Brexpiprazole
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| Non-proprietary name | Brexpiprazole | ||||||||||||||||||
| other names |
7- {4- [4- (1-Benzothiophen-4-yl) piperazin-1-yl] butoxy} quinolin-2 (1 H ) -one |
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| Molecular formula | C 25 H 27 N 3 O 2 S | ||||||||||||||||||
| Brief description |
White to off-white crystalline powder |
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| properties | |||||||||||||||||||
| Molar mass | 433.57 g mol −1 | ||||||||||||||||||
| solubility |
Practically insoluble in water, solubility is pH dependent |
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | |||||||||||||||||||
Brexpiprazole is an active ingredient in the group of antipsychotics and is indicated for the treatment of schizophrenia .
Development and marketing
Brexpiprazol Since July 2018 the European Union as Rxulti (holder: Otsuka Pharmaceutical Netherlands) and Switzerland (trade name Rexulti : authorization holder Lundbeck approved for oral treatment of schizophrenia in adults, in January 2019) Rexulti in Switzerland on the market .
It was approved in the USA since 2015; in addition to the treatment of schizophrenia, the preparation is also indicated there for the adjuvant therapy of major depressive disorder (MDD) ( Rexulti , Otsuka Pharmaceutical Co.).
Pharmacological properties
Brexpiprazole acts as an atypical neuroleptic . The substance acts as a dopamine D 2 receptor -Partialagonist and modulator to the serotonin receptors 5-HT 1A and 5-HT 2A and antagonist to α 1B - and α 2C -adrenoceptor s. The intrinsic activity of brexpiprazole at the dopamine D 2 receptor is between that of aripiprazole and a full antagonist. Brexpiprazole, however, is neither an isomer nor a metabolite of any other substance. The lower intrinsic activity at the dopamine D 2 receptor compared to aripiprazole and the higher binding affinities at the 5-HT 1A and 5-HT 2A receptors suggest an advantageous antipsychotic profile, without those with full D 2 receptor antagonism to provoke associated adverse effects.
Chemical-physical properties
Three different crystal structures and one dihydrate are known of the compound.
Commercial preparations
Rxulti (EU), Rexulti (CH, USA, CA)
See also
Individual evidence
- ↑ a b Assessment report Rxulti , accessed on June 27, 2019.
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
- ↑ European Medicines Agency: Rxulti on the website of the European Medicines Agency , accessed on 2 February of 2019.
- ↑ Rexulti ® at www.swissmedic.ch , accessed on June 27, 2019.
- ↑ FDA REXULTI ® (brexpiprazole) , accessed February 2, 2019.
- ↑ a b c "Brexpiprazole I: In Vitro and In Vivo Characterization of a Novel Serotonin-Dopamine Activity Modulator" [Kenji Maeda (2014, 06. 19.)]
- ↑ Leslie Citrome, A. i. Ota et al. a .: The effect of brexpiprazole (OPC-34712) and aripiprazole in adult patients with acute schizophrenia. In: International Clinical Psychopharmacology. 31, 2016, p. 192, doi : 10.1097 / YIC.0000000000000123 .
- ↑ Tarek A. Zeidan, Pranoti A. Tilak et al. a .: Structural Diversity of Brexpiprazole and Related Analogues: Impact on Solubility and Drug Delivery. In: Crystal Growth & Design. 18, 2018, p. 2326, doi : 10.1021 / acs.cgd.7b01747 .
