Clinical ReportsLifePearl microspheres loaded with irinotecan in the treatment of Liver-dominant metastatic colorectal carcinoma: feasibility, safety and pharmacokinetic studyMaleux, Geerta; Prenen, Hansb; Helmberger, Thomasc; Spriet, Isabelled; Isailovic, Tatjana(V)e; Pereira, PhilippefAuthor Information aDepartment of Radiology, University Hospital Leuven, Leuven bDepartment of Oncology, University Hospital Antwerp (UZ Antwerp), Antwerp, Belgium cInstitut für Diagnostische und Interventionelle Radiologie, München, Germany dUniversity of Leuven, Pharmacotechnology and Biopharmacy Leuven, Belgium eSchool of Medicine, University of Belgrade, Belgrade, Serbia fDepartment of Radiology, Minimal-Invasive Therapies and Nuclear Medicine, SLK Kliniken Heilbronn, Heilbronn, Germany Received 12 June 2020 Revised form accepted 6 July 2020 Correspondence to Geert Maleux, PhD, MD, Department of Vascular Surgery, University Hospital Leuven, Leuven, Belgium, Tel: +32 0 16 34 37 82; fax: +32 0 16 34 37 65; e-mail: [email protected] Anti-Cancer Drugs: November 2020 - Volume 31 - Issue 10 - p 1084-1090 doi: 10.1097/CAD.0000000000000980 Buy Metrics Abstract To evaluate pharmacokinetic and safety profile of LifePearl microspheres loaded with irinotecan (LifePearl-IRI) in the treatment of liver-dominant, metastatic colorectal carcinoma (LM-CRC) by transarterial chemoembolization. In a prospective, multicentre pharmacokinetic study, 14 patients with LM-CRC progressing on at least one line of chemotherapy were treated with LifePearl-IRI. Six patients received unilobar treatment, treating one lobe per session with 100 mg of irinotecan every 2 weeks. Eight patients received bilobar treatment, treating two lobes per session with 100 mg of irinotecan each (200 mg in total), every 4 weeks. At 24 h, near complete plasma clearance occurred for both irinotecan and SN-38, regardless of the dose. Mean plasma Cmax(100 mg) was 254.50 ± 104.17 ng/mL for irinotecan and 46.72 ± 13.75 ng/mL for SN-38. Mean Cmax(200 mg) was 970.09 ± 353.75 ng/mL for irinotecan and 118.45 ± 25.11 ng/mL for SN-38. Significantly higher Cmax-iri(200 mg) than Cmax-iri (100 mg) supported rate-limiting irinotecan-to-SN-38 conversion. Adverse events during the first 30 days upon initial treatment were hypertension in 21.4%, abdominal pain in 14.3%, and increased transaminases and fever in 7.1% of patients. Four serious adverse events were noted: respiratory failure, constipation, necrotizing pancreatitis, and ischaemic cholecystitis. Chemoembolization with LifePearl-IRI is technically feasible and relatively well tolerated, with a good pharmacokinetic profile and minimal systemic exposure of both irinotecan and SN-38, after both unilobar and bilobar treatment with 100 or 200 mg, respectively. Copyright © 2020 Wolters Kluwer Health, Inc. All rights reserved.