Lercanidipine

Summary

Lercanidipine (CHEMBL250270) is a phase-3 clinical-stage small molecule (ATC C08CA13); indicated across 3 conditions including cardiovascular disorder and hypertensive disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: C08CA13
• Indications: 3 conditions
• Clinical trials: 11
• Chemistry: 611.7 Da · C36H41N3O6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL250270
Name	Lercanidipine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	65866
ATC	C08CA13
Molecular formula	C36H41N3O6
Molecular weight	611.7
InChIKey	ZDXUKAKRHYTAKV-UHFFFAOYSA-N

SMILES: CC1=C(C(C(=C(N1)C)C(=O)OC(C)(C)CN(C)CCC(C2=CC=CC=C2)C3=CC=CC=C3)C4=CC(=CC=C4)[N+](=O)[O-])C(=O)OC

IUPAC name: 5-O-[1-[3,3-diphenylpropyl(methyl)amino]-2-methylpropan-2-yl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

Also known as: Lercanidipine, Lercanidipino, Lercanil, SID50112745, SID90340703, LERCANIDIPINE, lercanidipine

Parent form; salt/anhydrous children: CHEMBL2106419

Patent coverage: 1,813 distinct patent families (7,379 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 7,347 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 15 (assay-derived). Sample: Nuclear receptor ROR-gamma, 4’-phosphopantetheinyl transferase ffp, Ras-related protein Rab-9A, Cannabinoid receptor 1, Motilin receptor, Alpha-1A adrenergic receptor, Histamine H1 receptor, Kappa-type opioid receptor, Sodium-dependent dopamine transporter, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A.

Bioactivity

ChEMBL activities: 8 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P22002	7.34	AC50	46	nM	CHEMBL_ACT_25119893
NR1I2	6.54	AC50	285.7	nM	CHEMBL_ACT_25188451
NR1I2	6.05	AC50	890.3	nM	CHEMBL_ACT_25224529
OPRK1	5.42	AC50	3800	nM	CHEMBL_ACT_25129781
ADRA1A	5.24	AC50	5700	nM	CHEMBL_ACT_25138142
HRH1	5.19	AC50	6400	nM	CHEMBL_ACT_25212900
CNR1	5.18	AC50	6600	nM	CHEMBL_ACT_25181833
ADORA3	5.06	AC50	8800	nM	CHEMBL_ACT_25134588

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

3 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
cardiovascular disorder	4	MONDO:0004995	EFO:0000319
hypertensive disorder	3	MONDO:0005044	EFO:0000537
essential hypertension	2	MONDO:0001134	MONDO:0001134

Clinical trials

Total trials: 11.

Phase distribution

Phase	Trials
PHASE4	4
Not specified	4
PHASE2	2
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00564057	PHASE4	UNKNOWN	Effects of Antihypertensive Treatment in HIV Infected Patients: Candesartan Versus Lercanidipine
NCT01180413	PHASE4	COMPLETED	Intensive Vasodilator Therapy in Patients With Essential Hypertension
NCT01211314	PHASE4	TERMINATED	Antihypertensive Efficacy of Fixed Combination Drug
NCT02594410	PHASE4	COMPLETED	Zainidip in Renal Artery Stenosis
NCT01928628	PHASE3	COMPLETED	Phase III Clinical Study to Evaluate the Efficacy and Safety of the Combination of Lercanidipine/Valsartan in Hypertensive Patients
NCT01093807	PHASE2	COMPLETED	Efficacy and Safety of Lercanidipine and Enalapril in Patients With Essential Hypertension
NCT01122251	PHASE2	COMPLETED	Efficacy and Safety of Lercanidipine and Valsartan in Patients With Essential Hypertension
NCT03497156	Not specified	RECRUITING	Bariatric Surgery and Pharmacokinetics of Lercanidipine
NCT07020104	Not specified	RECRUITING	The Role of Skin Sodium Accumulation in Chronic Kidney Disease
NCT00160498	Not specified	COMPLETED	Testing the Efficacy of Different Dosages of Lercanidipine to Reduce Hypertensive Blood Pressure in Normal Weight and Obese Patients
NCT00424801	Not specified	TERMINATED	Effects of Intensive Long-Term Vasodilation in Hypertensive Patients With Microvascular Angina Pectoris

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).