Felodipine

Summary

Felodipine (CHEMBL1480) is an approved small-molecule calcium channel blocker (ATC C08CA02) targeting CFTR; indicated across 7 conditions including cardiovascular disorder and hypertensive disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C08CA02
• Targets: 1 (CFTR)
• Indications: 7 conditions
• Clinical trials: 11
• Chemistry: 384.2 Da · C18H19Cl2NO4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1480
Name	Felodipine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3333
ChEBI	CHEBI:585948
ATC	C08CA02
Molecular formula	C18H19Cl2NO4
Molecular weight	384.2
InChIKey	RZTAMFZIAATZDJ-UHFFFAOYSA-N

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

IUPAC name: 5-O-ethyl 3-O-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

ChEBI definition: The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris.

Pharmacological roles (ChEBI): calcium channel blocker, antihypertensive agent, vasodilator agent, anti-arrhythmia drug.

Also known as: C08CA02, Cabren, Cardioplen xl, Felodipine, Felodipine component of lexxel, Felodipino, Felogen xl, Felotens xl, Folpik xl, H 154/82, H-154/82, Keloc sr

Patent coverage: 8,399 distinct patent families (30,761 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 30,625 (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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
CFTR	CFTR	Potentiation	8.4	0.1%	P13569

Broader ChEMBL bioactivity targets: 33 (assay-derived). Sample: Microtubule-associated protein tau, Lysine-specific demethylase 4E, Prelamin-A/C, RecQ-like DNA helicase BLM, Ferritin light chain, Geminin, Endonuclease 4, Peripheral myelin protein 22, Sodium channel protein type 5 subunit alpha, Equilibrative nucleoside transporter 1.

Bioactivity

ChEMBL activities: 15 potent at pChembl ≥ 5 of 40 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P22002	7.69	AC50	20.4	nM	CHEMBL_ACT_25119377
ADORA3	6.22	Ki	597	nM	CHEMBL_ACT_7665350
ADORA3	5.98	IC50	1057	nM	CHEMBL_ACT_7665349
NR1I2	5.72	EC50	1900	nM	CHEMBL_ACT_15463793
SCN5A	5.6	AC50	2504	nM	CHEMBL_ACT_25158853
PGR	5.58	AC50	2600	nM	CHEMBL_ACT_25192719
PDE4D	5.5	AC50	3200	nM	CHEMBL_ACT_25185043
NR1I2	5.41	EC50	3900	nM	CHEMBL_ACT_15463750
CYP2C9	5.34	IC50	4580	nM	CHEMBL_ACT_7667439
NR1H4	5.3	IC50	4960	nM	CHEMBL_ACT_13348771
NR1I2	5.15	EC50	7100	nM	CHEMBL_ACT_15465486
ADORA3	5.1	AC50	7910	nM	CHEMBL_ACT_25133932
TBXA2R	5.08	AC50	8410	nM	CHEMBL_ACT_25154978
OPRK1	5.05	AC50	8876	nM	CHEMBL_ACT_25129177
NR3C1	5	AC50	9940	nM	CHEMBL_ACT_25175604

Target pathways

Aggregated over 1 target gene(s): CFTR.

Top Reactome pathways

11 total, by targets touching each:

Pathway	Targets	Genes
ABC-family protein mediated transport	1	CFTR
RHO GTPases regulate CFTR trafficking	1	CFTR
Defective CFTR causes cystic fibrosis	1	CFTR
Ub-specific processing proteases	1	CFTR
Cargo recognition for clathrin-mediated endocytosis	1	CFTR
Clathrin-mediated endocytosis	1	CFTR
RHOQ GTPase cycle	1	CFTR
Chaperone Mediated Autophagy	1	CFTR
Late endosomal microautophagy	1	CFTR
Aggrephagy	1	CFTR
Developmental Lineage of Pancreatic Ductal Cells	1	CFTR

Dominant GO biological processes

GO term	Targets
cholesterol biosynthetic process	1
water transport	1
bicarbonate transport	1
cholesterol transport	1
response to endoplasmic reticulum stress	1
transepithelial water transport	1
sperm capacitation	1
multicellular organismal-level water homeostasis	1
intracellular pH elevation	1
establishment of localization in cell	1
transmembrane transport	1
membrane hyperpolarization	1
positive regulation of enamel mineralization	1
cellular response to cAMP	1
amelogenesis	1

Indications & clinical

Indications

7 indications (3 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	4	MONDO:0005044	EFO:0000537
diabetes mellitus	4	MONDO:0005015	EFO:0000400
atherosclerosis	3	MONDO:0005311	EFO:0003914
coronary artery disorder	3	MONDO:0005010	EFO:0001645
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148

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
Not specified	4
PHASE1	2
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00348686	PHASE4	COMPLETED	Candesartan Effectiveness Study in Pro-B Type Natriuretic Peptides (BNP)
NCT00841880	PHASE4	COMPLETED	China Medical University Hospital (CMUH) Triapin Listing
NCT00861016	PHASE4	COMPLETED	Efficacy and Safety of Metoprolol Succinate Prolonged-Release Tablet in Patients With Mild to Moderate Hypertension
NCT02744872	PHASE4	COMPLETED	Copenhagen Acute Renal Complications After Transplantations Study Group
NCT00679653	PHASE3	COMPLETED	Blood Pressure and Weight Trajectory on a Dual Antihypertensive Combination Plus Sibutramine Versus Placebo in Obese Hypertensives
NCT00905333	PHASE1	COMPLETED	Evaluation of the Pharmacokinetic Interaction Between Candesartan and Felodipine After Ingestion of a Specific Meal
NCT02232269	PHASE1	COMPLETED	Coffee Interaction With the Antihypertensive Drug Felodipine
NCT00742066	Not specified	UNKNOWN	Role of AT1-receptor Blockers in Insulin-induced Vasodilation.
NCT01136863	Not specified	COMPLETED	Felodipine Event Reduction Study
NCT02311530	Not specified	COMPLETED	Bioequivalence Study of Felodipine ER Tablets 10 mg Under Fed Conditions
NCT02327247	Not specified	COMPLETED	Bioequivalence Study of Felodipine ER Tablets 10 mg Under Fasting Conditions

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 5 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

15 molecules share ≥1 primary target. Top 15 by shared-target count:

Molecule	Source	Status	Shared targets
IVACAFTOR	ChEMBL + PubChem	Phase 4 (approved)	CFTR
ELEXACAFTOR	ChEMBL	Phase 4 (approved)	CFTR
GLYBURIDE	ChEMBL	Phase 4 (approved)	CFTR
LUMACAFTOR	ChEMBL	Phase 4 (approved)	CFTR
TEZACAFTOR	ChEMBL	Phase 4 (approved)	CFTR
BAMOCAFTOR	ChEMBL	Phase 3	CFTR
QUERCETIN	ChEMBL	Phase 3	CFTR
RUTIN	ChEMBL	Phase 3	CFTR
GALICAFTOR	ChEMBL	Phase 2	CFTR
GENISTEIN	ChEMBL	Phase 2	CFTR
GLPG-2737	ChEMBL	Phase 2	CFTR
ICENTICAFTOR	ChEMBL	Phase 2	CFTR
NAVOCAFTOR	ChEMBL	Phase 2	CFTR
RISELCAFTOR	ChEMBL	Phase 2	CFTR
Tadalafil	PubChem	Approved	CFTR