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

General Information of Drug (ID: DML4H05)

• Drug Name: KX2-361 Drug Info
• Synonyms: KX-02

Indication

Disease Entry	ICD 11	Status	REF
Brain cancer	2A00	Phase 1	[1]
Glioblastoma multiforme	2A00.0	Phase 1	[2]

• Cross-matching ID:
  PubChem CID: 11545920
  CAS Number: CAS 897016-26-1
  TTD Drug ID: DML4H05

Molecule-Related Drug Atlas

Drug(s) Targeting Proto-oncogene c-Src (SRC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dasatinib	DMJV2EK	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[4]
Bosutinib	DMTI8YE	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[4]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[5]
Herbimycin A	DM6YWBF	Solid tumour/cancer	2A00-2F9Z	Approved	[6]
AL3818	DM3WP0N	Alveolar soft part sarcoma	2A60-2C35	Phase 3	[7]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[7]
Masitinib	DMRSNEU	Amyotrophic lateral sclerosis	8B60.0	Phase 3	[8]
KX-01	DMF0NA9	Actinic keratosis	EK90.0	Phase 3	[9]
Saracatinib	DMBLHGP	Hematologic tumour	2B33.Y	Phase 2	[10]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Proto-oncogene c-Src (SRC)	TT6PKBN	SRC_HUMAN	Inhibitor	[3]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800041844)
• [2] ClinicalTrials.gov (NCT02326441) Safety, Tolerability & PK of KX2-361 in Subjects w Adv. Malignancies Refractory to Conventional Therapies. U.S. National Institutes of Health.
• [3] 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. (Target id: 2206).
• [4] 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.
• [5] Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
• [6] In vivo antitumor activity of herbimycin A, a tyrosine kinase inhibitor, targeted against BCR/ABL oncoprotein in mice bearing BCR/ABL-transfected cells. Leuk Res. 1994 Nov;18(11):867-73.
• [7] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [8] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [9] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [10] Novel dual Src/Abl inhibitors for hematologic and solid malignancies.Expert Opin Investig Drugs.2010 Aug;19(8):931-45.
• [11] Clinical pipeline report, company report or official report of Turning Point Therapeutics.