.Pharmacolibrary.Drugs.ATC.L.L01FD03

Information

Trastuzumab emtansine (T-DM1) is an antibody-drug conjugate composed of the monoclonal antibody trastuzumab linked to the cytotoxic agent DM1. It is used primarily for the treatment of HER2-positive metastatic breast cancer in patients who have previously received trastuzumab and a taxane. It is an FDA- and EMA-approved therapy for this indication.

Pharmacokinetics

Pharmacokinetic parameters from adult female patients with HER2-positive metastatic breast cancer, based on published population PK study.

References

1. Chen, SC, et al., & Li, C (2017). Population pharmacokinetics and exposure-response of trastuzumab emtansine in advanced breast cancer previously treated with ≥2 HER2-targeted regimens. British journal of clinical pharmacology 83(12) 2767–2777. DOI:10.1111/bcp.13381 PUBMED:https://pubmed.ncbi.nlm.nih.gov/28733983

2. Gupta, M, et al., & Girish, S (2012). Clinical implications of pathophysiological and demographic covariates on the population pharmacokinetics of trastuzumab emtansine, a HER2-targeted antibody-drug conjugate, in patients with HER2-positive metastatic breast cancer. Journal of clinical pharmacology 52(5) 691–703. DOI:10.1177/0091270011403742 PUBMED:https://pubmed.ncbi.nlm.nih.gov/21953571

3. Yamamoto, H, et al., & Fujiwara, Y (2015). Phase I and pharmacokinetic study of trastuzumab emtansine in Japanese patients with HER2-positive metastatic breast cancer. Japanese journal of clinical oncology 45(1) 12–18. DOI:10.1093/jjco/hyu160 PUBMED:https://pubmed.ncbi.nlm.nih.gov/25332421

Revisions

• 06/2025 initial generated model