Bemcentinib (BGB324): A Comprehensive Monograph on a First-in-Class AXL Inhibitor in Oncology

Drug Profile and Chemical Characteristics

Identification and Nomenclature

Bemcentinib is an investigational small molecule drug classified as a first-in-class, selective inhibitor of the AXL receptor tyrosine kinase.[1] The compound has been developed under several code names and synonyms that reflect its history. It was originally discovered by Rigel Pharmaceuticals as R428 and is frequently referred to by this designation in preclinical literature.[3] Following its licensing by BerGenBio ASA for clinical development, it became widely known by the code BGB324 (or BGB-324) and was assigned the generic name Bemcentinib.[3]

The compound is cataloged across major chemical and pharmacological databases under a consistent set of identifiers, ensuring its unambiguous tracking in scientific literature and regulatory filings.

• Generic Name: Bemcentinib [1]
• Drug Type: Small Molecule [1]
• Synonyms and Code Names: BGB324, BGB-324, R428, R-428, AXL inhibitor BGB324 [2]
• DrugBank ID: DB12411 [1]
• CAS Number: 1037624-75-1 [1]
• PubChem CID: 46215462 [3]
• UNII (Unique Ingredient Identifier): 0ICW2LX8AS [1]
• ChEMBL ID: CHEMBL3809489 [3]
• KEGG ID: D11438 [3]
• IUPHAR/BPS ID: 10478 [3]
• WHO International Nonproprietary Name (INN) Number: 10631 [2]

Chemical Structure and Properties

Bemcentinib is a complex synthetic organic compound belonging to the aralkylamine class, characterized by an alkyl group substituted with an aromatic hydrocarbyl group.[1] Its structure incorporates several heterocyclic moieties, including pyridazine, triazole, and N-alkylpyrrolidine components, which are crucial for its interaction with the target kinase.[1]