Brexpiprazole : a new dopamine D₂receptor partial agonist for the treatment of schizophrenia and major depressive disorder
Copyright 2015 Prous Science, S.A.U. or its licensors. All rights reserved..
Brexpiprazole is a dopamine D₂receptor partial agonist. Compared with aripiprazole, it is more potent at 5-HT1A receptors and displays less intrinsic activity at D₂receptors. Brexpiprazole also has potent antagonistic activity at 5-HT2A as well as alpha-adrenergic receptors. In addition to results from phase II trials, data are available from two pivotal phase III, randomized, placebo-controlled trials of brexpiprazole for the acute treatment of schizophrenia and two pivotal phase III, randomized, placebo-controlled trials of adjunctive brexpiprazole for the acute treatment of major depressive disorder in patients with inadequate response to antidepressant medication treatment. Overall tolerability is promising, with rates of discontinuation due to adverse events lower or slightly higher than that observed for placebo. Although overall akathisia was more commonly observed with brexpiprazole than with placebo, the absolute risk increase attributable to brexpiprazole appears small. Short-term weight gain appears modest; however, outliers with an increase of ≥ 7% of body weight were evident in open-label long-term safety studies.
Medienart: |
E-Artikel |
---|
Erscheinungsjahr: |
2015 |
---|---|
Erschienen: |
2015 |
Enthalten in: |
Zur Gesamtaufnahme - volume:51 |
---|---|
Enthalten in: |
Drugs of today (Barcelona, Spain : 1998) - 51(2015), 7 vom: 04. Juli, Seite 397-414 |
Sprache: |
Englisch |
---|
Beteiligte Personen: |
Citrome, L [VerfasserIn] |
---|
Links: |
---|
Anmerkungen: |
Date Completed 04.01.2016 Date Revised 27.04.2017 published: Print Citation Status MEDLINE |
---|
doi: |
10.1358/dot.2015.51.7.2358605 |
---|
funding: |
|
---|---|
Förderinstitution / Projekttitel: |
|
PPN (Katalog-ID): |
NLM251722546 |
---|
LEADER | 01000naa a22002652 4500 | ||
---|---|---|---|
001 | NLM251722546 | ||
003 | DE-627 | ||
005 | 20231224162622.0 | ||
007 | cr uuu---uuuuu | ||
008 | 231224s2015 xx |||||o 00| ||eng c | ||
024 | 7 | |a 10.1358/dot.2015.51.7.2358605 |2 doi | |
028 | 5 | 2 | |a pubmed24n0839.xml |
035 | |a (DE-627)NLM251722546 | ||
035 | |a (NLM)26261843 | ||
040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
041 | |a eng | ||
100 | 1 | |a Citrome, L |e verfasserin |4 aut | |
245 | 1 | 0 | |a Brexpiprazole |b a new dopamine D₂receptor partial agonist for the treatment of schizophrenia and major depressive disorder |
264 | 1 | |c 2015 | |
336 | |a Text |b txt |2 rdacontent | ||
337 | |a ƒaComputermedien |b c |2 rdamedia | ||
338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
500 | |a Date Completed 04.01.2016 | ||
500 | |a Date Revised 27.04.2017 | ||
500 | |a published: Print | ||
500 | |a Citation Status MEDLINE | ||
520 | |a Copyright 2015 Prous Science, S.A.U. or its licensors. All rights reserved. | ||
520 | |a Brexpiprazole is a dopamine D₂receptor partial agonist. Compared with aripiprazole, it is more potent at 5-HT1A receptors and displays less intrinsic activity at D₂receptors. Brexpiprazole also has potent antagonistic activity at 5-HT2A as well as alpha-adrenergic receptors. In addition to results from phase II trials, data are available from two pivotal phase III, randomized, placebo-controlled trials of brexpiprazole for the acute treatment of schizophrenia and two pivotal phase III, randomized, placebo-controlled trials of adjunctive brexpiprazole for the acute treatment of major depressive disorder in patients with inadequate response to antidepressant medication treatment. Overall tolerability is promising, with rates of discontinuation due to adverse events lower or slightly higher than that observed for placebo. Although overall akathisia was more commonly observed with brexpiprazole than with placebo, the absolute risk increase attributable to brexpiprazole appears small. Short-term weight gain appears modest; however, outliers with an increase of ≥ 7% of body weight were evident in open-label long-term safety studies | ||
650 | 4 | |a Journal Article | |
650 | 4 | |a Research Support, Non-U.S. Gov't | |
650 | 4 | |a Review | |
650 | 4 | |a Brexpiprazole | |
650 | 4 | |a Dopamine D2 receptor partial agonist | |
650 | 4 | |a Major depressive disorder | |
650 | 4 | |a OPC-34712 | |
650 | 4 | |a Schizophrenia | |
650 | 7 | |a Dopamine Agonists |2 NLM | |
650 | 7 | |a Quinolones |2 NLM | |
650 | 7 | |a Receptors, Dopamine D2 |2 NLM | |
650 | 7 | |a Thiophenes |2 NLM | |
650 | 7 | |a brexpiprazole |2 NLM | |
650 | 7 | |a 2J3YBM1K8C |2 NLM | |
773 | 0 | 8 | |i Enthalten in |t Drugs of today (Barcelona, Spain : 1998) |d 1998 |g 51(2015), 7 vom: 04. Juli, Seite 397-414 |w (DE-627)NLM123139600 |x 1699-3993 |7 nnns |
773 | 1 | 8 | |g volume:51 |g year:2015 |g number:7 |g day:04 |g month:07 |g pages:397-414 |
856 | 4 | 0 | |u http://dx.doi.org/10.1358/dot.2015.51.7.2358605 |3 Volltext |
912 | |a GBV_USEFLAG_A | ||
912 | |a GBV_NLM | ||
951 | |a AR | ||
952 | |d 51 |j 2015 |e 7 |b 04 |c 07 |h 397-414 |