DELAVIRDINE

US Previously Marketed

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H28N6O3S
Molecular Weight	456.561
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)NC1=CC=CN=C1N2CCN(CC2)C(=O)C3=CC4=C(N3)C=CC(NS(C)(=O)=O)=C4

InChI

InChIKey=WHBIGIKBNXZKFE-UHFFFAOYSA-N

InChI=1S/C22H28N6O3S/c1-15(2)24-19-5-4-8-23-21(19)27-9-11-28(12-10-27)22(29)20-14-16-13-17(26-32(3,30)31)6-7-18(16)25-20/h4-8,13-15,24-26H,9-12H2,1-3H3

HIDE SMILES / InChI

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf | https://www.drugs.com/ppa/delavirdine.html

Delavirdine is a nonnucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine binds directly to reverse transcriptase (RT) and blocks RNA-dependent and DNA-dependent DNA polymerase activities. Delavirdine does not compete with template:primer or deoxynucleoside triphosphates. HIV-2 RT and human cellular DNA polymerases alfa, gamma, or delta are not inhibited by delavirdine. In addition, HIV-1 group O, a group of highly divergent strains that are uncommon in North America, may not be inhibited by delavirdine. Delavirdine is marketed under the trade name Rescriptor, indicated for the treatment of HIV-1 infection in combination with at least 2 other active antiretroviral agents when therapy is warranted. .

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Human immunodeficiency virus type 1 reverse transcriptase 70 Target ID: CHEMBL247 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/26162497 \| https://www.ncbi.nlm.nih.gov/pubmed/10514285	Inhibitor 8504		21.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
HIV-1 infection 156 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf	Primary		Approved 8583	RESCRIPTOR Approved Use RESCRIPTOR Tablets are indicated for the treatment of HIV-1 infection in combination with at least 2 other active antiretroviral agents when therapy is warranted. The following should be considered before initiating therapy with RESCRIPTOR in treatment-naive patients. There are insufficient data directly comparing antiretroviral regimens containing RESCRIPTOR with currently preferred 3-drug regimens for initial treatment of HIV. In studies comparing regimens consisting of 2 nucleoside reverse transcriptase inhibitors (NRTIs) (currently considered suboptimal) to RESCRIPTOR plus 2 NRTIs, the proportion of patients receiving the regimen containing RESCRIPTOR who achieved and sustained an HIV-1 RNA level <400 copies/mL over 1 year of therapy was relatively low (see DESCRIPTION OF CLINICAL STUDIES). Resistant virus emerges rapidly when RESCRIPTOR is administered as monotherapy. Therefore, RESCRIPTOR should always be administered in combination with other antiretroviral agents. Launch Date 1997

C_max

Value	Dose	Analyte	Population
12.6 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	200 mg 3 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
18.8 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	300 mg 3 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
26.6 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	400 mg 3 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.18 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	200 mg 3 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	N-DESISOPROPYL DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.88 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	300 mg 3 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	N-DESISOPROPYL DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.23 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	400 mg 3 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	N-DESISOPROPYL DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
35 μM DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/1999/20705s03lbl.pdf	400 mg 3 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
180 μM × h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/1999/20705s03lbl.pdf	400 mg 3 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
2.59 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	200 mg 3 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.33 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	300 mg 3 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.12 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	400 mg 3 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.71 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	200 mg 3 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	N-DESISOPROPYL DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
6.18 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	300 mg 3 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	N-DESISOPROPYL DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
7.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	400 mg 3 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	N-DESISOPROPYL DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.8 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/1999/20705s03lbl.pdf	400 mg 3 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Analyte	Population
2.3% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	200 mg 3 times / day steady-state, oral dose: 200 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.3% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	300 mg 3 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.3% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9164415/	400 mg 3 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
2% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/1999/20705s03lbl.pdf	400 mg 3 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAVIRDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
400 mg 3 times / day steady, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10348755	unhealthy, >18 years Health Status: unhealthy Age Group: >18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/10348755	Disc. AE: Rash, Oral lesion... Other AEs: Fever, Thrombocytopenia... AEs leading to discontinuation/dose reduction: Rash (grade 3-4, 36%) Oral lesion (1 patient) Function liver abnormal (2 patients) Headache (grade 4, 1 patient) Other AEs: Fever (grade 3, 1 patient) Thrombocytopenia (1 patient) Nausea (1 patient) Fatigue (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/10348755
400 mg 3 times / day multiple, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: multiple Dose: 400 mg, 3 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf	Disc. AE: Rash... AEs leading to discontinuation/dose reduction: Rash (3.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf

AEs

AE	Significance	Dose	Population
Fatigue	1 patient	400 mg 3 times / day steady, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10348755	unhealthy, >18 years Health Status: unhealthy Age Group: >18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/10348755
Nausea	1 patient	400 mg 3 times / day steady, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10348755	unhealthy, >18 years Health Status: unhealthy Age Group: >18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/10348755
Thrombocytopenia	1 patient	400 mg 3 times / day steady, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10348755	unhealthy, >18 years Health Status: unhealthy Age Group: >18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/10348755
Oral lesion	1 patient Disc. AE	400 mg 3 times / day steady, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10348755	unhealthy, >18 years Health Status: unhealthy Age Group: >18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/10348755
Function liver abnormal	2 patients Disc. AE	400 mg 3 times / day steady, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10348755	unhealthy, >18 years Health Status: unhealthy Age Group: >18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/10348755
Fever	grade 3, 1 patient	400 mg 3 times / day steady, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10348755	unhealthy, >18 years Health Status: unhealthy Age Group: >18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/10348755
Rash	grade 3-4, 36% Disc. AE	400 mg 3 times / day steady, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10348755	unhealthy, >18 years Health Status: unhealthy Age Group: >18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/10348755
Headache	grade 4, 1 patient Disc. AE	400 mg 3 times / day steady, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10348755	unhealthy, >18 years Health Status: unhealthy Age Group: >18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/10348755
Rash	3.2% Disc. AE	400 mg 3 times / day multiple, oral Highest studied dose Dose: 400 mg, 3 times / day Route: oral Route: multiple Dose: 400 mg, 3 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
	inhibitor 2438	substrate 1388 inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A 227 CYP2C19 2057 P-gp 1741 MRP1 116 MRP2 499 MRP3 246 CYP1A2 2153	CYP3A 220 P-gp 2052	P-gp 301

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 2333	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11225565/	negligible
MRP1 232	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/17172311/	yes [Inhibition 16.7 uM]
MRP2 625	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/17172311/	yes [Inhibition 16.7 uM]
MRP3 326	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/17172311/	yes [Inhibition 16.7 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf#page=3;https://pubmed.ncbi.nlm.nih.gov/11124228/ Page: 3.0	yes [Ki 12.8 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf#page=3;https://pubmed.ncbi.nlm.nih.gov/11124228/ Page: 3.0	yes [Ki 2.6 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf#page=3; https://pubmed.ncbi.nlm.nih.gov/11124228/ Page: 3.0	yes [Ki 24 uM]
CYP3A 317	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf#page=3;https://pubmed.ncbi.nlm.nih.gov/15544435/ Page: 3.0	yes [Ki 9.5 uM]	yes (co-administration study) Comment: coadministration of amprenavir with delavirdine resulted in an approximately 4-fold increase in amprenavir AUC to infinity (AUC∞) and a 6-fold increase in amprenavir Cmin Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf#page=3;https://pubmed.ncbi.nlm.nih.gov/15544435/ Page: 3.0
P-gp 1932	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/12180537/	yes
P-gp 1932	inhibitor 4027 Sources: https://aac.asm.org/content/48/4/1073	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf#page=3 Page: 3.0	likely
P-gp 2052	substrate 4014 Sources: https://aac.asm.org/content/48/4/1073	no
CYP3A 220	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf#page=3 Page: 3.0	yes	yes (co-administration study) Comment: Coadministration of RESCRIPTOR and drugs that induce CYP3A, such as rifampin, may decrease delavirdine plasma concentrations and reduce its therapeutic effect. With rifampin: 97% decrease in AUC Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020705s018lbl.pdf#page=3 Page: 3.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:119573	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:119573
ChemicalBook	CB8292151	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB8292151
eMolecules	1989427	https://www.emolecules.com/cgi-bin/more?vid=1989427
MolPort	MolPort-003-846-188	https://www.molport.com/shop/molecule-link/MolPort-003-846-188
ZINC	ZINC000018516586	http://zinc15.docking.org/substances/ZINC000018516586

PubMed

Title	Date	PubMed
Expanded-spectrum nonnucleoside reverse transcriptase inhibitors inhibit clinically relevant mutant variants of human immunodeficiency virus type 1.	1999 Dec	10582878
Long-term exposure of HIV type 1-infected cell cultures to combinations of the novel quinoxaline GW420867X with lamivudine, abacavir, and a variety of nonnucleoside reverse transcriptase inhibitors.	2000 Apr 10	10777142
Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues.	2000 Aug	10898683
Presence of 2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"-oxath iole-2",2"-dioxide) (TSAO)-resistant virus strains in TSAO-inexperienced HIV patients.	2000 Jun 10	10875608
Mutational analysis of trp-229 of human immunodeficiency virus type 1 reverse transcriptase (RT) identifies this amino acid residue as a prime target for the rational design of new non-nucleoside RT inhibitors.	2000 May	10779379
Selection and characterization of human immunodeficiency virus type 1 variants resistant to the (+) and (-) enantiomers of 2'-deoxy-3'-oxa-4'-thio-5-fluorocytidine.	2000 May	10770740
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.	2000 May 18	10821714
Delavirdine: clinical pharmacokinetics and drug interactions.	2001	11327199
The emerging roles of non-nucleoside reverse transcriptase inhibitors in antiretroviral therapy.	2001	11217868
Use of HIV protease inhibitors as pharmacoenhancers.	2001 Feb	11279888
Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138.	2001 Feb 1	11162823
Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.	2001 Feb 26	11229762
Interaction of delavirdine with human liver microsomal cytochrome P450: inhibition of CYP2C9, CYP2C19, and CYP2D6.	2001 Jan	11124228
Combination therapy with indinavir, ritonavir, and delavirdine and nucleoside reverse transcriptase inhibitors in patients with HIV/AIDS who have failed multiple antiretroviral combinations.	2001 May-Jun	11590527
Anti-human immunodeficiency virus drugs are ineffective against Pneumocystis carinii in vitro and in vivo.	2001 Nov 15	11679930
Drugs for HIV infection.	2001 Nov 26	11723420
The stereoselective targeting of a specific enzyme-substrate complex is the molecular mechanism for the synergic inhibition of HIV-1 reverse transcriptase by (R)-(-)-PPO464: a novel generation of nonnucleoside inhibitors.	2001 Nov 30	11572864
Can delavirdine substitute for ritonavir?	2001 Nov-Dec	11794866
Baseline antiretroviral drug susceptibility influences treatment response in patients receiving saquinavir-enhancing therapy.	2001 Nov-Dec	11742431
Non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors: past, present, and future perspectives.	2002	11945162
Lack of hepatotoxicity associated with nonnucleoside reverse transcriptase inhibitors.	2002 Apr 1	11917237
Synthesis, biological evaluation, and binding mode of novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles targeted at the HIV-1 reverse transcriptase.	2002 Apr 11	11931611
Rhabdomyolysis with acute renal failure probably related to the interaction of atorvastatin and delavirdine.	2002 Apr 15	11959068
Genotypic and phenotypic resistance patterns in early-stage HIV-1-infected patients failing initial therapy with stavudine, didanosine and nevirapine.	2002 Dec	12553483
Structural requirements for potent anti-human immunodeficiency virus (HIV) and sperm-immobilizing activities of cyclohexenyl thiourea and urea non-nucleoside inhibitors of HIV-1 reverse transcriptase.	2002 Dec	12444075
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.	2002 Dec 19	12477355
Nelfinavir urinary stones.	2002 Mar	11832739
Delavirdine increases drug exposure of ritonavir-boosted protease inhibitors.	2002 Mar 29	11964540
Pharmacia pilots patent share for HIV drug.	2003 Apr	12680360
Delavirdine malabsorption in HIV-infected subjects with spontaneous gastric hypoacidity.	2003 Feb	12616670
Simultaneous determination of nine antiretroviral compounds in human plasma using liquid chromatography.	2003 Feb 5	12505781
Pharmacokinetic interaction between amprenavir and delavirdine after multiple-dose administration in healthy volunteers.	2003 Jan	12534646
A V106M mutation in HIV-1 clade C viruses exposed to efavirenz confers cross-resistance to non-nucleoside reverse transcriptase inhibitors.	2003 Jan 3	12478089
Protease inhibitor-sparing regimens: new evidence strengthens position.	2003 Jun 1	12946062
Pfizer announces free drug program.	2003 Sep	14596253
Susceptibility of HIV-2, SIV and SHIV to various anti-HIV-1 compounds: implications for treatment and postexposure prophylaxis.	2004 Feb	15040537
Clinical efficacy of antiretroviral combination therapy based on protease inhibitors or non-nucleoside analogue reverse transcriptase inhibitors: indirect comparison of controlled trials.	2004 Jan 31	14742351
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants.	2004 May 6	15115397

Patents

Sample Use Guides

In Vivo Use Guide

HIV-1 infection (part of combination): Oral: 400 mg 3 times/day

Route of Administration: Oral

In Vitro Use Guide

In vitro anti-HIV-1 activity of delavirdine was assessed by infecting cell lines of lymphoblastic and monocytic origin and peripheral blood lymphocytes with laboratory and clinical isolates of HIV-1. IC50 and IC90 values (50% and 90% inhibitory concentrations) for laboratory isolates (n = 5) ranged from 0.005 to 0.030 uM and 0.04 to 0.10 uM, respectively. Mean IC50 of clinical isolates (n = 74) was 0.038 uM (range: 0.001 to 40 0.69 uM); 73 of 74 clinical isolates had an IC50

Name

Type

Language

DELAVIRDINE

Official Name

English

DELAVIRDINE [MI]

Preferred Name

English

DELAVIRDINE [VANDF]

Common Name

English

Delavirdine [WHO-DD]

Common Name

English

PIPERAZINE, 1-(3-((1-METHYLETHYL)AMINO)-2-PYRIDINYL)-4-((5-((METHYLSULFONYL)AMINO)-1H-INDOL-2-YL)CARBONYL)-

Systematic Name

English

delavirdine [INN]

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000009948