Hypericin

Summary

Hypericin (CHEMBL286494) is a phase-3 clinical-stage small-molecule antidepressant; indicated across 6 conditions including primary cutaneous t-cell non-hodgkin lymphoma and mycosis fungoides.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 6 conditions
• Clinical trials: 7
• Chemistry: 504.4 Da · C30H16O8

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL286494
Name	Hypericin
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	3663
ChEBI	CHEBI:5835
Molecular formula	C30H16O8
Molecular weight	504.4
InChIKey	YDOIFHVUBCIUHF-UHFFFAOYSA-N

SMILES: CC1=CC(=O)C2=C(C3=C(C=C(C4=C3C5=C2C1=C6C(=CC(=O)C7=C(C8=C(C=C(C4=C8C5=C67)O)O)O)C)O)O)O

IUPAC name: 9,11,13,16,18,20-hexahydroxy-5,24-dimethyloctacyclo[13.11.1.12,10.03,8.04,25.019,27.021,26.014,28]octacosa-1(26),2,4(25),5,8,10,12,14(28),15(27),16,18,20,23-tridecaene-7,22-dione

Pharmacological roles (ChEBI): antidepressant.

Also known as: Hipericin, Hypericin, Hypericina, Hypericine, Hypericum red, NSC-407313, SGX-301, SGX301, hypericin, SID26755796, SID26756738, SID124892429

Parent form; salt/anhydrous children: CHEMBL5314602

Patent coverage: 4,775 distinct patent families (16,266 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 15,968 (98%) 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: 24 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Microtubule-associated protein tau, Survival motor neuron protein, ATP-dependent DNA helicase Q1, RecQ-like DNA helicase BLM, Inositol monophosphatase 1, 4’-phosphopantetheinyl transferase ffp, Ferritin light chain, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Cysteine protease ATG4B.

Bioactivity

ChEMBL activities: 18 potent at pChembl ≥ 5 of 41 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD3	7.46	Ki	34.5	nM	CHEMBL_ACT_3285804
CRHR1	6.52	IC50	300	nM	CHEMBL_ACT_3285805
CRHR1	6.52	IC50	300	nM	CHEMBL_ACT_3285806
RECQL	6.45	Potency	354.8	nM	CHEMBL_ACT_5056304
RECQL	6.25	Potency	562.3	nM	CHEMBL_ACT_3684061
THRB	5.75	Potency	1778	nM	CHEMBL_ACT_3657092
THRB	5.75	Potency	1778	nM	CHEMBL_ACT_4019048
CBS	5.51	IC50	3100	nM	CHEMBL_ACT_18339651
MEN1	5.5	Potency	3162	nM	CHEMBL_ACT_4581384
P41921	5.43	IC50	3670	nM	CHEMBL_ACT_5137350
MAPT	5.35	Potency	4467	nM	CHEMBL_ACT_3960004
MAPT	5.35	Potency	4467	nM	CHEMBL_ACT_3962499
SNCA	5.12	IC50	7500	nM	CHEMBL_ACT_22754637
CYP3A4	5.06	IC50	8700	nM	CHEMBL_ACT_3285831
ATG4B	5.05	IC50	8900	nM	CHEMBL_ACT_24958656
HPGD	5.05	Potency	8912	nM	CHEMBL_ACT_4809118
Q27757	5	Potency	10000	nM	CHEMBL_ACT_3957760
P97697	5	Potency	10000	nM	CHEMBL_ACT_4411535

Target pathways

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

Indications & clinical

Indications

6 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
primary cutaneous T-cell non-Hodgkin lymphoma	3	MONDO:0000607	EFO:0002913
mycosis fungoides	3	MONDO:0009691	EFO:1001051
psoriasis	2	MONDO:0005083	EFO:1001494
HIV infectious disease	1	MONDO:0005109	EFO:0000764
T-cell non-Hodgkin lymphoma	1	MONDO:0015760	MONDO:0015760

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

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE2	4
PHASE1	2
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06470451	PHASE3	RECRUITING	Confirmatory Study of Topical HyBryte™ vs. Placebo for the Treatment of CTCL
NCT05380635	PHASE2	COMPLETED	PK and ECG Determinations Following 8 Weeks of HyBryte Treatment for Cutaneous T-Cell Lymphoma
NCT05442190	PHASE2	COMPLETED	Topical SGX302 for Mild-to-Moderate Psoriasis
NCT05872854	PHASE2	COMPLETED	Treatment of Mycosis Fungoides With Hypericin Ointment and Visible Light
NCT06149247	PHASE2	COMPLETED	HyBryte (Synthetic Hypericin) Versus Valchlor (Mechlorethamine) in the Treatment of CTCL
NCT00000645	PHASE1	COMPLETED	A Phase I Dose Escalation Study of Synthetic Hypericin in HIV-Infected Patients With Less Than 300 CD4 Lymphocytes
NCT00000792	PHASE1	COMPLETED	A Pharmacologically Guided Phase I/II Study of Daily Orally Administered Synthetic Hypericin in HIV-Infected Subjects

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).