Delavirdine

  • N-(2 - (4 - (3 - ( propan-2- ylamino) pyridin-2- yl ) piperazine -1 -carbonyl) - 1H-indol- 5-yl) methanesulfonamid (IUPAC)
  • Delavirdinum (Latin )
  • C22H28N6O3S ( delavirdine )
  • C22H28N6O3S · CH3SO3H ( delavirdine mesylate · )

J05AG02

Antiviral, non-nucleoside reverse transcriptase inhibitors

Non- competitive inhibition of reverse transcriptase

  • 456.56 g · mol -1 ( delavirdine )
  • 552.67 g · mol -1 ( delavirdine mesylate · )

226-228 ° C ( delavirdine )

Template: Infobox chemical / molecular formula search available

Delavirdine (trade name Rescriptor ® ( U.S., CDN); manufacturer Pfizer) is a drug used to treat HIV and its later stages as part of a combination therapy for HIV. The active ingredient is used in therapy as a mesylate.

In Europe, the drug is not yet approved at present.

Pharmacology

Delavirdine belongs to the class of non-nucleoside reverse transcriptase inhibitors ( NNRTI). The drug binds non- competitively to the reverse transcriptase of HIV-I, near the substrate binding site for nucleosides. Wherein the catalytically active site is blocked. It can bind only a few nucleosides and the polymerization is slowed significantly.

Pharmacokinetics

The active substance (usually three times per day ) taken by the oral route in the form of tablets. Absorption is rapid with a half -life of about six hours. Excretion is hepatic, making interactions with other substances metabolised by this route can not be excluded.

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank AIDS (journal)
226024
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