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

General Information of Drug (ID: DM04C9V)

• Drug Name: PKF-241-466 Drug Info
• Synonyms: PKF-241-466; CHEMBL306090; BDBM50240611; N*4*-(2,2-Dimethyl-1-methylcarbamoyl-propyl)-N*1*-hydroxy-2-hydroxymethyl-3-p-tolyl-succinamide

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 9907830
  TTD Drug ID: DM04C9V

Molecule-Related Drug Atlas

Drug(s) Targeting Tumor necrosis factor (TNF)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Thalidomide	DM70BU5	Adult T-cell leukemia/lymphoma		Approved	[3]
Nafamostat	DMU1XOD	Pancreatitis	DC31-DC34	Approved	[4]
Pentoxifylline	DMU3DNC	Alcoholic hepatitis	DB94.1	Approved	[5]
Lenalidomide	DM6Q7U4	Adult T-cell leukemia/lymphoma		Approved	[6]
Enbrel	DM7RNP3	Arthritis	FA20	Approved	[7]
Golimumab	DMHZV7X	Psoriatic arthritis	FA21	Approved	[8]
Certolizumab	DM5CL9Z	Rheumatoid arthritis	FA20	Approved	[9]
Etanercept	DMCV109	Arthritis	FA20	Approved	[10]
Adalimumab	DMQMV1B	Crohn disease	DD70	Approved	[11]
Infliximab	DMH7OIA	Crohn disease	DD70	Approved	[12]

Drug(s) Targeting TNF alpha converting enzyme (ADAM17)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Apratastat	DM8W4N9	Rheumatoid arthritis	FA20	Phase 2	[13]
Aderbasib	DMYOMSC	Breast cancer	2C60-2C65	Phase 1/2	[14]
GW-3333	DM3PMAZ	Chronic obstructive pulmonary disease	CA22	Preclinical	[15]
DPC-333	DM4JBQD	Inflammatory bowel disease	DD72	Terminated	[15]
IK-862	DMJA4UE	Discovery agent	N.A.	Investigative	[16]
SR-973	DMU48OD	Discovery agent	N.A.	Investigative	[17]
SL422	DM3I2US	Discovery agent	N.A.	Investigative	[18]
PKF-242-484	DMNDLAS	Discovery agent	N.A.	Investigative	[1]
N-hydroxy-3-(2-oxo-2H-chromen-3-yl)propanamide	DMWXUCT	Discovery agent	N.A.	Investigative	[19]
N-hydroxy-3-(6-methoxy-2-oxo-2H-chromen-3-yl)	DMA6EPH	Discovery agent	N.A.	Investigative	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
TNF alpha converting enzyme (ADAM17)	TT6AZXG	ADA17_HUMAN	Inhibitor	[1]
Tumor necrosis factor (TNF)	TTF8CQI	TNFA_HUMAN	Inhibitor	[2]

References

• [1] Current perspective of TACE inhibitors: a review. Bioorg Med Chem. 2009 Jan 15;17(2):444-59.
• [2] Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme. J Med Chem. 2002 May 23;45(11):2289-93.
• [3] Efficacy of different thalidomide regimens for patients with multiple myeloma and its relationship with TNF-alpha level. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2008 Dec;16(6):1312-5.
• [4] Clinical pipeline report, company report or official report of AstraZeneca (2009).
• [5] Targeted therapies in myelodysplastic syndromes: ASH 2003 review. Semin Hematol. 2004 Apr;41(2 Suppl 4):13-20.
• [6] Thalidomide and thalidomide analogues for maintenance of remission in Crohn's disease. Cochrane Database Syst Rev. 2009 Apr 15;(2):CD007351.
• [7] Oral pentoxifylline inhibits release of tumor necrosis factor-alpha from human peripheral blood monocytes : a potential treatment for aseptic loose... J Bone Joint Surg Am. 2001 Jul;83(7):1057-61.
• [8] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [9] Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96.
• [10] The potential of biologics for the treatment of asthma. Nat Rev Drug Discov. 2012 Dec;11(12):958-72.
• [11] Adalimumab for psoriasis patients who are non-responders to etanercept: open-label prospective evaluation. J Eur Acad Dermatol Venereol. 2009 Dec;23(12):1394-7.
• [12] Drug insight: tumor necrosis factor-converting enzyme as a pharmaceutical target for rheumatoid arthritis. Nat Clin Pract Rheumatol. 2008 Jun;4(6):300-9.
• [13] Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9.
• [14] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [15] Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
• [16] Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge. Bioorg Med Chem. 2008 Oct 1;16(19):8781-94.
• [17] Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63.
• [18] Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo. J Med Chem. 2001 Aug 2;44(16):2636-60.
• [19] Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation. Bioorg Med Chem. 2008 Jan 1;16(1):530-5.