Details of the Drug

General Information of Drug (ID: DMG9B1U)

• Drug Name: Elvitegravir
• Synonyms: EVG

Indication

Disease Entry	ICD 11	Status	REF
Human immunodeficiency virus infection	1C62	Approved	[1]

• ATC Code:
  J05AJ02: Elvitegravir
  J05AJ: Integrase inhibitors
  J05A: DIRECT ACTING ANTIVIRALS
  J05: ANTIVIRALS FOR SYSTEMIC USE
  J: ANTIINFECTIVES FOR SYSTEMIC USE
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 1:
  Molecular Weight (mw); 447.9
  Logarithm of the Partition Coefficient (xlogp); 5.3
  Rotatable Bond Count (rotbonds); 7
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 7
• ADMET Property:
  Half-life: The concentration or amount of drug in body reduced by one-half in 8.7 hours [2]
  Metabolism: The drug is metabolized via the CYP3A, and is secondarily glucuronidated via UGT1A1/3 enzymes []
• Chemical Identifiers:
  Formula: C23H23ClFNO5
  IUPAC Name: 6-[(3-chloro-2-fluorophenyl)methyl]-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxoquinoline-3-carboxylic acid
  Canonical SMILES: CC(C)[C@@H](CO)N1C=C(C(=O)C2=C1C=C(C(=C2)CC3=C(C(=CC=C3)Cl)F)OC)C(=O)O
  InChI: InChI=1S/C23H23ClFNO5/c1-12(2)19(11-27)26-10-16(23(29)30)22(28)15-8-14(20(31-3)9-18(15)26)7-13-5-4-6-17(24)21(13)25/h4-6,8-10,12,19,27H,7,11H2,1-3H3,(H,29,30)/t19-/m1/s1
  InChIKey: JUZYLCPPVHEVSV-LJQANCHMSA-N
• Cross-matching ID:
  PubChem CID: 5277135
  ChEBI ID: CHEBI:72289
  CAS Number: 697761-98-1
  UNII: 4GDQ854U53
  DrugBank ID: DB09101
  TTD ID: D0QD1G
  INTEDE ID: DR0570
  ACDINA ID: D00227

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Human immunodeficiency virus Integrase (HIV IN)	TT5FH9Y	POL_HV1B1	Modulator	[1]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4) Main DME	DE4LYSA	CP3A4_HUMAN	Substrate	[3]
UDP-glucuronosyltransferase 1A1 (UGT1A1) Main DME	DEYGVN4	UD11_HUMAN	Substrate	[4]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Elvitegravir (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Ivosidenib	DM8S6T7	Moderate	Increased metabolism of Elvitegravir caused by Ivosidenib mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[5]
Arn-509	DMT81LZ	Major	Increased metabolism of Elvitegravir caused by Arn-509 mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[6]
Erdafitinib	DMI782S	Major	Increased metabolism of Elvitegravir caused by Erdafitinib mediated induction of CYP450 enzyme.	Bladder cancer [2C94]	[7]
Pexidartinib	DMS2J0Z	Moderate	Increased metabolism of Elvitegravir caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[5]
Lumacaftor	DMCLWDJ	Major	Increased metabolism of Elvitegravir caused by Lumacaftor mediated induction of CYP450 enzyme.	Cystic fibrosis [CA25]	[6]
Eslicarbazepine	DMZREFQ	Moderate	Increased metabolism of Elvitegravir caused by Eslicarbazepine mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[5]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Elvitegravir caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[5]
Elagolix	DMB2C0E	Moderate	Increased metabolism of Elvitegravir caused by Elagolix mediated induction of CYP450 enzyme.	Uterine fibroid [2E86]	[5]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
FD&C blue no. 2	E00446	2723854	Colorant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Carmellose sodium	E00625	Not Available	Disintegrant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 3350	E00652	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyvinyl alcohol	E00666	Not Available	Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Water	E00035	962	Solvent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Elvitegravir 150 mg tablet	150 mg	Oral Tablet	Oral
Elvitegravir 85 mg tablet	85 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [2] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [3] FDA Label of Elvitegravir. The 2020 official website of the U.S. Food and Drug Administration.
• [4] Elvitegravir for the treatment of HIV infection. Drugs Today (Barc). 2014 Mar;50(3):209-17.
• [5] Cerner Multum, Inc. "Australian Product Information.".
• [6] Product Information. Genvoya (cobicistat/elvitegravir/emtricitabine/tenofov). Gilead Sciences, Foster City, CA.
• [7] Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.