NBI 42902
/ Neurocrine
- LARVOL DELTA
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June 02, 2018
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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