Drug intelligence / Profile preview

lomitapide + dextromethorphan

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

Overview

Lomitapide + dextromethorphan refers to a theoretical or proposed combination of two small molecule drugs: lomitapide, a microsomal triglyceride transfer protein (MTP) inhibitor used primarily for the treatment of homozygous familial hypercholesterolemia (HoFH), and dextromethorphan, a cough suppressant and central nervous system agent with activity as a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist and sigma-1 receptor agonist. No approved combination product containing these two agents is currently known or described in the scientific or regulatory literature. Lomitapide reduces LDL cholesterol by inhibiting MTP and thus the synthesis of very low-density lipoprotein (VLDL), while dextromethorphan has roles in cough suppression and novel antidepressant combinations via NMDA antagonism and monoamine reuptake inhibition.

02

Targets

SERT (Sodium-dependent serotonin transporter)SIGMAR1 (Sigma non-opioid intracellular receptor 1)NMDAR (Glutamate receptor ionotropic, NMDA)MTTP (Microsomal triglyceride transfer protein large subunit)NET (Norepinephrine Transporter)

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