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Zyprexa (Oral and IM)
Eli Lilly & Company
Drug Names(s): LY170053, olanzapine, olazepine, Zydis
Description: Zyprexa (Olanzapine), a thienobenzodiazepine, is similar in chemical structure and in mechanism of action to Clozapine (Clozaril). It is an atypical antipsychotic drug with a higher affinity for the serotonin 5-HT2 receptor relative to its affinity for the dopamine D-2 receptor. Though the exact mechanism is unclear (either due to a difference in affinities for such receptors or fast dissociation from the D-2 receptor), atypical antipsychotics are able to produce an antipsychotic effect (through blockade of D-2 receptors in the ventral striatum) with fewer extrapyramidal motor function side effects (or EPSs, which are caused by blockade of D-2 receptors in the dorsal striatum).
Zyprexa is an antagonist with high affinity binding to the following receptors: serotonin 5HT2A (3.5 nM), 5HT2C (14 nM), 5HT6, dopamine D1 (31 nM), dopamine D2 (11 nM), Dopamine D3, Dopamine D4 (9.6 nM), histamine H1 (0.6 nM), and adrenergic a1 (19 nM)receptors. It isan antagonist with moderate affinity binding for serotonin 5HT3 and muscarinic M1-5. Olanzapine binds weakly to GABAA, BZD, andß adrenergic receptors.
Deal Structure: Lilly pays a de minimis royalty for the Zydis formulation.
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