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

General Information of Drug (ID: DM7B650)

• Drug Name: RG-2833 Drug Info
• Synonyms: RG-FA; HDAC-1 inhibtors (Friedreich ataxia), RepliGen

Indication

Disease Entry	ICD 11	Status	REF
Friedreich's ataxia	8A03.10	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 56654642
  CAS Number: CAS 1215493-56-3
  TTD Drug ID: DM7B650

Molecule-Related Drug Atlas

Drug(s) Targeting Histone deacetylase 1 (HDAC1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Vorinostat	DMWMPD4	Adult acute monocytic leukemia		Approved	[4]
Romidepsin	DMT5GNL	Cutaneous T-cell lymphoma	2B01	Approved	[5]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[4]
HBI-8000	DMDWYUN	Non-small-cell lung cancer	2C25.Y	Registered	[2]
ITF2357	DMFZBNE	Duchenne dystrophy	8C70	Phase 3	[6]
NVP-LAQ824	DM8JWNA	Mood disorder	6A60-6E23	Phase 3	[7]
SNDX-275	DMH7W9X	Breast cancer	2C60-2C65	Phase 3	[8]
Phenylbutyrate	DMBHPDW	Urea cycle disorder	5C50.A	Phase 2	[9]
MGCD-0103	DM726HX	Non-small-cell lung cancer	2C25.Y	Phase 2	[4]
Resminostat	DMNE1FR	Hepatocellular carcinoma	2C12.02	Phase 2	[10]

Drug(s) Affected By Frataxin, mitochondrial (FXN)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[11]
Molsidomine	DM9MA8O	Angina pectoris	BA40	Approved	[12]
Betamethasone	DMAHJEF	Acute adrenal insufficiency		Approved	[12]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[13]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[14]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[15]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[16]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[17]
Deferiprone	DMS2M7O	Beta thalassemia	3A50.2	Approved	[12]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histone deacetylase 1 (HDAC1)	TT6R7JZ	HDAC1_HUMAN	Modulator	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Frataxin, mitochondrial (FXN)	OTE9U09A	FRDA_HUMAN	Gene/Protein Processing	[3]

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: 7501).
• [2] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [3] Epigenetic therapy for Friedreich ataxia. Ann Neurol. 2014 Oct;76(4):489-508. doi: 10.1002/ana.24260. Epub 2014 Sep 16.
• [4] Protein methyltransferases as a target class for drug discovery. Nat Rev Drug Discov. 2009 Sep;8(9):724-32.
• [5] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [6] Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Sep;14(3):471-9.
• [7] NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood. 2003 Oct 1;102(7):2615-22.
• [8] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
• [9] Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
• [10] 2011 Pipeline of 4SC AG.
• [11] Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
• [12] Pharmacological screening using an FXN-EGFP cellular genomic reporter assay for the therapy of Friedreich ataxia. PLoS One. 2013;8(2):e55940.
• [13] Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
• [14] Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
• [15] Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
• [16] Oxidative stress-dependent frataxin inhibition mediated alcoholic hepatocytotoxicity through ferroptosis. Toxicology. 2020 Dec 1;445:152584. doi: 10.1016/j.tox.2020.152584. Epub 2020 Oct 2.
• [17] Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
• [18] Increased mitochondrial ROS formation by acetaminophen in human hepatic cells is associated with gene expression changes suggesting disruption of the mitochondrial electron transport chain. Toxicol Lett. 2015 Apr 16;234(2):139-50.