Organon & Co. โ Sycrest EMA EPAR public assessment report (EMEA/H/C/001177, 2010)
Organon & Co. ยท 2010 ยท EMA EPAR public assessment report ยท company profile โ
Report summary
The EMA's assessment of Sycrest (asenapine) revealed a complex profile. Preclinical studies detailed its receptor binding, antipsychotic activity, and safety, highlighting low oral bioavailability. Clinical trials for schizophrenia showed inconsistent and often statistically insignificant efficacy compared to placebo, and inferiority to olanzapine, leading to a negative benefit-risk balance for this indication. For bipolar I disorder, however, asenapine demonstrated statistically significant improvements in manic symptoms compared to placebo. While safety concerns included extrapyramidal symptoms and other adverse events, the CHMP recommended marketing authorization for moderate to severe manic episodes in adults, contingent on a post-approval dose-finding study.
Key findings โ cited to the page
| Asenapine antagonism at H1 receptors (pKB) | 8.4 | ยท p.11 |
| Asenapine ED50 for 5-HT2A receptor occupancy | 0.005 mg/kg, subcutaneous | ยท p.11 |
| Asenapine ED50 for 5-HT2C receptor occupancy | 0.02 mg/kg, subcutaneous | ยท p.11 |
| Asenapine ED50 for ฮฑ1 receptor occupancy | 0.077 mg/kg, subcutaneous | ยท p.11 |
| Asenapine ED50 for D2 receptor occupancy | 0.1 mg/kg, subcutaneous | ยท p.11 |
| Asenapine ED50 for H1 receptor occupancy | 0.11 mg/kg, subcutaneous | ยท p.11 |
| Post-approval commitment for dose finding study | yes | Sycrest (asenapine) ยท p.87 |
| CHMP recommendation for Sycrest in bipolar I disorder | granting of the marketing authorisation | Sycrest (asenapine) ยท p.88 |
| Application submission date | 05 May 2009 | Sycrest ยท European Union ยท p.3 |
| Procedure start date | 27 May 2009 | Sycrest ยท European Union ยท p.4 |
| CHMP positive opinion date | 24 June 2010 | Sycrest ยท European Union ยท p.4 |
| Asenapine antagonism at ฮฑ2C receptors (pKB) | 6.8 | ยท p.11 |
Source: Organon & Co. โ ยท License: EMA - reuse permitted with acknowledgement. Summary and findings are extracted from the published document; every figure cites its page. Informational only โ not investment advice. Explore the Psychiatry library โ