Delving into the Latest Updates on Talaporfin Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Aptocine, Leserfin, Litx

+ [14]

Target-

Mechanism

Photosensitizers

Therapeutic Areas

NeoplasmsNervous System DiseasesDigestive System Disorders+ [1]

Active Indication

Esophageal CarcinomaBrain CancerLung Cancer

Inactive Indication

Breast CancerCardiovascular DiseasesChoroidal Neovascularization+ [16]

Originator Organization

Meiji Seika Pharma Co., Ltd.

Active Organization

Meiji Seika Pharma Co., Ltd.

Inactive Organization

Light Sciences Oncology, Inc.Light Sciences, Inc.

Drug Highest PhaseApproved

First Approval Date

JP (16 Oct 2003),

Lung Cancer

RegulationOrphan Drug (JP)

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Structure

Molecular FormulaC38H41N5Na4O9

InChIKeyDSZWCAQEOJGGCM-LBARBQQXSA-N

CAS Registry220201-34-3

We describe a case of gastric cancer treated by photodynamic therapy (PDT) with talaporfin sodium using a novel simultaneous light‐emitting method. An 82‐year‐old man was diagnosed with gastric cancer near the cardia with suspected deep submucosal invasion. Surgical resection was deemed high‐risk owing to an underlying pulmonary disease. After ruling out endoscopic procedures due to intense fibrosis resulting from the scarring, PDT with talaporfin sodium was chosen. PDT was successfully conducted using an endoscope with simultaneous light emission. The patient experienced a complete response to the treatment and showed no signs of recurrence during follow‐up. This case highlights the potential of PDT with talaporfin sodium as a viable alternative for challenging cases, particularly in patients unsuitable for surgery and endoscopic resection. Furthermore, the novel simultaneous light‐emitting method may improve the efficiency of the procedure. This case demonstrates the potential of PDT in gastric cancer treatment, especially for high‐risk patients.

01 Feb 2024·Journal of gastroenterology

Induction of ferroptosis by photodynamic therapy and enhancement of antitumor effect with ferroptosis inducers

Article

Author: Kataoka, Hiromi ; Kojima, Yuki ; Kubota, Eiji ; Shimura, Takaya ; Sasaki, Makiko ; Tanaka, Mamoru ; Ozeki, Keiji

BACKGROUND:

Photodynamic therapy (PDT) is an effective tumor treatment that involves the administration of a photosensitizer to generate cytotoxic ¹O₂ [reactive oxygen species (ROS)] from molecular oxygen that is produced from energy absorption following tumor irradiation at specific wavelengths. Ferroptosis is induced by the disruption of the glutathione peroxidase 4 (GPX4) antioxidant system, leading to lipid peroxidation. We hypothesized that talaporfin sodium-photodynamic therapy (TS-PDT)-generated ROS would lead to ferroptosis via accumulation of lipid peroxidation.

METHODS:

Cell viability assay in TS-PDT-treated cells in combination with a ferroptosis inhibitor (ferrostatin-1: Fer-1) or ferroptosis inducers (imidazole ketone erastin: IKE, Ras-selective lethal 3: RSL3) was performed. Accumulation of lipid peroxidation, GPX4 antioxidant system and cystine/glutamate antiporter (system xc^-) activity in TS-PDT-treated cells was investigated. In xenograft mice, the antitumor effect of TS-PDT in combination with ferroptosis inducers (IKE or sorafenib) was examined.

RESULTS:

TS-PDT-induced cell death was partly suppressed by Fer-1 and accompanied by lipid peroxidation. TS-PDT combined with IKE or RSL3 enhanced the induction of cell death. TS-PDT inhibited cystine uptake activity via system xc^-. In vivo, the combination of TS-PDT and ferroptosis inducers (IKE or sorafenib) reduced tumor volume.

CONCLUSION:

This study found that the mechanism underlying TS-PDT-induced ferroptosis constitutes direct lipid peroxidation by the generated ROS, and the inhibition of system xc^-, and that the combination of a ferroptosis inducer with TS-PDT enhances the antitumor effect of TS-PDT. Our findings suggest that ferroptosis-inducing therapies combined with PDT may benefit cancer patients.

01 Dec 2023·European journal of medicinal chemistry

Novel chlorin e6-based conjugates of tyrosine kinase inhibitors: Synthesis and photobiological evaluation as potent photosensitizers for photodynamic therapy

Article

Author: Yao, Jian-Zhong ; Sheng, Chun-Quan ; Han, Gui-Yan ; Li, Bu-Hong ; Huang, Fei ; Zhang, Xing-Jie ; Lin, Hui-Ying ; Li, Yu ; Lin, Hui-Yun ; Miao, Zhenyuan ; Lin, Mei-Yu

Since tyrosine kinase inhibitor (TKI) could reverse ABCG2-mediated drug-resistance, novel chlorin e₆-based conjugates of Dasatinib and Imatinib as photosensitizer (PS) were designed and synthesized. The results demonstrated that conjugate 10b showed strongest phototoxicity against HepG2 and B16-F10 cells, which was more phototoxic than chlorin e₆ and Talaporfin. It could reduce efflux of intracellular PS by inhibiting ABCG2 in HepG2 cells, and localize in mitochondria, lysosomes, golgi and ER, resulting in higher cell apoptosis rate and ROS production than Talaporfin. Moreover, it could induce cell autophagy and block cell cycle in S phase, and significantly inhibit tumor growth and prolong survival time on BALB/c nude mice bearing HepG2 xenograft tumor to a greater extent than chlorin e₆. Consequently, compound 10b could be applied as a promising candidate PS due to its good water-solubility and stability, low drug-resistance, high quantum yield of ¹O₂ and excellent antitumor efficacy in vitro and in vivo.

100 Deals associated with Talaporfin Sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
D01985	Talaporfin Sodium	L01	DB11812

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Esophageal Carcinoma	JP	Meiji Seika Pharma Co., Ltd.	20 May 2015
Brain Cancer	JP	Meiji Seika Pharma Co., Ltd.	20 Sep 2013
Lung Cancer	JP	Meiji Seika Pharma Co., Ltd.	16 Oct 2003

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Colorectal Cancer	Phase 3	AT	Light Sciences Oncology, Inc.	01 Feb 2007
Colorectal Cancer	Phase 3	BA	Light Sciences Oncology, Inc.	01 Feb 2007
Colorectal Cancer	Phase 3	HR	Light Sciences Oncology, Inc.	01 Feb 2007
Colorectal Cancer	Phase 3	DE	Light Sciences Oncology, Inc.	01 Feb 2007
Colorectal Cancer	Phase 3	IN	Light Sciences Oncology, Inc.	01 Feb 2007
Colorectal Cancer	Phase 3	IT	Light Sciences Oncology, Inc.	01 Feb 2007
Colorectal Cancer	Phase 3	LV	Light Sciences Oncology, Inc.	01 Feb 2007
Colorectal Cancer	Phase 3	PL	Light Sciences Oncology, Inc.	01 Feb 2007
Colorectal Cancer	Phase 3	RO	Light Sciences Oncology, Inc.	01 Feb 2007
Colorectal Cancer	Phase 3	RU	Light Sciences Oncology, Inc.	01 Feb 2007

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00440310 (CTgov)	Phase 3	Liver metastases \| Colorectal Cancer \| Local Neoplasm Recurrence	483	Interstitial light emitting diodes+leucovorin+irrinotecan+oxaliplatin+fluorouracil+Talaporfin sodium (Litx + Chemotherapy)	vntdrinkto(nmwxrkrjal) = cprtoqhljv nuqlylllus (ieoscnoegy, vhniakbnlr - qopgbtnonl) View more	-	25 Aug 2015
NCT00440310 (CTgov)	Phase 3		483	leucovorin+irrinotecan+oxaliplatin+fluorouracil (Chemotherapy Alone)	vntdrinkto(nmwxrkrjal) = ngpvcgfrzt nuqlylllus (ieoscnoegy, kcrmbtspqf - ymzlnqicec) View more	-	25 Aug 2015
JPRN-UMIN000003970 (ASCO_GI2012)	Phase 1	Oesophageal squamous cell carcinoma recurrent \| Esophageal Carcinoma	9	Talaporfin sodium-based PDT	zxamuxnipq(nnoglrwexf) = trwqhunekf kowazpuumr (vgrkykbian )	-	01 Feb 2012
ASCO2006	Not Applicable	Lung Cancer	204	Laserphyrin	kedvifpmod(ohdsrkfpdx) = xbaesoeurn hlsuftnlcj (easuevsqkn )	-	20 Jun 2006
ASCO2005	Phase 2	Colorectal Liver Metastases	10	Talaporfin sodium + intratumoral placement of LEDs	fwmbgrwtzg(yfsgyiluum) = aeribubvae aojxpmvghm (gjhmjrmwha )	-	01 Jun 2005