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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
Current developer: Light Sciences Oncology.
220201-34-3 (Talaporfin sodium
Chemical Formula: C38H37N5Na4O9
Molecular Weight: 799.69
Elemental Analysis: C, 57.07; H, 4.66; N, 8.76; Na,
11.50; O, 18.01
Talaporfin (free acid form)
Exact Mass: 711.29043
Molecular Weight: 711.76
Elemental Analysis: C,
64.12; H, 5.81; N, 9.84; O, 20.23
Availability and price:
sodium (purity > 95%) is in stock.
Chemical structure and
purity were confirmed by H1-NMR, C13-NMR, MS, HPLC analysis.
Express shipping cost: $30.00 inside USA
(overnight), $70.00 for international(3-5 days). Price
10 mg / $130.00
20 mg / $210.00
50 mg / $450.00
100 mg / $650.00
200 mg / $980.00
Grams in stock
at big discount price. Kilograms available through custom
500 mg / $1,950.00, 1 g /
$3,250.00, 2g/ $5,450.00
To ask for
quotation, please send email to
email@example.com to describe your needs. A representative
will respond your email shortly. We offer big discount for
orders of bulk quantities.
Quality control data:
Copies of C13-NMR, H1-NMR, HPLC, MS are
available upon request.
Information about this agent
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:
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
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
Highlight of recent research using Talaporfin sodium
Bile duct carcinoma treatment using talaporfin sodium:
The efficacy of adjuvant photodynamic therapy (PDT) using the new
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.
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:
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:
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
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:
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.
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