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Alternative Tumor-Targeting Strategies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Temoporfin (FoscanTM) is a second-generation photosensitizing agent (Figure 10.31) based on the chlorin chemical skeleton (Figure 10.28) that was introduced in the mid- to late 1990s. Used for PDT, it is photoactivated by red light at 652 nm. The main advantage of temoporfin over porfimer sodium is that it is a discrete chemical moiety containing one chlorin unit rather than a polymeric mixture (as with porfimer sodium). Structures of temoporfin (FoscanTM) and vertiporfen (VisudyneTM).
Drug and Chemical Photosensitivity: Exogenous
Published in Henry W. Lim, Herbert Hönigsmann, John L. M. Hawk, Photodermatology, 2007
James Ferguson, Vincent A. DeLeo
Two intravenous photosensitizers used therapeutically to induce phototoxic damage of systemic tumors, include Photofrin® (porfimer sodium) and Foscan® (temoporfin). Both are associated with persistent phototoxicity, which is visible wavelength–dependent and potentially severe. Following intravenous injection, patients who have been administered Photofrin are encouraged to avoid bright sunlight and even incandescent light for four to six weeks. Some patients may develop severe phototoxicity within the infusion arm beyond this period suggesting that the drug persists at a higher concentration at that site much longer than elsewhere in the body. Work is underway to produce agents more rapidly eliminated, although such an agent, Verteporfin, has been associated with severe skin photosensitization (60).
Trial watch: an update of clinical advances in photodynamic therapy and its immunoadjuvant properties for cancer treatment
Published in OncoImmunology, 2023
Mafalda Penetra, Luís G. Arnaut, Lígia C. Gomes-da-Silva
With the intention of surpassing the limitations of porfimer sodium toward a better photosensitizer, researchers have attempted to design new molecules that fulfill the properties of an ideal photosensitizer. Some progress has been made which led to the emergence of second-generation photosensitizers such as temoporfin (Fotolon®) and talaporfin (Foscan®) chlorins which are characterized by high absorptions at 650–660 nm: ε650 nm = 39000 M−1 cm−1 in EtOH; ε652 nm = 23000 M−1 cm−1 in H2O for temoporfin and ε654 nm = 40000 M−1 cm−1 in PBS for talaporfin14,15. PDT with temoporfin was approved for the treatment of advanced head and neck cancer by the European Medicines Agency (EMA) in 2001 but its market authorization was declined by the FDA. It requires lower PDT regimens (PS = 0.1 to 0.3 mg/kg and LD = 8 to 12 J/cm2), which denotes its higher potency when compared to porfimer sodium. On the other hand, talaporfin is only approved in Japan for the treatment of advanced lung cancer (2004) and esophageal cancer (2015). Patients submitted to PDT with temoporfin or talaporfin are advised to avoid light exposition for c.a. 2 weeks16,17.
Unification of medicines and excipients: The roles of natural excipients for promoting drug delivery
Published in Expert Opinion on Drug Delivery, 2023
Minfang Feng, Xingxing Dai, Cuiting Yang, Yingying Zhang, Yuting Tian, Qingsong Qu, Mengke Sheng, Zhixun Li, Xinhui Peng, Shuai Cen, Xinyuan Shi
Some studies have also incorporated bioactive ingredients like flavonoids [160] and essential oil [211] into liposomes to modify the liposome and named flavosome and invasome. These ingredients play a role in modulating deformability, increasing the fluidity of the lipid bilayers of the skin, etc. The addition of flavonoids makes the liposome more deformable, resulting in its ability to penetrate through the deeper layers of skin, endow liposomes with a specific pharmacological effect, and enhance their efficacy. For instance, dihydroquercetin or quercetin [160] was added to conventional liposomes to load meloxicam, which performed better deformability and improved meloxicam’s permeability through the skin. This flavosome co-delivery meloxicam and dihydroquercetin or quercetin to exert anti-inflammatory effects. However, it was observed that the EE of meloxicam decreased when increased quercetin concentration at 0.72 ± 0.01 mg/mL. The described effects may be related to quercetin the similar water solubility and log P value as meloxicam. Therefore, quercetin is likely to embed within the lipid layer and compete with meloxicam. Terpenes in the invasome disrupt the stratum corneum lipids’ tight structure and improve lipids’ fluidity to enhance transdermal penetration. NinaDragicevic-Curic et al. prepared the invasome to encapsulate Temoporfin which showed better penetration. A schematic diagram of the structure of the flavosome and invasome is shown in Figure 3.
Biopredictive tools for the development of injectable drug products
Published in Expert Opinion on Drug Delivery, 2022
Mônica Villa Nova, Kennard Gan, Matthias G. Wacker
Similar to other drug substances encapsulated in liposomes, the photosensitizer temoporfin exhibits poor aqueous solubility and cannot be administered without being formulated. Therefore, we employed an advanced in-silico model to calculate the pharmacokinetic parameters of non-liposomal temoporfin [33]. A better understanding of the distribution and elimination rates of temoporfin is crucial in the identification of the liposome-related accumulation and elimination rates. Temoporfin is a lipophilic compound with a high affinity to the lipid bilayer of the liposomes [124]. The release behavior is mainly driven by partitioning of the drug between the liposomes and the physiological acceptor phase. Serum proteins play a key role in solubilizing the compound [72]. These major influences were identified from the literature as outlined in the suggested workflow (Figure 2), followed by their integration into a computer model.