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

General Information of Drug (ID: DML6XSP)

Drug Name

Resiquimod Drug Info

Synonyms

Resiquimod [INN]; R 848; S 28463; R-848; S-28463; VML-600; 1-(4-Amino-2-ethoxymethyl-imidazo[4,5-c]quinolin-1-yl)-2-methyl-propan-2-ol; 1-[4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-ol; 1-[4-amino-2-(ethoxymethyl)imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-ol; 4-amino-2-(ethoxymethyl)-a,a-dimethyl-1h-imidazo[4,5-c]quinoline-1-ethanol; 4-amino-2-ethoxymethyl-alpha,alpha-dimethyl-1H-imidazo(4,5-c)quinoline-1-ethanol

Indication

Disease Entry	ICD 11	Status	REF
Actinic keratosis	EK90.0	Phase 2	[1]
Cutaneous T-cell lymphoma	2B01	Phase 2	[2]
Herpes simplex virus infection	1F00	Phase 1/2	[3]

Cross-matching ID

PubChem CID: 159603
ChEBI ID: CHEMBL383322
CAS Number: CAS 144875-48-9
TTD Drug ID: DML6XSP

Molecule-Related Drug Atlas

Molecule Type:

DTT

DOT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Toll-like receptor 7 (TLR7)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Imiquimod	DM1TMA3	Alopecia areata	ED70.2	Approved	[7]
Hydroxychloroquine	DMSIVND	Chronic renal failure	GB61.Z	Approved	[8]
ANA773	DMSC8YW	Hepatitis C virus infection	1E51.1	Phase 2a	[9]
GS-9620	DMG5C8D	Hepatitis B virus infection	1E51.0	Phase 2	[10]
IMO-3100	DMM549D	Psoriasis vulgaris	EA90	Phase 2	[11]
LOXORIBINE	DMIV9ZE	Immune System disease	4A01-4B41	Phase 2	[12]
GSK2245035	DMBWPZJ	Asthma	CA23	Phase 2	[13]
AZD-8848	DM0M7QW	Allergic rhinitis	CA08.0	Phase 2	[14]
Isatoribine	DMHOJ8W	Hepatitis C virus infection	1E51.1	Phase 2	[15]
PF-4878691	DM24I0N	Melanoma	2C30	Phase 2	[16]
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Drug(s) Targeting Toll-like receptor 8 (TLR8)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Selgantolimod	DMST4OR	Hepatitis B	1E51	Phase 2	[17]
Afimetoran	DM3HN3U	Systemic lupus erythematosus	4A40.0	Phase 2	[18]
NKTR-262	DMYR8LF	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[19]
CPG 52364	DMVDYTG	Systemic lupus erythematosus	4A40.0	Phase 1	[20]
CV8102	DMYD37G	Melanoma	2C30	Phase 1	[21]
MEDI9197	DM0J7UR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[22]
SBT6050	DMHBD3T	Solid tumour/cancer	2A00-2F9Z	Phase 1	[23]
VTX-1463	DM4ZIRK	Allergic rhinitis	CA08.0	Phase 1	[24]
DN1508052	DM0JT9C	Solid tumour/cancer	2A00-2F9Z	Phase 1	[25]
GSK5251738	DM8Y6DR	Hepatitis B	1E51	Phase 1	[26]
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Drug(s) Affected By Interleukin-12 subunit beta (IL12B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Nitric Oxide	DM1RBYG	Hypertension	BA00-BA04	Approved	[27]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[28]
Isoniazid	DM5JVS3	Latent tuberculosis infection		Approved	[29]
Marinol	DM70IK5	Anorexia nervosa cachexia	6B80	Approved	[30]
Ergotidine	DM78IME	Osteoarthritis	FA00-FA05	Approved	[31]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[32]
Capsaicin	DMGMF6V	Back pain	ME84.Z	Approved	[33]
Azacitidine	DMTA5OE	Acute myelogenous leukaemia	2A41	Approved	[34]
Dinoprostone	DMTYOPD	Medical abortion	JA00.1Z	Approved	[35]
Bryostatin-1	DM1JOXY	Alzheimer disease	8A20	Phase 2	[36]
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Drug(s) Affected By Interleukin-1 receptor-associated kinase 4 (IRAK4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[37]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[38]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[39]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[40]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[41]
Mifepristone	DMGZQEF	Cushing disease	5A70	Approved	[42]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[43]
Arsenic	DMTL2Y1	N. A.	N. A.	Approved	[44]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[42]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[45]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Toll-like receptor 7 (TLR7)	TTRJ1K4	TLR7_HUMAN	Modulator	[4]
Toll-like receptor 8 (TLR8)	TT8CWFK	TLR8_HUMAN	Modulator	[4]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Interleukin-1 receptor-associated kinase 4 (IRAK4)	OT9JTJWC	IRAK4_HUMAN	Post-Translational Modifications	[5]
Interleukin-12 subunit beta (IL12B)	OT0JF8A3	IL12B_HUMAN	Gene/Protein Processing	[6]

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References

1	ClinicalTrials.gov (NCT01583816) Dose-finding, Safety, Efficacy Trial of Topical Resiquimod in Patients With Multiple Actinic Keratosis Lesions. U.S. National Institutes of Health.
2	ClinicalTrials.gov (NCT03292406) A Safety, Efficacy and Pharmacokinetics Study of CD11301 for the Treatment of Cutaneous T-Cell Lymphoma (CTCL) (CTCL). U.S. National Institutes of Health.
3	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: 5051).
4	TLR agonists as vaccine adjuvants: comparison of CpG ODN and Resiquimod (R-848).Vaccine.2005 Nov 1;23(45):5263-70.
5	IRAK4 kinase activity controls Toll-like receptor-induced inflammation through the transcription factor IRF5 in primary human monocytes. J Biol Chem. 2017 Nov 10;292(45):18689-18698. doi: 10.1074/jbc.M117.796912. Epub 2017 Sep 18.
6	Differential regulation of interleukin 12 and interleukin 23 production in human dendritic cells. J Exp Med. 2008 Jun 9;205(6):1447-61. doi: 10.1084/jem.20071450. Epub 2008 May 19.
7	Imiquimod enhances IFN-gamma production and effector function of T cells infiltrating human squamous cell carcinomas of the skin. J Invest Dermatol. 2009 Nov;129(11):2676-85.
8	TLR7/9 antagonists as therapeutics for immune-mediated inflammatory disorders. Inflamm Allergy Drug Targets. 2007 Dec;6(4):223-35.
9	Clinical pipeline report, company report or official report of Anadys Pharmaceuticals (2011).
10	Pharmacokinetic and pharmacodynamic properties of GS-9620, a novel Toll-like receptor 7 agonist, demonstrate interferon-stimulated gene induction without detectable serum interferon at low oral doses. J Pharmacol Exp Ther. 2014 Jan;348(1):96-105.
11	Company report (Iderapharma)
12	The Toll-like receptor 7 (TLR7)-specific stimulus loxoribine uncovers a strong relationship within the TLR7, 8 and 9 subfamily. Eur J Immunol. 2003 Nov;33(11):2987-97.
13	Early clinical evaluation of the intranasal TLR7 agonist GSK2245035: Use of translational biomarkers to guide dosing and confirm target engagement. Clin Pharmacol Ther. 2015 Oct;98(4):369-80.
14	Repeated intranasal TLR7 stimulation reduces allergen responsiveness in allergic rhinitis. Respir Res. 2012 Jun 22;13:53.
15	Discovery of ANA975: an oral prodrug of the TLR-7 agonist isatoribine. Nucleosides Nucleotides Nucleic Acids. 2007;26(6-7):635-40.
16	The innate immune response, clinical outcomes, and ex vivo HCV antiviral efficacy of a TLR7 agonist (PF-4878691). Clin Pharmacol Ther. 2011 Jun;89(6):821-9.
17	Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B. J Med Chem. 2020 Sep 24;63(18):10188-10203.
18	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
19	Clinical pipeline report, company report or official report of Nektar Therapeutics.
20	Coley Pharmaceutical Group Diversifies Pipeline with First-in-Class TLR Antagonist for the Treatment of Systemic Lupus Erythematosus. Lupus Foundation of America, Inc. 2007.
21	Clinical pipeline report, company report or official report of CureVac.
22	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
23	Clinical pipeline report, company report or official report of Silverback Therapeutics.
24	VTX-1463, a novel TLR8 agonist for the treatment of allergic rhinitis. Expert Opin Investig Drugs. 2011 Jul;20(7):981-6.
25	Clinical pipeline report, company report or official report of Shanghai De Novo Pharmatech.
26	Clinical pipeline report, company report or official report of GlaxoSmithKline
27	Regulatory role of nitric oxide on monocyte-derived dendritic cell functions. J Interferon Cytokine Res. 2003 Aug;23(8):423-31. doi: 10.1089/107999003322277838.
28	[Effects of vitamin A on the differentiation, maturation and functions of dendritic cells from cord blood]. Zhonghua Er Ke Za Zhi. 2004 May;42(5):340-3.
29	Characterization of drug-specific signaling between primary human hepatocytes and immune cells. Toxicol Sci. 2017 Jul 1;158(1):76-89.
30	Alcohol and Cannabinoids Differentially Affect HIV Infection and Function of Human Monocyte-Derived Dendritic Cells (MDDC). Front Microbiol. 2015 Dec 22;6:1452. doi: 10.3389/fmicb.2015.01452. eCollection 2015.
31	Histamine inhibits the production of interleukin-12 through interaction with H2 receptors. J Clin Invest. 1998 Nov 15;102(10):1866-73. doi: 10.1172/JCI3692.
32	Systemic drugs inducing non-immediate cutaneous adverse reactions and contact sensitizers evoke similar responses in THP-1 cells. J Appl Toxicol. 2015 Apr;35(4):398-406. doi: 10.1002/jat.3033. Epub 2014 Aug 4.
33	Induction of the endoplasmic reticulum stress protein GADD153/CHOP by capsaicin in prostate PC-3 cells: a microarray study. Biochem Biophys Res Commun. 2008 Aug 8;372(4):785-91.
34	The effect of DNA methylation inhibitor 5-Aza-2'-deoxycytidine on human endometrial stromal cells. Hum Reprod. 2010 Nov;25(11):2859-69.
35	Prostaglandin E(2) is a selective inducer of interleukin-12 p40 (IL-12p40) production and an inhibitor of bioactive IL-12p70 heterodimer. Blood. 2001 Jun 1;97(11):3466-9. doi: 10.1182/blood.v97.11.3466.
36	Effect of serum and antioxidants on the immunogenicity of protein kinase C-activated chronic lymphocytic leukemia cells. J Immunother. 2005 Jan-Feb;28(1):28-39. doi: 10.1097/00002371-200501000-00004.
37	The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
38	The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
39	Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
40	Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
41	Acanthoic acid protectsagainst ethanol-induced liver injury: Possible role of AMPK activation and IRAK4 inhibition. Toxicol Lett. 2017 Nov 5;281:127-138. doi: 10.1016/j.toxlet.2017.09.020. Epub 2017 Sep 28.
42	Expression and modulation of progesterone induced blocking factor (PIBF) and innate immune factors in human leukemia cell lines by progesterone and mifepristone. Leuk Lymphoma. 2007 Aug;48(8):1610-7. doi: 10.1080/10428190701471999.
43	Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
44	Prenatal arsenic exposure and the epigenome: identifying sites of 5-methylcytosine alterations that predict functional changes in gene expression in newborn cord blood and subsequent birth outcomes. Toxicol Sci. 2015 Jan;143(1):97-106. doi: 10.1093/toxsci/kfu210. Epub 2014 Oct 10.
45	Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.