caplacizumab   Click here for help

GtoPdb Ligand ID: 9123

Synonyms: ALX-0081 | anti-vWF Nanobody | Cablivi® | caplacizumab-yhdp
Approved drug
caplacizumab is an approved drug (EMA (2018), FDA (2019))
Compound class: Antibody
Comment: Caplacizumab (ALX-0081) is a nanobody targeting von Willebrand factor (vWF) [5], with anti-thrombotic action [1]. NanobodyTM technology was commercially developed by Ablynx. Nanobodies are antibody derivatives comprising only the single variable domains (variable heavy, VH) whilst retaining full antigen binding capacity. Their relatively small size (compared to complete antibodies) provides the potential for alternative modes of delivery and the possibility of brain penetrance.
Annotated peptide sequences for this therapeutuc are available from its IMGT/mAb-DB record. BLAST protein sequence analysis of the peptide sequence submitted with the INN document for caplacizumab reveals a 100% match with SEQ ID NO: 90 claimed in patent US7807162 [4], which is preferred humanized variant 12A2H1 in the patent document.
Bioactivity Comments
The Kd value provided in the interaction table below is that for vWF binding by the wild type 12A2 series nanobody [4]. No Kd value is provided for the humanised 12A2H1 which has identical peptide sequence to caplacizumab (other 12A2 series humanised nanobodies are reported as having Kd values in the range 11-39nM) [4].
Selectivity at ligand targets
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
von Willebrand factor Primary target of this compound Hs Antibody Binding 8.5 pKd - 4
pKd 8.5 (Kd 3.1x10-9 M) [4]