Database for
Therapeutic Antibodies
Therapeutic Antibodies
| Entry ID | 154 |
| INN | Trastuzumab emtansine, ado-trastuzumab emtansine |
| Status | Approved |
| Drug code(s) | Trastuzumab-DM1, RG3502 |
| Brand name | Kadcyla |
| mAb sequence source | mAb humanized |
| General Molecular Category | ADC |
| Format, general category | Full length Ab conjugate |
| Format details | None |
| Isotype (Fc) | IgG1 |
| Light chain isotype | kappa |
| Linker | SMCC, Non-cleavable linker |
| Ave. DAR | 3.5 |
| Conjugated/fused moiety | Tubulin inhibitor, DM1 maytansine |
| Discovery method/technology | None |
| Target(s) | HER2 |
| Indications of clinical studies | Breast cancer, gastric cancer |
| Primary therapeutic area | Cancer |
| Most advanced stage of development (global) | Approved EU, US, Japan, Australia |
| Status | Active |
| Start of clinical phase (IND filing or first Phase 1) | July 02, 2006 |
| Start of Phase 2 | June 15, 2007 |
| Start of Phase 3 | February 15, 2009 |
| Date BLA/NDA submitted to FDA | August 27, 2012 |
| Year of first approval (global) | 2013 |
| Date of first US approval | February 22, 2013 |
| INN, US product name | ado-trastuzumab emtansine, trastuzumab emtansine |
| US or EU approved indications | Breast cancer (HER2-positive, late-stage (metastatic) cancer); adjuvant treatment of people with HER2-positive early breast cancer (EBC) who have residual invasive disease after neoadjuvant (before surgery) taxane and Herceptin® (trastuzumab)-based treatment. |
| Company | Genentech |
| Licensee/Partner | None |
| Comments about company or candidate | Date of issue of marketing authorisation valid throughout the European Union= November 15, 2013 |
| Full address of company | South San Francisco, California, United States North America United States of America https://www.gene.com/contact-us/visit-us |
DAR = 3.5 Trastuzumab emtansine (T-DM1) is an antibody-drug conjugate consisting of the anti-HER2 antibody trastuzumab linked via a nonreducible thioether linker to the maytansinoid antitubulin agent DM1. T-DM1 carries an average of 3.5 DM1 molecules per one molecule of trastuzumab. Each DM1 molecule is conjugated to trastuzumab via a non-reducible thioether linker (N-succinimidyl-4-(N-maleimidomethyl) cyclohexane-1-carboxylate; SMCC, MCC after conjugation)
| Anticipated events | None |
| Factor(s) contributing to discontinuation | None |