asenapine profile

asenapine : A racemate consisting of equal amounts of (R,R)- and (S,S)-asenapine. Used as its maleate salt for the acute treatment of schizophrenia and acute treatment of manic or mixed episodes associated with bipolar I disorder with or without psychotic features. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

(S,S)-asenapine : A 5-chloro-2-methyl-2,3,3a,12b-tetrahydrodibenzo[2,3:6,7]oxepino[4,5-c]pyrrole in which both of the stereocentres have S configuration. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	163091
CHEMBL ID	504548
CHEBI ID	71257
CHEBI ID	71253
SCHEMBL ID	678411
MeSH ID	M0513342

Synonym
AB01274757-01
org5222
secuado (transdermal asenapine)
(2s,6s)-9-chloro-4-methyl-13-oxa-4-azatetracyclo[12.4.0.0^{2,6}.0^{7,12}]octadeca-1(18),7,9,11,14,16-hexaene
gtpl22
PDSP2_001584
PDSP1_001600
chebi:71257 ,
CHEMBL504548 ,
trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1h-dibenz(2,3:6,7)oxepino(4,5-c)pyrrole
secuado
asenapine
65576-45-6
dtxcid3028974
65576-45-6 pound not85650-56-2
BCP9000326
einecs 265-829-4
jkz19v908o ,
hsdb 8061
1h-dibenz(2,3:6,7)oxepino(4,5-c)pyrrole, 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-, trans-
1h-dibenz(2,3:6,7)oxepino(4,5-c)pyrrole, 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-, (3ar,12br)-rel-
unii-jkz19v908o
asenapine [inn:ban]
AKOS015918056
BCPP000385
(s,s)-asenapine
trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1h-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole
(3as,12bs)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1h-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole
(3ars,12brs)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1h-dibenzo(2,3:6,7)oxepino(4,5-c)pyrrole
asenapine [mi]
asenapine [orange book]
asenapine [who-dd]
asenapine [inn]
asenapine [vandf]
SCHEMBL678411
1412458-61-7
trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1h-dibenzo[2,3;6,7]-oxepino[4,5-c]pyrrole
trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1h-dibenz[2,3:6,7]-oxepino[4,5-c]pyrrole
VSWBSWWIRNCQIJ-HUUCEWRRSA-N
trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1h-dibenz[2, 3:6,7]-oxepino[4,5-c]pyrrole
trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1h-dibenz[2,3:6,7]oxepino[4,5-c]-pyrrole
AB01274757_02
135883-07-7
Q27074536
AMY195
(3as,12bs)-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1h-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole
CS-0009346
asenapine (inn)
secuado (tn)
D11769
EN300-22049456
bdbm50549038
(2s,6s)-9-chloro-4-methyl-13-oxa-4-azatetracyclo[12.4.0.0?,?.0?,??]octadeca-1(18),7,9,11,14,16-hexaene
(+-)-asenapine
rac-(3ar,12br)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1h-dibenzo(2,3:6,7)oxepino(4,5-c)pyrrole
n05ah05
chebi:71253
asenapina
asenapinum
(3ar,12br)-rel-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1h-dibenz

Research Excerpts

Overview

Asenapine maleate (AM) is an atypical antipsychotic agent, that has been widely prescribed for the management of schizoaffective disorders. It presents higher affinity for serotonergic than dopaminergic receptors.

Excerpt	Reference	Relevance
"Asenapine is a novel psychopharmacologic agent under development for the treatment of schizophrenia and bipolar disorder. "	( Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. Shahid, M; Walker, GB; Wong, EH; Zorn, SH, 2009)	3.24
"Asenapine maleate (AM) is an atypical antipsychotic agent, that has been widely prescribed for the management of schizoaffective disorders. "	( Recent advances in the development of asenapine formulations. Narayan, R; Nayak, UY; Suresh, A, 2020)	2.27
"Asenapine is a second-generation antipsychotic with 5HT-2A antagonist and 5HT-1A/1B partial agonist properties, which provides a favorable profile in targeting schizophrenic symptoms, while reducing motor side effects and improving mood and cognition."	( Asenapine Transdermal Patch for the Management of Schizophrenia. Barlow, R; Bertrand, S; Cornett, EM; DeGraw, C; Derakhshanian, S; Hasoon, J; Kaye, AD; Kaye, AM; Menard, A; Rath, A; Urits, I; Viswanath, O; Zhou, M, 2020)	2.72
"Asenapine is a second-generation antipsychotic used to treat individuals with schizophrenia. "	( Efficacy and Safety of HP-3070, an Asenapine Transdermal System, in Patients With Schizophrenia: A Phase 3, Randomized, Placebo-Controlled Study. Citrome, L; Komaroff, M; Kuriki, M; Park, AS; Starling, BR; Terahara, T; Walling, DP; Zeni, CM, 2020)	2.28
"Asenapine maleate is a second-generation atypical antipsychotic agent used in the treatment of schizophrenia, a neuropsychiatric disorder. "	( Determination of Asenapine Maleate in Pharmaceutical and Biological Matrices: A Critical Review of Analytical Techniques over the Past Decade. Kotak, V; Patel, M; Patel, R; Tanna, N, 2022)	2.5
"Asenapine is a new atypical antipsychotic prescribed for the treatment of psychosis/bipolar disorders that presents higher affinity for serotonergic than dopaminergic receptors. "	( Asenapine modulates mood-related behaviors and 5-HT Abrial, E; Arnt, J; Delcourte, S; Didriksen, M; Etiévant, A; Haddjeri, N; Rovera, R, 2017)	3.34
"Asenapine is a new second-generation antipsychotic that is understudied in borderline personality disorder (BPD). "	( Efficacy and Tolerability of Asenapine Compared with Olanzapine in Borderline Personality Disorder: An Open-Label Randomized Controlled Trial. Bellino, S; Bozzatello, P; Rocca, P; Uscinska, M, 2017)	2.19
"Asenapine is a second-generation antipsychotic approved in Europe (brand name Sycrest"	( A Review of Asenapine in the Treatment of Bipolar Disorder. Montes, JM; Vieta, E, 2018)	1.58
"Asenapine is an anti-psychotic agent approved by the US-FDA for treatment of acute schizophrenia and manic or bipolar I disorder in adults. "	( Preferential Formulation of Second Generation Antipsychotic Asenapine as Inclusion Complex with Sulphobutylether-βCD (Captisol): In vitro and In vivo Evaluation. Avachat, AM; Avachat, CM; Coutinho, EC; Khan, EM; Kulkarni, JA; Martis, EAF; Padhye, S; Pradhan, R; Suryawanshi, TS, 2018)	2.17
"Asenapine is an atypical antipsychotic approved by US Food and Drug Administration in 2009 and by European Medicines Agency in 2010 for Schizophrenia and Bipolar Disorder treatment. "	( Systemic Administration of Antipsychotic Asenapine Pre or Postnatal does not Induce Anxiety-like Behaviors in Mice. Carrilho, CG; Coletti, RF; de Barros, JA; de Souza, TB; Farias, DM; Machado, S; Moreno, SE; Murillo-Rodriguez, E; Oliveira, MS; Veras, AB, 2018)	2.19
"Asenapine is a recent drug approved in the European Union for the treatment of bipolar disorder. "	( Enantioseparation and determination of asenapine in biological fluid micromatrices by HPLC with diode array detection. Bugamelli, F; Ferranti, A; Mandrioli, R; Mercolini, L; Protti, M; Rudge, J; Sanchez Blanco, T; Vignali, A, 2018)	2.19
"Asenapine is an atypical antipsychotic indicated for the management of type-I BD, with distinct pharmacokinetic and receptor affinity profiles."	( Management of asenapine treatment in clinical practice: Recommendations from a panel of experts. Benabarre, A; Iborra, P; Montes, JM; Mozos, A; Sáez, C; Vieta, E, )	1.21
"Asenapine is a new second-generation antipsychotic, available as a sublingual tablet, approved in Europe for the treatment of moderate-to-severe manic episodes in adults, and in US for manic or mixed episodes of bipolar I disorder in adults and adolescents."	( Asenapine: Pharmacological Aspects and Role in Psychiatric Disorders. Mishriky, R; Reyad, AA, 2019)	2.68
"Asenapine maleate (AM) is an atypical antipsychotic that, unlike many other antipsychotics, shows some efficacy in treating cognitive dysfunction in schizophrenia. "	( Asenapine maleate normalizes low frequency oscillatory deficits in a neurodevelopmental model of schizophrenia. Foute Nelong, T; Manduca, JD; Perreault, ML; Zonneveld, PM, 2019)	3.4
"Asenapine is a second-generation antipsychotic with a unique receptor binding profile, licensed for the treatment of manic episodes in adults with bipolar I disorder."	( Use of asenapine in clinical practice for the management of bipolar mania. Altamura, AC; González-Pinto, AM; Millet, B; Wiedemann, K; Young, AH, 2013)	1.57
"Asenapine is a new atypical antipsychotic. "	( [Medication of the month. asenapine (Sycrest]. Pitchot, W, 2013)	2.13
"Asenapine is a novel antipsychotic drug recently approved for the treatment of schizophrenia and manic disorders."	( Repeated asenapine treatment produces a sensitization effect in two preclinical tests of antipsychotic activity. Chen, Y; Li, M; Qin, R, 2013)	1.53
"Asenapine is a novel FDA-approved atypical antipsychotic for schizophrenia and bipolar disorder."	( Asenapine in the treatment of borderline personality disorder: an atypical antipsychotic alternative. Gasol, M; Gasol, X; Martín-Blanco, A; Pascual, JC; Patrizi, B; Soler, J; Villalta, L, 2014)	2.57
"Asenapine (Saphris®) is an atypical antipsychotic approved in the USA in 2009 for the treatment of schizophrenia and bipolar disorder. "	( Asenapine (Saphris®): GC-MS method validation and the postmortem distribution of a new atypical antipsychotic medication. Anderson, D; Mertens-Maxham, D; Miller, C; Pleitez, O; Wade, N, 2013)	3.28
"Asenapine is a second-generation (atypical) antipsychotic currently marketed for the treatment of schizophrenia and bipolar mania/mixed episodes."	( Asenapine review, part II: clinical efficacy, safety and tolerability. Citrome, L, 2014)	3.29
"Asenapine is a second-generation (atypical) antipsychotic currently marketed for the treatment of schizophrenia and bipolar mania/mixed episodes."	( Asenapine review, part I: chemistry, receptor affinity profile, pharmacokinetics and metabolism. Citrome, L, 2014)	3.29
"Asenapine (ASE) is a new second-generation antipsychotic developed and approved for the treatment of manic or mixed episodes associated with bipolar disorder."	( Cost-effectiveness of asenapine in the treatment of patients with bipolar I disorder with mixed episodes in an Italian context. Caresano, C; Di Sciascio, G; Fagiolini, A; Maina, G; Perugi, G; Ripellino, C; Vampini, C, 2014)	1.44
"Asenapine is a new antipsychotic drug that induces a long-lasting behavioral sensitization in adult rats. "	( Asenapine sensitization from adolescence to adulthood and its potential molecular basis. Chen, Y; Hu, G; Li, M; Qin, R; Shu, Q, 2014)	3.29
"Asenapine (ASE) is a novel atypical antipsychotic drug approved for the treatment of schizophrenia and bipolar disorder. "	( Effect of acute asenapine treatment on Fos expression in the forebrain structures under normal conditions and mild stress preconditioning in the rat. Cernackova, A; Horvathova, L; Kiss, A; Majercikova, Z; Osacka, J; Pecenak, J, 2014)	2.19
"Asenapine is a tetracyclic atypical antipsychotic used for treatment of schizophrenia and mania. "	( Asenapine alters the activity of monoaminergic systems following its subacute and long-term administration: an in vivo electrophysiological characterization. Blier, P; El Mansari, M; Oosterhof, CA, 2015)	3.3
"Asenapine (ASE) is a novel atypical antipsychotic used in schizophrenia treatment. "	( Effect of Asenapine on the Activity of Hypocretin Neurons in Normal and Unpredictable Mild Stress Preconditioned Rats. Kiss, A; Majercikova, Z, 2015)	2.26
"Asenapine is a second-generation antipsychotic with a unique pharmacological profile that was recently approved for the treatment of moderate/severe manic episodes. "	( Asenapine in the Treatment of Acute Mania: A Real-World Observational Study With 6 Months Follow-Up. Castelnovo, A; Cavallotti, S; D'Agostino, A; Gambini, O; Guanella, E; Ostinelli, EG, 2015)	3.3
"Asenapine is a relatively new atypical antipsychotic that is prescribed for schizophrenia and for bipolar mania."	( Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Barak, N; Einat, H; Ene, HM; Kara, NZ; Reshef Ben-Mordechai, T, 2016)	1.48
"Asenapine is an atypical antipsychotic for acute treatment of manic or mixed episodes associated with bipolar I disorder in adults. "	( Asenapine: Efficacy and safety of 5 and 10mg bid in a 3-week, randomized, double-blind, placebo-controlled trial in adults with a manic or mixed episode associated with bipolar I disorder. Hundt, C; Kelly, L; Landbloom, RL; Mackle, M; Mathews, M; McIntyre, RS; Snow-Adami, L; Wu, X, 2016)	3.32
"Asenapine is a recently developed atypical antipsychotic that is approved by the US Food and Drug Administration (FDA) for the treatment of schizophrenia."	( Asenapine versus placebo for schizophrenia. Basra, MK; Byers, A; Dutta, S; Hay, A; Sereno, M, 2015)	2.58
"Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. "	( Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Imanishi, T; Kondo, M; Koyama, T; Ohyama, M; Yamauchi, M, 2016)	3.32
"Asenapine is a sublingually absorbed newer second-generation antipsychotic that is approved for the treatment of schizophrenia and bipolar disorder in patients, with a lower extrapyramidal adverse effect potential. "	( Asenapine-Induced Acute Dystonia in an Adolescent Male. Bhattacharya, A; Bhuyan, D; Ghosh, S; Praharaj, SK, 2016)	3.32
"Asenapine is a second generation anti-psychotic approved in the USA in 2009 for the treatment of schizophrenia, but its efficacy has not been proven in Asian patients."	( Efficacy and safety of asenapine in Asian patients with an acute exacerbation of schizophrenia: a multicentre, randomized, double-blind, 6-week, placebo-controlled study. Bai, YM; Kim, JH; Kinoshita, T; Miyake, M; Oshima, N, 2016)	2.19
"Asenapine is a novel atypical antipsychotic that possesses a high serotonin (5-HT2A) to dopamine (D2) affinity ratio and alpha-adrenergic antagonism, which may be advantageous in treating PTSD."	( An Open Label Pilot Study of Adjunctive Asenapine for the Treatment of Posttraumatic Stress Disorder. Bartolucci, A; Berry, C; Birur, B; Davis, LL; Norrholm, S; Pilkinton, P, 2016)	1.42
"Asenapine is a newer antipsychotic that also has D4/D2 affinity ratio > 1."	( Asenapine for the Control of Physical Aggression: A Prospective Naturalist Pilot Study. Amon, JS; El-Mallakh, RS; Johnson, SB, 2017)	2.62
"Asenapine is a psychopharmacologic agent being developed for schizophrenia and bipolar disorder. "	( Electrophysiological characterization of the effects of asenapine at 5-HT(1A), 5-HT(2A), alpha(2)-adrenergic and D(2) receptors in the rat brain. Blier, P; El Mansari, M; Ghanbari, R; Shahid, M, 2009)	2.04
"Asenapine is a novel psychopharmacological agent that binds with high affinity and specificity to numerous dopamine, serotonin, noradrenaline (norepinephrine) and histamine receptor subtypes. "	( Asenapine. McCormack, PL; Weber, J, 2009)	3.24
"Asenapine maleate is a novel drug recently approved by the Food and Drug Administration for treatment of acute schizophrenia and for manic or mixed episodes of bipolar I disorder with or without psychotic features in adults."	( Asenapine maleate: a new drug for the treatment of schizophrenia and bipolar mania. Shahid, M; Tarazi, FI, 2009)	2.52
"Asenapine sublingual is a novel atypical antipsychotic approved in August 2009 for the acute treatment of schizophrenia, as well as for manic or mixed episodes as part of adult bipolar I disorder. "	( Pharmacology and efficacy of asenapine for manic and mixed states in adults with bipolar disorder. McIntyre, RS, 2010)	2.09
"Asenapine is a psychopharmacologic agent approved in the United States for the acute treatment of schizophrenia in adults and the acute treatment of manic or mixed episodes associated with bipolar I disorder with or without psychotic features in adults. "	( Effect of absorption site on the pharmacokinetics of sublingual asenapine in healthy male subjects. de Greef, R; Gerrits, M; Peeters, P, 2010)	2.04
"Asenapine is a new pharmacological agent for the acute treatment of schizophrenia and bipolar disorder. "	( Effects of asenapine, olanzapine, and risperidone on psychotomimetic-induced reversal-learning deficits in the rat. Idris, NF; Marston, HM; McLean, SL; Neill, JC; Shahid, M; Wong, EH, 2010)	2.19
"Asenapine is a new atypical antipsychotic medication with high affinity for D(2) and 5HT(2A) receptors that has been approved by the FDA in adults for the acute treatment of schizophrenia in the USA. "	( Evaluation of the clinical efficacy of asenapine in schizophrenia. Minassian, A; Young, JW, 2010)	2.07
"Asenapine is a recently approved agent with an acceptable cardiometabolic profile and exhibits similar efficacy as other antipsychotic medications, primarily on positive symptoms of schizophrenia. "	( Evaluation of the clinical efficacy of asenapine in schizophrenia. Minassian, A; Young, JW, 2010)	2.07
"Asenapine is a novel psychopharmacologic agent being developed for schizophrenia and bipolar disorder. "	( Effects of asenapine on prefrontal N-methyl-D-aspartate receptor-mediated transmission: involvement of dopamine D1 receptors. Jardemark, K; Marcus, MM; Shahid, M; Svensson, TH, 2010)	2.19
"Asenapine is an atypical antipsychotic approved by the US Food and Drug Administration in adults for treatment of schizophrenia or acute treatment, as monotherapy or adjunct therapy to lithium or valproate, of manic or mixed episodes of bipolar I disorder."	( Asenapine improves phencyclidine-induced object recognition deficits in the rat: evidence for engagement of a dopamine D1 receptor mechanism. Grayson, B; Idris, N; Neill, JC; Shahid, M; Snigdha, S, 2011)	2.53
"Asenapine is an atypical antipsychotic agent available in sublingual formulations (5 or 10 mg) and indicated in the US (Saphris) for the acute treatment, as monotherapy or adjunctive therapy, of manic and mixed episodes and in the EU (Sycrest) for the treatment of moderate to severe manic episodes, in adult patients with bipolar I disorder. "	( Asenapine: a review of its use in the management of mania in adults with bipolar I disorder. Chwieduk, CM; Scott, LJ, 2011)	3.25
"Asenapine is a sublingual preparation, in contrast to iloperidone and lurasidone, which are swallowed."	( Iloperidone, asenapine, and lurasidone: a brief overview of 3 new second-generation antipsychotics. Citrome, L, 2011)	1.46
"Asenapine is an atypical antipsychotic approved in the US for the treatment of schizophrenia and for the treatment, as monotherapy or adjunctive therapy to lithium or valproate, of acute manic or mixed episodes associated bipolar I disorder."	( Asenapine effects on cognitive and monoamine dysfunction elicited by subchronic phencyclidine administration. Elsworth, JD; Groman, SM; Jentsch, JD; Marston, H; Roth, RH; Shahid, M; Valles, R; Wong, E, 2012)	2.54
"Asenapine is a new psychopharmacologic agent approved for the acute and maintenance treatment of schizophrenia and the acute and maintenance treatment of manic and mixed episodes associated with bipolar I disorder. "	( Asenapine: a new antipsychotic option. Fuller, MA; Henry, JM, 2011)	3.25
"Asenapine is a recently introduced atypical antipsychotic approved by the FDA for bipolar mania and mixed states with or without psychotic features, as well as for the treatment and prevention of psychotic relapses in schizophrenia. "	( Asenapine: a synthesis of efficacy data in bipolar mania and schizophrenia. McIntyre, RS; Wong, R, 2012)	3.26
"Asenapine is a new, second-generation (atypical) antipsychotic medication with demonstrated efficacy for the acute and maintenance treatment of schizophrenia. "	( Asenapine: a clinical overview. Potkin, SG, 2011)	3.25
"Asenapine is a new second-generation antipsychotic (SGA) approved in September 2010 by the European Medicines Agency for the treatment of bipolar disorder. "	( [Asenapine in bipolar disorder: efficacy, safety and place in clinical practice]. Llorca, PM; Samalin, L; Tixeront, C, 2012)	2.73
"Asenapine is a novel antipsychotic drug approved for the treatment of acute schizophrenia, manic, or mixed episodes associated with bipolar I disorder, as a maintenance treatment of schizophrenia and as an adjunctive therapy with lithium or valproate for the acute treatment of manic or mixed episodes associated with bipolar I disorder in adults."	( The preclinical profile of asenapine: clinical relevance for the treatment of schizophrenia and bipolar mania. Neill, JC; Tarazi, FI, 2013)	2.13
"Asenapine is an approved treatment for schizophrenia in the United States."	( Meta-analyses of the efficacy of asenapine for acute schizophrenia: comparisons with placebo and other antipsychotics. Cazorla, P; Fennema, H; Mackle, M; Szegedi, A; van Duijnhoven, W; Verweij, P, 2012)	2.1
"Asenapine is a sublingually administered second-generation antipsychotic with proven efficacy for the treatment of moderate to severe manic episodes associated with bipolar I disorder in adults. "	( Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Bossini, L; Casamassima, F; Cuomo, A; Fagiolini, A; Forgione, RN; Goracci, A; Maccari, M; Morana, B; Pellegrini, F, 2013)	3.28
"Asenapine is a novel psychopharmacologic agent being developed for the treatment of schizophrenia and bipolar disorder."	( Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Frånberg, O; Jardemark, K; Konradsson, A; Marcus, MM; Schilström, B; Shahid, M; Svensson, TH; Wiker, C; Wong, EH, 2008)	3.23

Effects

Asenapine has a relatively low propensity for changes in metabolic parameters, body composition, sedation/somnolence and extrapyramidal side effects. It has a complex pharmacodynamic profile with affinities at multiple dopamine, serotonin, histamine, and α-adrenergic receptors.

Asenapine maleate (ASM) has been demonstrated as a safe and effective therapeutic agent under twice-daily administration. It has shown a comparable efficacy profile to other atypical antipsychotics and it is associated with a favourable metabolic profile and less weight gain.

Excerpt	Reference	Relevance
"Asenapine has a favourable tolerability profile, compared with other first-line agents, having a minimal impact on weight and metabolic parameters."	( Use of asenapine in clinical practice for the management of bipolar mania. Altamura, AC; González-Pinto, AM; Millet, B; Wiedemann, K; Young, AH, 2013)	1.57
"Asenapine has a favourable tolerability profile, having a minimal impact on weight and metabolic parameters."	( Management of schizophrenia: clinical experience with asenapine. Bressan, RA; Castle, DJ; Cortese, L; Mosolov, SN, 2013)	1.36
"Asenapine has a complex pharmacodynamic profile with affinities at multiple dopamine, serotonin, histamine, and α-adrenergic receptors, all at which asenapine functions as an antagonist. "	( Asenapine review, part I: chemistry, receptor affinity profile, pharmacokinetics and metabolism. Citrome, L, 2014)	3.29
"Asenapine has a broad pharmacological profile with significant effects on serotonergic receptors, hence it is reasonable to expect that asenapine may have some anxiolytic effects."	( Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Barak, N; Einat, H; Ene, HM; Kara, NZ; Reshef Ben-Mordechai, T, 2016)	1.48
"Asenapine has a relatively favourable tolerability profile."	( Asenapine for schizophrenia and bipolar disorder: a review of the efficacy and safety profile for this newly approved sublingually absorbed second-generation antipsychotic. Citrome, L, 2009)	2.52
"Asenapine has a relatively low propensity for changes in metabolic parameters, body composition, sedation/somnolence and extrapyramidal side effects, and is not associated with prolactin elevation or clinically significant electrocardiographic changes."	( Pharmacology and efficacy of asenapine for manic and mixed states in adults with bipolar disorder. McIntyre, RS, 2010)	1.37
"Asenapine has a broad receptor affinity profile for most serotonergic, dopaminergic, and adrenergic receptors, with no appreciable affinity for muscarinic receptors."	( Asenapine: a clinical overview. Potkin, SG, 2011)	2.53
"Asenapine maleate (ASM) has been demonstrated as a safe and effective therapeutic agent under twice-daily administration."	( Long-term sustained release Poly(lactic-co-glycolic acid) microspheres of asenapine maleate with improved bioavailability for chronic neuropsychiatric diseases. Guan, S; Ma, Y; Wang, YE; Zhai, J; Zhou, X, 2020)	1.51
"Asenapine has demonstrated efficacy in the management of bipolar disorders and schizophrenia, while a possible role in the management of borderline personality disorder and agitation needs further research."	( Asenapine: Pharmacological Aspects and Role in Psychiatric Disorders. Mishriky, R; Reyad, AA, 2019)	2.68
"Asenapine has a favourable tolerability profile, compared with other first-line agents, having a minimal impact on weight and metabolic parameters."	( Use of asenapine in clinical practice for the management of bipolar mania. Altamura, AC; González-Pinto, AM; Millet, B; Wiedemann, K; Young, AH, 2013)	1.57
"Asenapine has a favourable tolerability profile, having a minimal impact on weight and metabolic parameters."	( Management of schizophrenia: clinical experience with asenapine. Bressan, RA; Castle, DJ; Cortese, L; Mosolov, SN, 2013)	1.36
"Asenapine has shown a comparable efficacy profile to other atypical antipsychotics and it is associated with a favourable metabolic profile and less weight gain."	( Cost-effectiveness of asenapine in the treatment of schizophrenia in Canada. Beauchemin, C; Beillat, M; Gilbert, D; Lachaine, J; Mathurin, K, 2014)	1.44
"Asenapine has a complex pharmacodynamic profile with affinities at multiple dopamine, serotonin, histamine, and α-adrenergic receptors, all at which asenapine functions as an antagonist. "	( Asenapine review, part I: chemistry, receptor affinity profile, pharmacokinetics and metabolism. Citrome, L, 2014)	3.29
"Asenapine has a broad pharmacological profile with significant effects on serotonergic receptors, hence it is reasonable to expect that asenapine may have some anxiolytic effects."	( Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Barak, N; Einat, H; Ene, HM; Kara, NZ; Reshef Ben-Mordechai, T, 2016)	1.48
"Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests but had no effects in the open-field or the hyponeophagia tests."	( Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Barak, N; Einat, H; Ene, HM; Kara, NZ; Reshef Ben-Mordechai, T, 2016)	1.48
"Asenapine has been reported to be effective either in monotherapy or in combination with mood stabilers (lithium and valproate) in the treatment of manic or mixed episodes, with a lower propensity to induce, or being followed by, depressive symptoms, when compared to other SGAs."	( Current Trends on Antipsychotics: Focus on Asenapine. Baroni, S; Dell'Osso, L; Marazziti, D; Mucci, F; Mungai, F; Piccinni, A; Presta, S, 2016)	1.42
"Asenapine has potent antidopaminergic properties that are predictive of antipsychotic efficacy. "	( Asenapine effects in animal models of psychosis and cognitive function. Azar, MR; Geyer, MA; Gold, L; Marston, HM; Martin, FD; Meltzer, LT; Moore, CL; Serpa, KA; Shahid, M; Wong, EH; Young, JW, 2009)	3.24
"Asenapine has a relatively favourable tolerability profile."	( Asenapine for schizophrenia and bipolar disorder: a review of the efficacy and safety profile for this newly approved sublingually absorbed second-generation antipsychotic. Citrome, L, 2009)	2.52
"Asenapine has a relatively low propensity for changes in metabolic parameters, body composition, sedation/somnolence and extrapyramidal side effects, and is not associated with prolactin elevation or clinically significant electrocardiographic changes."	( Pharmacology and efficacy of asenapine for manic and mixed states in adults with bipolar disorder. McIntyre, RS, 2010)	1.37
"Asenapine has a broad receptor affinity profile for most serotonergic, dopaminergic, and adrenergic receptors, with no appreciable affinity for muscarinic receptors."	( Asenapine: a clinical overview. Potkin, SG, 2011)	2.53
"Asenapine has reported long-term efficacy for this indication and the potential to reduce the incidence of relapse."	( Asenapine: a clinical review of a second-generation antipsychotic. Pace, HA; Stoner, SC, 2012)	2.54

Actions

Excerpt	Reference	Relevance
"Asenapine displays quick and reliable effects on manic symptoms, very low risk of depressive switches, efficacy on depressive symptoms during manic and mixed episodes, usually good tolerability and continued longer-term efficacy on residual and subthreshold symptoms. "	( Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Bossini, L; Casamassima, F; Cuomo, A; Fagiolini, A; Forgione, RN; Goracci, A; Maccari, M; Morana, B; Pellegrini, F, 2013)	3.28

Treatment

Asenapine treatment resulted in dose-dependent, clinically relevant plasma levels. MADRS remission rate was stable regardless of baseline depressive symptom severity.

Excerpt	Reference	Relevance
"In asenapine-treated patients, the MADRS remission rate was stable regardless of baseline depressive symptom severity (range 64-67%), whereas remission decreased with increasing severity with olanzapine (63-38%) and placebo (49-25%)."	( DSM-5 mixed specifier for manic episodes: evaluating the effect of depressive features on severity and treatment outcome using asenapine clinical trial data. Berk, M; McIntyre, RS; Tohen, M; Weiller, E; Zhao, J, 2013)	1.11
"Asenapine treatment resulted in dose-dependent, clinically relevant plasma levels."	( The effects of the atypical antipsychotic asenapine in a strain-specific battery of tests for mania-like behaviors. Einat, H; Ene, HM; Kara, NZ, 2015)	1.4

Toxicity

Adverse events occurred at rates of 90%. Adverse event (AE) incidence was lower during the extension. The recommended asenapine starting dose is 10mg bid with the option to reduce the dose to 5mg bid.

Excerpt	Reference	Relevance
" placebo for commonly observed adverse reactions were 13 (95% CI 8-30) for akathisia (10 mg bid), 20 (95% CI 13-50) for oral hypoesthesia (5 mg bid) and 13 (95% CI 8-32) for somnolence (5 mg bid)."	( Asenapine for schizophrenia and bipolar disorder: a review of the efficacy and safety profile for this newly approved sublingually absorbed second-generation antipsychotic. Citrome, L, 2009)	1.8
" Treatment-related adverse events (AEs) occurred in 44% and 52%, 57%, and 41% of the asenapine at 5 and 10 mg BID, haloperidol, and placebo groups, respectively."	( Efficacy and safety of asenapine in a placebo- and haloperidol-controlled trial in patients with acute exacerbation of schizophrenia. Alphs, L; Cohen, M; Kane, JM; Panagides, J; Zhao, J, 2010)	0.9
" The incidence of treatment-emergent adverse events (AEs) was comparable (72."	( Short-term safety and pharmacokinetic profile of asenapine in older patients with psychosis. de Greef, R; Dubovsky, SL; Frobose, C; Panagides, J; Phiri, P, 2012)	0.63
" Adverse event (AE) incidence was lower during the extension (asenapine, 62%; olanzapine, 55%) than during the core study (78%, 80%)."	( Long-term efficacy and safety of asenapine or olanzapine in patients with schizophrenia or schizoaffective disorder: an extension study. Emsley, R; Naber, D; Panagides, J; Schoemaker, J; Stet, L; Vrijland, P, 2012)	0.9
" In this context, newer SGAs were developed to further improve the adverse effect burden of available agents."	( Body weight and metabolic adverse effects of asenapine, iloperidone, lurasidone and paliperidone in the treatment of schizophrenia and bipolar disorder: a systematic review and exploratory meta-analysis. Correll, CU; De Hert, M; Detraux, J; Sweers, K; van Winkel, R; Yu, W, 2012)	0.64
" There were no unexpected adverse events in the OLE, and PANSS total scores decreased by -16."	( Safety and Efficacy from an 8 Week Double-Blind Trial and a 26 Week Open-Label Extension of Asenapine in Adolescents with Schizophrenia. Braat, S; Findling, RL; Hundt, C; Landbloom, RP; Mackle, M; Mathews, M; Pallozzi, W; Wamboldt, MZ, 2015)	0.64
" The recommended asenapine starting dose is 10mg bid with the option to reduce the dose to 5mg bid if needed due to adverse effects/tolerability."	( Asenapine: Efficacy and safety of 5 and 10mg bid in a 3-week, randomized, double-blind, placebo-controlled trial in adults with a manic or mixed episode associated with bipolar I disorder. Hundt, C; Kelly, L; Landbloom, RL; Mackle, M; Mathews, M; McIntyre, RS; Snow-Adami, L; Wu, X, 2016)	2.22
" There were no significant differences in the incidence of treatment-emergent adverse events reported with asenapine 5 and 10 mg bid and placebo (84."	( Efficacy and safety of asenapine in Asian patients with an acute exacerbation of schizophrenia: a multicentre, randomized, double-blind, 6-week, placebo-controlled study. Bai, YM; Kim, JH; Kinoshita, T; Miyake, M; Oshima, N, 2016)	0.96
" Treatment-emergent adverse events (TEAEs) were assessed and predefined TEAEs of interest reported in addition to metabolic and anthropometric parameters."	( Long-term Safety of Asenapine in Pediatric Patients Diagnosed With Bipolar I Disorder: A 50-Week Open-Label, Flexible-Dose Trial. Chang, K; Durgam, S; Findling, RL; Landbloom, RL; Mackle, M; Snow-Adami, L; Wu, X, 2016)	0.76
" Select predefined treatment-emergent adverse events (TEAEs) and metabolic parameters were reported."	( Long-term safety and tolerability of asenapine: A double-blind, uncontrolled, long-term extension trial in adults with an acute manic or mixed episode associated with bipolar I disorder. Durgam, S; Ketter, TA; Landbloom, R; Mackle, M; Mathews, M; Wu, X, 2017)	0.73
"ASN was generally safe and well tolerated in adults with an acute manic or mixed episode associated with bipolar I disorder."	( Long-term safety and tolerability of asenapine: A double-blind, uncontrolled, long-term extension trial in adults with an acute manic or mixed episode associated with bipolar I disorder. Durgam, S; Ketter, TA; Landbloom, R; Mackle, M; Mathews, M; Wu, X, 2017)	0.73
" Safety endpoints included treatment-emergent adverse events (TEAEs) and dermal assessments."	( Efficacy and Safety of HP-3070, an Asenapine Transdermal System, in Patients With Schizophrenia: A Phase 3, Randomized, Placebo-Controlled Study. Citrome, L; Komaroff, M; Kuriki, M; Park, AS; Starling, BR; Terahara, T; Walling, DP; Zeni, CM, 2020)	0.84
" In 201 subjects, including 44 who had received placebo (P/A group) and 157 who had received asenapine (A/A group) in the feeder trial, adverse events occurred at rates of 90."	( Long-term safety and efficacy of sublingual asenapine for the treatment of schizophrenia: A phase III extension study with follow-up for 52 weeks (P06125)-Secondary publication. Hiraoka, S; Iwama, Y; Kinoshita, T; Takekita, Y; Tamura, F, 2023)	1.39

Pharmacokinetics

Asenapine has a complex pharmacodynamic profile with affinities at multiple dopamine, serotonin, histamine, and α-adrenergic receptors. Three phase 1, open-label, randomized studies characterized the pharmacokinetic (PK) profile of HP-3070.

Excerpt	Reference	Relevance
" With buccal administration, the area under the concentration-over-time curve (AUC(0-infinity)) and peak concentration (C(max)) were, respectively, 24%, and 19% higher than with sublingual administration; these routes were not bioequivalent."	( Effect of absorption site on the pharmacokinetics of sublingual asenapine in healthy male subjects. de Greef, R; Gerrits, M; Peeters, P, 2010)	0.6
" Pharmacokinetic parameters were determined from plasma concentration-time data, using standard noncompartmental methods."	( Asenapine pharmacokinetics in hepatic and renal impairment. Bockbrader, H; de Greef, R; Dogterom, P; Gibson, GL; Lasseter, K; Marbury, T; Peeters, P; Spaans, E, 2011)	1.81
" Clinical and pharmacokinetic assessments were performed in each group."	( Short-term safety and pharmacokinetic profile of asenapine in older patients with psychosis. de Greef, R; Dubovsky, SL; Frobose, C; Panagides, J; Phiri, P, 2012)	0.63
"Asenapine has a complex pharmacodynamic profile with affinities at multiple dopamine, serotonin, histamine, and α-adrenergic receptors, all at which asenapine functions as an antagonist."	( Asenapine review, part I: chemistry, receptor affinity profile, pharmacokinetics and metabolism. Citrome, L, 2014)	3.29
"To investigate the pharmacokinetic and tissue distribution study of ASPM following oral administration in rats, reversed-phase HPLC method was developed and validated."	( Preclinical pharmacokinetics and biodistribution studies of asenapine maleate using novel and sensitive RP-HPLC method. Gourishetti, K; Koteshwara, KB; Managuli, RS; Mutalik, S; Reddy, MS; Shenoy, RR, 2017)	0.7
" In pharmacokinetics study, half-life was 32."	( Preclinical pharmacokinetics and biodistribution studies of asenapine maleate using novel and sensitive RP-HPLC method. Gourishetti, K; Koteshwara, KB; Managuli, RS; Mutalik, S; Reddy, MS; Shenoy, RR, 2017)	0.7
"This study aimed to characterize the pharmacokinetic (PK) properties, safety, and tolerability of asenapine, and to develop a population PK model in pediatric patients with schizophrenia, bipolar disorder, or other psychiatric disorders."	( Asenapine pharmacokinetics and tolerability in a pediatric population. Carrothers, TJ; de Greef, R; Dennie, J; Dogterom, P; Findling, RL; Jakate, A; Johnson, M; Miltenburg, AM; Pilla Reddy, V; Riesenberg, R; Troyer, MD, 2018)	2.14
" The pharmacokinetic results in rats showed 50."	( Enhanced intestinal absorption of asenapine maleate by fabricating solid lipid nanoparticles using TPGS: elucidation of transport mechanism, permeability across Caco-2 cell line and in vivo pharmacokinetic studies. Mundada, V; Patel, M; Sawant, K, 2019)	0.79
"Three phase 1, open-label, randomized studies characterized the pharmacokinetic (PK) profile of HP-3070 by assessing its relative bioavailability compared with sublingual asenapine, its single-/multiple-dose PK and dose proportionality, and the effects of application site, ethnicity, and external heat on bioavailability."	( Pharmacokinetic Profile of the Asenapine Transdermal System (HP-3070). Castelli, M; Citrome, L; Komaroff, M; Starling, B; Suzuki, K; Terahara, T, )	0.61

Compound-Compound Interactions

Asenapine was an effective and well-tolerated atypical antipsychotic alternative to olanzapine in combination with divalproex for the short-term management of acute mania.

Excerpt	Reference	Relevance
"Atypical antipsychotics are used for the treatment of acute mania, either as monotherapy or in combination with lithium or divalproex, which have a better tolerability profile as compared with typical antipsychotics."	( Efficacy and Safety of Asenapine Versus Olanzapine in Combination With Divalproex for Acute Mania: A Randomized Controlled Trial. Arora, M; Gillani, Z; Mahajan, V; Praharaj, SK; Tandon, VR, )	0.44
"One hundred twenty patients aged 18 to 55 years, diagnosed with manic episode, were randomized to receive either flexible dose of sublingual asenapine (10-20 mg/d) or tablet olanzapine (10-20 mg/d), in combination with valproate 20 mg/kg per day for a period of 6 weeks."	( Efficacy and Safety of Asenapine Versus Olanzapine in Combination With Divalproex for Acute Mania: A Randomized Controlled Trial. Arora, M; Gillani, Z; Mahajan, V; Praharaj, SK; Tandon, VR, )	0.64
"This study found that asenapine was an effective and well-tolerated atypical antipsychotic alternative to olanzapine in combination with divalproex for the short-term management of acute mania."	( Efficacy and Safety of Asenapine Versus Olanzapine in Combination With Divalproex for Acute Mania: A Randomized Controlled Trial. Arora, M; Gillani, Z; Mahajan, V; Praharaj, SK; Tandon, VR, )	0.76
"Inhibition of cytochrome P450 (CYP) enzymes is the most common cause of harmful drug-drug interactions."	( In vitro inhibition of human cytochrome P450 enzymes by the novel atypical antipsychotic drug asenapine: a prediction of possible drug-drug interactions. Basińska-Ziobroń, A; Danek, PJ; Daniel, WA; Pukło, R; Wójcikowski, J, 2020)	0.78
"Antipsychotics are often used in combination with other psychotropic drugs to treat a variety of psychiatric disorders, as well as in combination with other drugs taken by patients with co-morbidities."	( Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy. Danek, PJ; Daniel, WA; Wójcikowski, J, 2020)	2

Bioavailability

Asenapine Maleate (ASPM) is a second generation antipsychotic used for the management of schizophrenia. It has very limited oral bioavailability due to its extensive first pass metabolism. Co-crystals with improved solubility/dissolution rate of asenAPine maleate were tested.

Excerpt	Reference	Relevance
" Bioavailability is 35% when taken sublingually, but < 2% if ingested."	( Asenapine for schizophrenia and bipolar disorder: a review of the efficacy and safety profile for this newly approved sublingually absorbed second-generation antipsychotic. Citrome, L, 2009)	1.8
" As asenapine's bioavailability is very low if ingested, asenapine is unique among the antipsychotics, in that it needs to be swallowed to be covertly 'cheeked'."	( Asenapine for schizophrenia and bipolar disorder: a review of the efficacy and safety profile for this newly approved sublingually absorbed second-generation antipsychotic. Citrome, L, 2009)	2.35
" Barriers to achieving compliance with asenapine include the recommendations of twice daily dosing, the need to avoid food and liquids for at least 10 minutes postadministration, the need for patient cooperation with sublingual administration, and the low bioavailability of the tablet if swallowed."	( Asenapine: a new antipsychotic option. Fuller, MA; Henry, JM, 2011)	2.08
" The bioavailability of asenapine at doses below the saturation solubility in the mouth does not change and is controlled primarily by mass transport equilibrium."	( Understanding the oral mucosal absorption and resulting clinical pharmacokinetics of asenapine. Bartlett, JA; van der Voort Maarschalk, K, 2012)	0.91
"The objective of this study is to increase ASPM bioavailability via transdermal route by improving the skin permeation using combined strategy of chemical and nano-carrier (transfersomal) based approaches."	( Nano-transfersomal formulations for transdermal delivery of asenapine maleate: in vitro and in vivo performance evaluations. Amirthalingam, M; Avadhani, K; Hegde, AR; Kalthur, G; Kondapalli, L; Managuli, RS; Menon, J; Mutalik, S; Shetty, PK; Shreya, AB, 2016)	0.68
" In vivo pharmacokinetic study was performed in rats to assess bioavailability by transdermal route against oral administration."	( Nano-transfersomal formulations for transdermal delivery of asenapine maleate: in vitro and in vivo performance evaluations. Amirthalingam, M; Avadhani, K; Hegde, AR; Kalthur, G; Kondapalli, L; Managuli, RS; Menon, J; Mutalik, S; Shetty, PK; Shreya, AB, 2016)	0.68
"05) increase in bioavailability upon transdermal application compared with oral route."	( Nano-transfersomal formulations for transdermal delivery of asenapine maleate: in vitro and in vivo performance evaluations. Amirthalingam, M; Avadhani, K; Hegde, AR; Kalthur, G; Kondapalli, L; Managuli, RS; Menon, J; Mutalik, S; Shetty, PK; Shreya, AB, 2016)	0.68
"Dual strategy of permeation enhancement was successful in increasing the transdermal permeation and bioavailability of ASPM."	( Nano-transfersomal formulations for transdermal delivery of asenapine maleate: in vitro and in vivo performance evaluations. Amirthalingam, M; Avadhani, K; Hegde, AR; Kalthur, G; Kondapalli, L; Managuli, RS; Menon, J; Mutalik, S; Shetty, PK; Shreya, AB, 2016)	0.68
" It is poorly absorbed when administered orally, hence exhibits poor oral bioavailability, which limits its use in clinical practice."	( Preferential Formulation of Second Generation Antipsychotic Asenapine as Inclusion Complex with Sulphobutylether-βCD (Captisol): In vitro and In vivo Evaluation. Avachat, AM; Avachat, CM; Coutinho, EC; Khan, EM; Kulkarni, JA; Martis, EAF; Padhye, S; Pradhan, R; Suryawanshi, TS, 2018)	0.72
"This study thus demonstrated that Captisol® inclusion complex is an effective strategy for solubility and bioavailability enhancement of asenapine."	( Preferential Formulation of Second Generation Antipsychotic Asenapine as Inclusion Complex with Sulphobutylether-βCD (Captisol): In vitro and In vivo Evaluation. Avachat, AM; Avachat, CM; Coutinho, EC; Khan, EM; Kulkarni, JA; Martis, EAF; Padhye, S; Pradhan, R; Suryawanshi, TS, 2018)	0.93
" Four groups of animals, previously treated with a dosage equivalent to 50% of the bioavailability obtained with a 20 mg daily use for human treatment, were exposed to the Open Field and Elevated plus Maze test."	( Systemic Administration of Antipsychotic Asenapine Pre or Postnatal does not Induce Anxiety-like Behaviors in Mice. Carrilho, CG; Coletti, RF; de Barros, JA; de Souza, TB; Farias, DM; Machado, S; Moreno, SE; Murillo-Rodriguez, E; Oliveira, MS; Veras, AB, 2018)	0.75
" The relative bioavailability of AM-SMEDDS was found to be 23."	( Novel Drug Delivery Approach via Self-Microemulsifying Drug Delivery System for Enhancing Oral Bioavailability of Asenapine Maleate: Optimization, Characterization, Cell Uptake, and In Vivo Pharmacokinetic Studies. Mundada, VP; Patel, MH; Sawant, KK, 2019)	0.72
"Self-emulsifying drug delivery systems (SES) were developed to improve oral bioavailability of asenapine maleate (ASM), an antipsychotic drug with challenging amphiphobic nature and extensive pre-systemic metabolism."	( Self-emulsifying drug delivery system for enhanced solubility of asenapine maleate: design, characterization, in vitro, ex vivo and in vivo appraisal. Avasarala, H; Dinakaran, SK; Jayanti, VR; Kakaraparthy, R, 2019)	0.97
"The aim of the present investigation was to fabricate and evaluate solid lipid nanoparticles (SLNs) of asenapine maleate (AM) to improve its oral bioavailability (BA)."	( Enhanced intestinal absorption of asenapine maleate by fabricating solid lipid nanoparticles using TPGS: elucidation of transport mechanism, permeability across Caco-2 cell line and in vivo pharmacokinetic studies. Mundada, V; Patel, M; Sawant, K, 2019)	1.01
"To prepare nanostructured lipid carriers (NLCs) loaded with asenapine maleate (ASPM) to increase its oral bioavailability by intestinal lymphatic uptake."	( Asenapine maleate-loaded nanostructured lipid carriers: optimization and in vitro, ex vivo and in vivo evaluations. Al-Jamal, KT; Faruqu, FN; Jain, S; Kushwah, V; Managuli, RS; Mutalik, S; Raut, SY; Shreya, AB; Wang, JT, 2019)	2.2
" ASPM-NLCs showed greater cellular uptake, superior preclinical oral bioavailability and higher efficacy in reducing the L-DOPA-carbidopa-induced locomotor count compared with plain drug."	( Asenapine maleate-loaded nanostructured lipid carriers: optimization and in vitro, ex vivo and in vivo evaluations. Al-Jamal, KT; Faruqu, FN; Jain, S; Kushwah, V; Managuli, RS; Mutalik, S; Raut, SY; Shreya, AB; Wang, JT, 2019)	1.96
" ASPM possesses low oral bioavailability due to extensive hepatic metabolism."	( Surface engineered nanoliposomal platform for selective lymphatic uptake of asenapine maleate: In vitro and in vivo studies. Al-Jamal, KT; Faruqu, FM; Jain, S; Managuli, RS; Mutalik, S; Pandey, A; Wang, JT, 2020)	0.79
" However, the bioavailability of AM is extremely poor due to the extensive first-pass metabolism."	( Recent advances in the development of asenapine formulations. Narayan, R; Nayak, UY; Suresh, A, 2020)	0.83
" We have also mentioned the unexplored domains which can be exploited for further enhancing the bioavailability of AM."	( Recent advances in the development of asenapine formulations. Narayan, R; Nayak, UY; Suresh, A, 2020)	0.83
" Moreover, the low bioavailability of ASM caused by first-pass metabolism and poor aqueous solubility also impairs the treatment effect."	( Long-term sustained release Poly(lactic-co-glycolic acid) microspheres of asenapine maleate with improved bioavailability for chronic neuropsychiatric diseases. Guan, S; Ma, Y; Wang, YE; Zhai, J; Zhou, X, 2020)	0.79
"Three phase 1, open-label, randomized studies characterized the pharmacokinetic (PK) profile of HP-3070 by assessing its relative bioavailability compared with sublingual asenapine, its single-/multiple-dose PK and dose proportionality, and the effects of application site, ethnicity, and external heat on bioavailability."	( Pharmacokinetic Profile of the Asenapine Transdermal System (HP-3070). Castelli, M; Citrome, L; Komaroff, M; Starling, B; Suzuki, K; Terahara, T, )	0.61
" It is available as a fast-dissolving sublingual tablet to avoid extensive first-pass metabolism with higher bioavailability as compared to oral formulations."	( Determination of Asenapine Maleate in Pharmaceutical and Biological Matrices: A Critical Review of Analytical Techniques over the Past Decade. Kotak, V; Patel, M; Patel, R; Tanna, N, 2022)	1.06
"To improve the solubility/dissolution rate of asenapine maleate and hence the bioavailability using the co-crystal approach."	( Enhancement of the Solubility of Asenapine Maleate Through the Preparation of Co-Crystals. Al-Nimry, SS; Khanfar, MS, 2022)	1.26
"Co-crystals with improved solubility/dissolution rate of asenapine maleate were prepared successfully and were expected to enhance the bioavailability of the drug."	( Enhancement of the Solubility of Asenapine Maleate Through the Preparation of Co-Crystals. Al-Nimry, SS; Khanfar, MS, 2022)	1.25
"Asenapine Maleate (ASPM) is a second generation antipsychotic used for the management of schizophrenia but with very limited oral bioavailability due to its extensive first pass metabolism."	( Design of long acting invasomal nanovesicles for improved transdermal permeation and bioavailability of asenapine maleate for the chronic treatment of schizophrenia. Abdel-Mottaleb, MMA; El-Ghany, EA; El-Tokhy, FS; Geneidi, AS, 2021)	2.28

Dosage Studied

Transdermal asenapine is a new first-in-class dosage form and provides a novel modality of administration. Obstacles to the use of this drug are recommendations for twice daily dosing and the need to avoid food or liquids for 10 min after administration.

Excerpt	Relevance	Reference
" Obstacles to the use of asenapine are the recommendations for twice daily dosing and the need to avoid food or liquids for 10 min after administration."	( Asenapine for schizophrenia and bipolar disorder: a review of the efficacy and safety profile for this newly approved sublingually absorbed second-generation antipsychotic. Citrome, L, 2009)	2.1
" The modal dosage of asenapine was 10 mg twice daily in both phases."	( A randomized placebo-controlled trial of asenapine for the prevention of relapse of schizophrenia after long-term treatment. Kane, JM; Mackle, M; Panagides, J; Snow-Adami, L; Szegedi, A; Zhao, J, 2011)	0.95
" Iloperidone and asenapine are dosed twice daily, in contrast to lurasidone, which is dosed once daily with food."	( Iloperidone, asenapine, and lurasidone: a brief overview of 3 new second-generation antipsychotics. Citrome, L, 2011)	1.08
" To understand its cognitive and neurochemical actions more fully, we explored the effects of short- and long-term dosing with asenapine on measures of cognitive and motor function in normal monkeys and in those previously exposed for 2 weeks to PCP; we further studied the impact of treatment with asenapine on dopamine and serotonin turnover in discrete brain regions from the same cohort."	( Asenapine effects on cognitive and monoamine dysfunction elicited by subchronic phencyclidine administration. Elsworth, JD; Groman, SM; Jentsch, JD; Marston, H; Roth, RH; Shahid, M; Valles, R; Wong, E, 2012)	2.03
" However, these agents differ from one another in terms of formulations, pharmacokinetics, and dosing and nonmetabolic adverse effect profile."	( Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. Bobo, WV, 2013)	1.83
" Here, we assessed monoamine system activities after two-day and 21-day asenapine administration at a dosage (0."	( Asenapine alters the activity of monoaminergic systems following its subacute and long-term administration: an in vivo electrophysiological characterization. Blier, P; El Mansari, M; Oosterhof, CA, 2015)	2.09
" Participants were assessed at baseline and after 12 weeks with the following instruments: the Clinical Global Impression Scale, Severity item (CGI-S), Hamilton Depression Rating Scale (HAM-D), Hamilton Anxiety Rating Scale (HAM-A), Social Occupational Functioning Assessment Scale (SOFAS), Borderline Personality Disorder Severity Index (BPDSI), Barratt Impulsiveness Scale, version 11 (BIS-11), Modified Overt Aggression Scale (MOAS), Self-Harm Inventory (SHI), and Dosage Record and Treatment Emergent Symptom Scale (DOTES)."	( Efficacy and Tolerability of Asenapine Compared with Olanzapine in Borderline Personality Disorder: An Open-Label Randomized Controlled Trial. Bellino, S; Bozzatello, P; Rocca, P; Uscinska, M, 2017)	0.75
" After rapid absorption through the oral mucosa, the pharmacokinetic profile of asenapine in pediatric patients is similar to that which is observed in adult patients, indicating that the recommended adult dosage does not need to be adjusted for pediatric use."	( Asenapine Treatment in Pediatric Patients with Bipolar I Disorder or Schizophrenia: A Review. Findling, RL; Grant, B; Stepanova, E, 2018)	2.15
" Four groups of animals, previously treated with a dosage equivalent to 50% of the bioavailability obtained with a 20 mg daily use for human treatment, were exposed to the Open Field and Elevated plus Maze test."	( Systemic Administration of Antipsychotic Asenapine Pre or Postnatal does not Induce Anxiety-like Behaviors in Mice. Carrilho, CG; Coletti, RF; de Barros, JA; de Souza, TB; Farias, DM; Machado, S; Moreno, SE; Murillo-Rodriguez, E; Oliveira, MS; Veras, AB, 2018)	0.75
" Finally, the article provides advice on dosing and overall management of asenapine treatment, including the combination with other treatments and the switch from other antipsychotics to asenapine."	( Management of asenapine treatment in clinical practice: Recommendations from a panel of experts. Benabarre, A; Iborra, P; Montes, JM; Mozos, A; Sáez, C; Vieta, E, )	0.72
" Transdermal asenapine is a new first-in-class dosage form and provides a novel modality of administration."	( Asenapine Transdermal Patch for the Management of Schizophrenia. Barlow, R; Bertrand, S; Cornett, EM; DeGraw, C; Derakhshanian, S; Hasoon, J; Kaye, AD; Kaye, AM; Menard, A; Rath, A; Urits, I; Viswanath, O; Zhou, M, 2020)	2.37
"Differences in psychiatric background and dose-response to asenapine in patients with schizophrenia were examined based on efficacy and safety, using data obtained in a double-blind, placebo-controlled trial."	( Divergence of dose-response with asenapine: a cluster analysis of randomized, double-blind, and placebo control study. Aoki, N; Funatsuki, T; Hiraoka, S; Iwama, Y; Kato, M; Kinoshita, T; Koshikawa, Y; Naito, M; Ogata, H; Sunada, N; Takano, C; Takekita, Y; Yamamoto, A; Yanagida, T, 2022)	1.25

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Class	Description
5-chloro-2-methyl-2,3,3a,12b-tetrahydrodibenzo[2,3:6,7]oxepino[4,5-c]pyrrole	An organic heterotetracyclic compound that is 2,3,3a,12b-tetrahydrodibenzo[2,3:6,7]oxepino[4,5-c]pyrrole bearing methyl and chloro substituents at positions 2 and 5 respectively.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Alpha-1D adrenergic receptor	Homo sapiens (human)	Ki	0.0012	0.0000	0.3609	10.0000	AID1682829
Alpha-1A adrenergic receptor	Homo sapiens (human)	Ki	0.0012	0.0000	0.2726	10.0000	AID1682829
Histamine H1 receptor	Homo sapiens (human)	Ki	0.0010	0.0000	0.5110	10.0000	AID1682828
Alpha-1B adrenergic receptor	Homo sapiens (human)	Ki	0.0012	0.0000	0.4713	10.0000	AID1682829
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
G protein-coupled receptor signaling pathway	Alpha-1D adrenergic receptor	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Alpha-1D adrenergic receptor	Homo sapiens (human)
positive regulation of cell population proliferation	Alpha-1D adrenergic receptor	Homo sapiens (human)
neuron-glial cell signaling	Alpha-1D adrenergic receptor	Homo sapiens (human)
cell-cell signaling	Alpha-1D adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-1D adrenergic receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Alpha-1D adrenergic receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Alpha-1D adrenergic receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Alpha-1D adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-1D adrenergic receptor	Homo sapiens (human)
MAPK cascade	Alpha-1A adrenergic receptor	Homo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressure	Alpha-1A adrenergic receptor	Homo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressure	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrine	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrine	Alpha-1A adrenergic receptor	Homo sapiens (human)
apoptotic process	Alpha-1A adrenergic receptor	Homo sapiens (human)
smooth muscle contraction	Alpha-1A adrenergic receptor	Homo sapiens (human)
signal transduction	Alpha-1A adrenergic receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Alpha-1A adrenergic receptor	Homo sapiens (human)
activation of phospholipase C activity	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Alpha-1A adrenergic receptor	Homo sapiens (human)
adult heart development	Alpha-1A adrenergic receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Alpha-1A adrenergic receptor	Homo sapiens (human)
response to xenobiotic stimulus	Alpha-1A adrenergic receptor	Homo sapiens (human)
response to hormone	Alpha-1A adrenergic receptor	Homo sapiens (human)
negative regulation of autophagy	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of cardiac muscle hypertrophy	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of synaptic transmission, GABAergic	Alpha-1A adrenergic receptor	Homo sapiens (human)
intracellular signal transduction	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of action potential	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of smooth muscle contraction	Alpha-1A adrenergic receptor	Homo sapiens (human)
calcium ion transport into cytosol	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of cardiac muscle contraction	Alpha-1A adrenergic receptor	Homo sapiens (human)
cell growth involved in cardiac muscle cell development	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of protein kinase C signaling	Alpha-1A adrenergic receptor	Homo sapiens (human)
pilomotor reflex	Alpha-1A adrenergic receptor	Homo sapiens (human)
neuron-glial cell signaling	Alpha-1A adrenergic receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Alpha-1A adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-1A adrenergic receptor	Homo sapiens (human)
cell-cell signaling	Alpha-1A adrenergic receptor	Homo sapiens (human)
inflammatory response	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
memory	Histamine H1 receptor	Homo sapiens (human)
visual learning	Histamine H1 receptor	Homo sapiens (human)
regulation of vascular permeability	Histamine H1 receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Histamine H1 receptor	Homo sapiens (human)
regulation of synaptic plasticity	Histamine H1 receptor	Homo sapiens (human)
cellular response to histamine	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H1 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
regulation of vasoconstriction	Alpha-1B adrenergic receptor	Homo sapiens (human)
intracellular signal transduction	Alpha-1B adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-1B adrenergic receptor	Homo sapiens (human)
regulation of cardiac muscle contraction	Alpha-1B adrenergic receptor	Homo sapiens (human)
neuron-glial cell signaling	Alpha-1B adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
cell-cell signaling	Alpha-1B adrenergic receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Alpha-1B adrenergic receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
protein binding	Alpha-1D adrenergic receptor	Homo sapiens (human)
identical protein binding	Alpha-1D adrenergic receptor	Homo sapiens (human)
alpha1-adrenergic receptor activity	Alpha-1D adrenergic receptor	Homo sapiens (human)
alpha1-adrenergic receptor activity	Alpha-1A adrenergic receptor	Homo sapiens (human)
protein binding	Alpha-1A adrenergic receptor	Homo sapiens (human)
protein heterodimerization activity	Alpha-1A adrenergic receptor	Homo sapiens (human)
histamine receptor activity	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H1 receptor	Homo sapiens (human)
neurotransmitter receptor activity	Histamine H1 receptor	Homo sapiens (human)
protein binding	Alpha-1B adrenergic receptor	Homo sapiens (human)
protein heterodimerization activity	Alpha-1B adrenergic receptor	Homo sapiens (human)
alpha1-adrenergic receptor activity	Alpha-1B adrenergic receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Alpha-1D adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1D adrenergic receptor	Homo sapiens (human)
nucleus	Alpha-1A adrenergic receptor	Homo sapiens (human)
nucleoplasm	Alpha-1A adrenergic receptor	Homo sapiens (human)
cytoplasm	Alpha-1A adrenergic receptor	Homo sapiens (human)
cytosol	Alpha-1A adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1A adrenergic receptor	Homo sapiens (human)
caveola	Alpha-1A adrenergic receptor	Homo sapiens (human)
nuclear membrane	Alpha-1A adrenergic receptor	Homo sapiens (human)
intracellular membrane-bounded organelle	Alpha-1A adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1A adrenergic receptor	Homo sapiens (human)
cytosol	Histamine H1 receptor	Homo sapiens (human)
plasma membrane	Histamine H1 receptor	Homo sapiens (human)
synapse	Histamine H1 receptor	Homo sapiens (human)
dendrite	Histamine H1 receptor	Homo sapiens (human)
plasma membrane	Histamine H1 receptor	Homo sapiens (human)
nucleus	Alpha-1B adrenergic receptor	Homo sapiens (human)
cytoplasm	Alpha-1B adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1B adrenergic receptor	Homo sapiens (human)
caveola	Alpha-1B adrenergic receptor	Homo sapiens (human)
nuclear membrane	Alpha-1B adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1B adrenergic receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID1345615	Human 5-HT1A receptor (5-Hydroxytryptamine receptors)	1996	Psychopharmacology, Mar, Volume: 124, Issue:1-2	Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1346264	Human 5-HT1B receptor (5-Hydroxytryptamine receptors)	1996	Psychopharmacology, Mar, Volume: 124, Issue:1-2	Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1346528	Human 5-HT1D receptor (5-Hydroxytryptamine receptors)	1996	Psychopharmacology, Mar, Volume: 124, Issue:1-2	Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1345788	Human D2 receptor (Dopamine receptors)	2009	Journal of psychopharmacology (Oxford, England), Jan, Volume: 23, Issue:1	Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
AID1346037	Human H1 receptor (Histamine receptors)	1996	Psychopharmacology, Mar, Volume: 124, Issue:1-2	Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID624210	Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A	1998	European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3	Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID624235	Agonists at Human 5-Hydroxytryptamine receptor 5-HT2A	1996	Psychopharmacology, Mar, Volume: 124, Issue:1-2	Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1346603	Human 5-ht1e receptor (5-Hydroxytryptamine receptors)	1996	Psychopharmacology, Mar, Volume: 124, Issue:1-2	Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID624210	Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A	1996	Psychopharmacology, Mar, Volume: 124, Issue:1-2	Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID624230	Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e	1996	Psychopharmacology, Mar, Volume: 124, Issue:1-2	Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
AID1345615	Human 5-HT1A receptor (5-Hydroxytryptamine receptors)	1998	European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3	Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID1259419	Human 5-HT2A receptor (5-Hydroxytryptamine receptors)	2009	Journal of psychopharmacology (Oxford, England), Jan, Volume: 23, Issue:1	Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.
AID1682828	Binding affinity to H1 histamine receptor (unknown origin)
AID343685	Ratio of drug level in brain to blood in Wistar rat	2008	Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13	Toward prediction of alkane/water partition coefficients.
AID1682829	Binding affinity to adrenergic alpha1 receptor (unknown origin)
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	10 (3.91)	18.2507
2000's	21 (8.20)	29.6817
2010's	186 (72.66)	24.3611
2020's	39 (15.23)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	50 (18.87%)	5.53%
Reviews	49 (18.49%)	6.00%
Case Studies	29 (10.94%)	4.05%
Observational	5 (1.89%)	0.25%
Other	132 (49.81%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (50)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Multicenter, Double-Blind, Flexible-Dose, 6-Month Extension Trial Comparing the Safety and Efficacy of Asenapine With Olanzapine in Subjects Who Completed the Protocol 25543 (NCT 00212836; P05817) [NCT00265343]	Phase 3	306 participants (Actual)	Interventional	2005-12-31	Completed
A Double-Blind, 9-Week Extension Study Evaluating the Safety and Maintenance of Effect of Asenapine vs. Olanzapine in the Treatment of Subjects With Acute Mania Clinical Trial Protocol A7501006 (Secondary Title: ARES) [NCT00143182]	Phase 3	504 participants (Actual)	Interventional	2005-01-07	Completed
A Randomized, Crossover Study Evaluating the Acceptability of Unflavored Asenapine and Raspberry Flavored Asenapine in Stable Subjects With A Psychotic Disorder [NCT00878462]	Phase 2	174 participants (Actual)	Interventional	2005-06-29	Completed
An Observational Drug Utilization Study of SYCREST^® (Asenapine) in the United Kingdom [NCT01498770]		42 participants (Actual)	Observational	2013-04-01	Completed
A Phase 3, Randomized, Placebo-Controlled, Double-Blinded Trial Evaluating the Safety and Efficacy of Asenapine in Subjects Continuing Lithium or Valproic Acid/Divalproex Sodium for the Treatment of an Acute Manic or Mixed Episode [NCT00145470]	Phase 3	326 participants (Actual)	Interventional	2005-06-02	Completed
A Phase III, Randomized, Placebo-Controlled, Double-Blind Trial Evaluating the Safety and Efficacy of Sublingual Asenapine vs. Olanzapine and Placebo in In-Patients With an Acute Manic Episode Clinical Trial Protocol 7501005 (Secondary Title: ARES) [NCT00159796]	Phase 3	489 participants (Actual)	Interventional	2004-12-14	Completed
A Multicenter, Double-Blind, Flexible -Dose, 6-Month Trial Comparing the Efficacy and Safety of Asenapine With Olanzapine in Stable Subjects With Predominant, Persistent Negative Symptoms of Schizophrenia. [NCT00145496]	Phase 3	468 participants (Actual)	Interventional	2004-12-31	Completed
A Randomized, Placebo-Controlled, Double-Blind Trial of Asenapine in the Prevention of Relapse After Long-Term Treatment of Schizophrenia [NCT00150176]	Phase 3	831 participants (Actual)	Interventional	2005-04-30	Completed
A Multicenter, Randomized, Double-Blind, Fixed-Dose, 6-Week Trial of the Efficacy and Safety of Asenapine Compared With Placebo Using Haloperidol Positive Control in Subjects With an Acute Exacerbation of Schizophrenia [NCT00156104]	Phase 3	460 participants (Actual)	Interventional	2005-07-01	Completed
A Multicenter, Randomized, Double-Blind, Flexible-Dose, 6-Week Trial of the Efficacy and Safety of Asenapine Compared With Placebo Using Olanzapine Positive Control in Subjects With an Acute Exacerbation of Schizophrenia [NCT00151424]	Phase 3	277 participants (Actual)	Interventional	2005-02-15	Completed
A Phase 3, Placebo-Controlled, Double-Blinded Continuation Trial Evaluating the Safety and Efficacy of Asenapine in Subjects Completing a 12-week Lead-in Trial and Continuing Lithium or Valproic Acid/Divalproex Sodium for the Treatment of an Acute Manic o [NCT00145509]	Phase 3	77 participants (Actual)	Interventional	2005-08-31	Completed
Long-Term Efficacy and Safety Evaluation of Asenapine (10-20 mg/Day) in With Schizophrenia or Schizoaffective Disorder, in a Multicenter Trial Using (10-20 mg/Day) as a Control [NCT00212771]	Phase 3	440 participants (Actual)	Interventional	2004-09-30	Completed
A Randomized, Parallel Group, Multiple Dose, 6-Week Study to Evaluate Safety, Tolerability, and Pharmacokinetics of Asenapine in Elderly Subjects With Psychosis. [NCT00281320]	Phase 3	122 participants (Actual)	Interventional	2006-02-28	Completed
An 8-week, Placebo-controlled, Double-blind, Randomized, Fixed-dose Efficacy and Safety Trial of Asenapine in Adolescent Subjects With Schizophrenia [NCT01190254]	Phase 3	306 participants (Actual)	Interventional	2010-09-28	Completed
A Phase 3b, Multicenter, Double-Blind, Fixed-Dose, Parallel-Group, Three Week Placebo Controlled Trial Evaluating the Safety and Efficacy of Asenapine in Subjects With Bipolar 1 Disorder Experiencing an Acute Manic or Mixed Episode (Protocol P05691 [Forme [NCT00764478]	Phase 3	367 participants (Actual)	Interventional	2012-04-06	Completed
A Multicenter, Double-Blind, Flexible -Dose, 6-Month Trial Comparing the Efficacy Safety of Asenapine With Olanzapine in Stable Subjects With Predominant, Persistent Negative Symptoms of Schizophrenia [NCT00212836]	Phase 3	481 participants (Actual)	Interventional	2005-04-21	Completed
A 26-week, Multi-center, Open-label, Flexible Dose, Long-term Safety Trial of Asenapine in Adolescent Subjects With Schizophrenia [NCT01190267]	Phase 3	204 participants (Actual)	Interventional	2010-09-28	Completed
A Multicentric, Open Label, Randomized, Balanced, Two Treatment, Three Period, Three Sequence, Crossover, Multiple Dose, Steady State Bioequivalence Study of Asenapine Sublingual Tablets, 10 mg Manufactured by AMNEAL PHARMACEUTICALS, USA With Reference Pr [NCT02072954]	Phase 2/Phase 3	48 participants (Actual)	Interventional	2013-11-30	Completed
A Multicenter, Double-Blind, Fixed-Dose, Long-Term Extension Trial of the Safety of Asenapine in Subjects Diagnosed With Bipolar 1 Disorder Who Completed Protocol P05691 (Formerly 041044) (Phase3B, Protocol P05692 [Formerly 041045]) [NCT01395992]	Phase 3	165 participants (Actual)	Interventional	2012-04-30	Completed
A Double-Blind, Placebo-Controlled Trial of Asenapine in the Prevention of Recurrence of a Mood Episode After Stabilization of an Acute Manic/Mixed Episode in Subjects With Bipolar 1 Disorder (Phase 3B, Protocol P06384) [NCT01396291]	Phase 3	561 participants (Actual)	Interventional	2011-12-31	Completed
A Multicenter, Randomized, Double-blind, Fixed-dose, 6-week Trial of the Efficacy and Safety of Asenapine Compared With Placebo in Subjects With an Acute Exacerbation of Schizophrenia (Phase 3) [NCT01098110]	Phase 3	532 participants (Actual)	Interventional	2010-05-25	Completed
A Phase III, Double-Blind, Randomized, Active-Controlled, Two-Armed, Multicenter, Efficacy and Safety Assessment (ACTAMESA) of Org 5222 and Olanzapine in the Treatment of Patients With Schizophrenia or Schizoaffective Disorder [NCT00212784]	Phase 3	1,225 participants (Actual)	Interventional	2003-09-04	Completed
A 12-Month Randomized, Open-Label Study of Caregiver Psycho-education and Skills Training in Patients Recently Diagnosed With Schizophrenia, Schizoaffective Disorder, or Schizophreniform Disorder and Receiving Paliperidone Palmitate or Oral Antipsychotic [NCT02600741]		296 participants (Actual)	Observational	2015-07-24	Completed
An Open-label, Randomized, Two Treatment, Multi-site, Multiple Dose, Steady State, Three-way, Reference-replicated Crossover, Pharmacokinetic Study to Determine the In-vivo Bioequivalence Between Asenapine 10 mg Sublingual Tablet and SAPHRIS® (Asenapine) [NCT01948024]	Phase 1	65 participants (Actual)	Interventional	2013-07-31	Completed
An Open-label Switch Study to Asenapine in the Early Stage of Psychosis [NCT01968161]	Phase 4	12 participants (Anticipated)	Interventional	2013-10-31	Not yet recruiting
Long-term Extension Trial of Asenapine in Subjects With Schizophrenia (Phase 3 ; Protocol No. P06125) [NCT01142596]	Phase 3	201 participants (Actual)	Interventional	2010-05-25	Completed
Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies [NCT02893371]		1,037,352 participants (Actual)	Observational	2016-09-30	Completed
A Multicenter, Randomized, Double-Blind, Flexible-Dose, Long-Term Extension Trial of the Safety and Maintenance of Effect of Asenapine Using Olanzapine Positive Control in Subjects Who Complete Protocols 041021 or 041022. [NCT00156091]	Phase 3	260 participants (Actual)	Interventional	2005-04-30	Completed
A Multicenter, Randomized, Double-Blind, Fixed-Dose, 6-Week Trial of the Efficacy and Safety of Asenapine Compared With Placebo Using Olanzapine Positive Control in Subjects With an Acute Exacerbation of Schizophrenia [NCT00156117]	Phase 3	417 participants (Actual)	Interventional	2005-05-12	Completed
Long-term Study of Asenapine in Subjects With Residual Subtype, Receiving Multiple or/and High Dose Drugs, or Treatment Refractory Schizophrenia (Protocol P06238) [NCT01244828]	Phase 3	157 participants (Actual)	Interventional	2011-04-05	Completed
A Sequential Groups, Open Label, Rising Multiple Dose Study to Assess the Pharmacokinetics, Safety and Tolerability of Sublingual Asenapine in a Pediatric Population With Schizophrenia or Bipolar I Disorder [NCT01206517]	Phase 1	30 participants (Actual)	Interventional	2010-07-18	Completed
Randomized Multicentric Open-label Phase III Clinical Trial to Evaluate the Efficacy of Continual Treatment Versus Discontinuation Based in the Presence of Prodromes in a First Episode of Non-affective Psychosis. [NCT01765829]	Phase 3	104 participants (Anticipated)	Interventional	2012-11-30	Recruiting
Efficacy and Safety of 3-Week Fixed-Dose Asenapine Treatment in Pediatric Acute Manic or Mixed Episodes Associated With Bipolar I Disorder (Protocol No. P06107) [NCT01244815]	Phase 3	404 participants (Actual)	Interventional	2011-06-16	Completed
A 50-Week Open-Label, Flexible-Dose Trial of Asenapine Extension Treatment to P06107 in Pediatric Subjects With Acute Manic or Mixed Episodes Associated With Bipolar I Disorder [NCT01349907]	Phase 3	322 participants (Actual)	Interventional	2011-06-16	Completed
A Single-center, Open-label, 2-way Crossover Relative Bioavailability and Safety Trial With Two Differing Strength Tablets (3 x 5 mg vs. 1 x 15 mg) of Sublingually Administered Org 5222 in Subjects With Schizophrenia or Schizoaffective Disorder. [NCT01101464]	Phase 2	8 participants (Actual)	Interventional	2002-10-31	Completed
A Multicenter, Double-Blind, Flexible-Dose, 6-Month Extension Trial Comparing the Safety and Efficacy of Asenapine With Olanzapine in Subjects Who Completed Protocol A7501013 [NCT00174265]	Phase 3	196 participants (Actual)	Interventional	2005-07-31	Completed
A Randomized, Placebo-Controlled Study to Evaluate the Efficacy and Tolerability of Asenapine With Flexible Dosing From 5mg to 20mg in Adults With Developmental Stuttering [NCT01684657]	Phase 3	32 participants (Anticipated)	Interventional	2012-09-30	Suspended(stopped due to Study transferring to another facility)
Asenapine for Bipolar Depression [NCT01807741]	Phase 2	51 participants (Actual)	Interventional	2013-09-30	Terminated(stopped due to funding ended due to recruitment delays)
A Multicenter, Randomized, Double-Blind, Flexible-Dose, Long-Term Extension Trial of the Safety and Maintenance of Effect of Asenapine Using Haloperidol Positive Control in Subjects Who Complete Protocol 041023 [NCT00156104] [NCT00156065]	Phase 3	187 participants (Actual)	Interventional	2005-09-30	Completed
A Randomized Comparison of Twice-Daily Versus Once-Daily Asenapine for Schizophrenia [NCT01549041]	Phase 4	30 participants (Actual)	Interventional	2012-04-30	Completed
Asenapine in the Treatment of Older Adults With Bipolar Disorder [NCT01460290]	Phase 4	15 participants (Actual)	Interventional	2011-10-31	Completed
A Multicenter, Double-Blind, Fixed-Dose, Long-Term Extension Trial of the Safety of Asenapine Using Olanzapine as an Active Control in Subjects Diagnosed With Schizophrenia Who Completed Protocol P05688 [NCT01617200]	Phase 3	105 participants (Actual)	Interventional	2012-12-31	Completed
An Open Label Pilot Study of Adjunctive Asenapine for the Treatment of Posttraumatic Stress Disorder [NCT01587118]	Phase 4	18 participants (Actual)	Interventional	2012-06-30	Completed
A Randomized, Double-Blind, Placebo-Controlled, Fixed-Dose, 6-Week, In-Patient Study to Assess Efficacy and Safety of HP-3070 in Subjects Diagnosed With Schizophrenia [NCT02876900]	Phase 3	617 participants (Actual)	Interventional	2016-08-31	Completed
A Randomized, Blinded, Comparison of Asenapine and Placebo as Adjunctive Treatment in Patients With Non-Psychotic Major Depressive Disorder Incompletely Responsive to Antidepressant Monotherapy [NCT01670019]	Phase 4	46 participants (Actual)	Interventional	2012-10-31	Completed
A Phase III, Randomized, Placebo-Controlled, Double-Blind Trial Evaluating the Safety and Efficacy of Sublingual Asenapine vs. Olanzapine and Placebo in In-Patients With an Acute Manic Episode Clinical Trial Protocol 7501004 (Secondary Title: ARES) [NCT00159744]	Phase 3	488 participants (Actual)	Interventional	2004-11-30	Completed
Treating Acutely Agitated Patients With Asenapine Sublingual Tablets: A Single-Dose, Randomized, Double-Blind Placebo Controlled Trial [NCT01400113]	Phase 4	120 participants (Actual)	Interventional	2012-04-30	Completed
Improving Metabolic Parameters of Antipsychotic Child Treatment (IMPACT) [NCT00806234]	Phase 4	127 participants (Actual)	Interventional	2009-01-31	Completed
A Multicenter, Randomized, Double-Blind, Fixed-Dose, 6-Week Trial of the Efficacy and Safety of Asenapine Compared With Placebo Using Olanzapine as an Active Control in Subjects With an Acute Exacerbation of Schizophrenia [NCT01617187]	Phase 3	360 participants (Actual)	Interventional	2012-12-04	Completed
A Double-Blind, 40-Week Continuation Study Evaluating the Safety of Asenapine and Olanzapine in the Treatment of Subjects With Acute Mania Clinical Trial Protocol A7501007 (Secondary Title: ARES) [NCT00159783]	Phase 3	218 participants (Actual)	Interventional	2005-07-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00145470 (28) [back to overview]	Number of Participants Achieving Young-Mania Rating Scale (Y-MRS) Responder Status
NCT00145470 (28) [back to overview]	Number of Participants Achieving Young-Mania Rating Scale (Y-MRS) Remitter Status
NCT00145470 (28) [back to overview]	Number of Participants Discontinuing Study Treatment Due to an AE
NCT00145470 (28) [back to overview]	Number of Participants Experiencing an Adverse Event (AE)
NCT00145470 (28) [back to overview]	Percentage of Participants Determined to be Ready to Discharge at Day 84 (Kaplan-Meier Estimation)
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline at Day 21 in Quality of Life as Determined by Short Form-36 Version 2 (SF-36v2)
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline at Day 84 in Quality of Life as Determined by Short Form-36 Version 2 (SF-36v2)
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Depression Score at Day 21
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Depression Score at Day 84
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Mania Score at Day 21
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Mania Score at Day 84
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Overall Bipolar Illness Score at Day 21
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Overall Bipolar Illness Score at Day 84
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Hamilton Anxiety Rating Scale (HAM-A) Score at Day 21
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Hamilton Anxiety Rating Scale (HAM-A) Score at Day 84
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in InterSePT Scale for Suicidal Thinking - Modified Version (ISST-Modified) Score at Day 21
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in InterSePT Scale for Suicidal Thinking - Modified Version (ISST-Modified) Score at Day 84
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Montgomery Asberg Depression Rating Scale (MADRS) Score at Day 21
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Montgomery Asberg Depression Rating Scale (MADRS) Score at Day 84
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Score at Day 21
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Score at Day 84
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q), General Activities Subscale Score at Day 21
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q), General Activities Subscale Score at Day 84
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Young-Mania Rating Scale (Y-MRS) Score at Day 21
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Young-Mania Rating Scale (Y-MRS) Score at Day 42
NCT00145470 (28) [back to overview]	Least Squares Mean Change From Baseline in Young-Mania Rating Scale (Y-MRS) Score at Day 84
NCT00145470 (28) [back to overview]	Mean Change From Baseline (CFB) at Day 21 in Neurocognitive Function as Determined by Central Nervous System Vital Signs (CNS-VS) Test Battery
NCT00145470 (28) [back to overview]	Mean Change From Baseline (CFB) at Day 84 in Neurocognitive Function as Determined by Central Nervous System Vital Signs (CNS-VS) Test Battery
NCT00145496 (3) [back to overview]	Change From Baseline in Body Weight
NCT00145496 (3) [back to overview]	Change From Baseline in Negative Symptoms of Schizophrenia Measured by the Negative Symptom Assessment (NSA) Scale Total Score
NCT00145496 (3) [back to overview]	Change From Baseline in Quality of Life Measured by the Quality of Life Scale (QLS) Total Score
NCT00145509 (4) [back to overview]	Change From Baseline to Week 52 on the Montgomery Asberg Depression Rating Scale (MADRS) Score
NCT00145509 (4) [back to overview]	Change From Baseline to Week 52 on the Young-Mania Rating Scale (Y-MRS) Score
NCT00145509 (4) [back to overview]	Number of Participants Who Discontinued Because of an Adverse Event
NCT00145509 (4) [back to overview]	Number of Participants Who Experienced an Adverse Event
NCT00150176 (2) [back to overview]	Time to Early Discontinuation for Any Reason
NCT00150176 (2) [back to overview]	Time to Relapse or an Impending Relapse
NCT00156065 (2) [back to overview]	Loss of Effect Over Time
NCT00156065 (2) [back to overview]	Median Survival Time of Effect
NCT00159783 (9) [back to overview]	Abdominal Girth
NCT00159783 (9) [back to overview]	Number of Participants With Laboratory Values Outside Normal Range
NCT00159783 (9) [back to overview]	Participants Who Experienced Adverse Event(s)
NCT00159783 (9) [back to overview]	Number of Participants With Markedly Abnormal Vital Sign Changes
NCT00159783 (9) [back to overview]	Number of Participants With Abnormal Physical Examination Findings
NCT00159783 (9) [back to overview]	Number of Participants With Abnormal Electrocardiogram
NCT00159783 (9) [back to overview]	Extrapyramidal Symptoms [EPS]
NCT00159783 (9) [back to overview]	Concomitant Medications
NCT00159783 (9) [back to overview]	Body Weight
NCT00174265 (2) [back to overview]	Change From Baseline in Quality of Life Measured by the Quality of Life Scale (QLS) Total Score
NCT00174265 (2) [back to overview]	Change From Baseline in Negative Symptoms of Schizophrenia Measured by the Negative Symptom Assessment (NSA) Scale Total Score
NCT00265343 (2) [back to overview]	Long-term Change in Negative Symptoms of Schizophrenia Measured by the Negative Symptom Assessment (NSA) Scale
NCT00265343 (2) [back to overview]	Change in Quality of Life Measured by Quality of Life Scale (QLS)
NCT00281320 (8) [back to overview]	Number of Participants Who Discontinued Because of an Adverse Event
NCT00281320 (8) [back to overview]	Number of Participants Who Experienced an Adverse Event
NCT00281320 (8) [back to overview]	Pharmacokinetics of Asenapine up to Doses of 10 mg BID in Elderly Subjects With Psychosis , Dn-Cmax
NCT00281320 (8) [back to overview]	Pharmacokinetics of Asenapine up to Doses of 10 mg BID in Elderly Subjects With Psychosis, AUC 0-12
NCT00281320 (8) [back to overview]	Pharmacokinetics of Asenapine up to Doses of 10 mg BID in Elderly Subjects With Psychosis, Cmin
NCT00281320 (8) [back to overview]	Pharmacokinetics of Asenapine up to Doses of 10 mg BID in Elderly Subjects With Psychosis, Dn-AUC 0-12
NCT00281320 (8) [back to overview]	Pharmacokinetics of Asenapine up to Doses of 10 mg BID in Elderly Subjects With Psychosis, Tmax
NCT00281320 (8) [back to overview]	Pharmacokinetics of Asenapine up to Doses of 10 mg BID in Elderly Subjects With Psychosis,Cmax
NCT00764478 (23) [back to overview]	Change From Baseline in CGI-BP-S Overall Score at Day 2, Day 4, Day 7, Day 14
NCT00764478 (23) [back to overview]	Change From Baseline in Montgomery Asberg Depression Rating Scale (MADRS) Total Score
NCT00764478 (23) [back to overview]	Change From Baseline in PANSS General Psychopathology Subscale Score
NCT00764478 (23) [back to overview]	Change From Baseline in PANSS Marder Factor Anxiety/Depression Symptom Score
NCT00764478 (23) [back to overview]	Percentage of Participants Who Are Y-MRS Responders at Day 2, Day 4, Day 7, Day 14
NCT00764478 (23) [back to overview]	Change From Baseline in PANSS Marder Factor Disorganized Thought Symptom Score
NCT00764478 (23) [back to overview]	Change From Baseline in PANSS Marder Factor Hostility/Excitement Symptom Score
NCT00764478 (23) [back to overview]	Change From Baseline in PANSS Marder Factor Negative Symptom Score
NCT00764478 (23) [back to overview]	Change From Baseline in PANSS Marder Factor Positive Symptom Score
NCT00764478 (23) [back to overview]	Change From Baseline in PANSS Negative Subscale Score
NCT00764478 (23) [back to overview]	Change From Baseline in PANSS Positive Subscale Score
NCT00764478 (23) [back to overview]	Change From Baseline in CGI-BP-S Depression Score
NCT00764478 (23) [back to overview]	Change From Baseline in Y-MRS Total Score at Day 2, Day 4, Day 7 and Day 14
NCT00764478 (23) [back to overview]	Percentage of Participants Who Are CGI-BP Improvement (CGI-BP-I) Responders of Depression Score
NCT00764478 (23) [back to overview]	Percentage of Participants Who Are CGI-BP Improvement (CGI-BP-I) Responders of Overall Bipolar Illness Score
NCT00764478 (23) [back to overview]	Percentage of Participants Who Are CGI-BP Improvement (CGI-BP-I) Responders of Mania Score
NCT00764478 (23) [back to overview]	Percentage of Participants Who Are Y-MRS Remitters at Day 2, Day 4, Day 7, Day 14, Day 21
NCT00764478 (23) [back to overview]	Change From Baseline in Positive And Negative Syndrome Scale (PANSS) Total Score
NCT00764478 (23) [back to overview]	Change From Baseline in Clinical Global Impression - Bipolar Mania - Severity of Illness (CGI-BP-S) Overall Score at Day 21
NCT00764478 (23) [back to overview]	Change From Baseline in Young Mania Rating Scale (Y-MRS) Total Score at Day 21
NCT00764478 (23) [back to overview]	Percentage of Participants Who Are Y-MRS Remitters at Day 21
NCT00764478 (23) [back to overview]	Percentage of Participants Who Are Y-MRS Responders at Day 21
NCT00764478 (23) [back to overview]	Change From Baseline in CGI-BP-S Mania Score
NCT00806234 (4) [back to overview]	Change in Whole Body Insulin Sensitivity Index
NCT00806234 (4) [back to overview]	Change in Low Density Lipoprotein (LDL) Cholesterol Level
NCT00806234 (4) [back to overview]	Body Mass Index (BMI) Z-score Change
NCT00806234 (4) [back to overview]	Triglyceride Levels
NCT01098110 (12) [back to overview]	Percentage of Participants Who Were PANSS Responders.
NCT01098110 (12) [back to overview]	Percentage of Participants Who Were Clinical Global Impressions - Improvement (CGI-I) Responders.
NCT01098110 (12) [back to overview]	Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score.
NCT01098110 (12) [back to overview]	Change From Baseline in PANSS Positive Symptom Score.
NCT01098110 (12) [back to overview]	Change From Baseline in PANSS Marder Factor Positive Symptom Score.
NCT01098110 (12) [back to overview]	Change From Baseline in PANSS Marder Factor Negative Symptom Score.
NCT01098110 (12) [back to overview]	Change From Baseline in PANSS Marder Factor Hostility/Excitement Symptom Score.
NCT01098110 (12) [back to overview]	Change From Baseline in PANSS Marder Factor Disorganized Thought Symptom Score.
NCT01098110 (12) [back to overview]	Change From Baseline in PANSS General Psychopathology Score.
NCT01098110 (12) [back to overview]	Change From Baseline in Clinical Global Impressions -Severity of Illness (CGI-S) Score.
NCT01098110 (12) [back to overview]	Change From Baseline in PANSS Negative Symptom Score.
NCT01098110 (12) [back to overview]	Change From Baseline in PANSS Marder Factor Anxiety/Depression Symptom Score.
NCT01101464 (3) [back to overview]	Pharmacokinetic Parameter of Area Under the Curve (AUC) of Two Differing Tablet Strengths (3 x 5 mg and 1 x 15 mg) of Sublingually Administered Org 5222 (Asenapine)
NCT01101464 (3) [back to overview]	Pharmacokinetic Parameter of Maximum Plasma Concentration (Cmax) of Two Differing Tablet Strengths (3 x 5 mg and 1 x 15 mg) of Sublingually Administered Org 5222 (Asenapine)
NCT01101464 (3) [back to overview]	Pharmacokinetic Parameter of Time of Occurrence of Cmax (Tmax) of Two Differing Tablet Strengths (3 x 5 mg and 1 x 15 mg) of Sublingually Administered Org 5222 (Asenapine)
NCT01142596 (23) [back to overview]	Median Time to Loss of Effect in Responders
NCT01142596 (23) [back to overview]	Change From Study P06124 Baseline in Body Mass Index (BMI) at Week 52
NCT01142596 (23) [back to overview]	Change From Study P06124 Baseline in DIEPSS Item 9 Score at Endpoint
NCT01142596 (23) [back to overview]	Change From Study P06124 Baseline in Drug-Induced Extrapyramidal Symptoms Scale (DIEPSS) Total Score at Endpoint
NCT01142596 (23) [back to overview]	Number of Participants With Non-serious AEs
NCT01142596 (23) [back to overview]	Number of Participants With Serious Adverse Events (AEs)
NCT01142596 (23) [back to overview]	Number of Participants Who Took Antiparkinsonian Drugs
NCT01142596 (23) [back to overview]	Number of Participants With Extrapyramidal Symptoms
NCT01142596 (23) [back to overview]	Percentage of Participants in Categories of Change in Weight From Study P06124 Baseline to Final Assessment
NCT01142596 (23) [back to overview]	Percentage of Participants in Categories of Change in Weight From Study P06125 Baseline to Final Assessment
NCT01142596 (23) [back to overview]	Percentage of Participants With Abnormalities on Electrocardiogram (ECG) at Study P06124 Baseline, Study P06125 Baseline and Week 52
NCT01142596 (23) [back to overview]	Change From Study P06125 Baseline in HbA1c at Week 52
NCT01142596 (23) [back to overview]	Change From Study P06125 Baseline in Insulin at Week 52
NCT01142596 (23) [back to overview]	Change From Study P06125 Baseline in Prolactin at Week 52
NCT01142596 (23) [back to overview]	Median Time to Loss of Effect in Non-Responders
NCT01142596 (23) [back to overview]	Change From Study P06124 Baseline in Fasting Glucose at Week 52
NCT01142596 (23) [back to overview]	Change From Study P06125 Baseline in Fasting Glucose at Week 52
NCT01142596 (23) [back to overview]	Change From Study P06125 Baseline in DIEPSS Total Score at Endpoint
NCT01142596 (23) [back to overview]	Change From Study P06125 Baseline in DIEPSS Item 9 Score at Endpoint
NCT01142596 (23) [back to overview]	Change From Study P06125 Baseline in BMI at Week 52
NCT01142596 (23) [back to overview]	Change From Study P06124 Baseline in Prolactin at Week 52
NCT01142596 (23) [back to overview]	Change From Study P06124 Baseline in Insulin at Week 52
NCT01142596 (23) [back to overview]	Change From Study P06124 Baseline in Glycosylated Hemoglobin (HbA1c) at Week 52
NCT01190254 (19) [back to overview]	Change From Baseline in PANSS Positive and Negative Subscale Scores Combined at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in PANSS Marder Hostility/Excitement Factor Score at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in PANSS Negative Subscale Score at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in PANSS Marder Positive Symptoms Factor Score at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in PANSS Marder Negative Symptoms Factor Score at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in PANSS Marder Disorganized Thoughts Factor Score at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in PANSS General Psychopathology Subscale Score at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in Clinical Global Impression of Severity (CGI-S) Score at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in PANSS Marder Anxiety/Depression Factor Score at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in Children's Global Assessment Scale (CGAS) Score at Day 56
NCT01190254 (19) [back to overview]	CGI-I Responders
NCT01190254 (19) [back to overview]	Clinical Global Impression of Improvement (CGI-I) Score at Day 56
NCT01190254 (19) [back to overview]	Total PANSS 30% Responders
NCT01190254 (19) [back to overview]	Kaplan-Meier Estimate of Cumulative Percentage of Participants With Total PANSS 30% Response at End of Study
NCT01190254 (19) [back to overview]	Kaplan-Meier Estimate of Cumulative Percentage of Participants With CGI-I Response at End of Study
NCT01190254 (19) [back to overview]	Change From Baseline in PQ-LES-Q Overall Score (i.e., Item 15) at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Total Score at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in Pediatric Quality of Life Enjoyment and Satisfaction Questionnaire (PQ-LES-Q) Total Score at Day 56
NCT01190254 (19) [back to overview]	Change From Baseline in PANSS Positive Subscale Score at Day 56
NCT01190267 (2) [back to overview]	Number of Participants Who Discontinued Study Drug During Extension Study Due to an AE
NCT01190267 (2) [back to overview]	Number of Participants With a Treatment-Emergent Adverse Event (AE) During Extension Study
NCT01206517 (4) [back to overview]	Area Under the Plasma Concentration-time Curve From 0 to 12 Hours Post Dose (AUC0-12) of Asenapine
NCT01206517 (4) [back to overview]	Maximum Plasma Concentration (Cmax) of Asenapine
NCT01206517 (4) [back to overview]	Time to Maximum Plasma Concentration (Tmax) of Asenapine
NCT01206517 (4) [back to overview]	Terminal Phase (Elimination) Half-life (t1/2) of Asenapine
NCT01244815 (17) [back to overview]	Change From Baseline in Children's Global Assessment Scale (CGAS) Score at Day 21
NCT01244815 (17) [back to overview]	Change From Baseline in Clinical Global Impression Scale for Use in Bipolar Disorder (CGI-BP) Overall Score at Day 21
NCT01244815 (17) [back to overview]	Change From Baseline in Pediatric Quality of Life Enjoyment and Satisfaction Questionnaire (PQ-LES-Q) Total Score at Day 21
NCT01244815 (17) [back to overview]	Change From Baseline in PQ-LES-Q Overall Score (i.e., Item 15) at Day 21
NCT01244815 (17) [back to overview]	Change From Baseline in Y-MRS Total Score at Day 21
NCT01244815 (17) [back to overview]	Total Y-MRS 50% Responders at Days 4, 7, 14 and 21
NCT01244815 (17) [back to overview]	Change From Baseline in CDRS-R Total Score at Day 14
NCT01244815 (17) [back to overview]	Change From Baseline in CDRS-R Total Score at Day 21
NCT01244815 (17) [back to overview]	Change From Baseline in CGI-BP Depression Score at Day 14
NCT01244815 (17) [back to overview]	Change From Baseline in CGI-BP Depression Score at Day 21
NCT01244815 (17) [back to overview]	Change From Baseline in CGI-BP Depression Score at Day 4
NCT01244815 (17) [back to overview]	Change From Baseline in CGI-BP Depression Score at Day 7
NCT01244815 (17) [back to overview]	Change From Baseline in CGI-BP Mania Score at Day 14
NCT01244815 (17) [back to overview]	Change From Baseline in CGI-BP Mania Score at Day 21
NCT01244815 (17) [back to overview]	Change From Baseline in CGI-BP Mania Score at Day 4
NCT01244815 (17) [back to overview]	Change From Baseline in CGI-BP Mania Score at Day 7
NCT01244815 (17) [back to overview]	Change From Baseline in Children's Depression Rating Scale, Revised (CDRS-R) Total Score at Day 7
NCT01244828 (9) [back to overview]	Change From Baseline in PANSS Total Score at Week 52
NCT01244828 (9) [back to overview]	Number of Participants With Extrapyramidal Symptoms
NCT01244828 (9) [back to overview]	Change From Baseline in Weight at Week 52
NCT01244828 (9) [back to overview]	Change From Baseline in Prolactin at Week 52
NCT01244828 (9) [back to overview]	Change From Baseline in PANSS Total Score at Final Assessment
NCT01244828 (9) [back to overview]	Change From Baseline in Insulin at Week 52
NCT01244828 (9) [back to overview]	Change From Baseline in HbA1c at Week 52
NCT01244828 (9) [back to overview]	Change From Baseline in BMI at Week 52
NCT01244828 (9) [back to overview]	Change From Baseline in Fasting Glucose at Week 52
NCT01349907 (16) [back to overview]	Percentage of Participants Who Were Y-MRS Total Score Remitters (Y-MRS ≤12)
NCT01349907 (16) [back to overview]	Percentage of Participants Who Were Y-MRS Total Score Responders
NCT01349907 (16) [back to overview]	Percentage of Participants With a CGAS Score of Equal or Greater Than 70
NCT01349907 (16) [back to overview]	Percentage of Participants With Emergent Depression Based on CDRS-R
NCT01349907 (16) [back to overview]	Percentage of CDRS-R Responders
NCT01349907 (16) [back to overview]	Change From Baseline in Children's Global Assessment Scale (CGAS)
NCT01349907 (16) [back to overview]	Change From Baseline in Children's Depression Rating Scale, Revised (CDRS-R) Total Score
NCT01349907 (16) [back to overview]	Time to First Total Y-MRS 50% Response
NCT01349907 (16) [back to overview]	Time to Failure to Maintain Response in Y-MRS Total Score
NCT01349907 (16) [back to overview]	Number of Participants Who Experienced Clinical or Laboratory Adverse Events
NCT01349907 (16) [back to overview]	Change From Baseline in Clinical Global Impression Scale for Assessing Depression (CGI-BP Depression)
NCT01349907 (16) [back to overview]	Change From Baseline in Clinical Global Impression Scale for Assessing Mania (CGI-BP Mania)
NCT01349907 (16) [back to overview]	Change From Baseline in Clinical Global Impression Scale for Assessing Overall Bipolar Illness (CGI-BP Overall)
NCT01349907 (16) [back to overview]	Change From Baseline in Pediatric Quality of Life Enjoyment and Satisfaction Questionnaires (PQ-LES-Q) Total Score
NCT01349907 (16) [back to overview]	Change From Baseline in PQ-LES-Q Overall Score
NCT01349907 (16) [back to overview]	Change From Baseline in Young Mania Rating Scale (Y-MRS) Total Score
NCT01400113 (1) [back to overview]	Positive and Negative Syndrome Scale - Excited Component
NCT01460290 (17) [back to overview]	Change in Cognitive Status as Measured by the Hopkins Verbal Learning Test (HVLT)
NCT01460290 (17) [back to overview]	Change in Cognitive Status as Measured by the Hopkins Verbal Learning Test (HVLT)
NCT01460290 (17) [back to overview]	Change in Cognitive Status as Measured by the Stroop Task
NCT01460290 (17) [back to overview]	Change in Depressive Symptoms as Measured by the Hamilton Depression Rating Scale (HAM-D)
NCT01460290 (17) [back to overview]	Change in Depressive Symptoms as Measured by the Montgomery Asberg Depression Rating Scale (MADRS)
NCT01460290 (17) [back to overview]	Change in Global Psychopathology as Measured by the Clinical Global Impression Scale for Use in Bipolar Illness (CGI-BP)
NCT01460290 (17) [back to overview]	Change in Perception of Mental Health as Measured by the Short Form General Health Survey (SF-12)
NCT01460290 (17) [back to overview]	Change in Perception of Physical Health as Measured by the Short Form General Health Survey (SF-12)
NCT01460290 (17) [back to overview]	World Health Organization Disability Assessment Scale (WHO-DAS)
NCT01460290 (17) [back to overview]	Change in Manic Symptoms as Measured by the Young Mania Rating Scale (YMRS)
NCT01460290 (17) [back to overview]	Change in Cognitive Status as Measured by the Trail Making Test
NCT01460290 (17) [back to overview]	Assessment of Motor Control Abnormality as Measured by the Simpson Angus Scale (SAS)
NCT01460290 (17) [back to overview]	Barnes Drug-induced Akathisia Rating Scale (BARS)
NCT01460290 (17) [back to overview]	Change in Bipolar Disorder Symptoms as Measured by the Brief Psychiatric Rating Scale (BPRS)
NCT01460290 (17) [back to overview]	Change in Cognitive Status as Measured by the Dementia Rating Scale (DRS)
NCT01460290 (17) [back to overview]	Change in Cognitive Status as Measured by the Hopkins Verbal Learning Test (HVLT)
NCT01460290 (17) [back to overview]	Change in Cognitive Status as Measured by the Hopkins Verbal Learning Test (HVLT)
NCT01549041 (2) [back to overview]	Patient Acceptance
NCT01549041 (2) [back to overview]	Change in Brief Psychiatric Rating Scale (BPRS) Total Score
NCT01587118 (2) [back to overview]	Change From Baseline in Brief Psychiatric Rating Scale (BPRS)
NCT01587118 (2) [back to overview]	Change From Baseline in Clinical Administered PTSD Scale (CAPS) Total
NCT01617187 (16) [back to overview]	Change From Baseline in Body Weight at Day 42
NCT01617187 (16) [back to overview]	Change From Baseline in PANSS Total Score at Day 42
NCT01617187 (16) [back to overview]	Percentage of Participants Who Are PANSS Responders (≥30% Reduction From Baseline in PANSS Total Score) at Day 42
NCT01617187 (16) [back to overview]	Change From Baseline in CGI-S Score at Days 4, 7, 14, 21, 28 and 35
NCT01617187 (16) [back to overview]	Change From Baseline in PANSS General Psychopathology Subscale Score at Days 4, 7, 14, 21, 28, 35 and 42
NCT01617187 (16) [back to overview]	Change From Baseline in PANSS Marder Factor Anxiety/Depression Symptom Score at Days 4, 7, 14, 21, 28, 35 and 42
NCT01617187 (16) [back to overview]	Change From Baseline in PANSS Marder Factor Disorganized Thought Symptom Score at Days 4, 7, 14, 21, 28, 35 and 42
NCT01617187 (16) [back to overview]	Change From Baseline in PANSS Marder Factor Negative Symptom Score at Days 4, 7, 14, 21, 28, 35 and 42
NCT01617187 (16) [back to overview]	Change From Baseline in PANSS Marder Factor Positive Symptom Score at Days 4, 7, 14, 21, 28, 35 and 42
NCT01617187 (16) [back to overview]	Change From Baseline in PANSS Negative Subscale Score at Days 4, 7, 14, 21, 28, 35 and 42
NCT01617187 (16) [back to overview]	Change From Baseline in PANSS Positive Subscale Score at Days 4, 7, 14, 21, 28, 35 and 42
NCT01617187 (16) [back to overview]	Change From Baseline in PANSS Total Score at Days 4, 7, 14, 21, 28 and 35
NCT01617187 (16) [back to overview]	Percentage of Participants Who Are Clinical Global Impression Scale-Improvement (CGI-I) Responders at Days 4, 7, 14, 21, 28, 35 and 42
NCT01617187 (16) [back to overview]	Percentage of Participants Who Are PANSS Responders (≥30% Reduction From Baseline in PANSS Total Score) at Days 4, 7, 14, 21, 28 and 35
NCT01617187 (16) [back to overview]	Change From Baseline in PANSS Marder Factor Hostility/Excitement Symptom Score at Days 4, 7, 14, 21, 28, 35 and 42
NCT01617187 (16) [back to overview]	Change From Baseline in CGI-S Score at Day 42
NCT01670019 (5) [back to overview]	Change in MADRS Total Score
NCT01670019 (5) [back to overview]	Clinical Remission Rate
NCT01670019 (5) [back to overview]	Clinical Response Rate
NCT01670019 (5) [back to overview]	Rates of Sustained Remission
NCT01670019 (5) [back to overview]	Study Completion Rate
NCT02876900 (2) [back to overview]	Evaluate Efficacy and Safety of Asenapine Maleate Patches Compared With Placebo Patches in Subjects Diagnosed With Schizophrenia as Measured Using the Syndrome Scale (PANSS) Total Score: Change From Baseline to Week 6.
NCT02876900 (2) [back to overview]	Evaluate Efficacy and Safety of Asenapine Maleate Patches Compared With Placebo Patches in Subjects Diagnosed With Schizophrenia as Measured Using the Clinical Global Impression - Severity of Illness Scale: Change From Baseline to Week 6.

Number of Participants Achieving Young-Mania Rating Scale (Y-MRS) Responder Status

The Y-MRS is a clinician-rated instrument used for assessing the symptoms of mania, composed of 11 items. For the 11 items, scores range from 0 (symptoms absent) to, depending on the item, either 4 (7 items) or 8 (4 items). Scores for individual items add to a total score (range: 0-60), with higher scores indicating greater symptom severity. At pre-specified time points, the number of participants achieving Y-MRS responder status was assessed, defined as the number of participants with a 50% decrease from baseline in Y-MRS total score. For evaluation of this endpoint, a LOCF analysis was used; baseline values are not eligible to be carried forward to missing post-baseline assessments. (NCT00145470)
Timeframe: Up to Day 84

Intervention	Participants (Count of Participants)
	Day 3	Day 7	Day 14	Day 21	Day 42	Day 63	Day 84
Asenapine	13	22	46	53	67	66	74
Placebo	10	25	34	44	52	52	56

Intervention	Score on a Scale (Least Squares Mean)
	PCS - Baseline	PCS - Change from Baseline at Day 21	MCS - Baseline	MCS - Change from Baseline at Day 21
Asenapine	51.64	-2.47	39.03	5.93
Placebo	50.49	-0.72	40.83	2.29

Intervention	Score on a Scale (Least Squares Mean)
	PCS - Baseline	PCS - Change from Baseline at Day 84	MCS - Baseline	MCS - Change from Baseline at Day 84
Asenapine	51.64	-0.95	39.03	2.49
Placebo	50.49	1.37	40.83	-1.05

Intervention	Score on a Scale (Least Squares Mean)
	Baseline	Change from Baseline at Day 21
Asenapine	2.3	-0.2
Placebo	2.3	-0.1

Intervention	Score on a Scale (Least Squares Mean)
	Baseline	Change from Baseline at Day 84
Asenapine	2.3	-0.1
Placebo	2.3	-0.1

Intervention	Score on a Scale (Least Squares Mean)
	Baseline	Change from Baseline at Day 42
Asenapine	27.9	-11.4
Placebo	28.2	-8.7

Intervention	Score on a Scale (Mean)
	Verbal Memory - Baseline	Visual Memory - Baseline	Processing Speed - Baseline	Social Acuity - Baseline	Reasoning - Baseline	Executive Functioning - Baseline	Working Memory - Baseline	Sustained Attention - Baseline	Composite Memory - Baseline	Verbal Memory - CFB at Day 21	Visual Memory - CFB at Day 21	Processing Speed - CFB at Day 21	Social Acuity - CFB at Day 21	Reasoning - CFB at Day 21	Executive Functioning - CFB at Day 21	Working Memory - CFB at Day 21	Sustained Attention - CFB at Day 21	Composite Memory - CFB at Day 21
Asenapine	44.6	38.2	39.5	2.7	1.3	16.9	2.9	13.5	82.8	0.8	-0.4	4.2	0.3	0.7	10.1	-0.4	-0.8	0.5
Placebo	43.6	38.0	34.3	2.8	2.1	17.6	2.9	14.0	81.6	-0.8	-0.3	3.8	1.0	0.3	4.4	0.2	0.3	-1.1

Intervention	kg (Mean)
	Baseline	Change From Baseline at Day 182
Asenapine	84.2	0.0
Olanzapine	84.7	2.6

Intervention	participants (Number)
	Days 1 - 7 (N asenapine = 191; N placebo = 191)	Days 8 - 14 (N asenapine = 190; N placebo = 189)	Days 15 - 21 (N asenapine = 184; N placebo = 175)	Days 22 - 28 (N asenapine = 181; N placebo = 165)	Days 29 - 35 (N asenapine = 176; N placebo = 154)	Days 36 - 42 (N asenapine = 176; N placebo = 143)	Days 43 - 49 (N asenapine = 173; N placebo = 136)	Days 50 - 56 (N asenapine = 166; N placebo = 129)	Days 57 - 63 (N asenapine = 166; N placebo = 126)	Days 64 - 70 (N asenapine = 163; N placebo = 122)	Days 71 - 77 (N asenapine = 162; N placebo = 120)	Days 78 - 84 (N asenapine = 162; N placebo = 116)	Days 85 - 91 (N asenapine = 158; N placebo = 113)	Days 92 - 98 (N asenapine = 153; N placebo = 105)	Days 99 - 105 (N asenapine = 150; N placebo = 100)	Days 106 - 112 (N asenapine = 150; N placebo = 98)	Days 113 - 119 (N asenapine = 149; N placebo = 97)	Days 120 - 126 (N asenapine = 148; N placebo = 88)	Days 127 - 133 (N asenapine = 148; N placebo = 87)	Days 134 - 140 (N asenapine = 146; N placebo = 86)	Days 141 - 147 (N asenapine = 145; N placebo = 84)	Days 148 - 154 (N asenapine = 142; N placebo = 82)	Days 155 - 161 (N asenapine = 141; N placebo = 78)	Days 162 - 168 (N asenapine = 139; N placebo = 75)	Days 169 - 175 (N asenapine = 137; N placebo = 73)	Days 176 - 182 (N asenapine = 135; N placebo = 71)	Days 183 - 189 (N asenapine = 75; N placebo = 39)	Days 190 - 196 (N asenapine = 9; N placebo = 9)	Days 197 - 203 (N asenapine = 2; N placebo = 2)	Days 204 - 210 (N asenapine = 0; N placebo = 1)
Asenapine	1	6	3	5	0	3	7	0	3	1	0	4	5	2	0	1	1	0	2	0	3	1	1	2	2	0	0	0	0	0
Placebo	2	14	10	11	11	7	7	3	4	2	4	3	8	4	2	1	8	1	0	1	1	3	3	1	1	1	0	0	0	0

Intervention	relapses (Number)
	Days 1 - 7 (N asenapine = 190; N placebo = 190)	Days 8 - 14 (N asenapine = 188; N placebo = 186)	Days 15 - 21 (N asenapine = 183; N placebo = 170)	Days 22 - 28 (N asenapine = 180; N placebo = 160)	Days 29 - 35 (N asenapine = 175; N placebo = 149)	Days 36 - 42 (N asenapine = 175; N placebo = 140)	Days 43 - 49 (N asenapine = 173; N placebo = 130)	Days 50 - 56 (N asenapine = 166; N placebo = 127)	Days 57 - 63 (N asenapine = 165; N placebo = 123)	Days 64 - 70 (N asenapine = 163; N placebo = 120)	Days 71 - 77 (N asenapine = 161; N placebo = 117)	Days 78 - 84 (N asenapine = 160; N placebo = 113)	Days 85 - 91 (N asenapine = 158; N placebo = 110)	Days 92 - 98 (N asenapine = 154; N placebo = 104)	Days 99 - 105 (N asenapine = 151; N placebo = 99)	Days 106 - 112 (N asenapine = 151; N placebo = 96)	Days 113 - 119 (N asenapine = 149; N placebo = 95)	Days 120 - 126 (N asenapine = 147; N placebo = 87)	Days 127 - 133 (N asenapine = 147; N placebo = 86)	Days 134 - 140 (N asenapine = 146; N placebo = 84)	Days 141 - 147 (N asenapine = 145; N placebo = 83)	Days 148 - 154 (N asenapine = 142; N placebo = 81)	Days 155 - 161 (N asenapine = 141; N placebo = 75)	Days 162 - 168 (N asenapine = 139; N placebo = 74)	Days 169 - 175 (N asenapine = 137; N placebo = 72)	Days 176 - 182 (N asenapine = 135; N placebo = 70)	Days 183 - 189 (N asenapine = 75; N placebo = 39)	Days 190 - 196 (N asenapine = 9; N placebo = 9)	Days 197 - 203 (N asenapine = 2; N placebo = 2)	Days 204 - 210 (N asenapine = 0; N placebo = 1)
Asenapine	0	1	2	2	0	1	5	1	1	2	1	2	0	0	0	0	2	0	0	0	0	0	0	1	2	0	0	0	0	0
Placebo	3	14	9	8	7	8	2	4	1	3	4	2	4	4	2	1	3	1	1	0	1	5	1	0	1	1	0	0	0	0

Intervention	Participants (Number)
	<=Week 1	>Week 1 to Week 2	>Week 2 to Week 4	>Week 4 to Week 8	>Week 8 to Week 12	>Week 12 to Week 16	>Week 16 to Week 20	>Week 20 to Week 24	>Week 24 to Week 28	>Week 28 to Week 32	>Week 32 to Week 36	>Week 36 to Week 40	>Week 40 to Week 44	>Week 44 to Week 48	>Week 48 to Week 52
Asenapine/Asenapine	15	4	14	3	1	1	1	3	1	3	0	0	0	0	5
Haloperidol/Haloperidol	6	4	3	1	1	4	1	0	0	1	0	1	0	0	2
Placebo/Asenapine	7	3	1	3	2	3	0	0	0	1	0	0	0	0	2

Intervention	Centimeters (cm) (Mean)
	Baseline	Change from baseline to Week 40 or endpoint
Asenapine	86.8	2.6
Olanzapine	89.4	5.0
Placebo/Asenapine	91.1	3.0

Intervention	Participants (Number)
	Biochemistry	Metabolic chemistry	Endocrinology/miscellaneous	Hematology
Asenapine	76	32	35	90
Olanzapine	115	96	39	83
Placebo/Asenapine	25	17	7	22

Intervention	Participants (Number)
	Sinus bradycardia	Bundle branch block right	ECG QRS complex prolonged	ECG ST segment depression	ECG T wave inversion	Supraventricular extrasystoles	Ventricular extrasystoles
Asenapine	2	1	0	0	0	0	0
Olanzapine	0	0	1	1	1	1	1
Placebo/Asenapine	0	0	0	0	0	0	0

Intervention	Units on a scale (Mean)
	AIMS	BARS	SARS
Asenapine	0.1	0.2	0.2
Olanzapine	0.0	0.1	0.3
Placebo/Asenapine	0.4	0.4	0.6

Intervention	Participants (Number)
	Participants with no concomitant medications	Participants with >=1 concomitant medication
Asenapine	21	58
Olanzapine	31	76
Placebo/Asenapine	10	22

Intervention	Units on a Scale (Least Squares Mean)
	Baseline	Change from Baseline at Day 365
Asenapine	45.3	12.4
Olanzapine	42.3	11.7

Intervention	Participants (Number)
Asenapine 2-10 mg Twice Daily (BID)	44
Asenapine 5-10 mg BID	44

Intervention	Score on a scale (Least Squares Mean)
	Day 2	Day 4	Day 7	Day 14
Asenapine 10 mg BID	-0.4	-0.7	-1.1	-1.3
Asenapine 5 mg BID	-0.5	-0.8	-1.0	-1.3
Placebo BID	-0.2	-0.4	-0.7	-1.0

Intervention	Score on a scale (Least Squares Mean)
	Day 7 (n=112,106, 117)	Day 21 (n =115, 110,123)
Asenapine 10 mg BID	-4.2	-5.1
Asenapine 5 mg BID	-4.3	-4.6
Placebo BID	-2.3	-2.5

Intervention	Percentage of participants (Number)
	Day 2 (n = 117,111,123)	Day 4 (n = 120,113,126)	Day 7 (n = 120,113,126)	Day 14 (n = 120,113,126)
Asenapine 10 mg BID	14.4	23.0	28.3	40.7
Asenapine 5 mg BID	12.0	21.7	31.7	36.7
Placebo BID	8.9	8.7	19.8	33.3

asenapine

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Biological Processes (46)

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Bioassays (16)

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Studies (256)

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Research Demand Index: 74.45

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Clinical Trials (50)

Trial Overview

Trial Outcomes

Number of Participants Achieving Young-Mania Rating Scale (Y-MRS) Responder Status

Number of Participants Achieving Young-Mania Rating Scale (Y-MRS) Remitter Status

Number of Participants Discontinuing Study Treatment Due to an AE

Number of Participants Experiencing an Adverse Event (AE)

Percentage of Participants Determined to be Ready to Discharge at Day 84 (Kaplan-Meier Estimation)

Least Squares Mean Change From Baseline at Day 21 in Quality of Life as Determined by Short Form-36 Version 2 (SF-36v2)

Least Squares Mean Change From Baseline at Day 84 in Quality of Life as Determined by Short Form-36 Version 2 (SF-36v2)

Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Depression Score at Day 21

Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Depression Score at Day 84

Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Mania Score at Day 21

Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Mania Score at Day 84

Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Overall Bipolar Illness Score at Day 21

Least Squares Mean Change From Baseline in Clinical Global Impressions for Use in Bipolar Disorder (CGI-BP) Severity of Overall Bipolar Illness Score at Day 84

Least Squares Mean Change From Baseline in Hamilton Anxiety Rating Scale (HAM-A) Score at Day 21

Least Squares Mean Change From Baseline in Hamilton Anxiety Rating Scale (HAM-A) Score at Day 84

Least Squares Mean Change From Baseline in InterSePT Scale for Suicidal Thinking - Modified Version (ISST-Modified) Score at Day 21

Least Squares Mean Change From Baseline in InterSePT Scale for Suicidal Thinking - Modified Version (ISST-Modified) Score at Day 84

Least Squares Mean Change From Baseline in Montgomery Asberg Depression Rating Scale (MADRS) Score at Day 21

Least Squares Mean Change From Baseline in Montgomery Asberg Depression Rating Scale (MADRS) Score at Day 84

Least Squares Mean Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Score at Day 21

Least Squares Mean Change From Baseline in Positive and Negative Syndrome Scale (PANSS) Score at Day 84

Least Squares Mean Change From Baseline in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q), General Activities Subscale Score at Day 21

Least Squares Mean Change From Baseline in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q), General Activities Subscale Score at Day 84

Least Squares Mean Change From Baseline in Young-Mania Rating Scale (Y-MRS) Score at Day 21

Least Squares Mean Change From Baseline in Young-Mania Rating Scale (Y-MRS) Score at Day 42

Least Squares Mean Change From Baseline in Young-Mania Rating Scale (Y-MRS) Score at Day 84

Mean Change From Baseline (CFB) at Day 21 in Neurocognitive Function as Determined by Central Nervous System Vital Signs (CNS-VS) Test Battery

Mean Change From Baseline (CFB) at Day 84 in Neurocognitive Function as Determined by Central Nervous System Vital Signs (CNS-VS) Test Battery

Change From Baseline in Body Weight

Change From Baseline in Negative Symptoms of Schizophrenia Measured by the Negative Symptom Assessment (NSA) Scale Total Score

Change From Baseline in Quality of Life Measured by the Quality of Life Scale (QLS) Total Score

Change From Baseline to Week 52 on the Montgomery Asberg Depression Rating Scale (MADRS) Score

Change From Baseline to Week 52 on the Young-Mania Rating Scale (Y-MRS) Score

Number of Participants Who Discontinued Because of an Adverse Event

Number of Participants Who Experienced an Adverse Event

Time to Early Discontinuation for Any Reason

Time to Relapse or an Impending Relapse

Loss of Effect Over Time

Median Survival Time of Effect

Abdominal Girth

Number of Participants With Laboratory Values Outside Normal Range

Participants Who Experienced Adverse Event(s)

Number of Participants With Markedly Abnormal Vital Sign Changes

Number of Participants With Abnormal Physical Examination Findings

Number of Participants With Abnormal Electrocardiogram

Extrapyramidal Symptoms [EPS]

Concomitant Medications

Body Weight

Change From Baseline in Quality of Life Measured by the Quality of Life Scale (QLS) Total Score

Change From Baseline in Negative Symptoms of Schizophrenia Measured by the Negative Symptom Assessment (NSA) Scale Total Score

Long-term Change in Negative Symptoms of Schizophrenia Measured by the Negative Symptom Assessment (NSA) Scale

Intervention	Score on a scale (Least Squares Mean)
	Day 2 (n=118,111,122)	Day 4 (n=120,113,125)	Day 7 (n=120,113,125)	Day 14 (n=120,113,125)	Day 21 (n=120,113,125)
Asenapine 10 mg BID	-0.2	-0.3	-0.4	-0.5	-0.5
Asenapine 5 mg BID	-0.2	-0.3	-0.3	-0.4	-0.4
Placebo BID	-0.2	-0.3	-0.1	-0.2	-0.1

Intervention	Percentage of participants (Number)
	Day 2 (n=113, 103, 116)	Day 4 (n=116, 106, 119)	Day 7 (n=117, 106, 119)	Day 14 (n=117, 106, 120)	Day 21 (n=117, 106, 121)
Asenapine 10 mg BID	28.2	32.1	35.8	42.5	44.3
Asenapine 5 mg BID	21.2	26.7	31.6	31.6	32.5
Placebo BID	11.2	19.3	23.5	26.7	28.9

Intervention	Percentage of participants (Number)
	Day 2 (n=118,111,123)	Day 4 (n=120,113,126)	Day 7 (n=120,113,126)	Day 14 (n=120,113,126)	Day 21 (n=120,113,126)
Asenapine 10 mg BID	45.9	64.6	78.8	83.2	82.3
Asenapine 5 mg BID	50.8	64.2	73.3	70.8	74.2
Placebo BID	37.4	55.6	61.1	65.1	64.3

Intervention	Percentage of participants (Number)
	Day 2 (n= 117,111, 123)	Day 4 (n= 104, 106,118)	Day 7 (n= 104, 101,110)	Day 14 (n= 96, 91,102)	Day 21 (n= 86, 83,93)
Asenapine 10 mg BID	11.7	15.1	24.8	27.5	43.4
Asenapine 5 mg BID	8.5	17.3	26.9	28.1	40.7
Placebo BID	5.7	10.2	17.3	24.5	34.4

Intervention	Score on a scale (Least Squares Mean)
Asenapine 5 mg BID	-1.6
Asenapine 10 mg BID	-1.7
Placebo BID	-1.1

Intervention	Score on a scale (Least Squares Mean)
Asenapine 5 mg BID	-14.4
Asenapine 10 mg BID	-14.9
Placebo BID	-10.9

Intervention	Percentage of participants (Number)
Asenapine 5 mg BID	34.2
Asenapine 10 mg BID	38.1
Placebo BID	30.2

Intervention	Percentage of participants (Number)
Asenapine 5 mg BID	45.0
Asenapine 10 mg BID	46.9
Placebo BID	39.7

Intervention	mU/L (Least Squares Mean)
Healthy Lifestyle Information	0.74
Switch Treatment + Healthy Lifestyle Instruction	0.42
Metformin Treatment + Healthy Lifestyle Instruction	-0.34

Intervention	mg/dL (Least Squares Mean)
Healthy Lifestyle Information	3.6
Switch Treatment + Healthy Lifestyle Instruction	-8.1
Metformin Treatment + Healthy Lifestyle Instruction	-4.1