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

General Information of Drug (ID: DMCDZ15)

• Drug Name: Evacetrapib Drug Info
• Synonyms: LY2484595

Indication

Disease Entry	ICD 11	Status	REF
Cardiovascular disease	BA00-BE2Z	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 49836058
  CAS Number: CAS 1186486-62-3
  TTD Drug ID: DMCDZ15
  INTEDE Drug ID: DR1878

Molecule-Related Drug Atlas

Drug(s) Targeting Cholesteryl ester transfer protein (CETP)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dalcetrapib	DMKNCVM	Acute coronary syndrome	BA41	Phase 3	[4]
Anacetrapib	DMP2BFG	Arteriosclerosis	BD40	Phase 3	[5]
JTT-302	DMGLVBI	Lipid metabolism disorder	5C52.Z	Phase 2	[2]
DRL-17822	DMGD3XT	Arteriosclerosis	BD40	Phase 2	[2]
TA-8995	DMAZHT0	Cardiovascular disease	BA00-BE2Z	Phase 2	[6]
BAY-60-5521	DMXIDWE	Arteriosclerosis	BD40	Phase 1	[7]
Torcetrapib	DMDHYM7	Hyperlipidaemia	5C80	Discontinued in Phase 2	[8]
CETi-1	DMUG5OB	Arteriosclerosis	BD40	Discontinued in Phase 2	[9]
CP-800569	DMZ0YU7	Arteriosclerosis	BD40	Discontinued in Phase 1	[10]
R7232	DMETAP8	Dyslipidemia	5C80-5C81	Discontinued in Phase 1	[4]

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	[11]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[12]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[13]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[14]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[15]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[16]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[17]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[18]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[12]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[19]

Drug(s) Metabolized By Cytochrome P450 2C8 (CYP2C8)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[20]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[21]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[21]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[22]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[23]
Diclofenac	DMPIHLS	Chronic renal failure	GB61.Z	Approved	[24]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[25]
Quinine	DMSWYF5	Malaria	1F40-1F45	Approved	[21]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[26]
Propofol	DMB4OLE	Anaesthesia	9A78.6	Approved	[27]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cholesteryl ester transfer protein (CETP)	TTFQAYR	CETP_HUMAN	Inhibitor	[2]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[3]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Substrate	[3]

References

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• [2] The dyslipidaemia market. Nat Rev Drug Discov. 2014 Nov;13(11):807-8.
• [3] Identification of cytochrome P450 enzymes involved in the metabolism of 4'-methoxy-alpha-pyrrolidinopropiophenone (MOPPP), a designer drug, in human liver microsomes. Xenobiotica. 2003 Oct;33(10):989-98.
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• [5] Assessment of a pharmacokinetic and pharmacodynamic interaction between simvastatin and anacetrapib, a potent cholesteryl ester transfer protein (C... Br J Clin Pharmacol. 2009 May;67(5):520-6.
• [6] Amgen To Acquire Privately-Held Dezima Pharma
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• [9] CETi-1. AVANT. Curr Opin Investig Drugs. 2004 Mar;5(3):334-8.
• [10] Pfizer. Product Development Pipeline. March 31 2009.
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• [15] 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.
• [16] 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.
• [17] Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
• [18] 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.
• [19] 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.
• [20] Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
• [21] Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
• [22] Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
• [23] Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
• [24] Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
• [25] Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
• [26] PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
• [27] Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.