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
SMILES
CC(C)NC1=C(N=CC=C1)N2CCN(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
| Molecular Formula | C22H28N6O3S |
| Molecular Weight | 456.561 |
| 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
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 21.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | RESCRIPTOR Approved UseRESCRIPTOR 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 Date8.6011203E11 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 |
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 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 |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 |
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 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 |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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% 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 |
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: |
unhealthy, >18 years n = 30 Health Status: unhealthy Condition: HIV infection Age Group: >18 years Sex: M+F Population Size: 30 Sources: |
Disc. AE: Rash, Oral lesion... Other AEs: Fever, Thrombocytopenia... AEs leading to discontinuation/dose reduction: Rash (grade 3-4, 36%) Other AEs:Oral lesion (1 patient) Function liver abnormal (2 patients) Headache (grade 4, 1 patient) Fever (grade 3, 1 patient) Sources: Thrombocytopenia (1 patient) Nausea (1 patient) Fatigue (1 patient) |
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 n = 412 Health Status: unhealthy Population Size: 412 Sources: |
Disc. AE: Rash... AEs leading to discontinuation/dose reduction: Rash (3.2%) Sources: |
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: |
unhealthy, >18 years n = 30 Health Status: unhealthy Condition: HIV infection Age Group: >18 years Sex: M+F Population Size: 30 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 n = 30 Health Status: unhealthy Condition: HIV infection Age Group: >18 years Sex: M+F Population Size: 30 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 n = 30 Health Status: unhealthy Condition: HIV infection Age Group: >18 years Sex: M+F Population Size: 30 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 n = 30 Health Status: unhealthy Condition: HIV infection Age Group: >18 years Sex: M+F Population Size: 30 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 n = 30 Health Status: unhealthy Condition: HIV infection Age Group: >18 years Sex: M+F Population Size: 30 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 n = 30 Health Status: unhealthy Condition: HIV infection Age Group: >18 years Sex: M+F Population Size: 30 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 n = 30 Health Status: unhealthy Condition: HIV infection Age Group: >18 years Sex: M+F Population Size: 30 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 n = 30 Health Status: unhealthy Condition: HIV infection Age Group: >18 years Sex: M+F Population Size: 30 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 n = 412 Health Status: unhealthy Population Size: 412 Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical 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: 3.0 |
|||
| yes | ||||
| yes |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical 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: 3.0 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Activity of non-nucleoside reverse transcriptase inhibitors against HIV-2 and SIV. | 1999 Aug 20 |
|
| Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus. | 1999 Jun 7 |
|
| Argentine plant extracts active against polymerase and ribonuclease H activities of HIV-1 reverse transcriptase. | 1999 May |
|
| 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 |
|
| N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1. | 1999 Sep 20 |
|
| Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives. | 2000 Mar 9 |
|
| 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 |
|
| Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase. | 2000 Sep 18 |
|
| 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 |
|
| High prevalence of genotypic and phenotypic HIV-1 drug-resistant strains among patients receiving antiretroviral therapy in Abidjan, Côte d'Ivoire. | 2001 Apr 15 |
|
| Antiviral drugs: current state of the art. | 2001 Aug |
|
| Use of HIV protease inhibitors as pharmacoenhancers. | 2001 Feb |
|
| Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. | 2001 Feb 26 |
|
| 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 |
|
| 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 |
|
| 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 |
|
| Synthesis and anti-HIV-1 activity of new delavirdine analogues carrying arylpyrrole moieties. | 2001 Nov |
|
| 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 |
|
| Baseline antiretroviral drug susceptibility influences treatment response in patients receiving saquinavir-enhancing therapy. | 2001 Nov-Dec |
|
| HIV-protease inhibitors alter retinoic acid synthesis. | 2001 Oct 19 |
|
| Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. | 2001 Sep 3 |
|
| Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). | 2001 Sep 3 |
|
| Interactions between antiretroviral drugs and drugs used for the therapy of the metabolic complications encountered during HIV infection. | 2002 |
|
| 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 |
|
| New anti-HIV agents and targets. | 2002 Nov |
|
| Effect of delavirdine on plasma lipids and lipoproteins in patients receiving antiretroviral therapy. | 2002 Sep 6 |
|
| 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 |
|
| A V106M mutation in HIV-1 clade C viruses exposed to efavirenz confers cross-resistance to non-nucleoside reverse transcriptase inhibitors. | 2003 Jan 3 |
|
| 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 |
Patents
Sample Use Guides
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
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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Jul 05 23:16:42 UTC 2023
by
admin
on
Wed Jul 05 23:16:42 UTC 2023
|
| Record UNII |
DOL5F9JD3E
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NDF-RT |
N0000009948
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
||
|
WHO-VATC |
QJ05AG02
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
||
|
LIVERTOX |
NBK547899
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
||
|
NDF-RT |
N0000175460
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
||
|
NCI_THESAURUS |
C97453
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
||
|
NDF-RT |
N0000175463
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
||
|
WHO-ATC |
J05AG02
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
100000083479
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
119573
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
DB00705
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
C65366
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
Delavirdine
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
7234
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
CHEMBL593
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
83816
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | RxNorm | ||
|
799
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
DOL5F9JD3E
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
M4152
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | Merck Index | ||
|
D020008
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
SUB06949MIG
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
DELAVIRDINE
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
5625
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
136817-59-9
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY | |||
|
DTXSID6022892
Created by
admin on Wed Jul 05 23:16:42 UTC 2023 , Edited by admin on Wed Jul 05 23:16:42 UTC 2023
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
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 |
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
METABOLIC ENZYME -> SUBSTRATE |
MAJOR
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
TRANSPORTER -> INHIBITOR | |||
|
METABOLIC ENZYME -> INHIBITOR | |||
|
BINDER->LIGAND |
BINDING
|
||
|
EXCRETED UNCHANGED |
URINE
|
||
|
METABOLIC ENZYME -> INDUCER | |||
|
METABOLIC ENZYME -> SUBSTRATE |
MINOR
|
||
|
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 |
|
||
| Tmax | PHARMACOKINETIC |
|
ORAL ADMINISTRATION |
|
||