5-Methoxypsoralen: A Review of its Effects in Psoriasis and Vitiligo
Abstract
Unlabelled 5-Methoxypsoralen, a naturally occurring linear furocoumarin, has been successfully used in combination with ultraviolet (UV) A irradiation [psoralen plus UV (PUVA)] to manage psoriasis and vitiligo. In patients and volunteers, PUVA 5-methoxypsoralen causes a dose-related increase in cutaneous photosensitivity. However, mean minimum phototoxic doses (MPD) were 30 to 50% greater with 5-methoxypsoralen than with 8-methoxypsoralen within individuals; this suggests lower photoactivity with 5-methoxypsoralen. In comparative clinical trials of parallel design, psoriasis clearance rates of > 90% or > 97% were observed in similar numbers of patients (60 to 77%) receiving oral PUVA 5-methoxypsoralen (typically 1.2 mg/kg) or oral PUVA 8-methoxypsoralen (0.6 mg/kg) treatment. Generally, 5-methoxypsoralen recipients required a greater total UVA exposure than 8-methoxypsoralen recipients to achieve end-point. However, study end-point was achieved sooner with oral or topical PUVA 5-methoxypsoralen in a small number of patients with psoriasis who received both treatments simultaneously and contralaterally. Up to 56% of patients with vitiligo achieved > 75% repigmentation with 5-methoxypsoralen (oral or topical) combined with UV irradiation (lamp or sun); the face and trunk were the most responsive areas. Lack of response to PUVA 5-methoxypsoralen treatment was observed in up to 16% of patients with psoriasis and, in 1 trial, in 22% of those with vitiligo. Lesion spreading during treatment of vitiligo was also observed in 7 (19%) patients in 1 study. The incidence and severity of adverse events was generally lower in PUVA 5-methoxypsoralen 1.2 mg/kg than in PUVA 8-methoxypsoralen 0.6 mg/kg recipients. Nausea and/or vomiting, pruritus and erythema were the most commonly reported adverse events in the short term; they occurred about 2 to 11 times more frequently in 8-methoxypsoralen than 5-methoxypsoralen recipients within clinical trials. Adverse hepatic events after oral administration of the drug were uncommon. Long term tolerability data for PUVA 5-methoxypsoralen are scarce; however, carcinogenicity was not reported during a 14-year observation period of 413 patients with psoriasis.Conclusion Similar lesion clearance rates were observed with oral 5- or 8-methoxypsoralen plus UVA exposure in patients with vitiligo or psoriasis, although patients given 5-methoxypsoralen often required a greater total UV exposure than 8-methoxypsoralen recipients. The incidence of short term cutaneous and gastrointestinal adverse effects is markedly less with 5-methoxypsoralen than with 8-methoxypsoralen, which is an advantage, although the long term tolerability of 5-methoxypsoralen has yet to be fully established. Nevertheless, in appropriately selected patients, PUVA 5-methoxypsoralen therapy may be recommended as an alternative first-line systemic treatment option for the management of vitiligo or psoriasis.
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8-Methoxypsoralen and 5-methoxypsoralen are used in PUVA therapy for hyperproliferative skin diseases including psoriasis and vitiligo.
“Furocoumarins including bifunctional 8-methoxypsoralen (8-MOP) and 5-methoxypsoralen (5-MOP) are still used in the so-called ''psoralen plus UVA (PUVA)'' therapy of rather frequent hyperproliferative skin diseases, including psoriasis and vitiligo (153-155).”
From Photoinduced Damage to Cellular DNA: Direct and Photosensitized Reactions<sup>†</sup> (2012) · cites this paper as [154]
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- Authors
- McNeely, W., & Goa, K. L.
- Corresponding author
- McNeely, Wendy
- Venue
- Drugs
- Published
- 1998
- Volume
- 56
- Issue
- 4
- Pages
- 667-690
- ISSN
- 0012-6667 (ISSN-L)
- OpenAlex
- W2052017457
- Cited by
- 79
- References
- 58
- Citations by year
- 2026: 4 · 2024: 2 · 2023: 5 · 2022: 3 · 2021: 2 · 2020: 3 · 2019: 4 · 2018: 4 · 2017: 1 · 2016: 5 · 2015: 4 · 2014: 1 · 2013: 3 · 2012: 4
- FWCI
- 0.60
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drugs (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Immunology and Microbiology › Immunology › Psoriasis: Treatment and Pathogenesis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › melanin and skin pigmentation
- Health Sciences › Medicine › Dermatology › Skin Protection and Aging
- Keywords
- 8-methoxypsoralen, PUVA, psoriasis, vitiligo, furocoumarins, phototoxicity, skin photosensitivity, adverse events, drug tolerability, repigmentation, treatment response
- MeSH terms
- 5-Methoxypsoralen, Humans, Methoxsalen, Psoriasis, Vitiligo
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