Elvitegravir

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Elvitegravir
Stribild (fixed-dose combination)
Other namesGS-9137
License data
Routes of
administration		By mouth
ATC code
Pharmacokinetic data
Protein binding98%
Metabolismliver, via CYP3A
Elimination half-life12.9 (8.7–13.7) hours
Excretionliver 93%, renal 7%
Identifiers
  • 6-[(3-Chloro-2-fluorophenyl)methyl]-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxoquinoline-3-carboxylic acid
JSmol)
  • Clc1cccc(c1F)Cc3c(OC)cc2c(C(=O)\C(=C/N2[C@H](CO)C(C)C)C(=O)O)c3
  • 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 checkY
  • Key:JUZYLCPPVHEVSV-LJQANCHMSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Elvitegravir (EVG) is an

Genvoya.[7]

According to the results of the phase II clinical trial, patients taking once-daily elvitegravir boosted by ritonavir had greater reductions in viral load after 24 weeks compared to individuals randomized to receive a ritonavir-boosted protease inhibitor.[8]

Medical uses

In the United States, elvitegravir can be obtained either as part of the combination pills

Genvoya, or as the single pill formulation Vitekta.[9]

Vitekta is

antiretroviral therapy. It must be used in combination with a protease inhibitor that is coadministered with ritonavir as well as additional antiretroviral drug(s).[10]

Adverse effects

The most common side effects of taking elvitegravir are

rashes, and vomiting.[10][11]

Interactions and contraindications

Elvitegravir is metabolised via the liver enzyme

St John's wort.[11]

HIV protease inhibitors.[11][12]
(But ritonavir also increases elvitegravir levels by inhibiting CYP3A.)

Furthermore, elvitegravir is a weak to medium inducer of CYP1A2, CYP2C19, CYP2C9, CYP3A, and a number of UGTs; the clinical relevance of these findings is however unclear.[11]

Pharmacology

Mechanism of action

Elvitegravir inhibits the enzyme

HIV-1, and of HIV-2 to a lesser extent. The virus needs this enzyme to integrate its genetic code into the host's DNA.[11]

Pharmacokinetics

The drug is taken by mouth. When taken together with ritonavir and a meal, it reaches highest blood plasma concentrations after four hours.

Plasma half-life when combined with ritonavir is 8.7 to 13.7 hours.[11]

References

  1. ^ "Phase III Clinical Trial of Elvitegravir". Gilead Press Release. 22 July 2008. Archived from the original on 2013-02-08.
  2. ^ "Gilead and Japan Tobacco Sign Licensing Agreement for Novel HIV Integrase Inhibitor". Gilead Press Release. March 22, 2008. Archived from the original on 2013-02-08.
  3. PMID 17977962
    .
  4. PMID 17933730
    .
  5. S2CID 24183976
    .
  6. ^ "FDA Approval Bulletin". Archived from the original on 2014-11-03.
  7. ^ "Press Announcements - FDA approves new treatment for HIV". www.fda.gov. Retrieved 2016-01-10.
  8. ^ Thaczuk D, Carter M (19 September 2007). "ICAAC: Best response to elvitegravir seen when used with T-20 and other active agents". Aidsmap.com. Archived from the original on 2010-01-02.
  9. ^ "FDA Approved Drug Listing". Retrieved March 3, 2017.
  10. ^ a b "Vitekta Package Insert". Foster City, CA: Gilead Sciences, Inc. 2014. Retrieved November 1, 2014 – via U.S. Food and Drug Administration.
  11. ^ a b c d e f Haberfeld H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag.
  12. S2CID 1964934
    .

External links

  • "Elvitegravir". Drug Information Portal. U.S. National Library of Medicine.
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