Active Ingredient History
Trastuzumab emtansine (ado-trastuzumab emtansine, trade name Kadcyla) is a combination between a monoclonal antibody and a small-molecule drug. Each molecule of trastuzumab emtansine consists of a single trastuzumab molecule with several molecules of DM1, a cytotoxic maytansinoid, attached. SMCC, or succinimidyl trans-4-(maleimidylmethyl)cyclohexane-1-carboxylate, is a heterobifunctional crosslinker, a type of chemical reagent that contains two reactive functional groups, a succinimide ester and a maleimide. The succinimide group of SMCC reacts with the free amino group of a lysine residue in the trastuzumab molecule and the maleimide moiety of SMCC links to the free sulfhydryl group of DM1, forming a covalent bond between the antibody and the DM1. Each trastuzumab molecule may be linked to zero to eight DM1 molecules (3.5 on average). Trastuzumab emtansine is an antibody-drug conjugate consisting of the recombinant anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab conjugated to the maytansinoid DM1. The trastuzumab moiety of this ADC binds to HER2 on tumor cell surface surfaces; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting cell division and the proliferation of cancer cells that overexpress HER2. Linkage of antibody and drug through a nonreducible linker has been reported to contribute to the improved efficacy and reduced toxicity of this ADC compared to similar ADCs constructed with reducible linkers. Trastuzumab emtansine is used for the treatment of patients with HER2-positive, metastatic breast cancer who previously received rastuzumab 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. Ado-trastuzumab emtansine is marketed under the brand name Kadcyla and is indicated for use in HER2-positive, metastatic breast cancer patients who have already used taxane and/or trastuzumab for metastatic disease or had their cancer recur within 6 months of adjuvant treatment. The FDA label has two precautions. First that ado-trastuzumab emtansine and trastuzumab cannot be interchanged. Second that there is a black box warning of serious side effects such as hepatotoxicity, embryo-fetal toxicity, and cardiac toxicity. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
---|
Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
---|
Ado-Trastuzumab Emtansine (Phase 2)
Bile Duct Neoplasms (Phase 2)
Brain Neoplasms (Phase 2)
Carcinoma (Phase 2)
Carcinoma, Merkel Cell (Phase 1)
Carcinoma, Non-Small-Cell Lung (Phase 2)
Cholangiocarcinoma (Phase 2)
Colonic Neoplasms (Phase 2)
Colorectal Neoplasms (Phase 2)
Electroconvulsive Therapy (Phase 2)
Endometrial Neoplasms (Phase 2)
Esophageal Neoplasms (Phase 2)
Gastrointestinal Neoplasms (Phase 2)
Genes, erbB-2 (Phase 1)
Glioma (Phase 2)
Heart Failure (Phase 2)
Hemangiosarcoma (Phase 2)
Hypertrophy, Left Ventricular (Phase 2)
Kidney Neoplasms (Phase 2)
Liver Neoplasms (Phase 2)
Lung Neoplasms (Phase 2)
Lymphoma (Phase 2)
Melanoma (Phase 2)
Multiple Myeloma (Phase 2)
Neoplasm Metastasis (Phase 2)
Neoplasms ()
Ovarian Neoplasms (Phase 2)
Pancreatic Neoplasms (Phase 2)
Prostatic Neoplasms (Phase 2)
Salivary Gland Neoplasms (Phase 2)
Sarcoma (Phase 2)
Skin Neoplasms (Phase 2)
Small Cell Lung Carcinoma (Phase 1/Phase 2)
Squamous Cell Carcinoma of Head and Neck (Phase 2)
Stomach Neoplasms (Phase 2/Phase 3)
Thyroid Neoplasms (Phase 2)
Triple Negative Breast Neoplasms (Phase 1)
Urinary Bladder Neoplasms (Phase 2)
Urologic Neoplasms (Phase 2)
Uterine Cervical Neoplasms (Phase 2)
Trial | Phase | Start Date | Organizations | Indications |
---|
Feedback
Data collection and curation is an ongoing process for CDEK - if you notice any information here to be missing or incorrect, please let us know! When possible, please include a source URL (we verify all data prior to inclusion).
Report issue