Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMO4GTC)

• Drug Name: Datopotamab deruxtecan Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Phase 3	[1]
Non-small-cell lung cancer	2C25	Phase 3	[2]

• Cross-matching ID: TTD Drug ID: DMO4GTC

Molecule-Related Drug Atlas

Drug(s) Targeting DNA topoisomerase I (TOP1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Irinotecan	DMP6SC2	Adenocarcinoma	2D40	Approved	[4]
Topotecan	DMP6G8T	Central nervous system neoplasm		Approved	[4]
B-Lactams	DMR8YD6	Bacterial infection	1A00-1C4Z	Approved	[5]
Belotecan hydrocholoride	DM3SRJZ	Small-cell lung cancer	2C25.Y	Approved	[6]
Topetecan	DMAE6LK	Small-cell lung cancer	2C25.Y	Approved	[7]
Karenitecin	DMCRGY4	Lung cancer	2C25.0	Phase 3	[8]
Camptothecin	DM6CHNJ	Solid tumour/cancer	2A00-2F9Z	Phase 3	[9]
Exatecan	DMCA7FN	Solid tumour/cancer	2A00-2F9Z	Phase 3	[10]
Edotecarin	DM3ZL7D	Gastric adenocarcinoma	2B72	Phase 3	[11]
Rubitecan	DMDWU1S	Human immunodeficiency virus infection	1C62	Phase 3	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
DNA topoisomerase I (TOP1)	TTGTQHC	TOP1_HUMAN	Inhibitor	[3]

References

• [1] ClinicalTrials.gov (NCT05374512) A Phase 3, Open-label, Randomised Study of Datopotamab Deruxtecan (Dato-DXd) Versus Investigator's Choice of Chemotherapy in Patients Who Are Not Candidates for PD-1/PD-L1 Inhibitor Therapy in First-line Locally Recurrent Inoperable or Metastatic Triple-negative Breast Cancer (TROPION Breast02). U.S.National Institutes of Health.
• [2] ClinicalTrials.gov (NCT05555732) A Randomized Phase 3 Study of Datopotamab Deruxtecan (Dato-DXd) and Pembrolizumab With or Without Platinum Chemotherapy in Subjects With No Prior Therapy for Advanced or Metastatic PD-L1 TPS <50% Non-squamous Non-small Cell Lung Cancer Without Actionable Genomic Alterations (TROPION-Lung07). U.S.National Institutes of Health.
• [3] Datopotamab Deruxtecan, a Novel TROP2-directed Antibody-drug Conjugate, Demonstrates Potent Antitumor Activity by Efficient Drug Delivery to Tumor Cells. Mol Cancer Ther. 2021 Dec;20(12):2329-2340.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [5] Luteolin, an emerging anti-cancer flavonoid, poisons eukaryotic DNA topoisomerase I. Biochem J. 2002 Sep 1;366(Pt 2):653-61.
• [6] Impact of natural products on developing new anti-cancer agents. Chem Rev. 2009 Jul;109(7):3012-43.
• [7] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [8] Characterization of protein kinase chk1 essential for the cell cycle checkpoint after exposure of human head and neck carcinoma A253 cells to a novel topoisomerase I inhibitor BNP1350. Mol Pharmacol.2000 Mar;57(3):453-9.
• [9] Topoisomerase I inhibitors: camptothecins and beyond. Nat Rev Cancer. 2006 Oct;6(10):789-802.
• [10] Phase I study of topoisomerase I inhibitor exatecan mesylate (DX-8951f) given as weekly 24-hour infusions three of every four weeks. Clin Cancer Res. 2001 Dec;7(12):3963-70.
• [11] Edotecarin: a novel topoisomerase I inhibitor. Clin Colorectal Cancer. 2005 May;5(1):27-36.
• [12] Rubitecan. Expert Opin Investig Drugs. 2006 Jan;15(1):71-9.