Project Description

Comparison of the antibody-drug conjugate Kadcyla® to other HER2 inhibitors

Clustering of compounds with the same targeting

  • Kadcyla® is a trastuzumab (anti-HER2) antibody conjugated to emtansine.

  • Since 2013 Kadcyla® has been approved for treatment of HER2-positive breast cancer.

  • We analyzed the IC50 values of Kadcyla® in the 102 cancer cell lines of the Oncolines™ panel and compared them to those of 166 preprofiled anti cancer drugs.

  • The Kadcyla® profile is most similar to pure trastuzumab (Herceptin®).

  • The Kadcyla® profile also resembles that of small molecule HER2 inhibitors such as irbinitinib and lapatinib.

  • Thus, the emtansine conjugation does not diminish the specificity of the cellular profile of Kadcyla®: it remains a highly selective HER2 inhibitor.

Link to the publication describing the methodology
Network tree of cellular responses of HER2 and EGFR inhibitors. Connections are drawn if the Pearson correlation between 10logIC50 profiles exceeds 0.5
Network tree of cellular responses of HER2 and EGFR inhibitors. Connections are drawn if the Pearson correlation between 10logIC50 profiles exceeds 0.5