Olanzapine is an antipsychotic drug used in the management of schizophrenia, bipolar 1 disorder, and agitation associated with these disorders. Olanzapine is a thienobenzodiazepine derivative and an atypical or second-generation antipsychotic agent.
- Mechanism
- Curator reviewed · 4 references
The activity of olanzapine is achieved by the antagonism of multiple neuronal receptors including the dopamine receptor D1, D2, D3 and D4 in the brain, the serotonin receptors 5HT2A, 5HT2C, 5HT3 and 5HT6, the alpha-1 adrenergic receptor, the histamine receptor H1 and multiple muscarinic receptors.
As abovementioned, olanzapine presents a wide profile of targets, however, its antagonistic effect towards the dopamine D2 receptor in the mesolimbic pathway is key as it blocks dopamine from having a potential action at the post-synaptic receptor. The binding of olanzapine to the dopamine D2 receptors is easily dissociable and hence, it allows for a certain degree of dopamine neurotransmission.
On the other hand, olanzapine acts in the serotonin 5HT2A receptors in the frontal cortex in a similar manner than the reported on dopamine D2 receptors. This determined effect allows for a decrease in adverse effects.
- Primary indication
- Olanzapine was initially used orally and intramuscularly for the chronic treatment of schizophrenia in patients over 13 years old and other psychiatric disorders such as bipolar I disorder including mixed or manic episodes.Curator reviewed · 14 structured indications
- Formula / weight
- C17H20N4S · 312.432 g/mol (avg)
- First approval
- Canada, 2007 · United States, 1996 · European Union, 2016
- Also known as
- Olanzapin
- Code names
- LY-170053 · TV-44749
- Brand names
Resolves to
KVWDHTXUZHCGIO-UHFFFAOYSA-NSMILESCN1CCN(CC1)C1=NC2=CC=CC=C2NC2=C1C=C(C)S2What you can answer from here — as of September 23, 2026
Which drugs share a target with Olanzapine, and which of those have an active Phase 3 trial?
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