Lacidipine

Summary

Lacidipine (CHEMBL460291) is a phase-3 clinical-stage small molecule (ATC C08CA09); 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: C08CA09
• Indications: 3 conditions
• Clinical trials: 11
• Chemistry: 455.5 Da · C26H33NO6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL460291
Name	Lacidipine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	5311217
ATC	C08CA09
Molecular formula	C26H33NO6
Molecular weight	455.5
InChIKey	GKQPCPXONLDCMU-CCEZHUSRSA-N

SMILES: CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2/C=C/C(=O)OC(C)(C)C)C(=O)OCC)C)C

IUPAC name: diethyl 2,6-dimethyl-4-[2-[(E)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]phenyl]-1,4-dihydropyridine-3,5-dicarboxylate

Also known as: 3,3’-iminobispropylamine, 3,3’-iminodipropylamine, Caldine, Dipropylamine, 3,3’-diamino-, Dipropylenetriamine, GR 43659X, GR-43659X, Lacidipine, Lacidipino, Molap, Motens, NSC-7773

Patent coverage: 3,379 distinct patent families (11,503 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 9,194 (80%) 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: 14 (assay-derived). Sample: Thromboxane-A synthase, Progesterone receptor, Sodium-dependent noradrenaline transporter, D(3) dopamine receptor, Kappa-type opioid receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Adenosine receptor A3, 3’,5’-cyclic-AMP phosphodiesterase 4D, Androgen receptor, Cytochrome P450 2C9.

Bioactivity

ChEMBL activities: 16 potent at pChembl ≥ 5 of 20 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P22002	6.5	AC50	320	nM	CHEMBL_ACT_25119378
CYP3A4	6.05	IC50	900	nM	CHEMBL_ACT_7772099
NR1I2	6	AC50	1000	nM	CHEMBL_ACT_25187988
NR1I2	5.82	AC50	1500	nM	CHEMBL_ACT_25224203
TBXAS1	5.77	IC50	1694	nM	CHEMBL_ACT_7776245
CYP2C19	5.7	IC50	2000	nM	CHEMBL_ACT_7772091
CYP2C9	5.7	IC50	2000	nM	CHEMBL_ACT_7772093
DRD3	5.68	Ki	2096	nM	CHEMBL_ACT_7772106
ADORA3	5.64	Ki	2281	nM	CHEMBL_ACT_7772024
P15207	5.58	Ki	2612	nM	CHEMBL_ACT_7776244
P15207	5.41	IC50	3918	nM	CHEMBL_ACT_7776243
ADORA3	5.39	IC50	4036	nM	CHEMBL_ACT_7772023
SLC6A2	5.25	Ki	5687	nM	CHEMBL_ACT_7772046
SLC6A2	5.24	IC50	5735	nM	CHEMBL_ACT_7772045
DRD3	5.21	IC50	6170	nM	CHEMBL_ACT_7772105
OPRK1	5.07	AC50	8600	nM	CHEMBL_ACT_25129178

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

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 11.

Phase distribution

Phase	Trials
PHASE4	4
PHASE1	4
PHASE3	1
PHASE2	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00328965	PHASE4	COMPLETED	Lacidipine In Mild To Moderate Essential Hypertension Patients With Type 2 Diabetes In Korea
NCT00460915	PHASE4	COMPLETED	Efficacy and Safety of Lacidipine and Amlodipine on Blood Pressure in Korean ISH Patients Aged 60 to 80 Years
NCT00533858	PHASE4	UNKNOWN	Effect of Lacidipine and Losartan on 24 Hour Systolic Blood Pressure Variability in Elderly Hypertensive Patients
NCT02235402	PHASE4	COMPLETED	A Randomised, Parallel-group, Double-blind, Double-dummy Study to Compare the Effects of Lacidipine Versus Bendrofluazide on Markers of Platelet Activation and Haemorheological Factors in Hypertensive Patients
NCT02177331	PHASE3	COMPLETED	Lacidipine in Medical Practice in Patients With Mild to Moderate Essential Hypertension
NCT02232607	PHASE2	COMPLETED	Efficacy and Safety of Lacidipine in Chronic Stable Angina
NCT02203500	PHASE1	COMPLETED	Tolerability and Pharmacokinetics of Lacidipine With and Without the Co-administration of Telmisartan in Female and Male Healthy Subjects
NCT02209649	PHASE1	COMPLETED	Bioavailability of Lacidipine and Telmisartan Fixed Dose Combination Tablets Relative to Separate Tablets in Healthy Subjects
NCT02218684	PHASE1	COMPLETED	Tolerability and Pharmacokinetics of Telmisartan in Combination With Lacidipine in Healthy Male Subjects
NCT02264158	PHASE1	COMPLETED	Influence of Telmisartan and Lacidipine, Combined or Alone, on QT Interval in Healthy Volunteers
NCT02240641	Not specified	TERMINATED	Effect of Caldine® on Renal Function in Balanced Hypertension

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 3 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

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