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801

801 is a novel podophyllotoxin and camptothecin combination that preserves the anti-tumor properties of both compounds, while reducing toxicity and drug resistance.

Podophyllotoxin and camptothecin

As related to tumor physiology, topoisomerase I and II repair strand breaks after DNA replication, and are found in higher concentrations in cancer cells than in normal cells. HIF-1α and VEGF are involved in tumor metastasis.

Podophyllotoxin is currently prescribed to inhibit topoisomerase II, while camptothecin is prescribed to inhibit topoisomerase I, HIF-1α, and VEGF.

However, both podophyllotoxin and camptothecin have relatively high toxicity profiles, and therefore can only be used in alternation. Such alternating treatment involving inhibition of either topoisomerase I or II builds drug resistance in many cancer patients over time.

801

801 combines podophyllotoxin and camptothecin, inhibiting both topoisomerase I and II concurrently. Early studies indicate that the compound has nearly no toxicity against normal cells, which would enable more aggressive treatment with less risk of drug resistance.