Drug intelligence / Profile preview

aprepitant + gabapentin

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

Overview

Aprepitant + gabapentin is a non-fixed-dose combination of two pharmaceutical agents, each with distinct mechanisms of action. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors, used primarily as an antiemetic to prevent acute and delayed nausea and vomiting associated with chemotherapy or surgery. Gabapentin is a gamma aminobutyric acid (GABA) analogue classified as an anticonvulsant; it reduces neuronal excitability and is used to treat partial seizures, postherpetic neuralgia, and restless legs syndrome. The combination has been studied in clinical trials for the prevention of refractory nausea and vomiting, particularly in oncology settings[2][4][5][6].

02

Targets

CACNA2D2 (α2δ-2)TACR1 (Neurokinin‑1 Receptor)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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