PURPOSEPhotodynamic therapy (PDT) schedules are based on sensitiser dose, light dose, and drug-light interval. The aim of the phase Ι study was to choose optimal dose and drug-light interval for PDT with photocyanine using pharmacokinetics (PK) and pharmacodynamics (PD).METHODSTwenty-eight cancer patients were enrolled. In trial A, 12 patients received one of four ascending doses of photocyanine intravenously 24 h prior to 180-270 J/cm² illumination. 0.2 mg/kg dose was infused to ten patients 12-48 h prior to 120 J/cm² illumination in trial B. In trial C, 0.1 mg/kg dose was infused to six patients 6 or 12 h prior to 180-270 J/cm² illumination. Serum concentrations of photocyanine were measured, and simulations were performed to assess the effect of drug exposure in tissue on responses.RESULTSAnalysis of photocyanine levels of patients indicated that the two-compartment model best fit the data. Simulations showed that the rates of the drug entering tissues and leaving tissues were equal at 8-12 h after injection. Patients experienced pain which was related to photocyanine serum levels, especially with serum levels above 2500 ng/ml. Fewer non-responders were observed at serum levels higher than 1000 ng/ml for illumination at least 12 h after administration.CONCLUSIONIt is the first report of human trials of photocyanine, and the results suggested that patients receive 180 J/cm² illumination about 20-30 min at serum concentrations of photocyanine between 1000 and 2500 ng/ml at least 10 h after administration.

01 Nov 2018·Journal of Chromatography AQ2 · CHEMISTRY

Development of a quantitative method for four photocyanine isomers using differential ion mobility and tandem mass spectrometry and its application in a preliminary pharmacokinetics investigation

Q2 · CHEMISTRY

Article

Author: Zheng, Xin ; Yu, Huaidong ; Jiang, Ji ; Cui, Xinge

Photodynamic therapy (PDT) has been accepted as an alternative treatment for cancer, and its target specificity can be achieved by controlling the location at which light activates the photosensitizer. Photocyanine, a novel anticancer phthalocyanine-based photosensitizer, is a mixture of 4 cis-isomers of a series of synthetic products, and accordingly, it is essential to verify whether there are differences in pharmacokinetics among the four isomers for clinical application, which requires reliable analytical methods to measure the plasma concentrations of the four isomers. An efficient LC-MS/MS method coupled with differential mobility spectrometry (DMS) for the simultaneous quantification of the four photocyanine isomers in human plasma was developed and validated herein. This method had a limit of quantification of 10 ng mL^-1 for each isomer and showed stable and reproducible inter- and intra-day results. Use of this method in preliminary pharmacokinetic studies in patients with esophageal cancer showed that the exposure and distribution of the four isomers were different, which had not been found in previous studies. The present research revealed that DMS was an effective tool for isomeric quantitation and that LC-DMS-MS/MS presented robust and reliable in biomatrix analysis. The method significantly improved peak separation and sensitivity compared with that of other LC-MS-based methods.

01 Sep 2014·Journal of Chromatographic ScienceQ4 · CHEMISTRY

Determination of Photocyanine in Human Serum by HPLC and Application to Pharmacokinetic Study

Q4 · CHEMISTRY

Article

Author: Li, Su ; Zhan, Jing ; Jian, Feng-Bi ; Zou, Ben-Yan ; Liao, Hai

Photocyanine, a novel amphoteric phthalocyanine drug, showed favorable anticancer activity in vivo. Pharmacokinetic study in cancer patients is an important component in dose administration choice. In this study, a rapid, sensitive analytical method based on high-performance liquid chromatography with ultraviolet detection was developed and validated for the determination of four isomers of photocyanine (FD1-4) in cancer patients. Sample preparation involved liquid-liquid extraction with a combination of ultrasound and N,N-dimethyl formamide. Calibration curves (1/x(2)) offered satisfactory linearity for the four isomers of photocyanine. The lower limit of quantification (LLOQ) for FD1-3 isomers was 30 ng/mL, and LLOQ for FD-4 was 5 ng/mL. Inter- and intra-day accuracies for four isomers ranged from 96.6 to 105.5%, and 95.0 to 103.6%, respectively. Inter- and intra-day precision ranged from 4.8 to 8.9%, and 3.6 to 12.2%, respectively. Stability studies showed that photocyanine was stable. This method was successfully used to quantify photocyanine in a pharmacokinetic study in which a single-dose of photocyanine (0.1 mg/kg) was intravenously administered to patients with cancer. On the basis of the discovery that photocyanine has a half-life of 57.5 h in vivo, we suggest that avoiding light for a longer period is essential for patients undergoing photocyanine therapy.

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Indication	Highest Phase	Country/Location	Organization	Date
Gastrointestinal Neoplasms	Phase 1	-	Fuzhou University	-
Gastrointestinal Neoplasms	Phase 1	-	Chinese Academy of Medical Sciences	-
Skin Neoplasms	Phase 1	-	Fuzhou University	-
Skin Neoplasms	Phase 1	-	Chinese Academy of Medical Sciences	-

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