Hesperidin

Summary

Hesperidin (CHEMBL449317) is a phase-3 clinical-stage small molecule; indicated across 2 conditions including osteoporosis and rheumatoid arthritis.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 24
• Chemistry: 610.6 Da · C28H34O15

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL449317
Name	Hesperidin
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	10621
ChEBI	CHEBI:28775
Molecular formula	C28H34O15
Molecular weight	610.6
InChIKey	QUQPHWDTPGMPEX-QJBIFVCTSA-N

SMILES: C[C@H]1[C@@H]([C@H]([C@H]([C@@H](O1)OC[C@@H]2[C@H]([C@@H]([C@H]([C@@H](O2)OC3=CC(=C4C(=O)C[C@H](OC4=C3)C5=CC(=C(C=C5)OC)O)O)O)O)O)O)O)O

IUPAC name: (2S)-5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxymethyl]oxan-2-yl]oxy-2,3-dihydrochromen-4-one

ChEBI definition: A disaccharide derivative that consists of hesperetin substituted by a 6-O-(α-L-rhamnopyranosyl)-β-D-glucopyranosyl moiety at position 7 via a glycosidic linkage.

Also known as: Diosvein, Hesperidin, NSC-31048, hesperidin, hesperidine, SID50086731, Hesperidine, SID144203999, HESPERIDIN, (2’S)-Hesperidin

Patent coverage: 9,030 distinct patent families (18,753 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 18,582 (99%) 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: 6 (assay-derived). Sample: Carboxy-terminal domain RNA polymerase II polypeptide A small phosphatase 1, Voltage-gated N-type calcium channel alpha-1B subunit/Amyloid beta A4 precursor protein-binding family A member 1, DNA polymerase beta, Glycogen synthase kinase-3 beta, Calmodulin-1, Lysine-specific histone demethylase 1A.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CACNA1B	5.02	IC50	9500	nM	CHEMBL_ACT_4304923

Target pathways

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

Indications & clinical

Indications

2 indications (0 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
osteoporosis	3	MONDO:0005298	EFO:0003882
rheumatoid arthritis	3	MONDO:0008383	EFO:0000685

Clinical trials

Total trials: 24.

Phase distribution

Phase	Trials
Not specified	12
PHASE2	5
PHASE3	4
PHASE4	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03471910	PHASE4	COMPLETED	Clinical Non-inferiority Study Between Diosmin 600mg & Diosmin + Hesperidin in Symptomatic Chronic Venous Insufficiency
NCT04358497	PHASE4	UNKNOWN	Endovascular Versus Medical Treatment for the Pelvic Congestion Syndrome
NCT06584799	PHASE3	RECRUITING	Venoactive Drug Treatment of Pelvic Venous Disorders
NCT00330096	PHASE3	COMPLETED	Effects of Hesperidin on Bone Mineral Density and Bone Metabolism of Postmenopausal Women
NCT02927483	PHASE3	UNKNOWN	Study to Assess the Efficacy and Safety of Endolex Forte VErsus Diosmin and Hesperidin in Reducing VeNous Insufficiency
NCT05243706	PHASE3	UNKNOWN	Evaluation of The Effect of Loratadine Versus Diosmin/Hesperidin Combination on Vinca Alkaloids Induced Neuropathy
NCT00545116	PHASE2	COMPLETED	Effects of Hesperidin on Bone Biomarkers in Postmenopausal Women
NCT00914251	PHASE2	UNKNOWN	Vascular Effects of Hesperidin in Metabolic Syndrome
NCT01773486	PHASE2	WITHDRAWN	Effects of Hesperidin on Insulin Sensitivity
NCT02610491	PHASE2	COMPLETED	The Effect of Hesperidin on Glucose / Insulin Metabolism
NCT04715932	PHASE2	COMPLETED	Study of Hesperidin Therapy on COVID-19 Symptoms (HESPERIDIN)
NCT04452799	EARLY_PHASE1	UNKNOWN	Hesperidin and Diosmin for Treatment of COVID-19
NCT07452562	Not specified	RECRUITING	Hesperidin RCT in MS
NCT01881204	Not specified	COMPLETED	Hesperidin and Bone Health in Postmenopausal Women
NCT03377140	Not specified	UNKNOWN	The Effects of Hesperidin on Biochemical Factors and Hepatic Fibrosis in Nonalcoholic Fatty Liver Disease
NCT03377153	Not specified	UNKNOWN	The Effects of Hesperidin and Flaxseed on Biochemical Factors and Hepatic Fibrosis in Nonalcoholic Fatty Liver Disease
NCT03734835	Not specified	UNKNOWN	The Effect of Supplementation of Flaxseed, Hesperidin, Flaxseed and Hesperidin Together in Metabolic Syndrome
NCT03734874	Not specified	UNKNOWN	The Effects of Hesperidin on Metabolic Syndrome
NCT03737422	Not specified	COMPLETED	The Effects of Hesperidin and Flaxseed in Prediabetes
NCT03984916	Not specified	COMPLETED	Study of the Bioavailability of Three Hesperidin Extracts.
NCT04145102	Not specified	COMPLETED	Evaluation of the Remineralizing and Antibacterial Effect of Natural Versus Synthetic Materials on Deep Carious Dentin
NCT04316390	Not specified	COMPLETED	Influence of Hesperidin and Vitamin C on Uric Acid Concentration
NCT04933591	Not specified	COMPLETED	Impact of Treatment With VENARUS® on the Level of Monocyte Chemoattractant Protein 1 in Varicose Veins Blood
NCT06402032	Not specified	COMPLETED	Clinical and Histological Evaluation of Hesperidin as a Direct Pulp Capping Material

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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