Antroquinonol A: Scalable Synthesis and Preclinical Biology of a Phase 2 Drug Candidate

The
fungal-derived Taiwanese natural product antroquinonol A has attracted
both academic and commercial interest due to its reported exciting
biological properties. This reduced quinone is currently in phase
II trials (USA and Taiwan) for the treatment of non-small-cell lung
carcinoma (NSCLC) and was recently granted orphan drug status by the
FDA for the treatment of pancreatic cancer and acute myeloid leukemia.
Pending successful completion of human clinical trials, antroquinonol
is expected to be commercialized under the trade name Hocena. A synthesis-enabled
biological re-examination of this promising natural product, however,
reveals minimal in vitro and in vivo antitumor activity in preclinical
models.