-10846
- n-(3-(3-cyanopyrazolo(1,5-a)pyrimidin-7-yl)phenyl)-n-ethylacetamide
- skp-1041
- sonata
- sonata
- sonata
- sonata
- sonata
- sonata
- starnoc
- zal-846
- zal-846
- zal-846
- zaleplon
- zaleplon
- zaleplon
- zaleplon
- zaleplon
- zaleplon
- zaleplon
- zaleplon
- zaleplon
- zaleplon
- zaleplon
- zaleplon
- zaleplon
- zelepion
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02374567 | Phase 3 | Jan 1, 2015 | Gottfried Wilhelm Leibniz Universität Hannover |
| NCT03489304 | Phase 2 | Apr 3, 2014 | University of Pennsylvania |
| NCT01277107 | Phase 2 | Jan 1, 2011 | Intec Pharma Ltd. |
| NCT01159652 | Phase 4 | Oct 1, 2010 | American Academy of Sleep Medicine, St. Luke's Hospital, Chesterfield, Missouri |
| NCT00878553 | Phase 2 | May 1, 2010 | Broward Research Group, Clinilabs, Emsellem MD PC, INC Research, Neurotrials Inc., Sleep Disorders Center of Georgia, Somnus Therapeutics, Inc., Vince & Associates |
| NCT00620620 | Phase 1 | Feb 1, 2008 | Alexza Pharmaceuticals, Inc. |
| NCT00829998 | Phase 1 | Feb 1, 2004 | Novum Pharmaceutical Research Services, Teva |
| NCT00829868 | Phase 1 | Feb 1, 2004 | Novum Pharmaceutical Research Services, Teva |
| NCT00694317 | N/A | Feb 1, 2004 | Novum Pharmaceutical Research Services, Roxane Laboratories |
| NCT00694187 | N/A | Jan 1, 2004 | Novum Pharmaceutical Research Services, Roxane Laboratories |
Organizations
Research & Development (17)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Novum Pharmaceutical Research Services | For profit | 4 | 0 | 2 | 2004 |
| Roxane Laboratories | For profit | 2 | 2 | 1 | 2004 |
| Teva | For profit | 2 | 2 | 1 | 2004 |
| Alexza Pharmaceuticals, Inc. | For profit | 1 | 1 | 1 | 2008 |
| American Academy of Sleep Medicine | Academic/Hospital | 1 | 0 | 1 | 2010 |
| Broward Research Group | Academic/Hospital | 1 | 0 | 1 | 2010 |
| Clinilabs | For profit | 1 | 0 | 1 | 2010 |
| Emsellem MD PC | Academic/Hospital | 1 | 0 | 1 | 2010 |
| Gottfried Wilhelm Leibniz Universität Hannover | Academic/Hospital | 1 | 1 | 1 | 2015 |
| INC Research | For profit | 1 | 0 | 1 | 2010 |
| Intec Pharma Ltd. | For profit | 1 | 1 | 1 | 2011 |
| Neurotrials Inc. | For profit | 1 | 0 | 1 | 2010 |
| Sleep Disorders Center of Georgia | Academic/Hospital | 1 | 0 | 1 | 2010 |
| Somnus Therapeutics, Inc. | For profit | 1 | 1 | 1 | 2010 |
| St. Luke's Hospital, Chesterfield, Missouri | Academic/Hospital | 1 | 1 | 1 | 2010 |
| University of Pennsylvania | Academic/Hospital | 1 | 1 | 1 | 2014 |
| Vince & Associates | For profit | 1 | 0 | 1 | 2010 |
Marketing (15)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| American Home Products | For profit | NDA | Aug 13, 1999 |
| Aurobindo Pharma | For profit | MKTG | Jun 6, 2008 |
| Chartwell Pharmaceuticals | For profit | MKTG | Jun 20, 2008 |
| Cipla | For profit | MKTG | Jun 20, 2008 |
| Hikma | For profit | MKTG | Nov 25, 2008 |
| Hikma | For profit | SYN | Jun 6, 2008 |
| Mylan | For profit | MKTG | Jun 6, 2008 |
| Natco Pharma | For profit | MKTG | Jun 6, 2008 |
| Orbion Pharms | For profit | MKTG | Sep 17, 2009 |
| Orchid Pharma | For profit | MKTG | Sep 17, 2009 |
| Pfizer | For profit | NDA2 | Aug 13, 1999 |
| Teva | For profit | MKTG | Jun 6, 2008 |
| Unichem | For profit | MKTG | Jun 6, 2008 |
| Upsher-Smith Laboratories | For profit | MKTG | Jun 6, 2008 |
| West-Ward Pharmaceutical | For profit | MKTG | Jun 6, 2008 |