trastuzumab

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Ligands
trastuzumab

GtoPdb Ligand ID: 5082

Synonyms: D5v8 | Herceptin® | R-597

trastuzumab is an approved drug (FDA (1998), EMA (2000))

Comment: Trastuzumab is a humanized IgG1κ monoclonal antibody targeting HER2.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.

Biosimilars:

Name	Trade name	Company	Clinical Phase	Indications
trastuzumab-dkst; MYL-1401O	Hertraz; Canmab; Ogivri	Mylan and Biocon	Approved in India, FDA 2017, EMA 2018 (Ogivri)	Breast cancer
trastuzumab-pkrb; CT-P6	Herzuma; Credima	Celltrion	Approved in S Korea, EMA & FDA 2018	Breast cancer
trastuzumab-dttb; SB3	Ontruzant	Samsung Bioepis	Approved (EMA 2017, FDA 2019)	All approved indications of the reference product
trastuzumab-beta; trastuzumab-anns; ABP-980 [3]	Kanjinti	Amgen/Allergan	Approved (EMA 2018, FDA 2019)	All approved indications of the reference product
trastuzumab-qyyp; PF-05280014	Trazimera	Pfizer	Approved (FDA 2019; see REFLECTIONS B327-02 trial NCT01989676)	All approved indications of the reference product
HLX02	Zercepac	Shanghai Henlius Biotech; Accord Healthcare	Approved (EMA 2020)	Approved to treat HER2 positive metastatic breast cancer

View more information in the IUPHAR Pharmacology Education Project: trastuzumab

Bioactivity Comments
The use of anti-HER2 monoclonals is covered by patent WO1989006692, in which the clone that produced trastuzumab is 4D5 [1]. Efficacy of the resultant monoclonals was assessed in vitro (for example ELISA for antigen binding and in vitro cellular assays for anti-tumour activity) but no affinity value for the interaction between the antibody and its antigen are provided in the patent.

Bioactivity Comments

The use of anti-HER2 monoclonals is covered by patent WO1989006692, in which the clone that produced trastuzumab is 4D5 [1]. Efficacy of the resultant monoclonals was assessed in vitro (for example ELISA for antigen binding and in vitro cellular assays for anti-tumour activity) but no affinity value for the interaction between the antibody and its antigen are provided in the patent.

Selectivity at catalytic receptors

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