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Details

Stereochemistry ACHIRAL
Molecular Formula C22H28N6O3S
Molecular Weight 456.563
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DELAVIRDINE

SMILES

CC(C)Nc1cccnc1N2CCN(CC2)C(=O)c3cc4cc(ccc4[nH]3)NS(=O)(=O)C

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

Molecular Formula C22H28N6O3S
Molecular Weight 456.563
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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. .

Originator

Curator's Comment:: # Pfizer

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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

860112000000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.18 μM
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
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
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
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
12.6 μM
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
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
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
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
180 μM × h
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
4.71 h
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
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
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
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
2.59 h
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
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
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
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
2%
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
2.3%
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%
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%
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
Doses

Doses

DosePopulationAdverse 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:
unhealthy, >18 years
Health Status: unhealthy
Age Group: >18 years
Sex: M+F
Sources:
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:
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:
unhealthy
Disc. AE: Rash...
AEs leading to
discontinuation/dose reduction:
Rash (3.2%)
Sources:
AEs

AEs

AESignificanceDosePopulation
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:
unhealthy, >18 years
Health Status: unhealthy
Age Group: >18 years
Sex: M+F
Sources:
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:
unhealthy, >18 years
Health Status: unhealthy
Age Group: >18 years
Sex: M+F
Sources:
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:
unhealthy, >18 years
Health Status: unhealthy
Age Group: >18 years
Sex: M+F
Sources:
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:
unhealthy, >18 years
Health Status: unhealthy
Age Group: >18 years
Sex: M+F
Sources:
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:
unhealthy, >18 years
Health Status: unhealthy
Age Group: >18 years
Sex: M+F
Sources:
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:
unhealthy, >18 years
Health Status: unhealthy
Age Group: >18 years
Sex: M+F
Sources:
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:
unhealthy, >18 years
Health Status: unhealthy
Age Group: >18 years
Sex: M+F
Sources:
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:
unhealthy, >18 years
Health Status: unhealthy
Age Group: >18 years
Sex: M+F
Sources:
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:
unhealthy
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



OverviewOther

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
negligible
yes [Inhibition 16.7 uM]
yes [Inhibition 16.7 uM]
yes [Inhibition 16.7 uM]
yes [Ki 12.8 uM]
yes [Ki 2.6 uM]
yes [Ki 24 uM]
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
Page: 3
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
likely
no
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
Page: 3
PubMed

PubMed

TitleDatePubMed
Activity of non-nucleoside reverse transcriptase inhibitors against HIV-2 and SIV.
1999 Aug 20
Synthesis and structure-activity relationships of the (alkylamino)piperidine-containing BHAP class of non-nucleoside reverse transcriptase inhibitors: effect of 3-alkylpyridine ring substitution.
1999 Oct 7
Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues.
2000 Aug
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.
2000 Jan 17
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
Piperidinylethyl, phenoxyethyl and fluoroethyl bromopyridyl thiourea compounds with potent anti-HIV activity.
2000 Sep
Clinical pharmacokinetics of non-nucleoside reverse transcriptase inhibitors.
2001
A single amino acid change at Leu-188 in the reverse transcriptase of HIV-2 and SIV renders them sensitive to non-nucleoside reverse transcriptase inhibitors.
2001
Saquinavir soft gelatin capsule: a comparative safety review.
2001
Delavirdine: clinical pharmacokinetics and drug interactions.
2001
Amino acid deletion at codon 67 and Thr-to-Gly change at codon 69 of human immunodeficiency virus type 1 reverse transcriptase confer novel drug resistance profiles.
2001 Apr
Determination of serum levels of thirteen human immunodeficiency virus-suppressing drugs by high-performance liquid chromatography.
2001 Apr 13
High prevalence of genotypic and phenotypic HIV-1 drug-resistant strains among patients receiving antiretroviral therapy in Abidjan, Côte d'Ivoire.
2001 Apr 15
Antiretrovirals: simultaneous determination of five protease inhibitors and three nonnucleoside transcriptase inhibitors in human plasma by a rapid high-performance liquid chromatography--mass spectrometry assay.
2001 Aug
Antiviral drugs: current state of the art.
2001 Aug
Inhibition of human cytochrome P450 isoforms by nonnucleoside reverse transcriptase inhibitors.
2001 Jan
Interaction of delavirdine with human liver microsomal cytochrome P450: inhibition of CYP2C9, CYP2C19, and CYP2D6.
2001 Jan
New developments in anti-HIV chemotherapy.
2001 Jan-Feb
Phenotypic hypersusceptibility to non-nucleoside reverse transcriptase inhibitors in treatment-experienced HIV-infected patients: impact on virological response to efavirenz-based therapy.
2001 Jun 15
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.
2001 Jun 7
New developments in anti-HIV chemotherapy.
2001 Nov
Anti-human immunodeficiency virus drugs are ineffective against Pneumocystis carinii in vitro and in vivo.
2001 Nov 15
Drugs for HIV infection.
2001 Nov 26
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
Can delavirdine substitute for ritonavir?
2001 Nov-Dec
HIV-protease inhibitors alter retinoic acid synthesis.
2001 Oct 19
Mismatched double-stranded RNA (polyI-polyC(12)U) is synergistic with multiple anti-HIV drugs and is active against drug-sensitive and drug-resistant HIV-1 in vitro.
2001 Sep
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
2001 Sep 3
Non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors: past, present, and future perspectives.
2002
Rhabdomyolysis with acute renal failure probably related to the interaction of atorvastatin and delavirdine.
2002 Apr 15
Pharmacokinetic interaction between amprenavir and delavirdine: evidence of induced clearance by amprenavir.
2002 Dec
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
Differential modulation of P-glycoprotein expression and activity by non-nucleoside HIV-1 reverse transcriptase inhibitors in cell culture.
2002 Jul
Delavirdine in rescue regimens.
2002 May-Jun
Polymorphisms of cytotoxic T-lymphocyte (CTL) and T-helper epitopes within reverse transcriptase (RT) of HIV-1 subtype C from Ethiopia and Botswana following selection of antiretroviral drug resistance.
2002 Nov
Effect of delavirdine on plasma lipids and lipoproteins in patients receiving antiretroviral therapy.
2002 Sep 6
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
2003 Dec 15
Provider bias in the selection of non-nucleoside reverse transcriptase inhibitor and protease inhibitor-based highly active antiretroviral therapy and HIV treatment outcomes in observational studies.
2003 Dec 5
Comparison of nine resistance interpretation systems for HIV-1 genotyping.
2003 Jun
Protease inhibitor-sparing regimens: new evidence strengthens position.
2003 Jun 1
Effects of imatinib mesylate (STI571, Glivec) on the pharmacokinetics of simvastatin, a cytochrome p450 3A4 substrate, in patients with chronic myeloid leukaemia.
2003 Nov 17
Modest decreases in NNRTI susceptibility do not influence virological outcome in patients receiving initial NNRTI-containing triple therapy.
2003 Oct
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
2003 Oct 9
Pfizer announces free drug program.
2003 Sep
Susceptibility of HIV-2, SIV and SHIV to various anti-HIV-1 compounds: implications for treatment and postexposure prophylaxis.
2004 Feb
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
2004 Feb 26
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
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
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 anti-HIV-1 activity of delavirdine was assessed by infecting cell lines of lymphoblastic and monocytic origin and peripheral blood lymphocytes
Substance Class Chemical
Created
by admin
on Sat Jun 26 00:55:58 UTC 2021
Edited
by admin
on Sat Jun 26 00:55:58 UTC 2021
Record UNII
DOL5F9JD3E
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DELAVIRDINE
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
DELAVIRDINE [VANDF]
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
DELAVIRDINE [WHO-DD]
Common Name English
DELAVIRDINE [MI]
Common Name English
Classification Tree Code System Code
NDF-RT N0000009948
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
WHO-VATC QJ05AG02
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
LIVERTOX 277
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
NDF-RT N0000175460
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
NCI_THESAURUS C97453
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
NDF-RT N0000175463
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
WHO-ATC J05AG02
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
Code System Code Type Description
DRUG BANK
DB00705
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
NCI_THESAURUS
C65366
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
LACTMED
Delavirdine
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
INN
7234
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
ChEMBL
CHEMBL593
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
RXCUI
83816
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY RxNorm
DRUG CENTRAL
799
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
FDA UNII
DOL5F9JD3E
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
MERCK INDEX
M4152
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY Merck Index
MESH
D020008
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
EVMPD
SUB06949MIG
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
WIKIPEDIA
DELAVIRDINE
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
PUBCHEM
5625
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
CAS
136817-59-9
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
EPA CompTox
136817-59-9
Created by admin on Sat Jun 26 00:55:59 UTC 2021 , Edited by admin on Sat Jun 26 00:55:59 UTC 2021
PRIMARY
Related Record Type Details
TRANSPORTER -> INHIBITOR
TARGET ORGANISM->INHIBITOR
Delavirdine has demonstrated an IC50 of 0.26 micromolar against recombinant reverse transcriptase; at 3 micromolar, it halted the spread of virus in MT-4 cells and blocked replication of primary HIV-1 isolates in peripheral blood lymphocytes, including zidovudine-resistant variants.
METABOLIC ENZYME -> INDUCER
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
MAJOR
METABOLIC ENZYME -> INHIBITOR
BINDER->LIGAND
BINDING
EXCRETED UNCHANGED
URINE
METABOLIC ENZYME -> INDUCER
METABOLIC ENZYME -> SUBSTRATE
MINOR
TRANSPORTER -> INHIBITOR
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> INDUCER
METABOLIC ENZYME -> INDUCER
Related Record Type Details
METABOLITE -> PARENT
Delavirdine is primarily metabolized by cytochrome P450 3A (CYP3A), but in vitro data suggest that delavirdine may also be metabolized by CYP2D6
MAJOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC 3 TIMES DAILY

DOSE

Tmax PHARMACOKINETIC ORAL ADMINISTRATION