Drug intelligence / Profile preview

Olanzapine + fosaprepitant

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Olanzapine + fosaprepitant is a combination of two pharmaceutical agents used primarily for the prevention of chemotherapy-induced nausea and vomiting (CINV). Olanzapine is an atypical antipsychotic that acts as an antagonist at multiple neuronal receptors, including dopamine D1-D4, serotonin 5HT2A/2C/3/6, alpha-1 adrenergic, histamine H1, and muscarinic receptors. Its antiemetic effect is mainly attributed to antagonism at dopamine and serotonin receptors in the central nervous system[6]. Fosaprepitant is a prodrug of aprepitant and functions as a neurokinin-1 (NK1) receptor antagonist; it blocks substance P from binding to NK1 receptors in the brainstem emetic center, thereby reducing both acute and delayed phases of chemotherapy-induced emesis[3][5]. This combination has been studied for its efficacy in preventing CINV in patients receiving highly or moderately emetogenic chemotherapy regimens[4][8].

02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)TACR1 (Neurokinin‑1 Receptor)DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)HTR6 (5-hydroxytryptamine receptor 6)

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