Conjugation site modulates the in vivo stability and therapeutic activity of antibody-drug conjugates

Ben‐Quan Shen, Keyang Xu, Luna Liu, +30

Nature Biotechnology

ImmunoengineeringImmunologyBioconjugationAntibody EngineeringImmunotherapeutics +6

Phase I Study of Trastuzumab-DM1, an HER2 Antibody-Drug Conjugate, Given Every 3 Weeks to Patients With HER2-Positive Metastatic Breast Cancer

Ian E. Krop, Muralidhar Beeram, Shanu Modi, +10

Journal of Clinical Oncology

Engineered Thio-Trastuzumab-DM1 Conjugate with an Improved Therapeutic Index to Target Human Epidermal Growth Factor Receptor 2–Positive Breast Cancer

Jagath R. Junutula, Kelly M. Flagella, Richard Graham, +17

Clinical Cancer Research

Impact of Drug Conjugation on Pharmacokinetics and Tissue Distribution of Anti-STEAP1 Antibody–Drug Conjugates in Rats

C. Andrew Boswell, Eduardo E. Mundo, Crystal Zhang, +16

Bioconjugate Chemistry

NanotherapeuticsLocal PharmacologyImmunologyCellular PharmacologyPharmacotherapy +21

The Effect of Different Linkers on Target Cell Catabolism and Pharmacokinetics/Pharmacodynamics of Trastuzumab Maytansinoid Conjugates

Hans K. Erickson, Gail D. Lewis Phillips, Douglas D. Leipold, +8

Molecular Cancer Therapeutics

Vitro PotencyImmunologyPharmacotherapyImmunotherapeuticsImmunotherapy +17

Preclinical safety profile of trastuzumab emtansine (T-DM1): Mechanism of action of its cytotoxic component retained with improved tolerability

Kirsten Achilles Poon, Kelly M. Flagella, Joseph C. Beyer, +7

Toxicology and Applied Pharmacology

Breast OncologyImmunologyCytotoxic ComponentImmunotherapeuticsUnconjugated Dm1 +16

Catabolic Fate and Pharmacokinetic Characterization of Trastuzumab Emtansine (T-DM1): an Emphasis on Preclinical and Clinical Catabolism

Ben‐Quan Shen, Daniela Bumbaca, Ola M. Saad, +9

Current Drug Metabolism

OncologyTrastuzumab EmtansineClinical CatabolismOncogenic AgentCatabolic Fate +11

Antitumor Activity of Targeted and Cytotoxic Agents in Murine Subcutaneous Tumor Models Correlates with Clinical Response

Harvey Wong, Edna F. Choo, Bruno Alicke, +8

Clinical Cancer Research

Modeling the efficacy of trastuzumab-DM1, an antibody drug conjugate, in mice

Nelson L. ‘Shasha’ Jumbe, Xin Yan, Douglas D. Leipold, +6

Journal of Pharmacokinetics and Pharmacodynamics

Drug TargetingAntibody Drug ConjugateMedicineImmunologyImmune Checkpoint Inhibitor +7

Effects of Anti-VEGF on Pharmacokinetics, Biodistribution, and Tumor Penetration of Trastuzumab in a Preclinical Breast Cancer Model

Cinthia V. Pastuskovas, Eduardo E. Mundo, Simon P. Williams, +21

Molecular Cancer Therapeutics