trastuzumab emtansine   Click here for help

GtoPdb Ligand ID: 6928

Synonyms: ado-trastuzumab emtansine | Kadcyla® | PRO-132365 | RG-3502
Approved drug
trastuzumab emtansine is an approved drug (EMA and FDA (2013))
Compound class: Antibody
Comment: Trastuzumab emtansine is a antibody-drug conjugate (ADC) containing a targeting antibody (anti-erbB2) conjugated to a cytotoxic drug (mertansine or DM1) [4]. The PubChem CID for the mertasine component compound is CID 11343137. Mertansine (or DM1) is a macrolide of the ansamycin type and can be isolated from plants of the genus Maytenus. It is known as a maytansinoid. This agent binds to the rhizoxin binding site on β-tubulin and functions in a similar fashion to the Vinca alkaloids.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.

Other trastuzumab-based antibody-drug conjugates (ADCs):
trastuzumab deruxtecan (fam-trastuzumab deruxtecan-nxki, DS-8201, Enhertu®; Daiichi Sankyo) delivers a topoisomerase I inhibitor payload [6-7]. It progressed through clinical development and received FDA approval in December 2019 as a treatment for metastatic breast cancer, and EMA authorisation for this indication followed in early 2021. Based on results from the DESTINY-Lung02 trial (NCT04644237) that demonstrated efficacy in patients with HER2 mutation-positive, unresectable/metastatic non-small cell lung cancer (NSCLC), Enhertu® was FDA approved as the first therapeutic for this type of NSCLC in August 2022.
trastuzumab duocarmazine (SYD985, a.k.a. trastuzumab vc-seco-DUBA, [vic-]trastuzumab duocarmazine; Synthon/Byondis) [2] delivers the highy cytotoxic DNA methylating pro-drug, seco-duocarmycinhydroxybenzamide- azaindole, to HER2-expressing cancer cells [5,7]. The payload is conjugated to the antibody via a linker that is cleaved once the ADC is internalised by cancer cells, and the pro-drug is then metabolised to the active toxin. SYD985 was granted fast track designation by the FDA in early 2018, based on positive phase 1 data [1]. This agent is in late stage clinical evaluation in metastatic breast cancer NCT03262935), and the FDA accepted Byondis' Biologics License Application for the use of SYD985 in patients with HER2-positive unresectable locally advanced or metastatic breast cancer in mid-2022.
Classification Click here for help
Compound class Antibody
Approved drug? Yes (EMA and FDA (2013))
International Nonproprietary Names Click here for help
INN number INN
9295 trastuzumab emtansine
Synonyms Click here for help
ado-trastuzumab emtansine | Kadcyla® | PRO-132365 | RG-3502
Database Links Click here for help
Specialist databases
IMGT/mAb-DB 357
Other databases
GtoPdb PubChem SID 178103510
PubChem SID 178103510
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Wikipedia Trastuzumab_emtansine