Padeliporfin

DRACPC ID  DRACPC0024

Active Ingredients   Padeliporfin

Description  A vascular-acting photosensitizer consisting of a water-soluble, palladium-substituted bacteriochlorophyll derivative with potential antineoplastic activity. Upon administration, paldeliporfin is activated locally when the tumor bed is exposed to low-power laser light; reactive oxygen species (ROS) are formed upon activation and ROS-mediated necrosis may occur at the site of interaction between the photosensitizer, light and oxygen. Vascular-targeted photodynamic therapy (VTP) with padeliporfin may allow tumor-site specific cytotoxicity while sparing adjacent normal tissues.

Synonyms  Palladium-Bacteriochlorophyll Derivative WST11; WST11; Padeliporfin

Type  Small Molecule

Disease  Low Risk Prostate Cancer

Classification

  

Peptide and derivative Photosensitizing Agents

Structure Information


Molecular Formula  C37H43N5O9PdS

Molecular Weight  840.3

Active Sequence  Not available

Sequence Length  Not available

Modification  Not available

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  palladium(II) (7S,8S,17R,18R)-13-acetyl-7-(2-carboxyethyl)-18-ethyl-5-(2-methoxy-2-oxoethyl)-2,8,12,17-tetramethyl-3-((2-sulfoethyl)carbamoyl)-7H,8H,17H,18H-porphyrin-21,23-diide

InChI  InChI=1S/C37H45N5O9S.Pd/c1-8-22-17(2)25-16-30-33(21(6)43)19(4)27(40-30)14-26-18(3)23(9-10-31(44)45)35(41-26)24(13-32(46)51-7)36-34(37(47)38-11-12-52(48,49)50)20(5)28(42-36)15-29(22)39-25;/h14-18,22-23H,8-13H2,1-7H3,(H5,38,39,40,41,42,43,44,45,47,48,49,50);/q;+2/p-2/t17-,18+,22-,23+;/m1./s1

InChI_Key MZRDSGWDVDESRC-VNWQTDIGSA-L

SMILES  [H][C@]1(C2=N/C([C@]1(C)[H])=C\C3=C(C(C(C)=O)=C([N-]3)/C=C4N=C([C@](CC)([C@]\4(C)[H])[H])/C=C5[N-]/C(C(C(NCCS(=O)(O)=O)=O)=C\5C)=C2/CC(OC)=O)C)CCC(O)=O.[Pd+2]

External Codes


PubChem CID  76961489

DrugBank Accession Number  DB15575

NCI Thesaurus Code  C78481  

UNII  EEO29FZT86   GSRS

CAS  759457-82-4



Drug approval


Drug indication
    Padeliporfin is indicated for the treatment of adults with previously untreated, unilateral, low-risk, adenocarcinoma of the prostate with a life expectancy greater than or equal to 10 years.

Drug Name Strength Dosage Form/Route Company Marketing Status Drug ID Approval year
Tookad unknown Injectable; Intravenous Steba Biotech S.A Prescription EMEA/H/C/004182 2017

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT04620239 Multicenter Phase 3 Pivotal Study to Evaluate the Safety and Efficacy of TOOKAD (Padeliporfin) Vascular Targeted Photodynamic Therapy in the Treatment of Low Grade Upper Tract Urothelial Cancer Transitional Cell Cancer of Renal Pelvis and Ureter Phase 3 Treatment
NCT03617003 Phase I Study of WST11 Phototherapy for Upper Tract Urothelial Carcinoma Upper Tract Urothelial Carcinoma Phase 1 Treatment
NCT00975429 Vascular-Targeted Photodynamic Therapy Using WST11 in Patients With Localized Prostate Cancer Prostate Cancer Phase 2 Treatment
NCT01573156 Vascular Targeted Photodynamic Therapy With WST11 for T1a Renal Tumours. PHASE IIa Histological Follow up Trial Renal Cancer Phase 1/2 Treatment
NCT03133650 A Phase I Trial of Vascular-Targeted Photodynamic Therapy in Esophagogastric Cancer Patients With Moderate to Severe Dysphagia Esophagogastric Cancer; Moderate to Severe Dysphagia Phase 1 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





DRACP is developed by Dr.Zheng's team.