Details of the Drug

General Information of Drug (ID: DMKEY6S)

• Drug Name: Margetuximab

Indication

Disease Entry	ICD 11	Status	REF
HER2-positive breast cancer	2C60-2C65	Approved	[1]
Gastric adenocarcinoma	2B72	Phase 2	[2], [3]
Gastrointestinal cancer	2C11	Phase 2	[4], [5]

• Drug Type: Antibody
• ADMET Property:
  Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 4120 mgday/L [6]
  Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 466 mg/L [6]
  Clearance: The clearance of drug is 0.22 L/day [6]
  Half-life: The concentration or amount of drug in body reduced by one-half in 19.2 days [6]
  Metabolism: The drug is metabolized via the into smaller peptides through various proteases and catabolic pathways [6]
  Vd: The volume of distribution (Vd) of drug is 5.47 L [6]
• Cross-matching ID:
  DrugBank ID: DB14967
  TTD ID: D01YYP

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	[1]

Molecular Expression Atlas of This Drug

• The Studied Disease: HER2-positive 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

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [4] 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: 8686).
• [5] ClinicalTrials.gov (NCT01828021) Phase 2 Study of the Monoclonal Antibody MGAH22 (Margetuximab) in Patients With Relapsed or Refractory Advanced Breast Cancer. U.S. National Institutes of Health.
• [6] FDA Approved Drug Products: MARGENZA (margetuximab) injection
• [7] 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.
• [8] 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).
• [9] Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
• [10] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [11] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [12] 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.
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [14] Clinical pipeline report, company report or official report of Roche (2009).
• [15] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [16] 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.