trastuzumab   Click here for help

GtoPdb Ligand ID: 5082

Synonyms: D5v8 | Herceptin® | R-597
Approved drug
trastuzumab is an approved drug (FDA (1998), EMA (2000))
Compound class: Antibody
Comment: Trastuzumab is a humanized IgG1κ monoclonal antibody targeting HER2.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.

NameTrade nameCompanyClinical PhaseIndications
trastuzumab-dkst; MYL-1401OHertraz; Canmab; OgivriMylan and Biocon Approved in India, FDA 2017, EMA 2018 (Ogivri)Breast cancer
trastuzumab-pkrb; CT-P6Herzuma; CredimaCelltrionApproved in S Korea, EMA & FDA 2018Breast cancer
trastuzumab-dttb; SB3OntruzantSamsung BioepisApproved (EMA 2017, FDA 2019)All approved indications of the reference product
trastuzumab-beta; trastuzumab-anns; ABP-980 [3]KanjintiAmgen/AllerganApproved (EMA 2018, FDA 2019)All approved indications of the reference product
trastuzumab-qyyp; PF-05280014TrazimeraPfizerApproved (FDA 2019; see REFLECTIONS B327-02 trial NCT01989676)All approved indications of the reference product
HLX02ZercepacShanghai Henlius Biotech; Accord HealthcareApproved (EMA 2020)Approved to treat HER2 positive metastatic breast cancer
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Summary of Clinical Use Click here for help
Trastuzumab is approved for use as adjuvant treatment of HER2 positive breast cancer, metastatic breast cancer and metastatic gastric cancer or gastroesophageal junction adenocarcinoma in patients who have not received prior treatment for metastatic disease.
Herceptin Hylecta® is a combination of trastuzumab plus recombinant hyaluronidase PH20 (hyaluronidase-oysk) that was FDA approved in early 2019 for the treatment of certain patients with HER2-positive early breast cancer. The hyaluronidase component facilitates reletively quick, subcutaneous delivery of the trastuzumab mAb component, in comparison to earlier formulations that relied on much slower intravenous delivery.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Trastuzumab binds to the cell surface HER2 epidermal growth factor receptor, whose upregulated expression promotes uncontrolled proliferation in many breast cancer cells [2]. It blocks the formation of the HER2 homodimers that are one of the functional signalling complexes that promote cancer cell proliferation. Trastuzumab blocks HER2 homodimer signalling and causes cell cycle arrest during the G1 phase, thereby inhibiting the replication of HER2 positive cancer cells.
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