Drug intelligence / Profile preview

aprepitant + olanzapine

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

A combination of aprepitant (a neurokinin-1 receptor antagonist) and olanzapine (an atypical antipsychotic) used for the prevention of chemotherapy-induced nausea and vomiting (CINV), particularly in patients receiving highly or moderately emetogenic chemotherapy regimens. This combination is typically administered with other antiemetics such as palonosetron and dexamethasone as a four-drug regimen for enhanced antiemetic efficacy. Aprepitant blocks substance P binding to NK1 receptors, while olanzapine blocks multiple neurotransmitters, including dopamine, serotonin, catecholamines, histamine, and acetylcholine in the central nervous system. Multiple studies have shown this combination provides superior control of CINV compared to standard regimens without olanzapine. It is generally well-tolerated, with common side effects being sedation and fatigue associated with olanzapine.

02

Targets

DRD4 (Dopamine D4 Receptor)HTR2A (Serotonin receptor 5-HT2A)CHRM5 (M5)HTR2C (5-hydroxytryptamine 2C receptor)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)HTR3A (5-hydroxytryptamine receptor 3A)TACR1 (Neurokinin‑1 Receptor)CHRM2 (M2)DRD1 (Dopamine D1 Receptor)ADRA1A (α1A)CHRM4 (M4)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)HTR6 (5-hydroxytryptamine receptor 6)CHRM3 (M3)

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