Cardiovascular Toxicities Associated with Intravenous Administration of P-Boronophenylalanine Formulations

LaHann, T. R.; Sills, C.; Hematillake, G.; Dymock, T.; Daniell, G.W.Bampfylde

doi:10.1007/978-1-4615-2978-1_104

Cited by 8 publications

(1 citation statement)

References 3 publications

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“…LAT1 is often upregulated in cancer cells providing the cancer-centric component for boron delivery. , BPA was recently approved in Japan as a 10 B delivery drug for BNCT of head and neck cancer . However, BPA does have drawbacks, such as low solubility requiring formulation with fructose or sorbitol; high-volume continuous infusion during BNCT; and in many cancers, low tumor delivery and low tumor-to-blood and normal tissue ratios. Thus, there is a need to identify new boron delivery drugs that improve these drawbacks of BPA.…”

Section: Introductionmentioning

confidence: 99%

Boronotyrosine, a Borylated Amino Acid Mimetic with Enhanced Solubility, Tumor Boron Delivery, and Retention for the Re-emerging Boron Neutron Capture Therapy Field

Raitano,

Martin,

Zhang

et al. 2023

J. Med. Chem.

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Boron neutron capture therapy (BNCT) is a reemerging binary cellular level cancer intervention that occurs through the interaction of a cancer-specific 10 boron ( 10 B) drug and neutrons. We created a new 10 B drug, 3-borono-L-tyrosine (BTS), that improves on the characteristics of the main historical BNCT drug 4-borono-L-phenylalanine (BPA). BTS has up to 4 times greater uptake in vitro than BPA and increased cellular retention. Like BPA, BTS uptake is mediated by the L-type amino acid transporter-1 (LAT1) but is less sensitive to natural amino acid competition. BTS can be formulated and bolus dosed at much higher levels than BPA, resulting in 2−3 times greater boron delivery in vivo. Fast blood clearance and greater tumor boron delivery result in superior tumor-to-blood ratios. BTS boron delivery appears to correlate with LAT1 expression. BTS is a promising boron delivery drug that has the potential to improve modern BNCT interventions.

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