Methoxsalen

Photoactivated Radical Generator — DERMATOLOGICALS

Key facts

Methoxsalen is an ofp drug in the Photoactivated Radical Generator class catalogued in DrugCentral. It was first approved by the FDA in 1954. Its mechanism of action is classified as Photoabsorption. DrugCentral lists 5 molecular targets, including CYP1A2, ACHE and TAS2R20. Recorded indications include Primary cutaneous T-cell lymphoma, Severe Recalcitrant Psoriasis and Vitiligo.

• Approval status: ofp (first approved 1954 by the FDA).
• Drug class: Photoactivated Radical Generator; Psoralen.
• Mechanism of action: Photoabsorption.
• Molecular targets: CYP1A2, ACHE, TAS2R20 and PPO2 (5 listed in DrugCentral).
• Indications: Primary cutaneous T-cell lymphoma, Severe Recalcitrant Psoriasis and Vitiligo.
• ATC code: D05AD02 (Psoralens for topical use).
• Molecular formula: C12H8O4; molecular weight 216.19 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Primary cutaneous T-cell lymphoma
• Severe Recalcitrant Psoriasis
• Vitiligo

Off-label uses (3)

• Alopecia areata
• Lichen planus
• Mycosis fungoides

Contraindications (17)

• Albinism
• Aphakia
• Basal cell carcinoma of skin
• Bilateral cataracts
• Breastfeeding (mother)
• Disease of liver
• Erythropoietic protoporphyria
• Hydroa vacciniforme
• Malignant melanoma
• Photosensitivity
• Porphyria
• Porphyria cutanea tarda
• Pregnancy, function
• Squamous cell carcinoma
• Systemic lupus erythematosus
• Variegate porphyria
• Xeroderma pigmentosum

Mechanism & targets

• Mechanism of action (MoA): Photoabsorption
• Established pharmacologic class: Photoactivated Radical Generator; Psoralen

Molecular targets (5)

Target	Gene	Action	Activity
Cytochrome P450 1A2	CYP1A2	unknown	IC50 7.40
Acetylcholinesterase	ACHE	unknown	IC50 6.12
Taste receptor type 2 member 20	TAS2R20	agonist	EC50 4.92
Polyphenol oxidase 2	PPO2	unknown	EC50 4.83
Amine oxidase [flavin-containing] A	MAOA	unknown	IC50 4.07

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1954-12-03	FDA	—	VALEANT PHARM INTL

ATC classification

ATC code	Therapeutic hierarchy
D05AD02	DERMATOLOGICALS › ANTIPSORIATICS › ANTIPSORIATICS FOR TOPICAL USE › Psoralens for topical use
D05BA02	DERMATOLOGICALS › ANTIPSORIATICS › ANTIPSORIATICS FOR SYSTEMIC USE › Psoralens for systemic use

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Product use in unapproved indication	965.5
Thrombosis in device	68.6
Pulmonary embolism	53.0
Disease progression	43.0
Drug effective for unapproved indication	36.2
Vascular access complication	34.1

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Methoxsalen is on its molecule page.

• Molecular formula: C₁₂H₈O₄
• Molecular weight: 216.19 g/mol
• CAS number: 298-81-7
• InChIKey: QXKHYNVANLEOEG-UHFFFAOYSA-N
• PubChem CID: 4114

COC1=C2OC=CC2=CC2=C1OC(=O)C=C2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Methoxsalen used for?

DrugCentral lists the following indications for Methoxsalen: Primary cutaneous T-cell lymphoma, Severe Recalcitrant Psoriasis and Vitiligo.

How does Methoxsalen work?

Methoxsalen is classified as Photoabsorption; its molecular targets in DrugCentral include CYP1A2, ACHE, TAS2R20 (agonist) and PPO2.

When was Methoxsalen first approved?

Methoxsalen was first approved by the FDA in 1954.

What drug class does Methoxsalen belong to?

Methoxsalen is in the Photoactivated Radical Generator class.

What is the chemical formula of Methoxsalen?

Methoxsalen has the molecular formula C12H8O4 and a molecular weight of 216.19 g/mol.

Sources

• DrugCentral drug card 30 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL416 — compound record and bioactivity
• PubChem CID 4114 — chemical identifiers
• DrugBank DB00553 — drug record
• FDA UNII U4VJ29L7BQ — substance identity
• DailyMed: FDA labels for Methoxsalen — current prescribing information (label search)
• UniProt P05177 (CYP1A2) — target protein
• UniProt P22303 (ACHE) — target protein
• UniProt P59543 (TAS2R20) — target protein
• UniProt P21397 (MAOA) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.