Trastuzumab Deruxtecan Chemical Properties

storage temp. 

Solution, -20°C, 2 years

solubility 

Soluble in acetonitrile

form 

Solid

color 

White to off-white

Trastuzumab Deruxtecan Usage And Synthesis

Uses

Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer[1][2].

Biological Activity

Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC).

in vitro

Trastuzumab deruxtecan (1 pM-10 nM; 5 days) inhibits the growth of HER2‐positive KPL‐4 cells, with an IC ₅₀ of 109.7 pM.
Trastuzumab deruxtecan (10 nM; 5 days) shows bystander killing effects in HER2‐negative MDA‐MB‐468 cells.

in vivo

Trastuzumab deruxtecan (3 mg/kg; a single iv) shows antitumor activity against not only HER2‐positive tumors but also HER2‐negative tumors under the co‐inoculated condition.

References

[1] Kumagai K, et al. Interstitial pneumonitis related to trastuzumab deruxtecan, a human epidermal growth factor receptor 2-targeting Ab-drug conjugate, in monkeys. Cancer Sci. 2020 Dec;111(12):4636-4645. DOI:10.1111/cas.14686
[2] Kotani D, et, al. Trastuzumab deruxtecan for the treatment of patients with HER2-positive gastric cancer. Ther Adv Med Oncol. 2021 Jan 7;13:1758835920986518. DOI:10.1177/1758835920986518
[3] Ogitani Y, et, al. Bystander killing effect of DS-8201a, a novel anti-human epidermal growth factor receptor 2 antibody-drug conjugate, in tumors with human epidermal growth factor receptor 2 heterogeneity. Cancer Sci. 2016 Jul;107(7):1039-46. DOI:10.1111/cas.12966
[4] Iwata TN, et, al. [Fam-] trastuzumab deruxtecan (DS-8201a)-induced antitumor immunity is facilitated by the anti-CTLA-4 antibody in a mouse model. PLoS One. 2019 Oct 1;14(10):e0222280. DOI:10.1371/journal.pone.0222280