Delavirdine

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Structural formula
Structural formula of delavirdine
General
Non-proprietary name Delavirdine
other names
  • N - {2- [4- (3- (Propan-2-ylamino) pyridin-2-yl) piperazin-1-carbonyl] -1 H -indol-5-yl} methanesulfonamide ( IUPAC )
  • Delavirdinum ( Latin )
Molecular formula
  • C 22 H 28 N 6 O 3 S (delavirdine)
  • C 22 H 28 N 6 O 3 S CH 3 SO 3 H (delavirdine mesylate)
External identifiers / databases
CAS number
  • 136817-59-9 (delavirdine)
  • 147221-93-0 (delavirdine mesylate)
PubChem 5625
DrugBank DB00705
Wikidata Q370244
Drug information
ATC code

J05 AG02

Drug class

Antivirals , non-nucleoside reverse transcriptase inhibitors

Mechanism of action

non-competitive inhibition of reverse transcriptase

properties
Molar mass
  • 456.56 g · mol -1 (delavirdine)
  • 552.67 g · mol -1 (delavirdine mesylate ·)
Physical state

firmly

Melting point

226–228 ° C (delavirdine)

safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling
no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Delavirdine (DLV) is a drug used to treat HIV- infected patients as part of combination therapy for HIV . The active ingredient is used pharmaceutically as a salt of methanesulfonic acid ( mesilate ).

Delavirdine is approved under the trade name Rescriptor (pharmaceutical company Pfizer ) in the USA and Canada ; there is no approval in Europe .

pharmacology

Delavirdine belongs to the class of non-nucleoside reverse transcriptase inhibitors (NNRTIs). The active ingredient binds non-competitively to the reverse transcriptase of HIV-I , near the substrate binding site for nucleosides . This blocks the catalytically active binding site. Only a few nucleosides can bind and the polymerization is slowed down significantly.

Pharmacokinetics

The active ingredient is taken orally in the form of tablets (usually three times a day). The absorption takes place quickly with a half-life of approx. Six hours. Excretion takes place hepatically , which means that interactions with other substances metabolized in this way cannot be ruled out.

literature

  • Conway B .: Initial therapy with protease inhibitor-sparing regimens: evaluation of nevirapine and delavirdine . In: Clin Infect Dis . Volume 30 Suppl 2, June 2000, pp. S130-S134, doi : 10.1086 / 313850 , PMID 10860897 . (free full text access)
  • M. Harris, C. Alexander, M. O'Shaughnessy, JS Montaner: Delavirdine increases drug exposure of ritonavir-boosted protease inhibitors. In: AIDS. Volume 16, Number 5, March 2002, pp. 798-799, PMID 11964540 .

Individual evidence

  1. ^ A b The Merck Index: An Encyclopedia of Chemicals, Drugs, and Biologicals , 14th Edition (Merck & Co., Inc.), Whitehouse Station, NJ, USA, 2006; P. 487, ISBN 978-0-911910-00-1 .
  2. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

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