A Cancer Research UK phase I trial combining the dinitrobenzamide prodrug CB1954 (tretazicar) and the NQO2 substrate EP-0152R (caricotamide) intravenously (IV) every 3 weeks


Session type:

Emma Cattell1, Debashis Sarker3, Diana Anderson3, Victoria Spanswick4, Scott Davies2, R Agarwal3, Nicki Heywood1, David Kerr2, Ian Judson3, John Hartley4, Mark Middleton1

1Churchill Hospital, Oxford, UK, 2University of Oxford, UK,3Royal Marsden Hospital, Sutton, UK, 4University College London, UK



CB1954 (CB) is a dinitrobenzamide prodrug that is converted in the presence of the enzyme NQO2 and co-substrate EP-0152R (EP) into a potent cytotoxic bifunctional alkylating agent.


Patients (pts) with histologically confirmed advanced solid tumours and WHO Performance Status 0 - 2 were treated with CB and EP. CB was administered IV over 15 minutes midway through a 4 hour IV infusion of EP every 3 weeks. Objectives were to determine the maximum tolerated dose (MTD) and dose limiting toxicities (DLT) of the combination, evaluate pharmacokinetics (PK) and pharmacodynamic (PD) effects and describe antitumour activity.