Trastuzumab
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Identification
- Summary
Trastuzumab is a monoclonal anti-human epidermal growth factor receptor 2 protein antibody used to treat HER2-positive breast, gastroesophageal, and gastric cancers.
- Brand Names
- Herceptin, Herceptin Hylecta, Herzuma, Kanjinti, Ontruzant, Perjeta-Herceptin, Phesgo, Trazimera
- Generic Name
- Trastuzumab
- DrugBank Accession Number
- DB00072
- Background
Produced in CHO cell cultures, trastuzumab is a recombinant IgG1 kappa, humanized monoclonal antibody 6 that selectively binds with high affinity in a cell-based assay (Kd = 5 nM) to the extracellular domain of the human epidermal growth factor receptor protein (HER2).12 It is used as a treatment of human epidermal growth factor receptor (HER)-2+ metastatic breast cancer, where there is a proven amplification of the HER-2 oncogene or over-expression of the HER-2 protein in tumours. It is suggested that the overexpression or gene amplification of HER2 has been found in about 20–30% of breast cancers and elevated activation of HER2 triggers multiple downstream pathways leading to abnormal proliferation of cancer cells 4. Trastuzumab binds to HER2 and suppresses cancer cell growth, proliferation, and survival directly and indirectly 4.
In December 2017, FDA approved OGIVRI (trastuzumab-dkst) as a biosimilar to Herceptin (trastuzumab) for the treatment of patients with breast or metastatic stomach cancer (gastric or gastroesophageal junction adenocarcinoma) whose tumors overexpress the HER2 gene (HER2+). It displays biosimilar properties as Herceptin according to clinical data. While Ogivri is the first biosimilar approved in the U.S. for the treatment of breast cancer or stomach cancer, it is the second biosimilar approved in the U.S. for the treatment of cancer. Herzuma (trastuzumab-pkrb) is a biosimilar drug approved in December 2018 for the treatment of HER2-overexpressing breast cancer. KANJINTI (trastuzumab-anns) is another biosimilar approved by the FDA in June 2019.16 ONTRUZANT, another biosimilar of Herceptin, was approved by Health Canada in February 2022.22,23 In November 2023, trastuzumab was also approved by the EMA under the brand name Herwenda.25
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- C6470H10012N1726O2013S42
- Protein Average Weight
- 145531.5 Da
- Sequences
>Anti-HER2 Light chain (1 and 2) DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPS RFSGSRSGTDFTLTISSLQPEDFATYYCQQHYTTPPTFGQGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
>Anti-HER2 Heavy chain (1 and 2) EVQLVESGGGLVQPGGSLRLSCAASGFNIKDTYIHWVRQAPGKGLEWVARIYPTNGYTRY ADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCSRWGGDGFYAMDYWGQGTLVTVSS ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGG PSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYN STYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREE MTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRW QQGNVFSCSVMHEALHNHYTQKSLSLSPGK
Download FASTA Format- Synonyms
- RHUMAB HER2
- Trastuzumab
- trastuzumab-anns
- trastuzumab-dkst
- trastuzumab-dttb
- trastuzumab-pkrb
- trastuzumab-qyyp
- External IDs
- 4D5V8
- ABP 980
- ABP-980
- DMB-3111
- EG-12014
- EG12014
- R-597
- SB-3
- SYD-977
- SYD977
Pharmacology
- Indication
For the adjuvant treatment of HER2-overexpressing breast cancer, trastuzumab is indicated in several clinical settings: as part of a treatment regimen consisting of doxorubicin, cyclophosphamide, and either paclitaxel or docetaxel; as part of a treatment regimen with docetaxel and carboplatin; or as monotherapy following multi-modality anthracycline-based therapy.12
Trastuzumab is indicated as a first-line treatment, in combination with paclitaxel, for metastatic HER2-overexpressing breast cancer, and as monotherapy in patients who have previously received one or more chemotherapy regimens in the metastatic setting.12 In Europe, trastuzumab can also be used in combination with paclitaxel or docetaxel for the treatment of metastatic HER2-positive breast cancer in adult patients and with an aromatase inhibitor in postmenopausal patients.24
For HER2-positive early breast cancer, the EMA approved trastuzumab as monotherapy following surgery, chemotherapy (neoadjuvant or adjuvant), and radiation or following adjuvant chemotherapy with doxorubicin and cyclophosphamide in combination with paclitaxel or docetaxel. It can also be used in combination with adjuvant chemotherapy consisting of docetaxel and carboplatin or with neoadjuvant chemotherapy followed by adjuvant trastuzumab therapy for locally advanced (including inflammatory) disease or tumors > 2 cm in diameter.24
Trastuzumab is also indicated, in combination with cisplatin and capecitabine or 5-fluorouracil, for the treatment of patients with HER2-overexpressing metastatic gastric or gastroesophageal junction adenocarcinoma who have not received prior treatment for metastatic disease by the FDA and EMA.12
Trastuzumab is indicated for subcutaneous administration - in combination with either hyaluronidase15 or both hyaluronidase and pertuzumab20 - for the treatment of adults with HER2-positive breast cancers.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Breast cancer Combination Product in combination with: Hyaluronidase (human recombinant) (DB06205) •••••••••••• ••••••••• Treatment of Breast cancer •••••••••••• ••••••••• Used in combination to treat Breast cancer Regimen in combination with: Carboplatin (DB00958), Docetaxel (DB01248) •••••••••••• •••••••••• ••••••• ••• •••••••• Used in combination to treat Breast cancer Regimen in combination with: Docetaxel (DB01248), Paclitaxel (DB01229) •••••••••••• •••• •••••••••••• •••• ••••••••••• ••• •••••••••••••••• •••••••••• ••••••• ••• •••••••• Treatment of Breast cancer •••••••••••• •••••••• ••••••••••••••••• •••••••••• ••••••• ••• •••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Trastuzumab exerts an antitumour activity and is used in the treatment of HER2-positive breast cancer. HER2 protein overexpression is observed in 20%-30% of primary breast cancers 7 thus HER2 presents as a useful therapeutic target for the treatment of breast cancers. Trastuzumab has been shown, in both in vitro assays and in animals, to inhibit the proliferation of human tumour cells that overexpress HER2. It works as a mediator of antibody-dependent cellular cytotoxicity, where it binds as an antibody to cells over-expressing HER2, leading to preferential cell death. Trastuzumab was also shown to inhibit angiogenesis of tumor cells in vivo 4. Higher doses and longer dosing intervals show no significant benefit over standard dose schedules 6. In patients with HER2 positive solid tumours, trastuzumab did not exert any clinically significant QTc interval duration.12
- Mechanism of action
Trastuzumab is a recombinant humanized IgG1 monoclonal antibody against the HER-2 receptor, a member of the epidermal growth factor receptors which is a photo-oncogene. Over-expressed in breast tumour cells, HER-2 overamplifies the signal provided by other receptors of the HER family by forming heterodimers 4. The HER-2 receptor is a transmembrane tyrosine kinase receptor that consists of an extracellular ligand-binding domain, a transmembrane region, and an intracellular or cytoplasmic tyrosine kinase domain. It is activated by the formation of homodimers or heterodimers with other EGFR proteins, leading to dimerization and autophosphorylation and/or transphosphorylation of specific tyrosine residues in EGFR intracellular domains 4. Further downstream molecular signaling cascades are activated, such as the Ras/Raf/mitogen-activated protein kinase (MAPK), the phosphoinositide 3-kinase/Akt, and the phospholipase Cγ (PLCγ)/protein kinase C (PKC) pathways that promote cell growth and survival and cell cycle progression 4. Due to upregulation of HER-2 in tumour cells, hyperactivation of these signaling pathways and abnormal cell proliferation is observed. Trastuzumab binds to the extracellular ligand-binding domain and blocks the cleavage of the extracellular domain of HER-2 to induce its antibody-induced receptor downmodulation 4, and subsequently inhibits HER-2-mediated intracellular signaling cascades. Inhibition of MAPK and PI3K/Akt pathways lead to an increase in cell cycle arrest, and the suppression of cell growth and proliferation 4. Trastuzumab also mediates the activation of antibody-dependent cell-mediated cytotoxicity (ADCC) 6 by attracting the immune cells, such as natural killer (NK) cells, to tumor sites that overexpress HER-2 4. While the drug alone has a minimal potential to induce complement-dependent cytotoxicity (CDC),8 one study demonstrated increased therapeutic effectiveness and a synergistic effect on uterine serous carcinoma cells in vitro when used in combination with pertuzumab, which also has minor effects on CDC alone. This study showed that only the combination of both cell-bound antibodies would be sufficient to bind and activate the complement component 1q (C1q) required to initiate the complement cascade reaction.9
Intrinsic trastuzumab resistance has been noted for some patients with HER-2 positive breast cancer. Mechanisms involving trastuzumab resistance include deficiency of phosphatase and tensin homologue and activation of phosphoinositide 3-kinase, and the overexpression of other surface receptors, such as insulin-like growth factor 6.
Target Actions Organism AReceptor tyrosine-protein kinase erbB-2 binderantibodyHumans - Absorption
Peak and trough plasma concentrations at steady state (between weeks 16 and 32) were approximately 123 and 79 mcg/mL, respectively. At the highest weekly dose studied (500 mg), mean peak serum concentration was 377 mcg/mL.12
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
After it binds to HER2, trastuzumab is metabolized intracellularly into smaller peptides and amino acids.6
- Route of elimination
Following metabolism, the complex elimination of trastuzumab in humans is mediated by epithelial cells in a dose-dependent (nonlinear) fashion.6 The renal excretion of trastuzumab is very low.6
- Half-life
The terminal half-life is approximately 28 days,6 but may decrease with lower doses - at the 10mg and 500mg doses, half-lives averaged approximately 1.7 and 12 days, respectively.11
- Clearance
The predicted steady-state clearance of trastuzumab is 0.173 - 0.337 L/day, dependent primarily on the dosing regimen.12 The clearance rate for subcutaneously administered trastuzumab, formulated with hyaluronidase for improved subcutaneous absorption, is 0.11 L/day.15
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
There is no experience with overdosage of trastuzumab in clinical trials - single doses >8 mg/kg have not been tested in humans.12 Trastuzumab can contribute to the development of ventricular dysfunction and congestive heart failure, particularly when used in combination (or temporally adjacent) to other cardiotoxic chemotherapies such as anthracyclines.12
- Pathways
Pathway Category Trastuzumab Action Pathway Drug action - Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Receptor tyrosine-protein kinase erbB-2 --- (A;G) G Allele, heterozygote ADR Directly Studied Patients with this genotype have increased risk of cardiotoxicity with trastuzumab. Details
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The risk or severity of neutropenia can be increased when Trastuzumab is combined with Abatacept. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Trastuzumab. Acetyldigitoxin Acetyldigitoxin may decrease the cardiotoxic activities of Trastuzumab. Adalimumab The risk or severity of neutropenia can be increased when Trastuzumab is combined with Adalimumab. Adenovirus type 7 vaccine live The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Trastuzumab. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- International/Other Brands
- Herclon (Roche)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Herceptin Injection, solution 600 mg Subcutaneous Roche Registration Gmb H 2016-09-08 Not applicable EU Herceptin Injection 150 mg/7.4mL Intravenous Genentech, Inc. 1998-09-25 Not applicable US Herceptin Injection, powder, lyophilized, for solution 150 mg/7.4mL Intravenous Genentech, Inc. 2017-02-10 Not applicable US Herceptin Powder, for solution 440 mg / vial Intravenous Hoffmann La Roche 1999-08-23 Not applicable Canada Herceptin Injection, powder, for solution 150 mg Intravenous Roche Registration Gmb H 2016-09-08 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Herceptin Hylecta Trastuzumab (600 mg/5mL) + Hyaluronidase (human recombinant) (10000 U/5mL) Injection, solution Subcutaneous Genentech, Inc. 2019-02-28 Not applicable US Ogivri Trastuzumab (440 mg / vial) + Water (20 mL / vial) Powder, for solution Intravenous Biosimilar Collaborations Ireland Limited 2019-06-06 Not applicable Canada Perjeta-herceptin Trastuzumab (440 mg / vial) + Pertuzumab (420 mg / 14 mL) Kit; Powder, for solution; Solution Intravenous Hoffmann La Roche 2013-05-09 Not applicable Canada Phesgo Trastuzumab (600 mg/10mL) + Hyaluronidase (human recombinant) (20000 U/10mL) + Pertuzumab (600 mg/10mL) Injection, solution Subcutaneous Genentech, Inc. 2020-06-29 Not applicable US Phesgo Trastuzumab (40 mg / mL) + Pertuzumab (80 mg / mL) Solution Subcutaneous Hoffmann La Roche 2021-04-08 Not applicable Canada
Categories
- ATC Codes
- L01FD01 — Trastuzumab
- L01FD — HER2 (Human Epidermal Growth Factor Receptor 2) inhibitors
- L01F — MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
- L01 — ANTINEOPLASTIC AGENTS
- L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic Agents
- Antineoplastic Agents, Immunological
- Antineoplastic and Immunomodulating Agents
- Biological Products
- Blood Proteins
- Cancer immunotherapy
- Cardiotoxic antineoplastic agents
- Complex Mixtures
- Globulins
- HER2 (Human Epidermal Growth Factor Receptor 2) inhibitors
- HER2 Receptor Antagonists
- HER2/Neu/cerbB2 Antagonists
- Immunoglobulins
- Immunoproteins
- Immunosuppressive Agents
- Immunotherapy
- Monoclonal antibodies and antibody drug conjugates
- Narrow Therapeutic Index Drugs
- Proteins
- Serum Globulins
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- P188ANX8CK
- CAS number
- 180288-69-1
References
- General References
- Bange J, Zwick E, Ullrich A: Molecular targets for breast cancer therapy and prevention. Nat Med. 2001 May;7(5):548-52. [Article]
- Menard S, Pupa SM, Campiglio M, Tagliabue E: Biologic and therapeutic role of HER2 in cancer. Oncogene. 2003 Sep 29;22(42):6570-8. [Article]
- Kute T, Lack CM, Willingham M, Bishwokama B, Williams H, Barrett K, Mitchell T, Vaughn JP: Development of Herceptin resistance in breast cancer cells. Cytometry A. 2004 Feb;57(2):86-93. [Article]
- Albanell J, Codony J, Rovira A, Mellado B, Gascon P: Mechanism of action of anti-HER2 monoclonal antibodies: scientific update on trastuzumab and 2C4. Adv Exp Med Biol. 2003;532:253-68. [Article]
- Tan AR, Swain SM: Ongoing adjuvant trials with trastuzumab in breast cancer. Semin Oncol. 2003 Oct;30(5 Suppl 16):54-64. [Article]
- Boekhout AH, Beijnen JH, Schellens JH: Trastuzumab. Oncologist. 2011;16(6):800-10. doi: 10.1634/theoncologist.2010-0035. Epub 2011 May 31. [Article]
- Vu T, Claret FX: Trastuzumab: updated mechanisms of action and resistance in breast cancer. Front Oncol. 2012 Jun 18;2:62. doi: 10.3389/fonc.2012.00062. eCollection 2012. [Article]
- Rogers LM, Veeramani S, Weiner GJ: Complement in monoclonal antibody therapy of cancer. Immunol Res. 2014 Aug;59(1-3):203-10. doi: 10.1007/s12026-014-8542-z. [Article]
- Mamidi S, Cinci M, Hasmann M, Fehring V, Kirschfink M: Lipoplex mediated silencing of membrane regulators (CD46, CD55 and CD59) enhances complement-dependent anti-tumor activity of trastuzumab and pertuzumab. Mol Oncol. 2013 Jun;7(3):580-94. doi: 10.1016/j.molonc.2013.02.011. Epub 2013 Feb 20. [Article]
- US Patent US6870034B2 (includes Trastuzumab heavy chain sequence) [Link]
- Health Canada Product Monograph: Ogivri (trastuzumab) powder for intravenous infusion [Link]
- FDA Approved Drug Products: Herceptin (trastuzumab) for intravenous injection [Link]
- FDA Approved Drug Products: Ogivri (trastuzumab-dkst) for intravenous infusion [Link]
- FDA Approved Drug Products: Herzuma (trastuzumab-pkrb) for intravenous infusion [Link]
- FDA Approved Drug Products: Herceptin Hylecta (trastuzumab and hyaluronidase-oysk) for subcutaneous injection [Link]
- FDA Approved Drug Products: Kanjinti (trastuzumab-anns) for intravenous infusion [Link]
- FDA Approved Drug Products: Ontruzant (trastuzumab-dttb) for intravenous infusion [Link]
- FDA Approved Drug Products: Trazimera (trastuzumab-qyyp) for intravenous infusion [Link]
- Genentech: Herceptin(R) MSDS [Link]
- FDA News Release: FDA Approves Breast Cancer Treatment That Can Be Administered At Home By Health Care Professional [Link]
- FDA Approved Drug Products: Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) for subcutaneous injection [Link]
- Health Canada Product Monograph: ONTRUZANT (trastuzumab) intravenous infusion [Link]
- GlobeNewsWire: Samsung Bioepis Announces Health Canada Approval of 150mg Single-use Vial and 440mg Multi-dose Vial of ONTRUZANT® (SB3), Trastuzumab Biosimilar for the Treatment of Adults with Early Breast Cancer, Metastatic Breast Cancer, and Metastatic Gastric Cancer [Link]
- EMA Product Information: HERWENDA (trastuzumab) Powder for concentrate for solution for infusion (December 2023) [Link]
- An overview of Herwenda and why it is authorised in the EU [Link]
- Trastuzumab: Antineoplastic agent; a recombinant DNA- derived humanized anti-HER2 monoclonal antibody (complete heavy chain sequence) [File]
- External Links
- UniProt
- P01857
- Genbank
- J00228
- KEGG Drug
- D03257
- PubChem Substance
- 46507516
- 224905
- ChEMBL
- CHEMBL1201585
- Therapeutic Targets Database
- DAP000391
- PharmGKB
- PA451743
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Trastuzumab
- MSDS
- Download (320 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Not Available Breast Cancer 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Not Available Gastric Cancer 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Not Available HER2/Neu-positive Breast Cancer 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Diagnostic Bone Metastases / Carcinoma Breast Stage IV / Hepatic Metastases / HER2/Neu-positive Breast Cancer / Metastases to lung / Metastases to soft tissue / Recurrent Breast Cancer 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Treatment Breast Cancer 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- DSM Corp.
- F Hoffmann-La Roche Ltd.
- Genentech Inc.
- Dosage Forms
Form Route Strength Injection Parenteral 150 mg Injection Intravenous 150 mg/7.4mL Injection Parenteral 600 MG/5ML Injection, powder, lyophilized, for solution Intravenous 150 mg/7.4mL Injection, solution Parenteral; Subcutaneous 600 MG/5ML Injection, solution Parenteral; Subcutaneous 600 MG Powder, for solution Intravenous 440 mg / vial Solution Intravenous Injection, solution 600 mg/5ml Injection, powder, lyophilized, for solution Intravenous 44000000 mg Injection, solution Subcutaneous 600 mg/5mL Injection, solution Subcutaneous Injection, powder, for solution Intravenous 440 mg Solution Subcutaneous 600 mg / 5 mL Solution Subcutaneous 600.00 mg Injection, solution Subcutaneous 600 mg Injection, powder, for solution Intravenous Solution Subcutaneous 600 mg Injection, powder, for solution 440 mg Injection, powder, for solution 440 mg/20ml Injection, powder, for solution Intravenous 420 mg Kit; powder, for solution Intravenous 440 mg / vial Solution Intravenous 150.00 mg Injection, powder, for solution Intravenous 150 mg/1vial Injection, solution, concentrate Intravenous 150 mg Injection, powder, lyophilized, for solution Intravenous 150 mg Injection, powder, for solution 100 mg Injection, powder, for solution 160 mg Injection, powder, for solution 160 mg/1vial Injection, powder, lyophilized, for solution Intravenous 150 mg/7.15mL Injection, powder, lyophilized, for solution Intravenous 420 mg/20mL Kit; powder, for solution Intravenous 420 mg / vial Injection, powder, for solution 150 mg Injection, powder, for solution Intravenous 150 mg Injection, powder, for solution Intravenous; Parenteral 150 MG Powder, for solution Intravenous Powder, for solution Intravenous 150 mg / vial Injection, powder, for solution Intravenous; Parenteral 420 MG Injection, powder, lyophilized, for solution Intravenous 150 mg/1 Kit Intravenous 420 mg/1 Powder, for solution Intravenous 150 mg Powder, for solution Intravenous 420 mg Kit; powder, for solution; solution Intravenous Solution Subcutaneous Solution Subcutaneous 6000000 mg Injection, powder, lyophilized, for solution; kit Intravenous 420 mg/20mL Injection, solution, concentrate Intravenous 150 mg/1vial Injection, solution, concentrate Intravenous 440 mg/1vial Injection, powder, lyophilized, for solution Intravenous 440 mg Solution Intravenous 440.00 mg Injection, powder, for solution; injection, powder, lyophilized, for solution Intravenous 440 mg/20ml Injection, powder, for solution Intravenous 60 mg Injection, powder, for solution Intravenous; Parenteral 60 mg Solution Intravenous Injection, powder, for solution Intravenous 440 mg/1vial Powder Intravenous 440 mg/1bottle Powder Intravenous 150 mg/1vial Powder Intravenous 150 mg/1bottle Injection, powder, for solution 100 mg/1vial - Prices
Unit description Cost Unit Herceptin 440 mg Solution Vial 3581.2USD vial Herceptin 440 mg vial 3443.46USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2103059 No 2005-03-22 2012-06-15 Canada
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 61 °C (FAB fragment), 71 °C (whole mAb) Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- BinderAntibody
- General Function
- Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-RHOA-DIAPH1 signaling pathway elicits the phosphorylation and thus the inhibition of GSK3B at cell membrane. This prevents the phosphorylation of APC and CLASP2, allowing its association with the cell membrane. In turn, membrane-bound APC allows the localization of MACF1 to the cell membrane, which is required for microtubule capture and stabilization
- Specific Function
- ATP binding
- Gene Name
- ERBB2
- Uniprot ID
- P04626
- Uniprot Name
- Receptor tyrosine-protein kinase erbB-2
- Molecular Weight
- 137909.27 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Leveque D, Gigou L, Bergerat JP: Clinical pharmacology of trastuzumab. Curr Clin Pharmacol. 2008 Jan;3(1):51-5. [Article]
- Lin A, Rugo HS: The role of trastuzumab in early stage breast cancer: current data and treatment recommendations. Curr Treat Options Oncol. 2007 Feb;8(1):47-60. [Article]
- Treish I, Schwartz R, Lindley C: Pharmacology and therapeutic use of trastuzumab in breast cancer. Am J Health Syst Pharm. 2000 Nov 15;57(22):2063-76; quiz 2077-9. [Article]
Drug created at June 13, 2005 13:24 / Updated at September 10, 2024 06:48