Vascular targeted photochemotherapy using padoporfin and padeliporfin as a method of the focal treatment of localised prostate cancer - clinician’s insight

Table 1 Selected physicochemical and pharmacokinetic properties of padoporfin and padeliporfin

Parameter	Value
	Padoporfin	Padeliporfin
logP (octanol-water)	1.38[55]	-0.19[55]
Apparent volume of distribution (mL)	10.9[55]	22.12[55]
Alfa half-life (min)	11.86[58]	21.65[55]
Beta half-life (h)	11.3[58]	-
Total body clearance (mL/min)	10.18[58]	20.89[55]
Maximal plasma concentration (mg/L)	119[58]	252[47]
Maximal plasma concentration time (min)	15[58]	22[47]
Plasma LDL binding (%)	330[61]	35[61]
Plasma HDL binding (%)	350[61]	315[61]
Plasma HDP binding (%)	315[61]	380[61]
Standard intravenous drug dose (mg/kg)	2[66]	4[61]
Standard radiation fluence (J/cm)	200[83]	200[66]
Drug-light interval (min)	10[66]	10[66]
Standard irradiation wavelength (nm)	763[66]	753[66]

¹Results obtained for mice with transplanted breast tumor cells after 5 mg/kg intravenous injection;

²Results obtained for healthy mice after 6 mg/kg intravenous injection;

³Results obtained for human protein fractions in vitro. LDL: Low level density lipoprotein; HDL: High density lipoprotein; HDP: High density protein.

Table 2 Vascular targeted photodynamic therapy using padoporfin and padeliporfin in the treatment of localised prostate cancer - clinical trials

Phase	No. of patients	Photosensitizer	Radiation	Ref.
I	10	Padoporfin, 0.1-2 mg/kg (0.1, 0.25, 1 and 2 mg/kg)	763 nm, 100-360 J/cm	Weersink et al[83]
I	24	Padoporfin, 0.1-2 mg/kg	763 nm, 100, 230 and 360 J/cm	Trachtenberg et al[56]
I/II	15	Padoporfin, 0.1-2 mg/kg	763 nm, 100 J/cm	Gertner et al[84]
I/II	34	Padoporfin, 2 mg/kg	763 nm, 100-300 J/cm	Arumainayagam et al[86]
I/II	30	Padeliporfin, 2, 4 and 6 mg/kg	753 nm, 200 and 300 J/cm	https://clinicaltrials.gov/ct2/show/NCT00946881[87]
II	28	Padoporfin, 2 mg/kg	763 nm, 0.1-1000 J/cm	Trachtenberg et al[57]
II	40	Padeliporfin, 2, 4 and 6 mg/kg	753 nm, 200 J/cm	Arumainayagam et al[72]
II	40	Padeliporfin, 2-6 mg/kg	753 nm, 200 J/cm	Quoraishi et al[74]
II	85	Padeliporfin, 4 mg/kg	753 nm, 200 J/cm	Azzouzi et al[88]
II	56	Padeliporfin, 4 mg/kg	753 nm, 200 J/cm	Eymerit-Morin et al[89]
II	86	Padeliporfin, 4 and 6 mg/kg	753 nm, 200 and 300 J/cm	https://clinicaltrials.gov/ct2/show/-NCT00975429[90]
II	117	Padeliporfin, 4 mg/kg	753 nm, 200 J/cm	Azzouzi et al[62]
II	40	Padeliporfin, 2, 4 and 6 mg/kg	753 nm, 200 J/cm	Moore et al[67]
II	40	Padeliporfin, 2, 4 and 6 mg/kg	753 nm, 200 and 300 J/cm	https://http://www.clinicaltrials.gov/ct2/show/nct00707356[92]
II/III	86	Padeliporfin, 4 mg/kg	753 nm, 200 J/cm	Azzouzi et al[91]
II/III	16	Padoporfin, 2 mg/kg	763 nm, no information on radiation fluence	https://http://www.clinicaltrials.gov/ct2/show/-nct00312442[93]
II/III	1	Padeliporfin, 4 mg/kg	753 nm, 200 J/cm	Azzouzi et al[94]
II/III	19	Padeliporfin, 4 and 6 mg/kg	753 nm, 200 and 300 J/cm	Lebdai et al[95]
III	81	Padeliporfin, 4 mg/kg	753 nm, 200 J/cm	https://clinicaltrials.gov/ct2/show/-NCT01875393[96]
III	400	Padeliporfin, 4 mg/kg	753 nm, 200 J/cm	https://clinicaltrials.gov/show/-NCT01310894[97]