Antibody drug conjugate technology has led to a novel drug delivery mechanism that is demonstrating success with positive outcomes for patients with cancer. It has also revived interest in certain agents that have historically been difficult to administer due to unacceptable toxicities despite significant potency and preclinical activity. Trastuzumab emtanzine (T-DM1) is a classic example of the positive clinical outcomes that have resulted from this technology. The unique properties of T-DM1, safety profile and proven efficacy have resulted in its recent approval as a new and unique agent in the armamentarium of agents used to treat metastatic HER-2 positive breast cancer. In this article we will review the clinical development of T-DM1 that lead to its recent approval and briefly discuss future directions. Keywords: trastuzumab; T-DM1; breast cancer; drug receptor. Received: April 20, 2013; Accepted: June 5, 2013; Published: August 10, 2013 Corresponding Author: Muaiad Kittaneh, Karmanos Cancer Institute, Detroit, Michigan, 4100 John R Street, Mailcode HW04HO, Detroit, MI 48201, USA. E-mail: kittanem@karmanos.org .