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

General Information of Drug (ID: DMWA74Y)

• Drug Name: Radotinib Drug Info
• Synonyms: IY-5511; IY-GV50205; Anticancer, Il-yang

Indication

Disease Entry	ICD 11	Status	REF
leukaemia	2A60-2B33	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 16063245
  CAS Number: CAS 926037-48-1
  TTD Drug ID: DMWA74Y

Molecule-Related Drug Atlas

Drug(s) Targeting Fusion protein Bcr-Abl (Bcr-Abl)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[3]
Dasatinib	DMJV2EK	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[3]
Nilotinib	DM7HXWT	Chronic myelogenous leukaemia	2A20.0	Approved	[4]
Asciminib	DM7EVUF	Chronic myeloid leukaemia	2A20	Approved	[5]
ABL 001	DMMF5K4	Chronic myeloid leukaemia	2A20	Phase 3	[6]
ICLUSIG	DM1SQSE	Acute lymphoblastic leukaemia	2A85	Phase 3	[7]
Bafetinib	DM7586F	Bone disease	FC0Z	Phase 2	[8]
AN-019	DMJ7QP8	Chronic myelogenous leukaemia	2A20.0	Phase 2	[9]
HQP1351	DMQ30X2	Chronic myeloid leukaemia	2A20	Phase 2	[10]
NPB-001-056	DM78KMT	Chronic myelogenous leukaemia	2A20.0	Phase 1/2	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fusion protein Bcr-Abl (Bcr-Abl)	TTS7G69	BCR_HUMAN-ABL1_HUMAN	Modulator	[2]

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: 7814).
• [2] Danusertib, an aurora kinase inhibitor.Expert Opin Investig Drugs.2012 Mar;21(3):383-93.
• [3] 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.
• [4] 2007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
• [5] Asciminib in Chronic Myeloid Leukemia after ABL Kinase Inhibitor Failure. N Engl J Med. 2019 Dec 12;381(24):2315-2326.
• [6] ABL001, a Potent Allosteric Inhibitor of BCR-ABL, Prevents Emergence of Resistant Disease When Administered in Combination with Nilotinib in an in Vivo Murine Model of Chronic Myeloid Leukemia, NorthBuilding, 2014, 120-125.
• [7] Ponatinib efficacy and safety in Philadelphia chromosome-positive leukemia: final 5-year results of the phase 2 PACE trial. Blood. 2018 Jul 26;132(4):393-404.
• [8] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [9] Design, synthesis and preclinical evaluation of NRC-AN-019. Int J Oncol. 2013 Jan;42(1):168-78.
• [10] Preclinical development of HQP1351, a multikinase inhibitor targeting a broad spectrum of mutant KIT kinases, for the treatment of imatinib-resistant gastrointestinal stromal tumors. Cell Biosci. 2019 Oct 26;9:88.
• [11] NPB001-05 inhibits Bcr-Abl kinase leading to apoptosis of imatinib-resistant cells. Front Biosci (Elite Ed). 2011 Jun 1;3:1273-88.