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

General Information of Drug (ID: DMMCA9V)

• Drug Name: SAR-113945 Drug Info
• Synonyms: S-0100229; S-0100658

Indication

Disease Entry	ICD 11	Status	REF
Osteoarthritis	FA00-FA05	Phase 2	[1]

• Cross-matching ID: TTD Drug ID: DMMCA9V

Molecule-Related Drug Atlas

Drug(s) Targeting Inhibitor of nuclear factor kappa-B kinase beta (IKKB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[3]
Parthenolide	DMCQBFT	N. A.	N. A.	Phase 2	[4]
IMD-1041	DMU1MR9	Alzheimer disease	8A20	Phase 2	[5]
IMD-0354	DMOFSLE	Acne vulgaris	ED80	Phase 1	[6]
MLN0415	DMG72VK	Arthritis	FA20	Discontinued in Phase 1	[7]
PF-228	DM32FKD	Discovery agent	N.A.	Investigative	[8]
5-Bromo-6-methoxy-9H-beta-carboline	DM157OQ	Discovery agent	N.A.	Investigative	[9]
Staurosporine	DM0E9BR	Discovery agent	N.A.	Investigative	[10]
5-amino-2-phenyl-oxazole-4-carboxylic acid amide	DMX37ZC	Discovery agent	N.A.	Investigative	[11]
5-amino-2-p-tolyl-oxazole-4-carboxylic acid amide	DM4SWJ7	Discovery agent	N.A.	Investigative	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Inhibitor of nuclear factor kappa-B kinase beta (IKKB)	TTJ3E9X	IKKB_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT01598415) Safety of Single Doses of SAR113945 and Efficacy and Safety of a New Formulation Given Into the Knee in Osteoarthritis Patients / Part II. U.S. National Institutes ofHealth.
• [2] The NF B pathway: a therapeutic target in glioblastoma. Oncotarget. 2011 August; 2(8): 646-653.
• [3] How acute promyelocytic leukaemia revived arsenic. Nat Rev Cancer. 2002 Sep;2(9):705-13.
• [4] The anti-inflammatory natural product parthenolide from the medicinal herb Feverfew directly binds to and inhibits IkappaB kinase. Chem Biol. 2001 Aug;8(8):759-66.
• [5] Inhibition of I B phosphorylation prevents load-induced cardiac dysfunction in mice. Am J Physiol Heart Circ Physiol. 2012 Dec 15;303(12):H1435-45.
• [6] I B kinase beta inhibitor IMD-0354 suppresses airway remodelling in a Dermatophagoides pteronyssinus-sensitized mouse model of chronic asthma. Clin Exp Allergy. 2011 Jan;41(1):104-15.
• [7] Company report (Millennium)
• [8] Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52.
• [9] Novel IKK inhibitors: beta-carbolines. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2419-22.
• [10] UCN-01: a potent abrogator of G2 checkpoint function in cancer cells with disrupted p53. J Natl Cancer Inst. 1996 Jul 17;88(14):956-65.
• [11] Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies. J Med Chem. 2006 May 18;49(10):2898-908.