Foscan (temoporfin) / Biolitec - LARVOL DELTA

Safety Profile and Therapeutic Efficacy of Photodynamic Therapy for Early-Stage Endobronchial Carcinoma (ERS 2025) - "The photosensitizers used were Photofrin, Chlorin E6, and Foscan. The study included 36 patients (mean age: 65.4 ± 7.6 years; 19% female; mean FEV1: 51.6 ± 21.1%; mean DLCO: 46.2 ± 21.7%) with 61 lesions, of which 68.9% were multilocular. Fibrin exudation occurred in 90.6% of PDT procedures (n = 53), resulting in complete airway obstruction in 30.2% of cases within the treated area. One patient required prolonged mechanical ventilation due to severe fibrin exudation."

Clinical • Lung Cancer • Oncology • Solid Tumor

Bis-quaternary ammonium BODIPY derivatives: Photophysical, antimicrobial, and antitumor photodynamic applications. (PubMed, Bioorg Chem) - "Among these, brominated BODIPYs II3 and II5 exhibited high ROS generation efficiency and significant photodynamic antitumor activity against Eca-109 cells in vitro (IC50 = 0.22 μM and 0.36 μM) and in vivo, comparable to the control drug m-THPC...Furthermore, they achieved effective biofilm inhibition efficiencies of 86.74% and 85.23%, respectively, through the disruption of membrane integrity. These findings hold significant promise for pioneering new multifunctional photosensitizers that enable combined or sequential antimicrobial and antitumor photodynamic therapies."

Journal • Oncology

trans-A2B-Corroles containing an oxime moiety: Novel photosensitizers for photodynamic therapy of lung cancer. (PubMed, Eur J Med Chem) - "The lead photosensitizers, with IC50 values below 50 nM and no cytotoxicity per se, outperformed Temoporfin, the active compound in Foscan®, a clinically approved PS. This highlights oxime-functionalized trans-A2B-corroles as promising candidates for photodynamic therapy of LC. The in vivo efficacy of one oxime-corrole based PDT was also evaluated using the chick embryo chorioallantoic membrane model demonstrating its potential as an effective photosensitizer in vivo."

Journal • Lung Cancer • Oncology • Solid Tumor

Exploring the impact of photodynamic therapy conditioning on endometrial cancer cells (EACR 2025) - "The results indicate that the remaining EC cells exhibited similar DT and invasion profiles after PDT. Nevertheless, temoporfin appears to potentiate the migration ability of HEC-1-A cells. FCT supports CIBB (doi:10.54499/UIDB/04539/2020; doi:10.54499/UIDP/04539/2020; doi:10.54499/LA/P/0058/2020); CQC (doi:10.54499/UIDB/00313/2020; doi:10.54499/UIDP/00313/2020; TEMA (doi:10.54499/UIDB/00481/2020), UIDP/00481/2020 (doi:10.54499/UIDP/00481/2020); Projects CarboNCT (doi:10.54499/2022.03596.PTDC) and Chem4LungCare (doi:10.54499/PTDC/QUI-QOR/0103/2021); PhD Scholarship from FCT and European Social Fund to BS (10.54499/2020.07672.BD)."

Endometrial Cancer • Oncology • Solid Tumor

Rational molecular design of two-photon activated temoporfin: a computational study for advanced photodynamic therapy. (PubMed, Phys Chem Chem Phys) - "Simulations in a biological membrane model confirmed favorable interactions and localization of the candidate PDT agents within lipid bilayers, supporting their potential for enhanced clinical applications. This study demonstrates that rational molecular design can improve both the optical properties and the drug-delivery proficiency of temoporfin, paving the way for more effective deep-tissue PDT treatments."

Journal • Oncology

Mechanistic insights into temoporfin-based photodynamic therapy: Ferroptosis as a critical regulator under normoxic and hypoxic conditions in head and neck cancer. (PubMed, J Photochem Photobiol B) - "Administration of the ferroptosis inhibitor BRD4770 under normoxic conditions reversed temoporfin-based PDT-induced reductions in glutathione peroxidase 4 (GPx4), increasing in light chain 3-II (LC3-II) and cleaved poly (ADP-ribose) polymerase (cleaved-PARP). This study confirms that hypoxia weakens the anticancer effects of temoporfin-based PDT and that ferroptosis plays a key role in temoporfin-based PDT-mediated cancer cell inhibition."

Journal • Head and Neck Cancer • Oncology • Oral Cancer • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • GPX4

Assessment of Bimodal Laser Photodynamic Therapy at Wavelenths of 410 nm and 653 nm for Oral Precancerous Lesions: An In Vitro and In Vivo Study. (PubMed, Photodiagnosis Photodyn Ther) - "The dual-wavelength PDT, optimized for m-THPC, exhibits superior photodynamic characteristics and excellent biosafety. It aligns well with realistic clinical applic ation scenarios and presents as an innovative and promising therapeutic modality for the treatment of oral leukoplakia."

Journal • Preclinical • Oncology • Oral Cancer

Significant Tumor Inhibition of Trimethyl-152-[L-aspartyl]pheophorbide a in Tumor Photodynamic Therapy‡. (PubMed, ChemMedChem) - "It exhibited excellent phototoxicity higher than reference compound m-THPC when irradiated by 650 nm light in vitro, and obvious photodynamic anti-tumor effect in vivo...The observed high efficacy was rationalized by efficient introduction into the blood by facile transfer through membranes, which is supported by molecular dynamics simulation studies. This work provides a new candidate photosensitizer for anti-cancer treatment."

Journal • Oncology

The Effects of Temoporfin-Mediated Photodynamic Inactivation on Leishmania tropica Promastigotes and Molecular Docking Analysis (PubMed, Mikrobiyol Bul) - "Temoporfin ile kırmızı ışık kombinasyonu, L.tropica promastigotlarını invaziv olmayan bir tedavi olarak inaktive etme potansiyeline sahiptir. Tedavide kullanılan FDT bileşenleri olan kırmızı ışık ve temoporfinin herhangi bir sitotoksik etkisinin bulunmaması, amastigot veya hayvan modelleri üzerine yapılacak daha ileri çalışmalar için önemli bir fırsat sunmakta ve potansiyel klinik uygulamalara zemin hazırlamaktadır."

Journal

Efficacy of Canal Disinfectants Temoporfin, Carbon Nanoparticles, and Er: YAG Laser on Martens Hardness, Smear Layer Removal, and Bond Strength of Glass Fiber Posts to Canal Dentin. (PubMed, Photodiagnosis Photodyn Ther) - "Push-out bond strength was highest in Group 2 (9.98 ± 0.14 MPa at the cervical level) and Group 4 (10.08 ± 0.21 MPa), while Group 1 showed a decrease in apical bond strength of (5.11 ± 0.19 MPa) CNPs and Er:YAG laser treatments, in comparison to Temoporfin and NaOCl, significantly increase dentin hardness and bond strength while reducing SL. This finding suggests that the incorporation of these innovative disinfection methods into endodontic procedures may enhance the durability and success of glass fiber post restorations."

Journal • Gastrointestinal Disorder

Exploring the GSTP1 inhibition potential of photosensitizer compounds for enhanced cancer treatment in photodynamic therapy. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "Among the tested photosensitizers, zinc phthalocyanine, hypericin, and temoporfin emerged as the top candidates, exhibiting binding energies of - 10.8, - 10.2, and - 9.8 kcal/mol, along with Ki values of 0.012, 0.033, and 0.064 µM, respectively. These compounds outperformed the reference inhibitor ethacrynic acid, which had a binding energy of - 6.6 kcal/mol and a Ki of 14.35 µM. These findings suggest that the dual action of these photosensitizers provides a promising strategy for combating cancer and overcoming treatment resistance."

Journal • Oncology • GSTP1

Efficient Delivering of a Photodynamic Therapy Drug into Cellular Membranes Rationalized by Molecular Dynamics. (PubMed, J Phys Chem B) - "In this article, we rationalize the behavior of a temoporfin-based PDT drug, commercialized under the name of Foscan, complexed by two β-cyclodextrin units, acting as drug carriers, in the presence of a lipid bilayer...The factors favoring penetration and dissociation have also been analyzed, together with membrane perturbation due to the interaction with the drug carrier complex. Our results confirm the suitability of this encapsulation strategy for PDT and rationalize the experimental results concerning its efficacy."

Journal

Screening of photosensitizers-ATP binding cassette (ABC) transporter interactions in vitro. (PubMed, Cancer Drug Resist) - " The ABCG2 inhibitor (fumitremorgin C) and P-gp inhibitor (valspodar) effectively blocked the transport mediated by ABCG2 and P-gp of rose bengal and BPD... In summary, our study provided new knowledge that temoporfin, talaporfin sodium, methylene blue, and indocyanine green are not substrates of ABCG2, P-gp, or MRP1...Rose bengal is a substrate of ABCG2, P-gp, and MRP1. The results presented here indicate ABC transporter substrate status as a possible cause for cellular resistance to photodynamic therapy with rose bengal, redaporfin, and BPD."

Journal • Preclinical • Breast Cancer • Oncology • Solid Tumor • ABCB1 • ABCC1 • ABCG2

Drug repositioning identifies potential autophagy inhibitors for the LIR motif p62/SQSTM1 protein. (PubMed, Comput Biol Chem) - "The results revealed that the kanamycin, velpatasvir, verteporfin, and temoporfin significantly decreased the binding of LIR to the p62 protein. Finally, we experimentally confirmed that Kanamycin can inhibit autophagy-associated acidic vesicular formation in breast cancer MCF-7 and MDA-MB 231 cells. These repositioned drugs may represent novel autophagy modulators in clinical management, warranting further investigation."

Journal • Breast Cancer • Oncology • Solid Tumor • SQSTM1

Spectroscopic insights into BSA-mediated deaggregation of m-THPC. (PubMed, Sci Rep) - "These results underscore the potential of BSA to preserve the monomeric form of m-THPC, mitigating aggregation-induced losses in singlet oxygen production. Our findings suggest that BSA-mediated delivery systems could play a crucial role in optimizing the clinical utility of hydrophobic photosensitizers like m-THPC."

Journal

High yield seedless synthesis of mini gold nanorods: partial silver decoupling allows effective nanorod elongation with tunable surface plasmon resonance beyond 1000 nm and CTAB-free functional coating for mTHPC conjugation. (PubMed, Nanoscale Adv) - "A single mild reducing agent, hydroquinone, allowed for up to ∼98% reaction yield from a gold precursor. A mechanism for elongation is proposed based on partial silver decoupling from the reaction. Finally, the particles were coated with various capping agents to allow functionalization and conjugation of mTHPC drug molecules, which are used in photodynamic treatments, and cytotoxic CTAB was removed to increase their biocompatibility."

Journal

Orthoflaviviral Inhibitors in Clinical Trials, Preclinical In Vivo Efficacy Targeting NS2B-NS3 and Cellular Antiviral Activity via Competitive Protease Inhibition. (PubMed, Molecules) - "NS3-NS4B inhibitors, such as JNJ-64281802 and EYU688, show promise, recently entering clinical trials, underscoring the importance of developing novel viral replication inhibitors targeting viral machinery. To date, the only NS2B-NS3 inhibitor that has undergone clinical trials is doxycycline, however, its mechanism of action and clinical efficacy as viral growth inhibitor require additional investigation. SYC-1307, an allosteric inhibitor, exhibits high in vivo efficacy, while temoporfin and methylene blue represent promising orthosteric non-competitive inhibitors. Compound 71, a competitive NS2B-NS3 inhibitor, emerges as a leading preclinical candidate due to its high cellular antiviral efficacy, minimal cytotoxicity, and favorable in vitro pharmacokinetic parameters. Challenges remain in developing competitive NS2B-NS3 inhibitors, including appropriate biochemical inhibition assays as well as the selectivity and conformational flexibility of the protease, complicating..."

Journal • Preclinical • Review • Dengue Fever • Infectious Disease

Computational modelling of the therapeutic outputs of photodynamic therapy on spheroid-on-chip models. (PubMed, J Photochem Photobiol B) - "The composition of PS is critical, as ALA-PpIX induces earlier cell death but accelerates oxygen consumption, especially in the outer layers, depriving the inner layers of oxygen necessary for PDT, which in turn disrupts and prolongs the exposure time compared to mTHPC and Photofrin. Despite the fluence rate directly influencing the singlet oxygen generation rate, increasing the fluence rate by 189 mW/cm2 would not significantly benefit us. Microwell height and inlet flow rate involve competing phenomena-increasing height or decreasing flow reduces oxygen supply and increases PS "washout" and its concentration."

Journal

Temoporfin-Conjugated PEGylated Poly(N,N-dimethylacrylamide)-Coated Upconversion Colloid for NIR-Induced Photodynamic Therapy of Pancreatic Cancer. (PubMed, Biomacromolecules) - "The coating consisted of alendronate-terminated poly[N,N-dimethylacrylamide-co-2-aminoethylacrylamide]-graft-poly(ethylene glycol) [P(DMA-AEM)-PEG-Ale] to ensure the chemical and colloidal stability of the particles in aqueous physiological fluids, thereby also improving the therapeutic efficacy. The designed particles were well tolerated by the human pancreatic adenocarcinoma cell lines CAPAN-2, PANC-1, and PA-TU-8902. After intratumoral injection of mTHPC-conjugated polymer-coated UCNPs and subsequent exposure to 980 nm NIR light, excellent PDT efficacy was achieved in tumor-bearing mice."

Journal • Gastrointestinal Cancer • Hepatology • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Solid Tumor

Effectiveness of photodynamic therapy on treatment response and survival in patients with recurrent oral squamous cell carcinoma: a systematic review. (PubMed, Photodiagnosis Photodyn Ther) - "Although treatment response differs between treatment protocols, PDT stands as a viable treatment option to be considered, as it can achieve therapeutic results and disease-free, long-lasting periods. Partial treatment responses may be of interest when achieving eligibility for other treatment strategies. Despite this study's limitations considering four photosensitisers, Photofrin® was the most used but more recent photosensitisers like Foscan have greater chemical stability, tissue penetration, and may be more efficacious on recurrent OSCC."

Journal • Review • Head and Neck Cancer • Oncology • Oral Cancer • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck

Repurposing anti-cancer porphyrin derivative drugs to target SARS-CoV-2 envelope. (PubMed, Biomed Pharmacother) - "Here, we characterize the ability of temoporfin, verteporfin, talaporfin and redaporfin to inactivate SARS-CoV-2 infectious particles. Our results suggest that viral envelope affinity, with penetration and destabilization of the lipid bilayer, seems critical to mediate PDs antiviral activity. Altogether, these findings open new avenues for the off-label application of temoporfin and verteporfin in the systemic treatment of COVID-19."

Journal • Infectious Disease • Novel Coronavirus Disease • Oncology • Respiratory Diseases

Third-Generation Anticancer Photodynamic Therapy Systems Based on Star-like Anionic Polyacrylamide Polymer, Gold Nanoparticles, and Temoporfin Photosensitizer. (PubMed, Molecules) - "In this study, we demonstrate, as proof of concept, a successful application of the developed PDT system for in vitro treatment of triple-negative breast cancer cells under irradiation with a low-power LED lamp (660 nm). We consider the developed nanocomposite to be a promising PDT system for application to other types of cancer."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

Understanding the interactions between repurposed drugs sertindole and temoporfin with receptor for advanced glycation endproducts: Therapeutic implications in cancer and metabolic diseases. (PubMed, J Mol Model) - "To gain deeper insights into the binding mechanisms of the elucidated candidate repurposed drugs, sertindole and temoporfin with RAGE, we conducted extensive all-atom MD simulations, spanning 500 nanoseconds (ns). These simulations elucidated the conformational dynamics and stability of the RAGE-sertindole and RAGE-temoporfin complexes."

Journal • Metastases • CNS Disorders • Metabolic Disorders • Oncology

Homologous-targeting biomimetic nanoparticles co-loaded with melittin and a photosensitizer for the combination therapy of triple negative breast cancer. (PubMed, J Mater Chem B) - "Here, we designed novel biomimetic nanoparticles based on homologous tumor cell membranes and poly(lactic-co-glycolic acid) (PLGA)/poly(beta-aminoester) (PBAE), denoted MDM@TPP, which efficiently coloaded the cytolytic peptide Mel and the photosensitizer mTHPC...Moreover, Mel combined with photodynamic therapy (PDT) can synergistically kill tumor cells and induce significant immunogenic cell death, thereby stimulating the maturation of dendritic cells (DCs). In 4T1 tumor-bearing mice, MDM@TPP nanoparticles effectively inhibited the growth and metastasis of primary tumors and finally prevented tumor recurrence by improving the immune response."

Combination therapy • Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

Comparative response to PDT with methyl-aminolevulinate and temoporfin in cutaneous and oral squamous cell carcinoma cells. (PubMed, Sci Rep) - "Therefore, we propose that intracellular localization of GSK3β could be a good marker of response to PDT in HNSCC. Although the molecular mechanism of response to PDT needs further elucidation, this work shows that the most MAL-resistant line of CSCC is more sensitive to Temoporfin."

Journal • Head and Neck Cancer • Oncology • Oral Cancer • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • GSK3B