Asenapine is a second-generation atypical antipsychotic drug with demonstrated efficacy in the treatment of mania associated with bipolar I disorder. |
Asenapine was also effective in the treatment of mixed states in patients with bipolar I disorder, as defined by the Diagnostic and Statistical Manual of Mental Disorders (DSM), 4th Edition, Text Revision, or major depressive disorder with mixed features, as defined by DSM-5. |
Several pharmacoeconomic studies have shown that asenapine is likely to be associated with lower healthcare costs and higher quality of life. |
1 Introduction
2 Pharmacokinetics
3 Pharmacodynamics
4 Therapeutic Efficacy
4.1 Randomised Controlled Trials and Extension Studies
Publication Length of observational period Source of funding | Treatment (N) | YMRS | CGI-BP | MADRS [mean (SD)] | ||||
---|---|---|---|---|---|---|---|---|
Reduction in total score Mean (SD) | Rate of response (%) | Rate of remission (%) | Overall severity Mean (SD) | Mania [mean (SD)] | Depression [mean (SD)] | |||
Adults
| ||||||||
McIntyre et al. [22] 3 weeks Schering-Plough, Pfizer Inc. | ASE flexible dose bid (189) | − 10.8 (0.8)a,c*** − 13.1 (0.8)b,c*** | 42.3** | 40.2** | − 1.2 (0.1)a,c** − 1.5 (0.1)b,c** | − 3.2 (0.5)a,c
| ||
OLA flexible dose bid (188) | − 12.6 (0.8)a,c*** − 13.9 (0.8)b,c*** | 50.0*** | 39.4* | − 1.4 (0.1)a,c*** − 1.6 (0.1)b,c** | − 4.2 (0.5)a,c** | |||
PBO (103) | − 5.5 (1.0)a,c
− 7.4 (1.1)b,c
| 25.2 | 22.3 | − 0.7 (0.13)a,c
− 1.0 (0.2)b,c
| − 1.8 (0.7)a,c
| |||
McIntyre et al. [23] 3 weeks Merck, Pfizer Inc. | ASE flexible dose bid (183) | − 11.5 (0.8)a,c**††
− 14.2 (0.9)b,c* | 42.6 | 35.5 | − 1.2 (0.10)a,c*†
− 1.6 (0.11)b,c** | − 3.0 (0.4)a,c
| ||
OLA flexible dose bid (203) | − 14.6 (0.8)a,c*** − 16.1 (0.8)b,c*** | 54.7** | 46.3* | − 1.5 (0.09)a,c*** − 1.7 (0.09)b,c*** | -4.1 (0.4)a,c** | |||
PBO (94) | − 7.8 (0.8)a
− 10.8 (1.2)b,c
| 34 | 30.9 | − 0.8 (0.13)a,c
− 1.1 (0.15)b,c
| -1.9 (0.6)a,c
| |||
McIntyre et al. [33] 9 weeks Schering-Plough, Pfizer Inc. | ASE flexible dose bid (175) | − 27.3 (0.64) | 77†
| 75†
| − 2.6 (0.12)c†
| − 2.9 (0.11)c†
| − 0.1 (0.09)c* | − 3.6 (0.69)c* |
OLA flexible dose bid (222) | − 23.7 (0.55) | 82 | 79 | − 2.4 (0.10)c
| − 2.8 (0.09)c
| 0.0 (0.08)c
| − 2.4 (0.61)c
| |
McIntyre et al. [34] 40 weeks Schering-Plough (now Merck & Co. Inc.), Pfizer Inc. | ASE flexible dose bid (76) | − 25.8 (10.3) | 93.4 | 93.4 | − 3.2 (1.3) | − 4.8 (6.5) | ||
OLA flexible dose bid (107) | − 26.1 (8.4) | 95.2 | 95.2 | − 3.2 (1.1) | − 3.2 (8.6) | |||
Landbloom et al. [24] 3 weeks Merck & Co. Inc. | ASE 5 mg bid (120) | − 14.4* | 45.0 | 40.7 | − 1.6 (0.12)c* | − 5.8 (0.71)c** | ||
ASE 10 mg bid (113) | − 14.9** | 46.9 | 43.4 | − 1.7 (0.12)c** | − 5.9 (0.73)c** | |||
PBO (126) | − 10.9 | 39.7 | 34.4 | − 1.1 (0.11)c
| − 3.2 (0.70)c
| |||
Ketter et al. [25] 26 weeks Forest Research Institute Inc. (an Allergan affiliate), Merck & Co Inc. | ASE 5 mg bid/ASE 5 mg bid (120) | − 22.9 | 44 | 43 | − 2.4 | |||
ASE 10 mg bid/ASE 10 mg bid (113) | − 22.0 | 42 | 34 | − 2.3 | ||||
PBO/ASE 5 mg bid (126) | − 22.3 | 50 | 44 | − 2.3 | ||||
Szegedi et al. [26] 3 weeks Merck, Pfizer Inc. | LI or VAL + ASE flexible dose bid (158) | − 10.3 (0.8)* | 34.2 | 33.5* | − 1.0 (0.09)** | − 1.1 (0.10)** | ||
LI or VAL + PBO (166) | − 7.9 (0.8) | 27.0 | 21.5 | − 0.7 (0.09) | − 0.8 (0.09) | |||
Szegedi et al. [26] 12 weeks Merck, Pfizer Inc. | LI or VAL + ASE flexible dose bid (158) | − 12.7 (0.9)** | 47.7* | 43.2* | − 1.2 (0.11)* | − 1.5 (0.12)*** | ||
LI or VAL + PBO (166) | − 9.3 (0.9) | 34.4 | 30.1 | − 0.8 (0.11) | − 1.0 (0.11) | |||
Paediatric patients
| ||||||||
Findling et al. [27] 3 weeks Merck & Co. Inc. | ASE 2.5 mg bid (101) | − 12.8*** | 42* | –0.6 (− 0.9, − 0.3)d*** | ||||
ASE 5 mg bid (98) | − 14.9*** | 54*** | –0.7 (− 0.9, − 0.4)d*** | |||||
ASE 10 mg bid (98) | − 15.8*** | 52*** | –0.7 (− 1.0, − 0.4)d*** | |||||
PBO (98) | 9.6 | 28 | ||||||
Findling et al. [28] 26 weeks Merck & Co. Inc., Allergan Inc. | ASE flexible dose bid (321) | − 6.9 | 50 | 68.5 |