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
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
| 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
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 |
|---|---|---|
| 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 |
|
| Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues. | 2000 Aug |
|
| 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 |
|
| Saquinavir soft gelatin capsule: a comparative safety review. | 2001 |
|
| The emerging roles of non-nucleoside reverse transcriptase inhibitors in antiretroviral therapy. | 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 |
|
| Use of HIV protease inhibitors as pharmacoenhancers. | 2001 Feb |
|
| Impact of clinical reverse transcriptase sequences on the replication capacity of HIV-1 drug-resistant mutants. | 2001 Jul 5 |
|
| A randomized trial of nelfinavir, ritonavir, or delavirdine in combination with saquinavir-SGC and stavudine in treatment-experienced HIV-1-infected patients. | 2001 Mar-Apr |
|
| Baseline antiretroviral drug susceptibility influences treatment response in patients receiving saquinavir-enhancing therapy. | 2001 Nov-Dec |
|
| 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 |
|
| Simple and rapid quantification of the non-nucleoside reverse transcriptase inhibitors nevirapine, delavirdine, and efavirenz in human blood plasma using high-performance liquid chromatography with ultraviolet absorbance detection. | 2002 Jul 5 |
|
| Rifampin and rifabutin drug interactions: an update. | 2002 May 13 |
|
| Effect of delavirdine on plasma lipids and lipoproteins in patients receiving antiretroviral therapy. | 2002 Sep 6 |
|
| Comparison of nine resistance interpretation systems for HIV-1 genotyping. | 2003 Jun |
|
| Hypersusceptibility to non-nucleoside reverse transcriptase inhibitors in HIV-1. | 2003 Jun 13 |
|
| Identification and prediction of promiscuous aggregating inhibitors among known drugs. | 2003 Oct 9 |
|
| 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
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
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Sat Jun 26 00:55:58 UTC 2021
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| Record UNII |
DOL5F9JD3E
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| Record Status |
Validated (UNII)
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| Record Version |
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Official Name | English | ||
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Common Name | English | ||
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Systematic Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
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NDF-RT |
N0000009948
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WHO-VATC |
QJ05AG02
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LIVERTOX |
277
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NDF-RT |
N0000175460
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NCI_THESAURUS |
C97453
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NDF-RT |
N0000175463
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WHO-ATC |
J05AG02
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DB00705
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C65366
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Delavirdine
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7234
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CHEMBL593
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83816
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799
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DOL5F9JD3E
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M4152
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PRIMARY | Merck Index | ||
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D020008
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SUB06949MIG
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DELAVIRDINE
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5625
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136817-59-9
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136817-59-9
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TRANSPORTER -> INHIBITOR | |||
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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.
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METABOLIC ENZYME -> INDUCER | |||
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SALT/SOLVATE -> PARENT | |||
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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METABOLIC ENZYME -> INHIBITOR | |||
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BINDER->LIGAND |
BINDING
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EXCRETED UNCHANGED |
URINE
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METABOLIC ENZYME -> INDUCER | |||
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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TRANSPORTER -> INHIBITOR | |||
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TRANSPORTER -> INHIBITOR | |||
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METABOLIC ENZYME -> INDUCER | |||
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METABOLIC ENZYME -> INDUCER |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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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
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ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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| Biological Half-life | PHARMACOKINETIC |
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3 TIMES DAILY |
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| Tmax | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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