- •This first-in-man clinical trial established the safety, pharmacokinetics, maximum tolerated and recommended phase II dose for the doxorubicin (Dox) prodrug DTS-201 in solid tumour patients.
- •DTS-201 was administered at four dose levels ranging from 80 to 400 mg/m2, equivalent to 45–225 mg/m2 of conventional Dox per administration, resulting in high cumulative anthracycline exposure.
- •Diarrhoea, vomiting and neutropenia were dose limiting and 400 mg/m2 DTS-201 was the maximum tolerated and recommended phase II dose for the enzyme-activated prodrug.
- •DTS-201 is well tolerated and safe in solid tumour patients and is not associated with treatment-related severe cardiac adverse events, even at very high acute and cumulative anthracycline doses tested.
- •More than half of the patients derived clinical benefit during treatment with DTS-201, achieving either disease stabilisation or a confirmed partial response.
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