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], [2], [3]
Gastric adenocarcinoma	2B72	Application submitted	[4]
HER2-positive breast cancer	2C60-2C65	Application submitted	[4]

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 [5]
Half-life: The concentration or amount of drug in body reduced by one-half in 28 days [6]
Metabolism: The drug is metabolized via the intracellularly into smaller peptides and amino acids [6]

Cross-matching ID

DrugBank ID: DB00072
TTD ID: D04WFL
VARIDT ID: DR01171

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	[7], [8], [9]

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Molecular Interaction Atlas (MIA)

MIA Detail

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)

MEA Detail

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]	[20]
Teriflunomide	DMQ2FKJ	Major	Additive immunosuppressive effects by the combination of Trastuzumab and Teriflunomide.	Hyper-lipoproteinaemia [5C80]	[21]
Denosumab	DMNI0KO	Moderate	Additive myelosuppressive effects by the combination of Trastuzumab and Denosumab.	Low bone mass disorder [FB83]	[22]
Cladribine	DM3JDRP	Major	Additive immunosuppressive effects by the combination of Trastuzumab and Cladribine.	Mature B-cell leukaemia [2A82]	[20]
Alemtuzumab	DMZL3IV	Moderate	Additive myelosuppressive effects by the combination of Trastuzumab and Alemtuzumab.	Mature B-cell leukaemia [2A82]	[23]
Thalidomide	DM70BU5	Major	Additive thrombogenic effects by the combination of Trastuzumab and Thalidomide.	Multiple myeloma [2A83]	[24]
Tecfidera	DM2OVDT	Moderate	Additive immunosuppressive effects by the combination of Trastuzumab and Tecfidera.	Multiple sclerosis [8A40]	[25]
Siponimod	DM2R86O	Major	Additive immunosuppressive effects by the combination of Trastuzumab and Siponimod.	Multiple sclerosis [8A40]	[26]
Fingolimod	DM5JVAN	Major	Additive immunosuppressive effects by the combination of Trastuzumab and Fingolimod.	Multiple sclerosis [8A40]	[27]
Ocrelizumab	DMEZ2KH	Moderate	Additive immunosuppressive effects by the combination of Trastuzumab and Ocrelizumab.	Multiple sclerosis [8A40]	[28]
Ozanimod	DMT6AM2	Major	Additive immunosuppressive effects by the combination of Trastuzumab and Ozanimod.	Multiple sclerosis [8A40]	[20]
Omacetaxine mepesuccinate	DMPU2WX	Moderate	Additive immunosuppressive effects by the combination of Trastuzumab and Omacetaxine mepesuccinate.	Myeloproliferative neoplasm [2A20]	[29]
Efalizumab	DMCKL5V	Moderate	Additive immunosuppressive effects by the combination of Trastuzumab and Efalizumab.	Psoriasis [EA90]	[30]
Canakinumab	DM8HLO5	Moderate	Additive immunosuppressive effects by the combination of Trastuzumab and Canakinumab.	Rheumatoid arthritis [FA20]	[31]
Rilonacept	DMGLUQS	Moderate	Additive immunosuppressive effects by the combination of Trastuzumab and Rilonacept.	Rheumatoid arthritis [FA20]	[31]
Golimumab	DMHZV7X	Major	Additive immunosuppressive effects by the combination of Trastuzumab and Golimumab.	Rheumatoid arthritis [FA20]	[32]
Leflunomide	DMR8ONJ	Major	Additive myelosuppressive effects by the combination of Trastuzumab and Leflunomide.	Rheumatoid arthritis [FA20]	[21]
Anthrax vaccine	DM9GSWY	Moderate	Antagonize the effect of Trastuzumab when combined with Anthrax vaccine.	Sepsis [1G40-1G41]	[33]
Azathioprine	DMMZSXQ	Moderate	Additive myelosuppressive effects by the combination of Trastuzumab and Azathioprine.	Transplant rejection [NE84]	[26]
Ganciclovir	DM1MBYQ	Moderate	Additive myelosuppressive effects by the combination of Trastuzumab and Ganciclovir.	Virus infection [1A24-1D9Z]	[26]
Valganciclovir	DMS2IUH	Moderate	Additive myelosuppressive effects by the combination of Trastuzumab and Valganciclovir.	Virus infection [1A24-1D9Z]	[26]
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References

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4	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5	FDA Approved Drug Products: Herceptin (trastuzumab) for intravenous injection
6	Trastuzumab. Oncologist. 2011;16(6):800-10. doi: 10.1634/theoncologist.2010-0035. Epub 2011 May 31.
7	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.
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10	Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
11	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: 7422).
12	Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
13	Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
14	2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
15	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
16	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
17	Clinical pipeline report, company report or official report of Roche (2009).
18	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
19	A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
20	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
21	Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
22	Product Information. Prolia (denosumab). Amgen USA, Thousand Oaks, CA.
23	Product Information. Campath (alemtuzumab) Berlex, Richmond, CA.
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25	Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA.
26	Cerner Multum, Inc. "Australian Product Information.".
27	Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
28	Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
29	Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
30	Product Information. Raptiva (efalizumab). Genentech, South San Francisco, CA.
31	Product Information. Arcalyst (rilonacept). Regeneron Pharmaceuticals Inc, Tarrytown, NY.
32	Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA.
33	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]