Perhexiline

Summary

Perhexiline (CHEMBL75880) is an approved small-molecule cardiovascular drug (ATC C08EX02); indicated across 5 conditions including cardiovascular disorder and hypertrophic cardiomyopathy.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C08EX02
• Indications: 5 conditions
• Clinical trials: 9
• Chemistry: 277.5 Da · C19H35N

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL75880
Name	Perhexiline
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	4746
ChEBI	CHEBI:35553
ATC	C08EX02
Molecular formula	C19H35N
Molecular weight	277.5
InChIKey	CYXKNKQEMFBLER-UHFFFAOYSA-N

SMILES: C1CCC(CC1)C(CC2CCCCN2)C3CCCCC3

IUPAC name: 2-(2,2-dicyclohexylethyl)piperidine

Pharmacological roles (ChEBI): cardiovascular drug.

Also known as: Perhexilina, Perhexiline, perhexiline, Perhexilene, PERHEXILINE, SID174006795

Parent form; salt/anhydrous children: CHEMBL1334033

Patent coverage: 1,672 distinct patent families (5,064 SureChEMBL compound mentions), from 1 matched compound structure(s). 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: 31 (assay-derived). Sample: Muscarinic acetylcholine receptor M4, 5-hydroxytryptamine receptor 2B, Tyrosine-protein kinase Fyn, Alpha-2A adrenergic receptor, Adrenergic receptor alpha-1, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Epidermal growth factor receptor, Muscarinic acetylcholine receptor M5, Muscarinic acetylcholine receptor M2.

Bioactivity

ChEMBL activities: 29 potent at pChembl ≥ 5 of 47 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P15823	6.7	Kd	199.5	nM	CHEMBL_ACT_971044
CHRM4	6.3	Ki	500.9	nM	CHEMBL_ACT_7732158
CHRM1	6.18	Ki	652.8	nM	CHEMBL_ACT_7732152
CHRM3	6.18	Ki	661	nM	CHEMBL_ACT_7732156
CHRM5	6.11	Ki	785.4	nM	CHEMBL_ACT_7732160
CYP2D6	6.03	IC50	940.8	nM	CHEMBL_ACT_7732083
CHRM5	5.96	IC50	1093	nM	CHEMBL_ACT_7732159
SIGMAR1	5.96	Ki	1092	nM	CHEMBL_ACT_7734245
EGFR	5.83	IC50	1485	nM	CHEMBL_ACT_7734214
SIGMAR1	5.58	IC50	2599	nM	CHEMBL_ACT_7734244
CHRM1	5.57	IC50	2710	nM	CHEMBL_ACT_7732151
CHRM3	5.51	IC50	3119	nM	CHEMBL_ACT_7732155
SLC6A2	5.49	Ki	3267	nM	CHEMBL_ACT_7730038
SLC6A2	5.48	IC50	3294	nM	CHEMBL_ACT_7730037
KCNH2	5.46	AC50	3500	nM	CHEMBL_ACT_25118800
CHRM4	5.45	IC50	3592	nM	CHEMBL_ACT_7732157
FYN	5.39	IC50	4064	nM	CHEMBL_ACT_7734216
CHRM2	5.31	AC50	4900	nM	CHEMBL_ACT_25215575
GHSR	5.21	AC50	6200	nM	CHEMBL_ACT_25173374
SLC6A3	5.15	AC50	7055	nM	CHEMBL_ACT_25124595
SLC6A2	5.14	AC50	7236	nM	CHEMBL_ACT_25145638
KCNH2	5.11	IC50	7762	nM	CHEMBL_ACT_1033548
KCNH2	5.11	IC50	7762	nM	CHEMBL_ACT_1429842
KCNH2	5.11	IC50	7762	nM	CHEMBL_ACT_2358286
KCNH2	5.11	IC50	7762	nM	CHEMBL_ACT_2645534
KCNH2	5.11	IC50	7800	nM	CHEMBL_ACT_325571
KCNH2	5.11	IC50	7762	nM	CHEMBL_ACT_5218913
MC3R	5.08	AC50	8285	nM	CHEMBL_ACT_25184040
HTR1A	5.04	AC50	9100	nM	CHEMBL_ACT_25217642

Target pathways

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

Indications & clinical

Indications

5 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
hypertrophic cardiomyopathy	3	MONDO:0005045	EFO:0000538
heart failure	2	MONDO:0005252	EFO:0003144
diastolic heart failure	2	MONDO:0006727	EFO:1000899

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

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
PHASE2	5
PHASE2/PHASE3	2
PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00845364	PHASE2/PHASE3	COMPLETED	Metabolic Support With Perhexiline to Protect Myocardium Undergoing Coronary Artery Surgery
NCT00989508	PHASE2/PHASE3	UNKNOWN	Myocardial Protection With Perhexiline in Left Ventricular Hypertrophy
NCT02431221	PHASE3	WITHDRAWN	Efficacy, Safety, and Tolerability of Perhexiline in Subjects With Hypertrophic Cardiomyopathy and Heart Failure
NCT00500552	PHASE2	COMPLETED	Perhexiline Therapy in Patients With Hypertrophic Cardiomyopathy
NCT00628056	PHASE1/PHASE2	UNKNOWN	Mechanisms Responsible for Cardiac and Skeletal Muscle Energetic Impairment in Diabetes
NCT00839228	PHASE2	COMPLETED	Perhexiline Therapy in Heart Failure With Preserved Ejection Fraction Syndrome
NCT00841139	PHASE2	COMPLETED	Metabolic Manipulation in Chronic Heart Failure
NCT02862600	PHASE2	TERMINATED	Open-Label Study of Perhexiline in Patients With Hypertrophic Cardiomyopathy and Moderate to Severe Heart Failure
NCT04426578	PHASE2	UNKNOWN	Role of Perhexiline in Hypertrophic Cardiomyopathy

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).