DELAVIRDINE

ChemicalBook > CAS DataBase List > DELAVIRDINE

Product Name: DELAVIRDINE
CAS No.: 136817-59-9
Chemical Name: DELAVIRDINE
Synonyms: U-90152;DELAVIRDINE;Bhap-U 90152;Delavirdine D8;Unii-dol5F9jd3e;DELAVIRDINE USP/EP/BP;147221-93-0 (Mesylate);$2200/10G,$5700/50G,96% ,IN STOCK;Delavirdine & Delavirdine Mesylate;Delavirdine - U 90152 | Rescriptor
CBNumber: CB8292151
Molecular Formula: C22H28N6O3S
Formula Weight: 456.56
MOL File: 136817-59-9.mol

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DELAVIRDINE Property

Melting point:: 226-228°C
Boiling point:: 732.0±70.0 °C(Predicted)
Density: 1.388
storage temp.: -20°C Freezer
solubility: Chloroform (Slightly), Methanol (Slightly)
form: Solid
pka: pKa1 4.56; pKa2 8.9(at 25℃)
color: Pale Yellow
Water Solubility: 30g/L(temperature not stated)

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC

Product number: D230625
Product name: Delavirdine
Packaging: 25mg
Price: $305
Updated: 2021/12/16

Usbiological

Product number: D2710
Product name: Delavirdine
Packaging: 10mg
Price: $403
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FD20973
Product name: Delavirdine
Packaging: 25mg
Price: $500
Updated: 2021/12/16

Medical Isotopes, Inc.

Product number: 8801
Product name: Delavirdine
Packaging: 10mg
Price: $845
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FD20973
Product name: Delavirdine
Packaging: 2mg
Price: $150
Updated: 2021/12/16

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DELAVIRDINE Chemical Properties,Usage,Production

Description

Delavirdine, a bisheteroarylpiperazine derivative, is a potent nonnucleoside RT inhibitor of activity specific for HIV-1. The U.S. FDA has approved this drug for use in combination with other anti-HIV agents. In Phase I/II study trials, it demonstrated sustained improvements in CD4 cell counts, p24 antigen levels, and RNA viral load. Promising results were obtained when the drug was used in two- or three-drug combinations with nucleoside drugs. Combination of delavirdine with ddI, ddC, or ZDV demonstrated additive or synergistic effects. Delavirdine with ZDV, however, was more beneficial in early HIV infection. Combinations of nevirapine and delavirdine had an antagonistic effect on HIV-1 RT inhibition.

Chemical Properties

Crystalline Solid

Uses

A bisheteroarylpiperazine (BHAP) reverse transcriptase inhibitor.

Indications

Delavirdine (Rescriptor) is approved for the treatment of HIV-1 infection in adults and adolescents over age 16 as part of a combination therapy. Rash accompanied by pruritus is the most frequent adverse effect of this agent; however, it usually resolves within several weeks of treatment. Severe skin reactions are rare. Headache, nausea, vomiting, diarrhea, fatigue, and elevated hepatic enzymes also may be associated with delavirdine administration.

Definition

ChEBI: The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor ith activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection.

brand name

Rescriptor (Agouron).

Acquired resistance

The predominant amino acid substitution associated with resistance is at position 236 of the HIV reverse transcriptase.

General Description

Delavirdine (Rescriptor) must be used with at least twoadditional antiretroviral agents to treat HIV-1 infections.The oral absorption of delavirdine is rapid, and peakplasma concentrations develop in 1 hour. Extensive metabolismoccurs in the liver by CYP isozyme 3A (CYP3A) orpossibly CYP2D6. Bioavailability is 85%. Unlike nevirapine,which is 48% protein bound, delavirdine is more than98% protein bound. The half-life is 2 to 11 hours, andelimination is 44% in feces, 51% in urine, and less than 5%unchanged in urine. Delavirdine induces its own metabolism.Oral dosage forms are supplied as a 200-mg capsuleand a 100-mg tablet.

Pharmaceutical Applications

A complex piperazine derivative, formulated for oral administration.

Mechanism of action

Delavirdine directly inhibits RT and DNA-directed DNA polymerase activities of HIV-1 after the formation of the enzyme–substrate complexes, thereby causing chain-termination effects.

Pharmacokinetics

Oral absorption: Not known/available C_max 400 mg oral thrice daily: c. 19.3 mg/L C_min 400 mg oral thrice daily: c. 8.3 mg/L Plasma half-life: c. 6 h Volume of distribution: c. 0.7 L/kg Plasma protein binding: c. 98% Absorption and distribution
It is rapidly absorbed following oral administration. Food has no significant effect on absorption. It is distributed predominantly into blood plasma and CNS penetration is poor. The semen:plasma ratio is about 0.02. It is not known if it is distributed into breast milk.
Metabolism and excretion
Several metabolites are formed by the CYP3A4 isoform of cytochrome P₄₅₀ and it is a potent inhibitor of this enzyme system. Around 44% of the drug is recovered in feces and 51% in urine, about 5% as unchanged drug. Given the predominant hepatic metabolism, caution should be exercised in patients with impaired hepatic function.

Clinical Use

Treatment of HIV disease in adults and children over 12 years of age (in combination with other antiretroviral agents)
Delavirdine has fallen out of favor with the increasing preference for antiretrovirals than can be dosed twice or once daily.

Side effects

Around 18% of patients experience a diffuse, maculopapular, erythematous and often pruritic rash. Dose titration does not appear to reduce the incidence of this side effect. The rash usually first appears within 1 month of commencing therapy and resolves within 2 weeks without dose modification. In about 4% of cases it is severe enough to warrant discontinuation of treatment.

DELAVIRDINE Preparation Products And Raw materials

Raw materials

Furan

Preparation Products

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View Lastest Price from DELAVIRDINE manufacturers

Henan Fengda Chemical Co., Ltd

Product: DELAVIRDINE 136817-59-9
Price: US $8.00-2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: g-kg-tons, free sample is available
Release date: 2024-04-24

Wuhan Quanjinci New Material Co.,Ltd.

Product: Delavirdine 136817-59-9
Price: US $80.00/kg
Min. Order: 1kg
Purity: 0.99
Supply Ability: 1000000tons
Release date: 2023-11-03

Dideu Industries Group Limited

Product: DELAVIRDINE 136817-59-9
Price: US $1.10/g
Min. Order: 1g
Purity: 99.9%
Supply Ability: 100 Tons Min
Release date: 2021-07-15

136817-59-9, DELAVIRDINERelated Search:

Indinavir NETOBIMIN (R)-7-(3-Aminohexahydro-1H-azepin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid DNA, SINGLE STRANDED, IMM. ON CELLULOSE, FROM CALF THYMUS* Tenofovir disoproxil ALOSETRON Pyruvic acid Ganciclovir 4-[[4-[[4-[(E)-2-cyanoethenyl]-2,6-dimethyl-phenyl]amino]pyrimidin-2-yl]amino]benzonitrile Etravirine Delavirdine mesylate DELAVIRDINE DELAVIRDINE, MESYLATE 3-(Ethylamino)-2-(1-piperazinyl)pyridine 3-Pyridinamine,2-(1-piperazinyl)-(9CI) 3-PYRIDYLAMINE, N-(1-METHYLETHYL)-2-(1-PIPERAZINYL)-,DIHYDROCHLORIDE MONOHYDRATE 2-(4-METHYLPIPERAZINO)-3-PYRIDINAMINE DELAVIRDINE, [3H]-

U-90152

DELAVIRDINE

1-(3-((1-Methylethyl)amino)-2-pyridinyl)-4-((5-((methylsulfonyl)amino)-1H-indol-2-yl)carbonyl)piperazine

147221-93-0 (Mesylate)

2-(4-(5-Methanesulfonamido-1H-indol-2-ylcarbonyl)-1-piperazinyl)-N-(1-methylethyl)-3-pyridinamine

Bhap-U 90152

Unii-dol5F9jd3e

Delavirdine & Delavirdine Mesylate

1-[3-(Isopropylamino)-2-pyridyl]-4-[(5-methanesulfonamidoindol-2-yl)carbonyl]piperazine

1-[3-[(1-Methylethyl)amino]-2-pyridinyl]-4-[[5-[(methylsulfonyl)amino]-1H-indol-2-y1]carbonyl]piperazine

N-[2-[[4-[3-[(1-Methylethyl)amino]-2-pyridinyl]-1-piperazinyl]carbonyl]-1H-indol-5-yl]methanesulfonamide

MethanesulfonaMide, N-[2-[[4-[3-[(1-Methylethyl)aMino]-2-pyridinyl]-1-piperazinyl]carbonyl]-1H-indol-5-yl]-

N-(2-(4-(3-(IsopropylaMino)pyridin-2-yl)piperazine-1-carbonyl)-1H-indol-5-yl)MethanesulfonaMide

$2200/10G,$5700/50G,96% ,IN STOCK

Delavirdine - U 90152 | Rescriptor

DELAVIRDINE USP/EP/BP

Delavirdine D8

136817-59-9

C22H28N6O3S

Anti-virals

Inhibitors

Intermediates & Fine Chemicals

Non-nucleoside Reverse Transcriptase

Pharmaceuticals

Anti-viral Compounds

API