Details of the Drug

General Information of Drug (ID: DMRSN2C)

• Drug Name: MB-12066
• Synonyms: B-lapachone (obesity), Mazence; Beta-lapachone (obesity), Mazence

Indication

Disease Entry	ICD 11	Status	REF
Obesity	5B81	Phase 2	[1]

• Cross-matching ID: TTD ID: D0TU7V

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
NAD-dependent deacetylase sirtuin-1 (SIRT1)	TTUF2HO	SIR1_HUMAN	Modulator	[2]

Molecular Expression Atlas of This Drug

• The Studied Disease: Obesity
• ICD Disease Classification: 5B81

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
NAD-dependent deacetylase sirtuin-1 (SIRT1)	DTT	SIRT1	7.82E-01	-0.16	-0.27

References

• [1] ClinicalTrials.gov (NCT02029586) Therapeutic Exploratory Phase 2 Study to Evaluate the Safety and Efficacy of MB12066 in Patients With Nonalcoholic Fatty Liver Disease(NAFLD) Except Cirrhosis. U.S. National Institutes of Health.
• [2] Pharmacological activation of Sirt1 ameliorates polyglutamine-induced toxicity through the regulation of autophagy.PLoS One.2013 Jun 10;8(6):e64953.
• [3] Sirtuin modulators: an updated patent review (2012 - 2014).Expert Opin Ther Pat. 2015 Jan;25(1):5-15.
• [4] Sirtuin 1 activator SRT2104 protects Huntington's disease mice. Ann Clin Transl Neurol. 2014 Dec;1(12):1047-52.
• [5] Sirtuin 1 (SIRT1): the misunderstood HDAC. J Biomol Screen. 2011 Dec;16(10):1153-69.
• [6] SRT2379, a small-molecule SIRT1 activator, fails to reduce cytokine release in a human endotoxemia model. Critical Care 2013, 17(Suppl 4):P8.
• [7] The Sirt1 Activators SRT2183 and SRT3025 Inhibit RANKL-Induced Osteoclastogenesis in Bone Marrow-Derived Macrophages and Down-Regulate Sirt3 in Sirt1 Null Cells. PLoS One. 2015 Jul 30;10(7):e0134391.
• [8] Novel cambinol analogs as sirtuin inhibitors: synthesis, biological evaluation, and rationalization of activity. J Med Chem. 2009 May 14;52(9):2673-82.
• [9] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).