lifastuzumab vedotin   Click here for help

GtoPdb Ligand ID: 8405

Synonyms: DNIB0600A | RG-7599 | RG7599
Compound class: Antibody
Comment: Lifastuzumab vedotin is an antibody drug conjugate containing an anti-SLC34A2 (sodium phosphate 2 transporter) monoclonal antibody linked to the toxin monomethyl auristatin E (MMAE, aka vedotin; PubChem CID 11542188).
Peptide sequence information for this antibody is available from its IMGT/mAb-DB record. Peptide sequence match identifies US8535675 as the covering patent [2], and also identifies the target antigen denoted as TAT211 in this patent as the sodium phosphate transporter.
Bioactivity Comments
Patent US8535675 [2] identifies clone 10H1.11.4B, as the lead which went on to be conjugated to the toxin payload, but does not provide an affinity value for this monoclonal's binding to SLC34A2. The primary target is tagged based on biological evidence provided in the patent.
Selectivity at transporters
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
Sodium phosphate 2 Primary target of this compound Hs Antibody Binding - - - 2
⤷ [2]
Targets where the ligand is described in the comment field
Target Comment
Sodium phosphate 2 NaPi2b is highly expressed by ovarian and non-small cell lung cancer (NSCLC) carcinomas, and is being actively pursued as a drug target for these tumours. XMT-1536 (Mersana Therapeutics) has entered Phase 1 proof-of-concept trial NCT03319628. Lifastuzumab vedotin (Genentech) reached Phase 2 evaluation, but trial NCT01991210 was terminated as the test agent failed to increase progression-free survival compared to standard-of-care pegylated liposomal doxorubicin, in ovarian cancer patients [1]. XMT-1536 and lifastuzumab vedotin are NaPi2b-directed monoclonal antibody-drug conjugates (ADCs).