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

General Information of Drug (ID: DMAO04B)

• Drug Name: CEP-32496 Drug Info
• Synonyms: AB-024; B-RAF kinase inhibitors (melanoma), Ambit/Cephalon

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[1] , [2]

• Cross-matching ID:
  PubChem CID: 56846693
  CAS Number: CAS 1188910-76-0
  TTD Drug ID: DMAO04B
  VARIDT Drug ID: DR00774

Molecule-Related Drug Atlas

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[5]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	Approved	[6]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[6]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[7]
Selpercatinib	DMZR15V	Non-small-cell lung cancer	2C25.Y	Approved	[8]
Pralsetinib	DMWU0I2	Non-small-cell lung cancer	2C25.Y	Approved	[9]
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[10]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[11]
GSK3179106	DM2KCIP	Inflammatory bowel disease	DD72	Phase 1	[12]
BOS172738	DM9L0D8	Solid tumour/cancer	2A00-2F9Z	Phase 1	[13]

Drug(s) Targeting Serine/threonine-protein kinase B-raf (BRAF)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dabrafenib	DMX6OE3	Melanoma	2C30	Approved	[14]
Vemurafenib	DM62UG5	Melanoma	2C30	Approved	[6]
LGX818	DMNQXV8	Melanoma	2C30	Approved	[15]
PLX8394	DMRTD7I	Solid tumour/cancer	2A00-2F9Z	Phase 2	[16]
BGB-283	DMVYTG7	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[17]
ARQ 736	DMP9ZT1	Solid tumour/cancer	2A00-2F9Z	Phase 1	[18]
RO-5212054	DML4C3Q	Solid tumour/cancer	2A00-2F9Z	Phase 1	[19]
ASN003	DMJCX6D	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
BMS-908662	DM3K8VM	Solid tumour/cancer	2A00-2F9Z	Phase 1	[20]
ABM-1310	DMS1HR3	Solid tumour/cancer	2A00-2F9Z	Phase 1	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Proto-oncogene c-Ret (RET)	TT4DXQT	RET_HUMAN	Inhibitor	[3]
Serine/threonine-protein kinase B-raf (BRAF)	TTWCGQT	BRAF_HUMAN	Inhibitor	[4]

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: 7880).
• [2] ClinicalTrials.gov (NCT01877811) CEP-32496 in Patients With Advanced Solid Tumors in Phase 1 and Advanced Melanoma and Metastatic Colorectal Cancer in Phase 2. 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] Clinical pipeline report, company report or official report of Ambit Biosciences.
• [5] 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.
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [7] 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.
• [8] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [9] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [10] 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).
• [11] Clinical pipeline report, company report or official report of Turning Point Therapeutics.
• [12] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [13] National Cancer Institute Drug Dictionary (drug name Zeteletinib).
• [14] Clinical pipeline report, company report or official report of GlaxoSmithKline (2011).
• [15] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [16] Identification of PLX4032-resistance mechanisms and implications for novel RAF inhibitors. Pigment Cell Melanoma Res. 2014 Mar;27(2):253-62.
• [17] BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. Mol Cancer Ther. 2015 Oct;14(10):2187-97.
• [18] National Cancer Institute Drug Dictionary (drug id 688029).
• [19] National Cancer Institute Drug Dictionary (drug id 680347).
• [20] Clinical pipeline report, company report or official report of Exelixis (2011).
• [21] Clinical pipeline report, company report or official report of ABM Therapeutics.