Elbasvir

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Elbasvir
Clinical data
Trade namesZepatier (combination with grazoprevir)
Other namesMK-8742
License data
Routes of
administration		Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding>99.9%
MetabolismCYP3A4
Elimination half-life24 hours
Excretion>90% via faeces, <1% via urine
Identifiers
  • Dimethyl N,N’-([(6S)-6H-indolo[1,2-c] [1,3]benzoxazine-3,10-diyl]bis{1H-imidazole-5,2-diyl-(2S)-pyrrolidine-2,1-diyl[(2S)-1-oxo-3-methylbutane-1,2-diyl]})biscarbamate
JSmol)
  • CC(C)[C@@H](C(=O)N1CCC[C@H]1c2[nH]cc(n2)c3ccc4c(c3)cc-5n4[C@@H](Oc6c5ccc(c6)c7c[nH]c(n7)[C@@H]8CCCN8C(=O)[C@H](C(C)C)NC(=O)OC)c9ccccc9)NC(=O)OC
  • InChI=1S/C49H55N9O7/c1-27(2)41(54-48(61)63-5)45(59)56-20-10-14-37(56)43-50-25-34(52-43)30-17-19-36-32(22-30)23-39-33-18-16-31(24-40(33)65-47(58(36)39)29-12-8-7-9-13-29)35-26-51-44(53-35)38-15-11-21-57(38)46(60)42(28(3)4)55-49(62)64-6/h7-9,12-13,16-19,22-28,37-38,41-42,47H,10-11,14-15,20-21H2,1-6H3,(H,50,52)(H,51,53)(H,54,61)(H,55,62)/t37-,38-,41-,42-,47-/m0/s1
  • Key:BVAZQCUMNICBAQ-PZHYSIFUSA-N

Elbasvir is a drug approved by the

Zepatier, either with or without ribavirin.[2]

Elbasvir is a highly potent and selective

NS5A replication complex.[3] It has only been investigated as a combination product with other complementary hepatitis C antiviral drugs such as grazoprevir and MK-3682, and it is unclear whether elbasvir would show robust antiviral activity if it was administered by itself. Nevertheless, combination products of this type represent the most successful approach yet developed for actually curing hepatitis C, rather than merely slowing the progression of the disease.[4]

Side effects

Side effects have only been assessed in the combination with grazoprevir; see Elbasvir/grazoprevir#Side effects.[citation needed]

Interactions

Elbasvir is degraded by the liver enzyme

St. John's wort, can lead to ineffectively low plasma levels of elbasvir. Combination with CYP3A4 inhibitors may increase plasma levels.[5]

Pharmacology

Mechanism of action

Further information: Discovery and development of NS5A inhibitors § Mechanism of action

The substance blocks

virus replication and assembly.[5]

Pharmacokinetics

Elbasvir reaches peak plasma concentrations three hours after oral intake together with grazoprevir (variation between patients: three to six hours). In hepatitis C patients, steady state concentrations are found after about six days.

alpha-1-acid glycoprotein. Part of the substance is oxidised in the liver, largely by the enzyme CYP3A4. The biological half-life is 24 hours on average. Over 90% are excreted via the faeces, and less than 1% via the urine.[5][6]

References

  1. ^ FDA approves Zepatier for treatment of chronic hepatitis C genotypes 1 and 4. January 28, 2016
  2. PMID 25467591
    .
  3. S2CID 10543092
    .
  4. S2CID 207199323
    .
  5. ^ a b c Haberfeld H, ed. (2016). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag.
  6. ^ FDA Professional Drug Information on Zepatier.
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