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

General Information of Drug (ID: DMB9861)

• Drug Name: Rilapladib Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Arteriosclerosis	BD40	Phase 1	[1]
Cardiovascular disease	BA00-BE2Z	Phase 1	[2]

• Cross-matching ID:
  PubChem CID: 9918381
  CAS Number: CAS 412950-08-4
  TTD Drug ID: DMB9861

Molecule-Related Drug Atlas

Drug(s) Targeting Thymidine kinase 1 (TK1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Penciclovir	DMOUMDV	Herpes simplex labialis	1F00.01	Approved	[6]
DEOXYCYTIDINE	DMYE5LJ	Acute myeloid leukaemia	2A60	Approved	[7]
TK-DLI	DM26I8H	Graft-versus-host disease	4B24	Preregistration	[8]
FV-100	DMZARP1	Varicella zoster virus infection	1E91	Phase 3	[9]
Radiosensitizer gene therapy	DMN1ZEU	Pancreatic cancer	2C10	Phase 3	[10]
RP101	DMNIYSZ	Infectious disease	1A00-CA43.1	Phase 2/3	[11]
HQK-1004	DM3WX0K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[12]
Ad-OC-hsvTK/valacyclovir	DM9GLHO	Prostate cancer	2C82.0	Phase 1	[13]
Thymidine kinase-expressing adenovirus and ganciclovir suicide gene therapy	DMO8SGD	Solid tumour/cancer	2A00-2F9Z	Phase 1	[14]
Sitimagene ceradenovec	DM0T2QV	Brain cancer	2A00	Discontinued in Phase 3	[15]

Drug(s) Targeting Phospholipase A2 (PLA2G1B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cholic Acid	DM7OKQV	Cholelithiasis	DC11	Approved	[6]
Miltefosine	DMND304	Chronic urticaria		Approved	[16]
Clocortolone	DM9ZMQH	Exanthem		Approved	[17]
Clobetasol	DMUXP52	Rosacea	ED90.0	Approved	[18]
Diflorasone	DMI9PRJ	Exanthem		Approved	[19]
AllerB	DM78DOT	Allergy	4A80-4A85	Phase 2b	[20]
URSOLIC ACID	DM4SOAW	Metabolic syndrome x	5C50-5D2Z	Phase 2	[21]
MANOALIDE	DMB4A8I	Arthritis	FA20	Phase 2	[22]
MRX-4	DMQZWYE	Allergic rhinitis	CA08.0	Phase 2	[23]
MRX-6	DMLVQKF	Contact dermatitis	EK0Z	Phase 2	[24]

Drug(s) Targeting Platelet-activating factor acetylhydrolase (PLA2G7)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GSK2647544	DM3KARJ	Alzheimer disease	8A20	Phase 1	[25]
Indolizine derivative 1	DM4GZBI	N. A.	N. A.	Patented	[26]
Bicyclic pyrimidine derivative 2	DMJP16K	N. A.	N. A.	Patented	[26]
RPAF-AH	DMOVJ60	Sepsis	1G40-1G41	Discontinued in Phase 3	[27]
GSK568859	DM6E84O	Arteriosclerosis	BD40	Discontinued in Phase 1	[25]
Goxalapladib	DMSGUY9	Arteriosclerosis	BD40	Discontinued in Phase 1	[28]
(1r)-1,2,2-trimethylpropyl (r)-methylphosphinate	DMVE34H	Discovery agent	N.A.	Investigative	[29]
Benzaldehyde O-benzoyloxime	DMB7DFT	Discovery agent	N.A.	Investigative	[30]
(E)-(thiophen-2-ylmethylidene)amino benzoate	DMHSJAT	Discovery agent	N.A.	Investigative	[31]
3,4-difluorobenzaldehyde O-benzoyloxime	DMFV3Y9	Discovery agent	N.A.	Investigative	[30]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Phospholipase A2 (PLA2G1B)	TT9V5JH	PA21B_HUMAN	Modulator	[3]
Platelet-activating factor acetylhydrolase (PLA2G7)	TTDNFMT	PAFA_HUMAN	Inhibitor	[4]
Thymidine kinase 1 (TK1)	TTP3QRF	KITH_HUMAN	Inhibitor	[5]

References

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• [3] Effect of treatment for 12 weeks with rilapladib, a lipoprotein-associated phospholipase A2 inhibitor, on arterial inflammation as assessed with 18F-fluorodeoxyglucose-positron emission tomography imaging.J Am Coll Cardiol.2014 Jan 7-14;63(1):86-8.
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• [7] Species- or isozyme-specific enzyme inhibitors. 5. Differential effects of thymidine substituents on affinity for rat thymidine kinase isozymes. J Med Chem. 1982 Jun;25(6):644-9.
• [8] Company report (Takara Bio)
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• [13] Phase I dose escalation clinical trial of adenovirus vector carrying osteocalcin promoter-driven herpes simplex virus thymidine kinase in localized and metastatic hormone-refractory prostate cancer. Hum Gene Ther. 2003 Feb 10;14(3):227-41.
• [14] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [15] Sitimagene ceradenovec: a gene-based drug for the treatment of operable high-grade glioma. Future Oncol. 2010 Nov;6(11):1691-710.
• [16] Novel antifungal agents, targets or therapeutic strategies for the treatment of invasive fungal diseases: a review of the literature (2005-2009). Rev Iberoam Micol. 2009 Mar 31;26(1):15-22.
• [17] Clocortolone pivalate: a paired comparison clinical trial of a new topical steroid in eczema/atopic dermatitis. Cutis. 1980 Jan;25(1):96-8.
• [18] Utilization of epidermal phospholipase A2 inhibition to monitor topical steroid action. Br J Dermatol. 1984 Jul;111 Suppl 27:195-203.
• [19] Structures from powders: diflorasone diacetate. Steroids. 2009 Jan;74(1):102-11.
• [20] Successful immunotherapy with T-cell epitope peptides of bee venom phospholipase A2 induces specific T-cell anergy in patients allergic to bee venom. J Allergy Clin Immunol. 1998 Jun;101(6 Pt 1):747-54.
• [21] Synthesis of benzoyl phenyl benzoates as effective inhibitors for phospholipase A2 and hyaluronidase enzymes. Bioorg Med Chem Lett. 2005 Sep 15;15(18):4100-4.
• [22] Manoalide, a phospholipase A2 inhibitor, inhibits arachidonate incorporation and turnover in brain phospholipids of the awake rat. Neurochem Res. 1998 Oct;23(10):1251-7.
• [23] Phospholipase A2, group IVA (cytosolic, calcium-dependent) (PLA2G4A). SciBX 1(41); doi:10.1038/scibx.2008.999. Nov. 13 2008
• [24] A novel treatment of contact dermatitis by topical application of phospholipase A2 inhibitor: a double-blind placebo-controlled pilot study. Int J Immunopathol Pharmacol. 2007 Jan-Mar;20(1):191-5.
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• [26] Inhibitors of phospholipase A2 and their therapeutic potential: an update on patents (2012-2016).Expert Opin Ther Pat. 2017 Feb;27(2):217-225.
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• [29] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [30] Potent inhibitors of lipoprotein-associated phospholipase A(2): benzaldehyde O-heterocycle-4-carbonyloxime. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5576-9.
• [31] (E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1525-7.