Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 59, Issue 7, Pages 2918-2927Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b02025
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Funding
- Research Council of Norway
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Oncolytic immunotherapies represent a new promising strategy in the treatment of cancer. In our efforts to develop oncolytic peptides, we identified a series of chemically modified 9-mer cationic peptides that were highly effective against both drug-resistant and drug-sensitive cancer cells and with lower toxicity toward normal cells. Among these peptides, LTX-315 displayed superior anticancer activity and was selected as a lead candidate. This peptide showed relative high plasma protein binding abilities and a human plasma half-life of 160 min, resulting in formation of nontoxic metabolites. In addition, the lead candidate demonstrated relatively low ability to inhibit CYP450 enzymes. Collectively these data indicated as a new anticancer agent for intratumoral administration and is currently being evaluated in a phase I/IIa study.
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