Borofalan

Borofalan
Borofalan 10B
Clinical data
Trade namesSteboronine
Other names
  • Borofalan(10B)
  • Borofalan B-10
  • Boronophenylalanine
  • L-4-Boronophenylalanine
  • 10B-L-BPA
Identifiers
  • (2S)-2-Amino-3-(4-boronophenyl)propanoic acid
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.215.136
Chemical and physical data
FormulaC9H12B2NO4
Molar mass219.82 g·mol−1
3D model (JSmol)
  • B(C1=CC=C(C=C1)C[C@@H](C(=O)O)N)(O)O

  • 10B: [10B](C1=CC=C(C=C1)C[C@@H](C(=O)O)N)(O)O
  • InChI=1S/C9H12BNO4/c11-8(9(12)13)5-6-1-3-7(4-2-6)10(14)15/h1-4,8,14-15H,5,11H2,(H,12,13)/t8-/m0/s1
  • Key:NFIVJOSXJDORSP-QMMMGPOBSA-N

  • 10B: InChI=1S/C9H12BNO4/c11-8(9(12)13)5-6-1-3-7(4-2-6)10(14)15/h1-4,8,14-15H,5,11H2,(H,12,13)/t8-/m0/s1/i10-1
  • Key:NFIVJOSXJDORSP-ULMHTEDTSA-N

Borofalan (also known as borofalan(10B)) is a boron-containing pharmaceutical compound used as a boron carrier in boron neutron capture therapy (BNCT) for the treatment of cancer.[1][2] It is a boronic acid derivative of phenylalanine enriched with the isotope boron-10.[2][3] Borofalan has been approved in Japan for the treatment of unresectable, locally advanced, or locally recurrent head and neck cancer.[1][4]

Medical uses

Borofalan is used in BNCT for patients with recurrent or locally advanced head and neck cancer, including squamous-cell carcinoma and non-squamous-cell carcinoma.[3][5] It is administered as an intravenous infusion over 2 hours, followed by neutron irradiation.[3] In the open-label phase II clinical trial JHN002, borofalan was evaluated in combination with a cyclotron-based epithermal neutron source for recurrent or locally advanced head and neck cancer.[3] Post-marketing surveillance in Japan conducted nationwide after approval confirmed the safety and efficacy of BNCT with borofalan in patients with locally advanced or recurrent head and neck cancer in a real-world setting.[5]

Mechanism of action

Due to its structural similarity to phenylalanine, it is preferentially taken up by cancer cells via amino acid transporters.[3] Borofalan then acts as a radiation sensitizer by delivering boron-10 to tumor cells, where it captures thermal neutrons during BNCT, leading to the production of high-energy alpha particles and lithium-7 nuclei that cause localized cell death.[6]

History

Borofalan was developed by Stella Pharma Corporation.[1] It received manufacturing and marketing approval in Japan from the Pharmaceuticals and Medical Devices Agency (PMDA) in 2020 for use in BNCT for unresectable, locally advanced, or locally recurrent head and neck cancer.[1][4] Borofalan is marketed under the brand name Steboronine.[1]

Boronophenylalanine-fructose complex (BPA-F) is a derivative of borofalan in which a molecule of fructose is bound to the boronic acid.[7] It is designed for improved water solubility and pharmacokinetics.[8]

References

  1. ^ a b c d e "Report on the Deliberation Results March 3, 2020 Pharmaceutical Evaluation Division" (PDF). Pharmaceuticals and Medical Devices Agency (PMDA). March 3, 2020. Retrieved January 25, 2026.
  2. ^ a b CID 25033700 from PubChem
  3. ^ a b c d e Hirose, Katsumi; Konno, Akiyoshi; Hiratsuka, Junichi; Yoshimoto, Seiichi; Kato, Takahiro; Ono, Koji; Otsuki, Naoki; Hatazawa, Jun; Tanaka, Hiroki; Takayama, Kanako; Wada, Hitoshi; Suzuki, Motohisa; Sato, Mariko; Yamaguchi, Hisashi; Seto, Ichiro; Ueki, Yuji; Iketani, Susumu; Imai, Shigeki; Nakamura, Tatsuya; Ono, Takashi; Endo, Hiromasa; Azami, Yusuke; Kikuchi, Yasuhiro; Murakami, Masao; Takai, Yoshihiro (2021). "Boron neutron capture therapy using cyclotron-based epithermal neutron source and borofalan (10B) for recurrent or locally advanced head and neck cancer (JHN002): An open-label phase II trial". Radiotherapy and Oncology. 155: 182–187. doi:10.1016/j.radonc.2020.11.001. PMID 33186684.
  4. ^ a b Kanno, Hitoshi; Nagata, Hironori; Ishiguro, Akihiro; Tsuzuranuki, Satoshi; Nakano, Shintaro; Nonaka, Takahiro; Kiyohara, Koushin; Kimura, Toshinari; Sugawara, Akihiko; Okazaki, Yuzuru; Takae, Shinichi; Nakabayashi, Tetsuo; Arai, Hiroyuki; Suzuki, Hiroshi (2021). "Designation Products: Boron Neutron Capture Therapy for Head and Neck Carcinoma". The Oncologist. 26 (7): e1250–e1255. doi:10.1002/onco.13805. PMC 8265361. PMID 33928712.
  5. ^ a b Sato, Mariko; Hirose, Katsumi; Takeno, Satoshi; Aihara, Teruhito; Nihei, Keiji; Takai, Yoshihiro; Hayashi, Toshimitsu; Bando, Kosuke; Kimura, Hitomi; Tsurumi, Keisuke; Ono, Koji (2024). "Safety of Boron Neutron Capture Therapy with Borofalan(10B) and Its Efficacy on Recurrent Head and Neck Cancer: Real-World Outcomes from Nationwide Post-Marketing Surveillance". Cancers. 16 (5): 869. doi:10.3390/cancers16050869. PMC 10931064. PMID 38473231.
  6. ^ "Borofalan (10B)". NCI Cancer Dictionary. National Cancer Institute. Retrieved January 25, 2026.
  7. ^ "Boronophenylalanine-fructose-complex". NCI Cancer Dictionary. National Cancer Institute. Retrieved January 25, 2026.
  8. ^ "Boronophenylalanine Fructose Complex". MassiveBio. 11 December 2025. Retrieved January 25, 2026.
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