lorvotuzumab mertansine

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Ligands
lorvotuzumab mertansine

GtoPdb Ligand ID: 7431

Synonyms: BB-10901 | IMGN901

Comment: Lorvotuzumab mertansine is an antibody-drug conjugate (ADC) combining an anti-NCAM1 (CD56) monoclonal antibody with the maytansinoid DM1 (PubChem CID 71301226) tubulin inhibitor [2].
Annotated peptide sequences for this antibody are available from its IMGT/mAb-db record. Patent US5639641 [4] describes the resurfacing of murine anti-CD56 monoclonal antibody N901, to improve its therapeutic efficacy in preparation for use as a human drug. A protein BLAST search matches the variable region of the light chain of lorvotuzumab, with sequence 36 from the patent, sequence 36 being a CDR grafted version of N901. No affinity data for the interaction between the preferred engineered antibody and the molecular target is provided in the patent.

No information available.

No information available.

Summary of Clinical Use
Lorvotuzumab mertansine has potential to target CD56 (NCAM1) +ve cancers, including Merkel cell carcinoma (MCC), small-cell lung cancer (SCLC) [6], ovarian cancer, multiple myeloma [3,5] and others [1]. Both the US FDA and European Medicines Agency (EMA) have granted this therapeutic orphan medicinal product designation for the treatment of MCC. This antibody is in clinical trial in patients with advanced SCLC (see ClinicalTrials.gov).

Summary of Clinical Use

Lorvotuzumab mertansine has potential to target CD56 (NCAM1) +ve cancers, including Merkel cell carcinoma (MCC), small-cell lung cancer (SCLC) [6], ovarian cancer, multiple myeloma [3,5] and others [1]. Both the US FDA and European Medicines Agency (EMA) have granted this therapeutic orphan medicinal product designation for the treatment of MCC. This antibody is in clinical trial in patients with advanced SCLC (see ClinicalTrials.gov).

Mechanism Of Action and Pharmacodynamic Effects
This antibody is designed with Targeted Antibody Payload (TAP) technology, that is the antibody delivers a toxic compound to specific cells, in this case cells expressing the CD56 (NCAM1) cell surface protein. Following endocytic internalisation of the conjugate, the toxin is metabollically liberated in the cell interior, where it acts as a tubulin inhibitor. The final therapeutic result is targeted cell death.

Mechanism Of Action and Pharmacodynamic Effects

This antibody is designed with Targeted Antibody Payload (TAP) technology, that is the antibody delivers a toxic compound to specific cells, in this case cells expressing the CD56 (NCAM1) cell surface protein. Following endocytic internalisation of the conjugate, the toxin is metabollically liberated in the cell interior, where it acts as a tubulin inhibitor. The final therapeutic result is targeted cell death.