Efonidipine is a dihydropyridine calcium-channel blocker used primarily in the management of hypertension. It is a long-acting calcium-channel antagonist with activity against both L-type and T-type calcium channels. Efonidipine has the molecular formula C34H38N3O7P, molecular weight of approximately 631.7 g/mol, and CAS Number 111011-63-3.
Efonidipine API is a pharmaceutical active ingredient belonging to the dihydropyridine class of calcium-channel blockers. Its pharmacological activity is associated with inhibition of calcium ion entry through voltage-dependent calcium channels, producing vasodilation and reduction of blood pressure.
Efonidipine is marketed in Japan and has been associated with the treatment of hypertension. Unlike conventional dihydropyridine calcium-channel blockers that primarily act on L-type channels, efonidipine also blocks T-type calcium channels.
Efonidipine is a substituted 1,4-dihydropyridine compound containing a nitrophenyl group and a phosphinate/phosphine-oxide-containing structural moiety. Its chemical structure distinguishes it from conventional dihydropyridine calcium-channel blockers.
Chemical Name: 2-(N-benzylanilino)ethyl 5-(5,5-dimethyl-2-oxo-1,3,2λ5-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate
Molecular Formula: C34H38N3O7P
Molecular Weight: 631.7 g/mol
CAS Number: 111011-63-3
UNII: 40ZTP2T37Q
PubChem CID: 119171
DrugBank ID: DB09235
ChEBI ID: CHEBI:146221
Development Code: NZ-105
Brand: Landel
Efonidipine is a calcium-channel blocker that inhibits L-type and T-type calcium channels. Blocking calcium influx into vascular smooth muscle contributes to vasodilation and reduction in vascular resistance. Its T-type calcium-channel activity has also been investigated in relation to attenuation of reflex tachycardia.
Efonidipine is primarily associated with the treatment of hypertension. Its dual L-type and T-type calcium-channel blocking activity provides a pharmacological profile that differs from many conventional dihydropyridine calcium-channel blockers.
Efonidipine API should be manufactured, tested and released according to the applicable approved product specification and relevant pharmaceutical quality requirements.
Quality evaluation may include:
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 1.0% |
| Melting Point | 150°C – 154°C |