NBI 42902 / Neurocrine Biosciences - LARVOL DELTA

A targeted tubulysin B hydrazide conjugate for the treatment of LHRH receptor-positive cancers. (PubMed, Bioconjug Chem) - "...To reduce such unwanted uptake by peptide scavenger receptors in the liver and kidneys, we have explored the use of a nonpeptidic LHRH-R antagonist (NBI42902) to construct an LHRH-R targeted tubulysin conjugate (BOEPL-L3-TubBH)...That these complete responses are LHRH-R targeted was then established by showing that identical treatment of receptor-negative (SKOV3) tumors yields no anti-tumor response. Overall, these data provide a proof-of-concept that LHRH-R specific targeting of an extremely toxic drug like tubulysin B can treat LHRH-R positive tumors without causing significant toxicity to healthy cells."

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