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

General Information of Drug (ID: DM752PU)

• Drug Name: MGCD516 Drug Info
• Synonyms: Sitravatinib

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[1]
Breast cancer	2C60-2C65	Phase 2	[2]
Non-small-cell lung cancer	2C25.Y	Phase 1/2	[3]

• Cross-matching ID:
  PubChem CID: 25212148
  CAS Number: CAS 1123837-84-2
  TTD Drug ID: DM752PU

Molecule-Related Drug Atlas

Drug(s) Targeting Vascular endothelial growth factor receptor 3 (FLT-4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[8]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[9]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[10]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[11]
PI-88	DMGZPX6	Hepatocellular carcinoma	2C12.02	Phase 3	[12]
Taberminogene vadenovec	DMW5PHL	Vascular restinosis	BE2Z	Phase 3	[13]
ABT-869	DMREDYP	Solid tumour/cancer	2A00-2F9Z	Phase 3	[14]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[15]
VATALANIB	DMY0UEQ	Solid tumour/cancer	2A00-2F9Z	Phase 2	[16]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[17]

Drug(s) Targeting Proto-oncogene c-Met (MET)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[18]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[19]
Amivantamab	DMZ7AMY	Non-small-cell lung cancer	2C25	Approved	[20]
Capmatinib	DMYCXKL	Non-small-cell lung cancer	2C25.Y	Approved	[21]
Tepotinib	DMUQ0E8	Non-small-cell lung cancer	2C25	Approved	[22]
RG3638	DMTQJE0	Gastric adenocarcinoma	2B72	Phase 3	[4]
Savolitinib	DMALFKX	Renal cell carcinoma	2C90	Phase 3	[3]
Beperminogene perplasmid	DM6RWBN	Critical limb ischemia	BD4Y	Phase 3	[23]
Tivantinib	DMNVP8Q	Hepatocellular carcinoma	2C12.02	Phase 3	[24]
CMX-2043	DMPSCVY	Cardiac disease	BA00-BE2Z	Phase 2	[25]

Drug(s) Targeting Proto-oncogene c-Ret (RET)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[26]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[18]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[18]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[27]
Selpercatinib	DMZR15V	Non-small-cell lung cancer	2C25.Y	Approved	[28]
Pralsetinib	DMWU0I2	Non-small-cell lung cancer	2C25.Y	Approved	[29]
CEP-32496	DMAO04B	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[3]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[30]
GSK3179106	DM2KCIP	Inflammatory bowel disease	DD72	Phase 1	[31]
BOS172738	DM9L0D8	Solid tumour/cancer	2A00-2F9Z	Phase 1	[32]

Drug(s) Targeting Protein kinase (PK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LY2801653	DM0KJDY	Biliary tract cancer	2C17	Phase 2	[3]
MGCD265	DMRPCF2	Non-small-cell lung cancer	2C25.Y	Phase 2	[3]
ENMD-2076	DMJZVPB	Acute myeloid leukaemia	2A60	Phase 2	[3]
RV-568	DM652CM	Asthma	CA23	Phase 2	[33]
TG02	DMZFIGQ	Anaplastic astrocytoma	2A00.0	Phase 1/2	[34]
LX-7101	DM2LYIN	Glaucoma/ocular hypertension	9C61	Phase 1/2	[35]
Cyclocreatine	DM1I7UO	Virus infection	1A24-1D9Z	Discontinued in Phase 1	[36]

Drug(s) Targeting Vascular endothelial growth factor receptor 2 (KDR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[37]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[38]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[18]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[39]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[40]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[27]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[41]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[8]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[19]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[9]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Protein kinase (PK)	TTU8W4S	NOUNIPROTAC	Inhibitor	[3]
Proto-oncogene c-Met (MET)	TTNDSF4	MET_HUMAN	Inhibitor	[4]
Proto-oncogene c-Ret (RET)	TT4DXQT	RET_HUMAN	Inhibitor	[5]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[6]
Vascular endothelial growth factor receptor 3 (FLT-4)	TTDCBX5	VGFR3_HUMAN	Inhibitor	[7]

References

• [1] ClinicalTrials.gov (NCT04887870) Study of Sitravatinib With or Without Other Anticancer Therapies Receiving Clinical Benefit From Parent Study. U.S. National Institutes of Health.
• [2] ClinicalTrials.gov (NCT04123704) Sitravatinib in Metastatic Breast Cancer. U.S. National Institutes of Health.
• [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. (Target id: 1815).
• [5] 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: 2185).
• [6] 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: 1813).
• [7] 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: 1814).
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• [11] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [12] Company report (Medigen)
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• [20] Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC. Cancer Discov. 2020 Aug;10(8):1194-1209.
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• [24] 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: 7948).
• [25] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [26] Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96.
• [27] 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.
• [28] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [29] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [30] Clinical pipeline report, company report or official report of Turning Point Therapeutics.
• [31] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [32] National Cancer Institute Drug Dictionary (drug name Zeteletinib).
• [33] Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92.
• [34] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [35] Design, synthesis and biological characterization of selective LIMK inhibitors. Bioorg Med Chem Lett. 2015 Sep 15;25(18):4005-10.
• [36] Direct determination of creatine kinase equilibrium constants with creatine or cyclocreatine substrate. Biochim Biophys Acta. 1989 Oct 19;998(3):317-20.
• [37] Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
• [38] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [39] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
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