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  Talaporfin  Sodium

Description of Talaporfin sodium: Talaporfin sodium is  a natural chlorophyll-based, and water soluble PDT photosensitizer consisting of chlorin e6, derived from chlorophyll, and L-aspartic acid with photosensitizing activity. After intratumoral activation by light emitting diodes, talaporfin sodium forms an extended high energy conformational state that generates singlet oxygen, which can kill target tissues with minimal side effects through vascular closure and apoptosis. Constant illumination can activate each molecule of talaporfin many times, resulting in a continuous supply of singlet oxygen molecules. Talaporfin kills all tumour cells in the targeted zone, rather than only the minority of cells undergoing rapid division, as in the case of chemotherapy. There are no serious toxicities to date. Talaporfin sodium was approved in 2004 in Japan, and is currently in phase III trials in USA. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer: Light Sciences Oncology.

Talaporfin (INN, also known as aspartyl chlorin, mono-L-aspartyl chlorine e6, NPe6, or LS11) is a photosensitizer used in photodynamic therapy (PDT). It absorbs red light at 664nm normally provided by a laser tuned to this wavelength. Talaporfin was approved in Japan (in 2004) for PDT of lung cancer and marketed as Laserphyrin.

Development status: talaporfin was approved in Japan in 2004, but not yet in USA.  Light Sciences Oncology (LSO) is developing Aptocine™ (talaporfin sodium) for solid tumors as well as other indications such as BPH. Aptocine is a water-soluble drug targeted by a small, single-use, disposable drug activator included with the drug. Aptocine is designed to provide tolerable, effective, and repeatable treatments for patients. LSO has completed treatment of patients in a Phase 3 trial of Aptocine in hepatocellular carcinoma (HCC) and in a Phase 3 trial for metastatic colorectal cancer (MCRC). LSO is also conducting clinical trials in benign prostatic hyperplasia (BPH), or enlargement of the prostate, and has clinical or preclinical programs in cardiovascular, ophthalmic, and dermatologic diseases. Aptocine has three potential primary mechanisms of action: direct tumor cytotoxicity, apoptosis due to vascular shutdown, and anti-tumor immune stimulation. In clinical studies to date, Aptocine has been well-tolerated with no evidence that Aptocine causes the serious toxicities associated with traditional cancer treatments. (source: http://www.lsoncology.com/).

Chemical and physical properties of Talaporfin:
Talaporfin is dark blue-green powder, soluble in water. Talaporfin is also hygroscopic and light sensitive. Therefore talaporfin should be stored under dry and protected from light (easily way to this is to use alumina foil to wrap the container).  Talaporfin's absorption max (phosphate buffer, pH 7.4): 400 nm, 654 nm (e 180000, 40000). Absorption max (dioxane): 402 nm, 663 nm (EmM 111, 38).

Useful data about talaporfin sodium:

The singlet oxygen quantum yield of  talaporfin was 0.5– 0.8 (0.56 in water and 0.77 in methanol). Talaporfin sodium has a serum t1⁄2 alpha of 9 hours and is excreted unmetabolized, predominantly by the biliary system. (Cancer. 2003 Oct 15;98(8):1767-71.)

Original Literature References of Talaporfin: Semisynthetic derivative of chlorin e6, q.v. Photosensitizer activated at 664 nm by laser or light-emitting diode-based light infusion device. Causes irreversible tumor blood vessel closure. Prepn: J. C. Bommer, B. F. Burnham, EP 168831; eidem, US 4675338 (1986, 1987 both to Nippon Petrochemicals). Photophysical properties: J. D. Spikes, J. C. Bommer, J. Photochem. Photobiol. B 17, 135 (1993); L. Li et al., ibid. 67, 51 (2002). Chemical and NMR structural studies: S. Gomi et al., Heterocycles 48, 2231 (1998). Safety assessment in treatment of refractory solid tumors: R. A. Lustig et al., Cancer 98, 1767 (2003). Clinical evaluation in lung cancer: H. Kato et al., Lung Cancer 42, 103 (2003).

Highlight of recent research using Talaporfin sodium

Bile duct carcinoma treatment using talaporfin sodium: The efficacy of adjuvant photodynamic therapy (PDT) using the new photosensitizer, talaporfin sodium (TPS), was assessed in 7 patients with bile duct carcinoma (BDC). Locally advanced tumor occluding bile duct was relieved by PDT and patency was maintained for 16 months. Two patients developed mild photodermatitis but no severe morbidity. One patient died of other disease, and two patients died of liver metastasis within 6 months, but local recurrence was not observed. Three patients maintained cancer-free survival for 6-13 months. One patient survived with good status for 24 months. Adjuvant TPS-PDT is a safe and useful treatment for local control of BDC. Compared to the conventional PDT, the patient's quality of life is remarkably improved.  (source: Anticancer Res. 2012 Nov;32(11):4931-8.).

Local failure after chemoradiotherapy for esophageal cancer using  talaporfin sodium: 9 patients with local failure after CRT or RT for ESCC were enrolled and treated in groups of 3 individuals to the third fluence level. No DLT was observed at any fluence level. Phototoxicity was not observed, but one subject had grade 1 fever, three had grade 1 esophageal pain, and 1 had grade 1 dysphagia. Five of 9 patients (55.6%) achieved a complete response after PDT. PDT using talaporfin sodium and a diode laser was safe for local failure after RT in patients with esophageal cancer. The recommended fluence for the following phase II study is 100 J/cm². (source: Radiat Oncol. 2012 Jul 23;7:113. doi: 10.1186/1748-717X-7-113.)

Malignant gliomas using  talaporfin sodium. PDT achieved a response rate of 80% at the treated sites in the 6 patients with newly diagnosed malignant gliomas. In these patients, the median progression-free survival time was 23 months. The median survival time in 3 patients who died was 26 months, and the remaining 3 patients survived for more than 3 years with a good Karnofsky Performance Scale (KPS). In the 8 patients with recurrent tumors who received PDT, their response rate was low (25.0%), their gliomas recurred 3 months after PDT, and their survival time was only 9 months following PDT. No adverse events directly attributable to PDT occurred in any patients. Protection against light was only required for approximately 3 days after PDT.  PDT in addition to surgical resection achieved better therapeutic results than conventional protocols, especially in patients with newly diagnosed malignant gliomas.  (source: Photodiagnosis Photodyn Ther. 2012 Jun;9(2):91-9).

Sonodynamically-induced antitumor effect of NPe6. The rate of ultrasonically-induced damage on isolated sarcoma 180 cells in air-saturated suspension was enhanced two-fold with 80 μM NPe6. The co-administration of 25 mg/kg NPe6 followed by ultrasonic exposure at 2 MHz suppressed the growth of implanted colon 26 cell tumors at an intensity at which ultrasound alone showed only a slight antitumor effect. These in vitro and in vivo results suggest that NPe6 is a potential sensitizer for sonodynamic tumor treatment. The enhancement of cell damage by NPe6 was significantly inhibited by histidine, which may suggest reactive oxygen species plays a primary role in sonodynamically-induced antitumor effect. (source: Anticancer Res. 2011 Feb;31(2):501-6.)

1: Miki Y, Akimoto J, Yokoyama S, Homma T, Tsutsumi M, Haraoka J, Hirano K, Beppu M. Photodynamic Therapy in Combination with Talaporfin Sodium Induces Mitochondrial Apoptotic Cell Death Accompanied with Necrosis in Glioma Cells. Biol Pharm Bull. 2012 Nov 29. [Epub ahead of print] PubMed PMID: 23196427.

2: Nanashima A, Abo T, Nonaka T, Nonaka Y, Morisaki T, Uehara R, Ohnita K, Fukuda D, Murakami G, Tou K, Kunizaki M, Hidaka S, Tsuchiya T, Takeshita H, Nakao K, Nagayasu T. Photodynamic therapy using talaporfin sodium (Laserphyrin®) for bile duct carcinoma: a preliminary clinical trial. Anticancer Res. 2012 Nov;32(11):4931-8. PubMed PMID: 23155262.

3: Nonaka Y, Nanashima A, Nonaka T, Uehara M, Isomoto H, Abo T, Nagayasu T. Synergic effect of photodynamic therapy using talaporfin sodium with conventional anticancer chemotherapy for the treatment of bile duct carcinoma. J Surg Res. 2012 Jul 13. [Epub ahead of print] PubMed PMID: 22835954.

4: Yano T, Muto M, Yoshimura K, Niimi M, Ezoe Y, Yoda Y, Yamamoto Y, Nishisaki H, Higashino K, Iishi H. Phase I study of photodynamic therapy using talaporfin sodium and diode laser for local failure after chemoradiotherapy for esophageal cancer. Radiat Oncol. 2012 Jul 23;7:113. doi: 10.1186/1748-717X-7-113. PubMed PMID: 22824179; PubMed Central PMCID: PMC3410784.

5: Horimatsu T, Muto M, Yoda Y, Yano T, Ezoe Y, Miyamoto S, Chiba T. Tissue damage in the canine normal esophagus by photoactivation with talaporfin sodium (laserphyrin): a preclinical study. PLoS One. 2012;7(6):e38308. doi: 10.1371/journal.pone.0038308. Epub 2012 Jun 13. PubMed PMID: 22719875; PubMed Central PMCID: PMC3374776.

6: Akimoto J, Haraoka J, Aizawa K. Preliminary clinical report on safety and efficacy of photodynamic therapy using talaporfin sodium for malignant gliomas. Photodiagnosis Photodyn Ther. 2012 Jun;9(2):91-9. doi: 10.1016/j.pdpdt.2012.01.001. Epub 2012 Feb 28. PubMed PMID: 22594978.

7: Bromley E, Briggs B, Keltner L, Wang SS. Characterization of cutaneous photosensitivity in healthy volunteers receiving talaporfin sodium. Photodermatol Photoimmunol Photomed. 2011 Apr;27(2):85-9. doi: 10.1111/j.1600-0781.2011.00573.x. PubMed PMID: 21392111.

8: Ito A, Kimura T, Miyoshi S, Ogawa S, Arai T. Photosensitization reaction-induced acute electrophysiological cell response of rat myocardial cells in short loading periods of talaporfin sodium or porfimer sodium. Photochem Photobiol. 2011 Jan-Feb;87(1):199-207. doi: 10.1111/j.1751-1097.2010.00846.x. Epub 2010 Nov 29. PubMed PMID: 21114668.

9: Kishi K, Yano M, Inoue M, Miyashiro I, Motoori M, Tanaka K, Goto K, Eguchi H, Noura S, Yamada T, Ohue M, Ohigashi H, Ishikawa O. Talaporfin-mediated photodynamic therapy for peritoneal metastasis of gastric cancer in an in vivo mouse model: drug distribution and efficacy studies. Int J Oncol. 2010 Feb;36(2):313-20. PubMed PMID: 20043064.

10: Wang S, Bromley E, Xu L, Chen JC, Keltner L. Talaporfin sodium. Expert Opin Pharmacother. 2010 Jan;11(1):133-40. doi: 10.1517/14656560903463893. Review. PubMed PMID: 20001435.

11: Tomioka Y, Kushibiki T, Awazu K. Evaluation of oxygen consumption of culture medium and in vitro photodynamic effect of talaporfin sodium in lung tumor cells. Photomed Laser Surg. 2010 Jun;28(3):385-90. doi: 10.1089/pho.2008.2468. PubMed PMID: 19860571.

12: Ohshiro T, Nakajima T, Ogata H, Kishi K. Histological responses of cutaneous vascular lesions following photodynamic therapy with talaporfin sodium: a chicken comb model. Keio J Med. 2009 Sep;58(3):176-84. PubMed PMID: 19826211.

13: Tsurubuchi T, Zoboronok A, Yamamoto T, Nakai K, Yoshida F, Shirakawa M, Matsuda M, Matsumura A. The optimization of fluorescence imaging of brain tumor tissue differentiated from brain edema--in vivo kinetic study of 5-aminolevulinic acid and talaporfin sodium. Photodiagnosis Photodyn Ther. 2009 Mar;6(1):19-27. doi: 10.1016/j.pdpdt.2009.03.005. Epub 2009 May 5. PubMed PMID: 19447368.

14: Namatame H, Akimoto J, Matsumura H, Haraoka J, Aizawa K. Photodynamic therapy of C6-implanted glioma cells in the rat brain employing second-generation photosensitizer talaporfin sodium. Photodiagnosis Photodyn Ther. 2008 Sep;5(3):198-209. doi: 10.1016/j.pdpdt.2008.08.001. Epub 2008 Oct 22. PubMed PMID: 19356656.

15: Nakagishi Y, Morimoto N, Fujita M, Ozeki Y, Maehara T, Kikuchi M, Morimoto Y. Amelioration of airway stenosis in rabbit models by photodynamic therapy with talaporfin sodium (NPe6). Photochem Photobiol. 2009 May-Jun;85(3):714-8. doi: 10.1111/j.1751-1097.2008.00472.x. Epub 2008 Nov 19. PubMed PMID: 19067947.

16: Torikai E, Kageyama Y, Kohno E, Hirano T, Koide Y, Terakawa S, Nagano A. Photodynamic therapy using talaporfin sodium for synovial membrane from rheumatoid arthritis patients and collagen-induced arthritis rats. Clin Rheumatol. 2008 Jun;27(6):751-61. Epub 2007 Dec 8. PubMed PMID: 18066613.

17: Usuda J, Tsutsui H, Honda H, Ichinose S, Ishizumi T, Hirata T, Inoue T, Ohtani K, Maehara S, Imai K, Tsunoda Y, Kubota M, Ikeda N, Furukawa K, Okunaka T, Kato H. Photodynamic therapy for lung cancers based on novel photodynamic diagnosis using talaporfin sodium (NPe6) and autofluorescence bronchoscopy. Lung Cancer. 2007 Dec;58(3):317-23. Epub 2007 Aug 15. PubMed PMID: 17698240.

18: Kujundzić M, Vogl TJ, Stimac D, Rustemović N, Hsi RA, Roh M, Katicić M, Cuenca R, Lustig RA, Wang S. A Phase II safety and effect on time to tumor progression study of intratumoral light infusion technology using talaporfin sodium in patients with metastatic colorectal cancer. J Surg Oncol. 2007 Nov 1;96(6):518-24. PubMed PMID: 17671969.

19: Ohmori S, Arai T. In vitro behavior of Porfimer sodium and Talaporfin sodium with high intensity pulsed irradiation. Lasers Med Sci. 2006 Dec;21(4):213-23. Epub 2006 Sep 22. PubMed PMID: 17024319.

20: Tsukagoshi S; Tokyo Cooperative Oncology Group. [Development of a novel photosensitizer, talaporfin sodium, for the photodynamic therapy (PDT)]. Gan To Kagaku Ryoho. 2004 Jun;31(6):979-85. Review. Japanese. PubMed PMID: 15222124.

21: Lustig RA, Vogl TJ, Fromm D, Cuenca R, Alex Hsi R, D'Cruz AK, Krajina Z, Turić M, Singhal A, Chen JC. A multicenter Phase I safety study of intratumoral photoactivation of talaporfin sodium in patients with refractory solid tumors. Cancer. 2003 Oct 15;98(8):1767-71. PubMed PMID: 14534895.

22: Talaporfin sodium. LS 11, ME 2906, mono-L-aspartyl chlorine e6, NP e6, NPE 6, taporfin sodium. Drugs R D. 2003;4(2):135-7. PubMed PMID: 12723579.

23: Talaporfin: LS 11, LS11, ME 2906, mono-L-aspartyl chlorin e6, NP e6, NPE 6, taporfin sodium. Drugs R D. 2003;4(1):69-71. Review. Corrected and republished in: Drugs R D. 2003;4(2):135-7. PubMed PMID: 12568643.