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 | US: First approval for Breast Cancer (KADCYLA is indicated, as a single agent, for the treatment of patients with HER2-positive, metastatic breast cancer who previously received trastuzumab and a taxane, separately or in combination. Patients should have either: Received prior therapy for metastatic disease, or Developed disease recurrence during or within six months of completing adjuvant therapy.). Supplemental approvals for Breast Cancer (KADCYLA is indicated, as a single agent, for the treatment of patients with HER2-positive, metastatic breast cancer who previously received trastuzumab and a taxane, separately or in combination. Patients should have either: Received prior therapy for metastatic disease, or Developed disease recurrence during or within six months of completing adjuvant therapy. KADCYLA is indicated, as a single agent, for the adjuvant treatment of patients with HER2-positive early breast cancer who have residual invasive disease after neoadjuvant taxane and trastuzumab-based treatment). [as of February 2, 2022 label]. EU: First approval for Breast Cancer (KADCYLA, as a single agent, is indicated for the treatment of adult patients with HER2-positive, unresectable locally advanced or metastatic breast cancer who previously received trastuzumab and a taxane, separately or in combination. Patients should have either: Received prior therapy for locally advanced or metastatic disease, or Developed disease recurrence during or within six months of completing adjuvant therapy.). Supplemental approvals for Breast Cancer (Early Breast Cancer (EBC): KADCYLA, as a single agent, is indicated for the adjuvant treatment of adult patients with HER2-positive early breast cancer who have residual invasive disease, in the breast and/or lymph nodes, after neoadjuvant taxane-based and HER2-targeted therapy. Metastatic Breast Cancer (MBC): KADCYLA, as a single agent, is indicated for the treatment of adult patients with HER2-positive, unresectable locally advanced or metastatic breast cancer who previously received trastuzumab and a taxane, separately or in combination. Patients should have either: Received prior therapy for locally advanced or metastatic disease, or Developed disease recurrence during or within six months of completing adjuvant therapy) [as per EPAR - Product Information last updated on March 22, 2023]. |
| 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 |