padeliporfin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
benzoporphyrin derivatives	5273	759457-82-4

Description:

Molecule	Description
Synonyms: padeliporfin tookad padeliporfin potassium padeliporfin dipotassium	Padeliporfin is retained within the vascular system. When activated with 753 nm wavelength laser light, padeliporfin triggers a cascade of pathophysiological events resulting in focal necrosis within a few days. Activation within the illuminated tumour vasculature, generates oxygen radicals causing local hypoxia that induces the release of nitric oxide radicals. This results in transient arterial vasodilatation that triggers the release of the vasoconstrictor, endothelin-1. Rapid consumption of the NO radicals, by oxygen radicals, leads to the formation of reactive nitrogen species (RNS) (e.g. peroxynitrite), in parallel to arterial constriction. In addition, impaired deformability is thought to enhance erythrocyte aggregability and formation of blood clots at the interface of the arterial supply (feeding arteries) and tumour microcirculation, results in occlusion of the tumour vasculature. This is enhanced by RNS-induced endothelial cell apoptosis and initiation of self-propagated tumour cells necrosis through peroxidation of their membrane. Molecular weight: 768.19 Formula: C34H39N5O7PdS CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: 157.56 ALOGS: ROTB: None

Molecule

Description

Synonyms:

padeliporfin
tookad
padeliporfin potassium
padeliporfin dipotassium

Padeliporfin is retained within the vascular system. When activated with 753 nm wavelength laser light, padeliporfin triggers a cascade of pathophysiological events resulting in focal necrosis within a few days. Activation within the illuminated tumour vasculature, generates oxygen radicals causing local hypoxia that induces the release of nitric oxide radicals. This results in transient arterial vasodilatation that triggers the release of the vasoconstrictor, endothelin-1. Rapid consumption of the NO radicals, by oxygen radicals, leads to the formation of reactive nitrogen species (RNS) (e.g. peroxynitrite), in parallel to arterial constriction. In addition, impaired deformability is thought to enhance erythrocyte aggregability and formation of blood clots at the interface of the arterial supply (feeding arteries) and tumour microcirculation, results in occlusion of the tumour vasculature. This is enhanced by RNS-induced endothelial cell apoptosis and initiation of self-propagated tumour cells necrosis through peroxidation of their membrane.

Molecular weight: 768.19
Formula: C34H39N5O7PdS
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA: 157.56
ALOGS:
ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Nov. 10, 2017	EMA	STEBA Biotech S.A

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01XD07	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Sensitizers used in photodynamic/radiation therapy

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Adenocarcinoma of prostate	indication	399490008	DOID:2526

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

ID	Source
EEO29FZT86	UNII
698393-30-5	SECONDARY_CAS_RN
C2698706	UMLSCUI
CHEMBL4594284	ChEMBL_ID
76961489	PUBCHEM_CID
DB15575	DRUGBANK_ID
CHEMBL4594285	ChEMBL_ID
D10973	KEGG_DRUG
8679	INN_ID
C456120	MESH_SUPPLEMENTAL_RECORD_UI
C503696	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None