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+ [17]

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

View All Structures (2)

Porphyrins have emerged as highly effective photosensitizers in the field of photodynamic therapy (PDT) because of their high singlet oxygen generation efficiency. However, most porphyrin derivatives do not have adequate water solubility and cell membrane permeability suitable for use in PDT. In addition, they frequently suffer from low durability under photoirradiation. Here, we propose rotaxane-type photosensitizers, in which a porphyrin axle is irreversibly encapsulated within cyclodextrins (CDs), to overcome the drawbacks of porphyrins for PDT. The rotaxane-type photosensitizers were synthesized in high yields by employing a cooperative capture strategy. The CD derivatives worked as a transparent shell to impart a porphyrin axle not only with water solubility but also with photostability. These rotaxanes showed higher cell membrane permeability and photoinduced cytotoxic abilities than talaporfin sodium, presently used as a clinical photosensitizer. The rotaxane-based photosensitizer could have potential for being ideal PDT drugs.

01 Oct 2024·World Neurosurgery

The Safety of Intraoperative Photodynamic Diagnosis Using 5-Aminolevulinic Acid Combined with Talaporfin Sodium Photodynamic Therapy in Recurrent High-Grade Glioma

Article

Author: Miki, Shunichiro ; Matsuda, Masahide ; Kohzuki, Hidehiro ; Tsurubuchi, Takao ; Ishikawa, Eiichi ; Sugii, Narushi ; Zaboronok, Alexander

BACKGROUNDIntraoperative photodynamic diagnosis (PDD) using 5-aminolevulinic acid (5-ALA) is a widely adopted technique to enhance the extent of resection during high-grade glioma (HGG) surgery. Recent updates to the package insert for 5-ALA in Japan now allow its use in combination with drugs that may induce photosensitivity, such as talaporfin sodium (TS). TS is employed in intraoperative photodynamic therapy (PDT) and has been shown to improve overall survival. The combination of 5-ALA with TS is expected to offer further benefits. However, the safety of this combination had not been established. This study reports on the safety of 5-ALA-PDD with TS-PDT in the treatment of recurrent HGG.METHODS7 patients with recurrent HGG underwent tumor resection using a combination of 5-ALA-PDD and TS-PDT. The incidence of photosensitivity as an adverse effect associated with 5-ALA and TS was evaluated as described in the package insert. Adverse events were assessed according to the Common Terminology Criteria for Adverse Events (CTCAE) version 5.0.RESULTSTumor-specific fluorescence intensity was strong in 4 cases and weak in 3. Photosensitivity occurred in only 1 patient (14.3%). Three patients exhibited CTCAE grade 1 or 2 abnormal liver function, and 1 patient experienced CTCAE grade 1 γ-GTP elevation. All abnormalities improved during follow-up.CONCLUSIONSThe combined use of 5-ALA-PDD and TS-PDT for HGG surgery did not increase the risk of serious adverse events in our study. Further investigations with a larger number of cases are needed for a more accurate assessment of its safety and efficacy.

01 Jul 2024·Biomedicine & Pharmacotherapy

Repurposing anti-cancer porphyrin derivative drugs to target SARS-CoV-2 envelope

Article

Author: Cadima-Couto, Iris ; Schaberle, Fabio A ; Arnaut, Luis G ; Castanho, Miguel A R B ; Arnaut, Zoe A ; Mendonça, Diogo A ; Buga, Carolina C ; Cruz-Oliveira, Christine

Antiviral medicines to treat COVID-19 are still scarce. Porphyrins and porphyrin derivatives (PDs) usually present broad-spectrum antiviral activity with low risk of resistance development. In fact, some PDs are clinically approved to be used in anti-cancer photodynamic therapy and repurposing clinically approved PDs might be an alternative to treat COVID-19. Here, we characterize the ability of temoporfin, verteporfin, talaporfin and redaporfin to inactivate SARS-CoV-2 infectious particles. PDs light-dependent and -independent effect on SARS-CoV-2 infectivity were evaluated. PDs photoactivation successfully inactivated SARS-CoV-2 with very low concentrations and light dose. However, only temoporfin and verteporfin inactivated SARS-CoV-2 in the dark, being verteporfin the most effective. PDs treatment reduced viral load in infected Caco-2 cells, while not inducing cytotoxicity. Furthermore, light-independent treatment with temoporfin and verteporfin act on early stages of viral infection. Using lipid vehicles as membrane models, we characterized PDs interaction to the viral envelope. Verteporfin presented the lowest IC50 for viral inactivation and the highest partition coefficients (K_p) towards lipid bilayers. Curiously, although temoporfin and redaporfin presented similar K_ps, redaporfin did not present light-independent antiviral activity, and only temoporfin and verteporfin caused lipid membrane disorder. In fact, redaporfin is located closer to the bilayer surface, while temoporfin and verteporfin are located closer to the centre. Our results suggest that viral envelope affinity, with penetration and destabilization of the lipid bilayer, seems critical to mediate PDs antiviral activity. Altogether, these findings open new avenues for the off-label application of temoporfin and verteporfin in the systemic treatment of COVID-19.

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
Unresectable Hepatocellular Carcinoma	Discovery	HR	Light Sciences Oncology, Inc.	01 Jul 2006
Unresectable Hepatocellular Carcinoma	Discovery	KR	Light Sciences Oncology, Inc.	01 Jul 2006
Unresectable Hepatocellular Carcinoma	Discovery	IN	Light Sciences Oncology, Inc.	01 Jul 2006
Unresectable Hepatocellular Carcinoma	Discovery	PH	Light Sciences Oncology, Inc.	01 Jul 2006
Unresectable Hepatocellular Carcinoma	Discovery	MY	Light Sciences Oncology, Inc.	01 Jul 2006
Unresectable Hepatocellular Carcinoma	Discovery	RS	Light Sciences Oncology, Inc.	01 Jul 2006
Unresectable Hepatocellular Carcinoma	Discovery	SE	Light Sciences Oncology, Inc.	01 Jul 2006
Unresectable Hepatocellular Carcinoma	Discovery	SG	Light Sciences Oncology, Inc.	01 Jul 2006
Unresectable Hepatocellular Carcinoma	Discovery	TH	Light Sciences Oncology, Inc.	01 Jul 2006
Unresectable Hepatocellular Carcinoma	Discovery	HK	Light Sciences Oncology, Inc.	01 Jul 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


UEGW2024	Not Applicable	Neoplasms	-	Talaporfin PDT	mglbyakkng(tpmlqolaou) = kdvzaeydzz hrjqvfyipk (nysnnubvqp ) View more	-	13 Oct 2024
UEGW2024	Not Applicable	Neoplasms	-	Talaporfin (STING knockout cells)	mglbyakkng(tpmlqolaou) = oghhsbhhwi hrjqvfyipk (nysnnubvqp ) View more	-	13 Oct 2024
UEGW2019	Not Applicable	Esophageal Carcinoma	-	Talaporfin sodium	alxuptgsmn(tzhklvcnow) = osyexdisiu fwedybsyzs (qmdypnrxuz )	-	01 Oct 2019
NCT00440310 (CTgov)	Phase 3	Liver metastases \| Colorectal Cancer \| Local Neoplasm Recurrence	483	Interstitial light emitting diodes+leucovorin+irrinotecan+oxaliplatin+fluorouracil+Talaporfin sodium (Litx + Chemotherapy)	(giwqpbbudw) = xmesaituna wiimrghsts (mhpdxmrwzj, snomecdtta - ypdqntexwx) View more	-	25 Aug 2015
NCT00440310 (CTgov)	Phase 3		483	leucovorin+irrinotecan+oxaliplatin+fluorouracil (Chemotherapy Alone)	(giwqpbbudw) = ftljfgvhzd wiimrghsts (mhpdxmrwzj, wlvlxuxawi - htseirhzox) View more	-	25 Aug 2015
JPRN-UMIN000003970 (ASCO_GI2012)	Phase 1	Oesophageal squamous cell carcinoma recurrent \| Esophageal Carcinoma	9	Talaporfin sodium-based PDT	(snvgasdgac) = tswspygihl jjdxkemvvx (kosaoybuip )	-	01 Feb 2012
ASCO2006	Not Applicable	Lung Cancer	204	Laserphyrin	(syyljhjxwo) = nuhmxqimap oqdwgmmbsw (taxdvfhufx )	-	20 Jun 2006
ASCO2005	Phase 2	Colorectal Liver Metastases	10	Talaporfin sodium + intratumoral placement of LEDs	(irqyhebmwt) = gbvxwspktw bjdksqdowo (wlthogbkwi )	-	01 Jun 2005