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emopamil
- Development stage
- Unknown
- Lead developer
- BASF
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral (investigational/experimental)
01
Overview
Emopamil is a small molecule phenylalkylamine calcium channel antagonist and P-glycoprotein (P-gp) inhibitor. It has been studied for its ability to prevent renal injury after warm and cold ischemia and can reduce ischemia-induced neuronal cell damage. Emopamil also reverses multidrug resistance in certain cancer cell lines by inhibiting P-glycoprotein. Mechanistically, it acts as a calcium channel blocker and binds with high affinity to the emopamil binding protein (EBP), which is involved in cholesterol biosynthesis as a Δ8–Δ7 sterol isomerase. The drug has optically active stereoisomers; the racemic mixture and (-)-enantiomer are pharmacologically active while the (+)-enantiomer is not effective. Emopamil reached up to Phase II clinical trials but development appears discontinued[1][2][3][4].
- Other names
- emopamiloemopamilum2-isopropyl-5-(methyl-(2-phenylethyl)amino)-2-phenylpentanenitrile
02
Targets
EBP (Sterol isomerase (emopamil-binding protein))ABCB1 (P-glycoprotein)SIGMAR1 (Sigma non-opioid intracellular receptor 1)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)
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