Details of the Drug

General Information of Drug (ID: DMZQOUX)

Drug Name
Trastuzumab
Synonyms Herceptin; Herceptin (TN); Trastuzumab (INN); Trastuzumab (genetical recombination); Trastuzumab (genetical recombination) (JAN); Trastuzumab (ERBB2 mAb inhibitor)
Indication
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Approved [1]
Inflammatory breast cancer 2C62 Approved [2]
Lung cancer 2C25.0 Approved [3]
Gastric adenocarcinoma 2B72 Application submitted [4]
HER2-positive breast cancer 2C60-2C65 Application submitted [4]
Gastric cancer 2B72 Investigative [5]
⏷ Show the Full List of Indication(s)
Therapeutic Class
Anticancer Agents
Drug Type
Antibody
Sequence
>light chain (1 and 2)
DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPS
RFSGSRSGTDFTLTISSLQPEDFATYYCQQHYTTPPTFGQGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
>heavy chain (1 and 2)
EVQLVESGGGLVQPGGSLRLSCAASGFNIKDTYIHWVRQAPGKGLEWVARIYPTNGYTRY
ADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCSRWGGDGFYAMDYWGQGTLVTVSS
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPPKSCDKTHTCPPCPAPELLG
GPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQY
NSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRD
ELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSR
WQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
ADMET Property
Clearance
The clearance of drug is 0.173-0.337 L/day [6]
Half-life
The concentration or amount of drug in body reduced by one-half in 28 days [7]
Metabolism
The drug is metabolized via the intracellularly into smaller peptides and amino acids [7]
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Neoplasm related morbidities Not Available ERBB2 OTOAUNCK [8]
Cross-matching ID
DrugBank ID
DB00072
TTD ID
D04WFL
VARIDT ID
DR01171
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Erbb2 tyrosine kinase receptor (HER2) TT6EO5L ERBB2_HUMAN Not Available [9]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Receptor tyrosine-protein kinase erbB-2 (ERBB2) OTOAUNCK ERBB2_HUMAN Drug Response [8]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Breast cancer
ICD Disease Classification 2C60-2C65
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Erbb2 tyrosine kinase receptor (HER2) DTT ERBB2 5.67E-03 -1.26 -2.05
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Trastuzumab (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Roflumilast DMPGHY8 Moderate Additive immunosuppressive effects by the combination of Trastuzumab and Roflumilast. Asthma [CA23] [10]
Teriflunomide DMQ2FKJ Major Additive immunosuppressive effects by the combination of Trastuzumab and Teriflunomide. Hyper-lipoproteinaemia [5C80] [11]
Denosumab DMNI0KO Moderate Additive myelosuppressive effects by the combination of Trastuzumab and Denosumab. Low bone mass disorder [FB83] [12]
Cladribine DM3JDRP Major Additive immunosuppressive effects by the combination of Trastuzumab and Cladribine. Mature B-cell leukaemia [2A82] [10]
Alemtuzumab DMZL3IV Moderate Additive myelosuppressive effects by the combination of Trastuzumab and Alemtuzumab. Mature B-cell leukaemia [2A82] [13]
Thalidomide DM70BU5 Major Additive thrombogenic effects by the combination of Trastuzumab and Thalidomide. Multiple myeloma [2A83] [14]
Tecfidera DM2OVDT Moderate Additive immunosuppressive effects by the combination of Trastuzumab and Tecfidera. Multiple sclerosis [8A40] [15]
Siponimod DM2R86O Major Additive immunosuppressive effects by the combination of Trastuzumab and Siponimod. Multiple sclerosis [8A40] [16]
Fingolimod DM5JVAN Major Additive immunosuppressive effects by the combination of Trastuzumab and Fingolimod. Multiple sclerosis [8A40] [17]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Trastuzumab and Ocrelizumab. Multiple sclerosis [8A40] [18]
Ozanimod DMT6AM2 Major Additive immunosuppressive effects by the combination of Trastuzumab and Ozanimod. Multiple sclerosis [8A40] [10]
Omacetaxine mepesuccinate DMPU2WX Moderate Additive immunosuppressive effects by the combination of Trastuzumab and Omacetaxine mepesuccinate. Myeloproliferative neoplasm [2A20] [19]
Efalizumab DMCKL5V Moderate Additive immunosuppressive effects by the combination of Trastuzumab and Efalizumab. Psoriasis [EA90] [20]
Canakinumab DM8HLO5 Moderate Additive immunosuppressive effects by the combination of Trastuzumab and Canakinumab. Rheumatoid arthritis [FA20] [21]
Rilonacept DMGLUQS Moderate Additive immunosuppressive effects by the combination of Trastuzumab and Rilonacept. Rheumatoid arthritis [FA20] [21]
Golimumab DMHZV7X Major Additive immunosuppressive effects by the combination of Trastuzumab and Golimumab. Rheumatoid arthritis [FA20] [22]
Leflunomide DMR8ONJ Major Additive myelosuppressive effects by the combination of Trastuzumab and Leflunomide. Rheumatoid arthritis [FA20] [11]
Anthrax vaccine DM9GSWY Moderate Antagonize the effect of Trastuzumab when combined with Anthrax vaccine. Sepsis [1G40-1G41] [23]
Azathioprine DMMZSXQ Moderate Additive myelosuppressive effects by the combination of Trastuzumab and Azathioprine. Transplant rejection [NE84] [16]
Ganciclovir DM1MBYQ Moderate Additive myelosuppressive effects by the combination of Trastuzumab and Ganciclovir. Virus infection [1A24-1D9Z] [16]
Valganciclovir DMS2IUH Moderate Additive myelosuppressive effects by the combination of Trastuzumab and Valganciclovir. Virus infection [1A24-1D9Z] [16]
⏷ Show the Full List of 21 DDI Information of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5082).
2 Efficacy and safety of neoadjuvant pertuzumab and trastuzumab in women with locally advanced, inflammatory, or early HER2-positive breast cancer (NeoSphere): a randomised multicentre, open-label, phase 2 trial. Lancet Oncol. 2012 Jan;13(1):25-32.
3 Trastuzumab Deruxtecan in HER2-Mutant Non-Small-Cell Lung Cancer. N Engl J Med. 2022 Jan 20;386(3):241-251.
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 The KEYNOTE-811 trial of dual PD-1 and HER2 blockade in HER2-positive gastric cancer. Nature. 2021 Dec;600(7890):727-730.
6 FDA Approved Drug Products: Herceptin (trastuzumab) for intravenous injection
7 Trastuzumab. Oncologist. 2011;16(6):800-10. doi: 10.1634/theoncologist.2010-0035. Epub 2011 May 31.
8 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
9 Her2/neu is not a commonly expressed therapeutic target in melanoma -- a large cohort tissue microarray study. Melanoma Res. 2004 Jun;14(3):207-10.
10 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
11 Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
12 Product Information. Prolia (denosumab). Amgen USA, Thousand Oaks, CA.
13 Product Information. Campath (alemtuzumab) Berlex, Richmond, CA.
14 Bennett CL, Nebeker JR, Samore MH, et al "The Research on Adverse Drug Events and Reports (RADAR) project." JAMA 293 (2005): 2131-40. [PMID: 15870417]
15 Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA.
16 Cerner Multum, Inc. "Australian Product Information.".
17 Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
18 Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
19 Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
20 Product Information. Raptiva (efalizumab). Genentech, South San Francisco, CA.
21 Product Information. Arcalyst (rilonacept). Regeneron Pharmaceuticals Inc, Tarrytown, NY.
22 Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA.
23 CDC. Centers for Disease Control and Prevention/ "Recommendations of the advisory committtee on immunization practices (ACIP): use of vaccines and immune globulins in persons with altered immunocompetence." MMWR Morb Mortal Wkly Rep 42(RR-04) (1993): 1-18. [PMID: 20300058]