Mechanism of action 2016 Apr 15;62(8):972-9. doi: 10.1093/cid/civ1213. Cytotoxic doses are well above therapeutic doses, providing a wide safety margin.
Consequently, the induction and selection of mutations conferring resistance to this drug may be slower and more difficult, resulting in its antiviral effect remaining unchanged for prolonged periods. Clipboard, Search History, and several other advanced features are temporarily unavailable. Darunavir was approved for medical use in the United States in 2006 and in the European Union in February 2007.It is indicated for the treatment of human immunodeficiency virus (HIV-1) infection in adults and children three years of age and older when co-administered with ritonavir, in combination with other antiretroviral agents.Darunavir is generally well tolerated by people. Darunavir may interact with medications commonly taken by people with HIV/AIDS such as other antiretrovirals, and antacids such as proton pump inhibitors and H2 receptor antagonists. Immature, non-infectious viral particles are Elsevier Science Drugs.
There are no problems of pharmacodynamic antagonism with any of these drugs. Darunavir is a human immunodeficiency virus type 1 (HIV-1) protease nonpeptidic inhibitor, with activity against HIV. Elsevier Science Furthermore, these characteristics allow oral administration (preferably with meals), once-daily administration in non-resistant HIV strains, and a less complicated treatment regimen with improved convenience in highly varied contexts, including mild-to-moderate renal and hepatic impairment. Upon oral administration, darunavir selectively targets and binds to the active site of HIV-1 protease, and inhibits the dimerization and catalytic activity of HIV-1 protease. Darunavir, in the form of darunavir ethanolate, has the following chemical name: [(1 S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl) propyl]-carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester monoethanolate.
Online ahead of print. This site needs JavaScript to work properly. Rash is the most common side effect (7% of patients).Darunavir may interact with medications commonly taken by people with Darunavir is a nonpeptidic inhibitor of protease (PR) that lodges itself in the active site of PR through a number of hydrogen bonds.The chemical activity of the HIV-1 protease depends on two residues in the active site, Asp25 and Asp25’, one from each copy of the homodimer.In the US and UK, healthcare costs were estimated to be lower with boosted darunavir than with investigator-selected control protease inhibitors in treatment-experienced patients.Darunavir was approved for use in the United States in June 2006 and for use in the European Union in February 2007.The development of first-generation clinical inhibitors was founded on creating more protease-ligand interactions through hydrogen bonding and hydrophobic interactions.O=S(=O)(c1ccc(N)cc1)N(CC(C)C)C[C@@H](O)[C@@H](NC(=O)O[C@H]2CO[C@H]3OCC[C@@H]23)Cc4ccccc4InChI=1S/C27H37N3O7S/c1-18(2)15-30(38(33,34)21-10-8-20(28)9-11-21)16-24(31)23(14-19-6-4-3-5-7-19)29-27(32)37-25-17-36-26-22(25)12-13-35-26/h3-11,18,22-26,31H,12-17,28H2,1-2H3,(H,29,32)/t22-,23-,24+,25-,26+/m0/s1 MBio. 2018 Mar 6;9(2). Mechanism of Darunavir (DRV)'s High Genetic Barrier to HIV-1 Resistance: A Key V32I Substitution in Protease Rarely Occurs, but Once It Occurs, It Predisposes HIV-1 To Develop DRV Resistance. 2009;69(4):477-503. doi: 10.2165/00003495-200969040-00007.Drugs. Darunavir is an orally-bioavailable non-peptidic inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that selectively inhibits HIV-1 protease enzyme induced cleavage of gag and gag-pol poly-proteins preventing the maturation of virions and also inhibits the dimerization of HIV-1 protease suppressing proteolytic activity and subsequent replication of HIV-1. doi: 10.1016/s0213-005x(08)76547-9. This drug is a nonpeptide PI, with a distinct chemical structure that, by conferring it drug with enhanced binding affinity and a slower dissociation rate, makes it more potent than the remaining PIs developed to date. The potential of darunavir for pharmacological interactions is highly acceptable and this drug can be administered without dose adjustments with almost all antiretroviral agents except maraviroc, lopinavir, saquinavir and tipranavir.
The spectrum of action is very wide, and darunavir is effective against all subtypes of HIV-1 and against HIV-2 and acts well in mononuclear and monocyte/macrophage cell lines.
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