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

General Information of Drug (ID: DMMK42O)

• Drug Name: Roquinimex Drug Info
• Synonyms: Linomide

Indication

Disease Entry	ICD 11	Status	REF
Rheumatoid arthritis	FA20	Discontinued in Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 54676478
  ChEBI ID: CHEBI:92056
  CAS Number: CAS 84088-42-6
  TTD Drug ID: DMMK42O
  INTEDE Drug ID: DR1443

Molecule-Related Drug Atlas

Drug(s) Targeting Interleukin-2 (IL2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aldesleukin	DM4YMIS	Acute myelogenous leukaemia	2A41	Approved	[4]
Daclizumab	DM6OZQV	Aplastic anemia	3A70	Approved	[5]
AIR-insulin	DM8SYTE	Diabetic complication	5A2Y	Phase 3	[6]
TG-4010	DMWE3GB	Bipolar disorder	6A60	Phase 2/3	[7]
BNZ-1	DM8JQZC	Cutaneous T-cell lymphoma	2B01	Phase 2	[8]
IL-2/CD40L-expressing leukemia vaccine	DMIHQ5G	Chronic lymphocytic leukaemia	2A82.0	Phase 2	[9]
Carboxyamidotriazole orotate	DMN5JCX	Glioblastoma multiforme	2A00.0	Phase 2	[10]
Leuvectin	DM5LQEI	Melanoma	2C30	Phase 2	[11]
Human interleukin-2	DM0NJWG	Renal cell carcinoma	2C90	Phase 2	[12]
L19-IL-2 fusion protein	DMI2XP1	Lymphoma	2A80-2A86	Phase 2	[13]

Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[14]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[15]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[16]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[17]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[18]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[19]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[20]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[21]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[15]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[22]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Interleukin-2 (IL2)	TTF89GD	IL2_HUMAN	Modulator	[2]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4) Main DME	DE4LYSA	CP3A4_HUMAN	Substrate	[3]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001478)
• [2] The novel immunomodulator, Linomide, stimulates interleukin-2-induced human natural killer (NK) cell and PHA-stimulated T cell proliferation from normal donors. Leuk Res. 1996 Jan;20(1):57-63.
• [3] Identification of cytochrome P4503A as the major subfamily responsible for the metabolism of roquinimex in man. Xenobiotica. 2000 Sep;30(9):905-14.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [5] 2016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76.
• [6] The AIR inhaled insulin system: system components and pharmacokinetic/glucodynamic data. Diabetes Technol Ther. 2007 Jun;9 Suppl 1:S41-7.
• [7] A phase II study of Tg4010 (Mva-Muc1-Il2) in association with chemotherapy in patients with stage III/IV Non-small cell lung cancer. J Thorac Oncol. 2008 Jul;3(7):735-44.
• [8] Clinical pipeline report, company report or official report of Bioniz Therapeutics.
• [9] Immunotherapy of high-risk acute leukemia with a recipient (autologous) vaccine expressing transgenic human CD40L and IL-2 after chemotherapy and a... Blood. 2006 Feb 15;107(4):1332-41.
• [10] J Clin Oncol 32:5s, 2014 (suppl; abstr 2071).
• [11] Intratumoral interleukin 2 for renal-cell carcinoma by direct gene transfer of a plasmid DNA/DMRIE/DOPE lipid complex. World J Urol. 2000 Apr;18(2):152-6.
• [12] Clinical pipeline report, company report or official report of Immunservice.
• [13] National Cancer Institute Drug Dictionary (drug id 665656).
• [14] Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
• [15] Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
• [16] Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
• [17] Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
• [18] Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
• [19] Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
• [20] Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
• [21] The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
• [22] Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.