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dexniguldipine
- Development stage
- Unknown
- Modality
- Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Dexniguldipine is the (+)-(R) enantiomer of niguldipine and belongs to the dihydropyridine class of compounds. It is a small molecule with antineoplastic activity and notable potency for overcoming multidrug resistance in cancer models. Its mechanism involves binding to P-glycoprotein (ABCB1), thereby inhibiting its drug efflux function and modulating multidrug resistance. Dexniguldipine also exhibits selective antiproliferative effects in various tumor models. Clinical studies have shown tolerable toxicity profiles with oral or intravenous administration; however, its oral bioavailability is low. The compound has reached phase II clinical trials for cancer indications[6][7][10].
- Other names
- Dexniguldipino(R)-(-)-niguldipineniguldipine-(R)-(-)Dexniguldipine [INN]GTPL463GTPL-463GTPL 463SCHEMBL724137SCHEMBL-724137SCHEMBL 724137CHEMBL436150CHEMBL-436150CHEMBL 436150CHEMBL2051956CHEMBL-2051956CHEMBL 2051956
02
Targets
ABCB1 (P-glycoprotein)
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