photosensitizing agents


Summary: Drugs that are pharmacologically inactive but when exposed to ultraviolet radiation or sunlight are converted to their active metabolite to produce a beneficial reaction affecting the diseased tissue. These compounds can be administered topically or systemically and have been used therapeutically to treat psoriasis and various types of neoplasms.

Top Publications

  1. Magli A, Forte R, Tortori A, Capasso L, Marsico G, Piozzi E. Epithelium-off corneal collagen cross-linking versus transepithelial cross-linking for pediatric keratoconus. Cornea. 2013;32:597-601 pubmed publisher
    ..To compare efficiency and safety of epithelium-off corneal cross-linking (CXL) and transepithelial cross-linking (TE-CXL) in pediatric patients with progressive keratoconus...
  2. St Denis T, Dai T, Izikson L, Astrakas C, Anderson R, Hamblin M, et al. All you need is light: antimicrobial photoinactivation as an evolving and emerging discovery strategy against infectious disease. Virulence. 2011;2:509-20 pubmed publisher
  3. Touboul D, Efron N, Smadja D, Praud D, Malet F, Colin J. Corneal confocal microscopy following conventional, transepithelial, and accelerated corneal collagen cross-linking procedures for keratoconus. J Refract Surg. 2012;28:769-76 pubmed publisher
    ..To compare early corneal healing following conventional, transepithelial, and accelerated corneal collagen cross-linking (CXL) protocols...
  4. Qian J, Wang D, Cai F, Zhan Q, Wang Y, He S. Photosensitizer encapsulated organically modified silica nanoparticles for direct two-photon photodynamic therapy and in vivo functional imaging. Biomaterials. 2012;33:4851-60 pubmed publisher
    ..Finally, we showed that the nanoprobes could target the subcutaneously xenografted tumor of a mouse for long time observations. ORMOSIL nanoparticles have great potentials for disease diagnosis and clinical therapies. ..
  5. Mitsunaga M, Ogawa M, Kosaka N, Rosenblum L, Choyke P, Kobayashi H. Cancer cell-selective in vivo near infrared photoimmunotherapy targeting specific membrane molecules. Nat Med. 2011;17:1685-91 pubmed publisher
    ..Target-selective PIT enables treatment of cancer based on mAb binding to the cell membrane. ..
  6. Sakamoto F, Doukas A, Farinelli W, Tannous Z, Su Y, Smith N, et al. Intracutaneous ALA photodynamic therapy: dose-dependent targeting of skin structures. Lasers Surg Med. 2011;43:621-31 pubmed publisher
    ..Potentially, intradermal ALA-PDT using various ALA concentrations may be useful for treating vascular lesions (malformations, hemangiomas, tumors), EG/AG disorders, fat or deep targets in skin. ..
  7. Zha Z, Yue X, Ren Q, Dai Z. Uniform polypyrrole nanoparticles with high photothermal conversion efficiency for photothermal ablation of cancer cells. Adv Mater. 2013;25:777-82 pubmed publisher
  8. Idris N, Gnanasammandhan M, Zhang J, Ho P, Mahendran R, Zhang Y. In vivo photodynamic therapy using upconversion nanoparticles as remote-controlled nanotransducers. Nat Med. 2012;18:1580-5 pubmed publisher
    ..As the first demonstration, to the best of our knowledge, of the photosensitizer-loaded UCN as an in vivo-targeted PDT agent, this finding may serve as a platform for future noninvasive deep-cancer therapy...
  9. Korbelik M, Madiyalakan R, Woo T, Haddadi A. Antitumor efficacy of photodynamic therapy using novel nanoformulations of hypocrellin photosensitizer SL052. Photochem Photobiol. 2012;88:188-93 pubmed publisher
    ..The longer time interval produced higher tumor cure rates with all SL052 preparations. With both drug-light intervals, PDT based on SL052-PLGA-NPs produced superior therapeutic benefit compared with the other two SL052 formulations. ..

More Information


  1. Tan X, Luo S, Wang D, Su Y, Cheng T, Shi C. A NIR heptamethine dye with intrinsic cancer targeting, imaging and photosensitizing properties. Biomaterials. 2012;33:2230-9 pubmed publisher
    ..This dye may hold promise as a candidate multifunctional theranostic agent for future tumor targeted imaging and photodynamic therapy. ..
  2. Galperin G, Berra M, Tau J, Boscaro G, Zarate J, Berra A. Treatment of fungal keratitis from Fusarium infection by corneal cross-linking. Cornea. 2012;31:176-80 pubmed publisher
    ..To evaluate the efficacy of corneal cross-linking (CXL) (riboflavin-UV-A) as a simple therapy in Fusarium keratitis...
  3. Chibebe Junior J, Fuchs B, Sabino C, Junqueira J, Jorge A, Ribeiro M, et al. Photodynamic and antibiotic therapy impair the pathogenesis of Enterococcus faecium in a whole animal insect model. PLoS ONE. 2013;8:e55926 pubmed publisher
    ..faecium strain more susceptible to vancomycin action. In summary, G. mellonella provides an invertebrate model host to study the antimicrobial PDT and to explore combinatorial aPDT-based treatments. ..
  4. Wernli J, Schumacher S, Spoerl E, Mrochen M. The efficacy of corneal cross-linking shows a sudden decrease with very high intensity UV light and short treatment time. Invest Ophthalmol Vis Sci. 2013;54:1176-80 pubmed publisher
    ..Further experiments are necessary to validate these results for in vivo human corneal tissue. Additionally, safety aspects at high intensities must be investigated. ..
  5. Jerjes W, Upile T, Alexander Mosse C, Hamdoon Z, Morcos M, Morley S, et al. Prospective evaluation of 110 patients following ultrasound-guided photodynamic therapy for deep seated pathologies. Photodiagnosis Photodyn Ther. 2011;8:297-306 pubmed publisher
  6. Garcia V, Fernandes L, Macarini V, de Almeida J, Martins T, Bosco A, et al. Treatment of experimental periodontal disease with antimicrobial photodynamic therapy in nicotine-modified rats. J Clin Periodontol. 2011;38:1106-14 pubmed publisher
    ..Antimicrobial photodynamic therapy was an effective adjunctive treatment to SRP for induced periodontitis in nicotine-modified rats. ..
  7. Bown S. Photodynamic therapy for photochemists. Philos Trans A Math Phys Eng Sci. 2013;371:20120371 pubmed publisher
  8. Abbas S, Jerjes W, Upile T, Vaz F, Hopper C. The palliative role of PDT in recurrent advanced nasopharyngeal carcinoma: case series. Photodiagnosis Photodyn Ther. 2012;9:142-7 pubmed publisher
    ..Photodynamic therapy was very successful palliative therapy for this small group of recurrent advanced nasopharyngeal cancer patients. ..
  9. Del Buey M, Cristóbal J, Casas P, Goñi P, Clavel A, Mínguez E, et al. Evaluation of in vitro efficacy of combined riboflavin and ultraviolet a for Acanthamoeba isolates. Am J Ophthalmol. 2012;153:399-404 pubmed publisher
    ..However, in vitro results do not always indicate in vivo efficacy, so future studies should test the validity of this treatment for Acanthamoeba keratitis. ..
  10. Guleng G, Helsing P. Photodynamic therapy for basal cell carcinomas in organ-transplant recipients. Clin Exp Dermatol. 2012;37:367-9 pubmed publisher
    ..There was only one recurrence during a total follow-up period of 407 months. PDT seems to be an effective treatment option for BCC in immunosuppressed OTRs. ..
  11. Pereira Gonzales F, Maisch T. Photodynamic inactivation for controlling Candida albicans infections. Fungal Biol. 2012;116:1-10 pubmed publisher
    ..The use of APDT as an antimicrobial topical agent against superficial and cutaneous diseases represents an effective method for eliminating microorganisms. ..
  12. Huang L, Xuan Y, Koide Y, Zhiyentayev T, Tanaka M, Hamblin M. Type I and Type II mechanisms of antimicrobial photodynamic therapy: an in vitro study on gram-negative and gram-positive bacteria. Lasers Surg Med. 2012;44:490-9 pubmed publisher
    ..The differences in NaN(3) inhibition may reflect differences in the extent of PS binding to bacteria (microenvironment) or differences in penetration of NaN(3) into cell walls of bacteria. ..
  13. Maisch T, Spannberger F, Regensburger J, Felgenträger A, Bäumler W. Fast and effective: intense pulse light photodynamic inactivation of bacteria. J Ind Microbiol Biotechnol. 2012;39:1013-21 pubmed publisher
  14. Jarvi M, Patterson M, Wilson B. Insights into photodynamic therapy dosimetry: simultaneous singlet oxygen luminescence and photosensitizer photobleaching measurements. Biophys J. 2012;102:661-71 pubmed publisher
    ..These studies improve our understanding of PDT processes, demonstrate that SOL is a valuable gold-standard dose metric, and show that when used judiciously, photobleaching can serve as a surrogate for (1)O(2) dose...
  15. Kaya V, Utine C, Yilmaz O. Intraoperative corneal thickness measurements during corneal collagen cross-linking with hypoosmolar riboflavin solution in thin corneas. Cornea. 2012;31:486-90 pubmed publisher
    ..11 ± 27.94 ?m, respectively) (P < 0.01 for both). The iatrogenic swelling effect of the hypoosmolar riboflavin solution might be short acting and not durable throughout the UVA application in collagen cross-linking procedure. ..
  16. Huang Y, Tanaka M, Vecchio D, García Díaz M, Chang J, Morimoto Y, et al. Photodynamic therapy induces an immune response against a bacterial pathogen. Expert Rev Clin Immunol. 2012;8:479-94 pubmed publisher
    ..The data emphasize the importance of considering the host immune response in PDT for infectious disease. ..
  17. Saggu S, Hung H, Quiogue G, Lemasters J, Nieminen A. Lysosomal signaling enhances mitochondria-mediated photodynamic therapy in A431 cancer cells: role of iron. Photochem Photobiol. 2012;88:461-8 pubmed publisher
    ..These results support the conclusion that chelatable iron stored in the lysosomes enhances the efficacy of bafilomycin-mediated PDT and that lysosomal disruption augments PDT with Pc 4. ..
  18. Chouikrat R, Seve A, Vanderesse R, Benachour H, Barberi Heyob M, Richeter S, et al. Non polymeric nanoparticles for photodynamic therapy applications: recent developments. Curr Med Chem. 2012;19:781-92 pubmed
    ..This review, based on the chemical nature of the nanoparticles will discuss recent advances in the area of non polymeric nanoparticles for photodynamic therapy applications. ..
  19. Filippello M, Stagni E, O Brart D. Transepithelial corneal collagen crosslinking: bilateral study. J Cataract Refract Surg. 2012;38:283-91 pubmed publisher
    ..Its noninvasive nature makes it potentially useful in cases in which epithelial debridement is ideally avoided, such as pediatric cases, uncooperative patients, and thin corneas with thicknesses nearing 380 ?m. ..
  20. Silva E, Schaberle F, Monteiro C, Dabrowski J, Arnaut L. The challenging combination of intense fluorescence and high singlet oxygen quantum yield in photostable chlorins--a contribution to theranostics. Photochem Photobiol Sci. 2013;12:1187-92 pubmed publisher
    ..These dual functional agents use nearly all the energy absorbed to perform the desired functions and are appropriate for theranostics applications...
  21. Murakami T, Nakatsuji H, Inada M, Matoba Y, Umeyama T, Tsujimoto M, et al. Photodynamic and photothermal effects of semiconducting and metallic-enriched single-walled carbon nanotubes. J Am Chem Soc. 2012;134:17862-5 pubmed publisher
    ..More importantly, cancer cell killing by PDE of s-SWNTs has been disclosed for the first time. ..
  22. Kashiwabuchi R, Carvalho F, Khan Y, Hirai F, Campos M, McDonnell P. Assessment of fungal viability after long-wave ultraviolet light irradiation combined with riboflavin administration. Graefes Arch Clin Exp Ophthalmol. 2013;251:521-7 pubmed publisher
  23. Rosetta P, Vinciguerra R, Romano M, Vinciguerra P. Corneal collagen cross-linking window absorption. Cornea. 2013;32:550-4 pubmed publisher
    ..After a minimum follow-up of 3 months, none of the patients had recurrence of the infection. CXL-WA is a promising technique of treatment of infectious corneal ulcers, delaying or preventing more invasive approaches. ..
  24. Kulbacka J, Nowak M, Skołucka N, Saczko J, Kotulska M. The influence of electroporation on in vitro photodynamic therapy of human breast carcinoma cells. Folia Biol (Praha). 2011;57:112-8 pubmed
    ..The data presented show up to 10-fold greater efficacy of the combined method, with very significantly reduced drug exposure times. ..
  25. Suri K, Hammersmith K, Nagra P. Corneal collagen cross-linking: ectasia and beyond. Curr Opin Ophthalmol. 2012;23:280-7 pubmed publisher
    ..This article reviews the literature published in the past 3 years about the expanding spectrum of cross-linking as a therapeutic modality and its complications...
  26. Jerjes W, Hamdoon Z, Hopper C. Photodynamic therapy in the management of potentially malignant and malignant oral disorders. Head Neck Oncol. 2012;4:16 pubmed
    ..The role of photodynamic therapy in the management of oral potentially malignant disorders and early oral cancer is being discussed. ..
  27. Caporossi A, Mazzotta C, Baiocchi S, Caporossi T, Denaro R, Balestrazzi A. Riboflavin-UVA-induced corneal collagen cross-linking in pediatric patients. Cornea. 2012;31:227-31 pubmed
    ..In pediatric age, a good functional response and keratoconus stability was obtained after corneal cross-linking in a 36-month follow-up. ..
  28. Hashimoto M, Prates R, Kato I, Núñez S, Courrol L, Ribeiro M. Antimicrobial photodynamic therapy on drug-resistant Pseudomonas aeruginosa-induced infection. An in vivo study. Photochem Photobiol. 2012;88:590-5 pubmed publisher
    ..Mice survival was increased on 24?h. Thus, this result suggests that aPDT may also be a novel prophylactic treatment in the care of burned patients. ..
  29. Abbas S, Jerjes W, Upile T, Vincent A, Hopper C. Treatment of Kimura disease with photodynamic therapy: a case study. Photodiagnosis Photodyn Ther. 2012;9:83-6 pubmed publisher
    ..Photodynamic therapy was very effective in controlling disease progression in this patient who suffers from Kimura disease. ..
  30. Krammer B, Verwanger T. Molecular response to hypericin-induced photodamage. Curr Med Chem. 2012;19:793-8 pubmed
    ..The different modes of cellular responses depend mainly on the PDT-protocol, photosensitizer localisation, cellular damage protection and the available intracellular energy. ..
  31. Moore C, Emberton M, Bown S. Photodynamic therapy for prostate cancer--an emerging approach for organ-confined disease. Lasers Surg Med. 2011;43:768-75 pubmed publisher
    ..This review will look at the work done to date, and the ongoing studies which help to define the place of PDT as a useful treatment modality for organ-confined prostate cancer. ..
  32. Bostad M, Berg K, Høgset A, Skarpen E, Stenmark H, Selbo P. Photochemical internalization (PCI) of immunotoxins targeting CD133 is specific and highly potent at femtomolar levels in cells with cancer stem cell properties. J Control Release. 2013;168:317-26 pubmed publisher
    ..The excellent high efficacy and selectivity of eliminating CD133-expressing cells by PCI warrant further pre-clinical evaluations of this novel therapeutic approach. ..
  33. Gokhale N. Corneal endothelial damage after collagen cross-linking treatment. Cornea. 2011;30:1495-8 pubmed publisher
    ..Corneal thickness is not the only factor for corneal endothelial damage after cross-linking procedure. ..
  34. Vega Estrada A, Alio J, Plaza Puche A, Marshall J. Outcomes of a new microwave procedure followed by accelerated cross-linking for the treatment of keratoconus: a pilot study. J Refract Surg. 2012;28:787-93 pubmed publisher
    ..To analyze the initial data obtained in a group of patients treated with microwave keratoplasty followed by accelerated corneal collagen cross-linking (CXL) for the correction of keratoconus...
  35. Chatzis N, Hafezi F. Progression of keratoconus and efficacy of pediatric [corrected] corneal collagen cross-linking in children and adolescents. J Refract Surg. 2012;28:753-8 pubmed publisher
    ..To study the progression rate of keratoconus and assess the clinical outcome of corneal collagen cross-linking (CXL) with riboflavin and ultraviolet A light in children and adolescent patients up to 3 years after treatment...
  36. Zotta P, Moschou K, Diakonis V, Kymionis G, Almaliotis D, Karamitsos A, et al. Corneal collagen cross-linking for progressive keratoconus in pediatric patients: a feasibility study. J Refract Surg. 2012;28:793-9 pubmed publisher
    ..To evaluate the outcomes of corneal collagen cross-linking (CXL) in pediatric patients with bilateral progressive keratoconus...
  37. Ferrari G, Iuliano L, Viganò M, Rama P. Impending corneal perforation after collagen cross-linking for herpetic keratitis. J Cataract Refract Surg. 2013;39:638-41 pubmed publisher
    ..However, corneal infection is itself a possible complication of this treatment. We describe a case of severe corneal thinning and melting in a woman who had a CXL procedure as a treatment for herpetic keratitis...
  38. Wang J, Giuntini F, Eggleston I, Bown S, MacRobert A. Photochemical internalisation of a macromolecular protein toxin using a cell penetrating peptide-photosensitiser conjugate. J Control Release. 2012;157:305-13 pubmed publisher
    ..This study demonstrates that the cell penetrating peptide-photosensitiser bioconjugation strategy is a promising and versatile approach for enhancing the therapeutic potential of bioactive agents through photochemical internalisation. ..
  39. Costa L, Faustino M, Neves M, Cunha A, Almeida A. Photodynamic inactivation of mammalian viruses and bacteriophages. Viruses. 2012;4:1034-74 pubmed publisher
  40. Yoo J, Kim C, Chung C, Jeong Y, Kang D. 5-aminolevulinic acid-incorporated poly(vinyl alcohol) nanofiber-coated metal stent for application in photodynamic therapy. Int J Nanomedicine. 2012;7:1997-2005 pubmed publisher
    ..Necrosis and apoptosis of tumor cells occurred similarly for ALA and ALA- PVA nanofiber treatments. The ALA-PVA nanofiber-coated stent is a promising candidate for therapeutic use with cholangiocarcinoma. ..
  41. Diez B, Ernst G, Teijo M, Batlle A, Hajos S, Fukuda H. Combined chemotherapy and ALA-based photodynamic therapy in leukemic murine cells. Leuk Res. 2012;36:1179-84 pubmed publisher
    ..Thus, ALA-PDT can overcome drug resistance and is a good candidate for using treating multidrug resistant (MDR) cells. ..
  42. Meire M, Coenye T, Nelis H, De Moor R. Evaluation of Nd:YAG and Er:YAG irradiation, antibacterial photodynamic therapy and sodium hypochlorite treatment on Enterococcus faecalis biofilms. Int Endod J. 2012;45:482-91 pubmed publisher
  43. Kharkwal G, Sharma S, Huang Y, Dai T, Hamblin M. Photodynamic therapy for infections: clinical applications. Lasers Surg Med. 2011;43:755-67 pubmed publisher
    ..We expect more to see applications of PDT to more challenging infections using advanced antimicrobial photosensitizers targeted to microbial cells in the years to come. ..
  44. Schumacher S, Oeftiger L, Mrochen M. Equivalence of biomechanical changes induced by rapid and standard corneal cross-linking, using riboflavin and ultraviolet radiation. Invest Ophthalmol Vis Sci. 2011;52:9048-52 pubmed publisher
    ..The new rapid protocol shortens the treatment duration by more than two thirds, from 30 to 9 minutes. The safety of the higher intensities must be addressed in further clinical studies. ..
  45. Kato I, Prates R, Sabino C, Fuchs B, Tegos G, Mylonakis E, et al. Antimicrobial photodynamic inactivation inhibits Candida albicans virulence factors and reduces in vivo pathogenicity. Antimicrob Agents Chemother. 2013;57:445-51 pubmed publisher
    ..The absence of alterations in daughter cells indicates that APDI effects are transitory. The MIC reduction for fluconazole following APDI suggests that this antifungal could be combined with APDI to treat C. albicans infections. ..
  46. Price M, Tenkman L, Schrier A, Fairchild K, Trokel S, Price F. Photoactivated riboflavin treatment of infectious keratitis using collagen cross-linking technology. J Refract Surg. 2012;28:706-13 pubmed publisher
    ..To evaluate riboflavin/ultraviolet-A (UVA) as an adjunct treatment for infectious keratitis...
  47. Wang J, Berg K, Høgset A, Bown S, MacRobert A. Photophysical and photobiological properties of a sulfonated chlorin photosensitiser TPCS(2a) for photochemical internalisation (PCI). Photochem Photobiol Sci. 2013;12:519-26 pubmed publisher
    ..The results demonstrate the favourable photophysical and photobiological properties of TPCS(2a) for PCI, which induces the relocalisation of a macromolecular anti-cancer toxin inside cells and significantly enhances cell death. ..
  48. Qiao X, Zhou J, Xiao J, Wang Y, Sun L, Yan C. Triple-functional core-shell structured upconversion luminescent nanoparticles covalently grafted with photosensitizer for luminescent, magnetic resonance imaging and photodynamic therapy in vitro. Nanoscale. 2012;4:4611-23 pubmed publisher
    ..Compared with the clinical commercial contrast agent Gd-DTPA, the as-fabricated nanomaterial showed a comparable longitudinal relaxivities value (r(1)) and similar imaging effect. ..
  49. Chen F, Zhang S, Bu W, Chen Y, Xiao Q, Liu J, et al. A uniform sub-50 nm-sized magnetic/upconversion fluorescent bimodal imaging agent capable of generating singlet oxygen by using a 980 nm laser. Chemistry. 2012;18:7082-90 pubmed publisher
    ..We envision that such a PDT drug will become a potential theranostic nanomedicine for future near-infrared laser-triggered photodynamic therapy and simultaneous magnetic/optical bimodal imaging...
  50. Vetter J, Brueckner S, Tubic Grozdanis M, Vossmerbaumer U, Pfeiffer N, Kurz S. Modulation of central corneal thickness by various riboflavin eyedrop compositions in porcine corneas. J Cataract Refract Surg. 2012;38:525-32 pubmed publisher
    ..05). There was considerable variation in the final CCT as a result of varying riboflavin eyedrop compositions. No author has a financial or proprietary interest in any material or method mentioned. ..
  51. Vera D, Haynes M, Ball A, Dai T, Astrakas C, Kelso M, et al. Strategies to potentiate antimicrobial photoinactivation by overcoming resistant phenotypes. Photochem Photobiol. 2012;88:499-511 pubmed publisher
    ..This review discusses the different antimicrobial PDT strategies and highlights the need for highly informative and comprehensive discovery approaches. ..
  52. Tomizawa Y, Tian J. Photodynamic therapy for unresectable cholangiocarcinoma. Dig Dis Sci. 2012;57:274-83 pubmed publisher
    ..PDT has also been reported to have a favorable outcome as adjuvant and neoadjuvant therapy for CC. Although accumulated data and local expertise are limited, PDT can be regarded as a standard palliative therapy for unresectable CC...
  53. Ryumina A, Serebrovskaya E, Shirmanova M, Snopova L, Kuznetsova M, Turchin I, et al. Flavoprotein miniSOG as a genetically encoded photosensitizer for cancer cells. Biochim Biophys Acta. 2013;1830:5059-67 pubmed publisher
    ..This is the first study to assess phototoxicity of miniSOG in cancer cells. The results suggest an effective ontogenetic tool and may be of interest for molecular and cell biology and biomedical applications. ..