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Ritonavir

Product Name
Ritonavir
CAS No.
155213-67-5
Chemical Name
Ritonavir
Synonyms
Norvi;Norvir;RITONA;CS-477;ABT-538;A 84538;Ritonavi;RITONAVIR;litonavir;NSC 693184
CBNumber
CB0119429
Molecular Formula
C37H48N6O5S2
Formula Weight
720.94
MOL File
155213-67-5.mol
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Ritonavir Property

Melting point:
120-122°C
Boiling point:
947.0±65.0 °C(Predicted)
Density 
1.239±0.06 g/cm3(Predicted)
Flash point:
2℃
storage temp. 
room temp
solubility 
DMSO: soluble10mg/mL (clear solution, warmed)
pka
11.47±0.46(Predicted)
form 
powder
color 
white to beige
Water Solubility 
5mg/L(ms)
Merck 
14,8238
InChIKey
NCDNCNXCDXHOMX-XGKFQTDJSA-N
CAS DataBase Reference
155213-67-5(CAS DataBase Reference)
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Safety

Hazard Codes 
Xi,Xn
Risk Statements 
36/38-20/21/22-41
Safety Statements 
26-37/39-36/37-39
RIDADR 
UN 1648 3 / PGII
WGK Germany 
3
RTECS 
XA5310000
HS Code 
29341000
Hazardous Substances Data
155213-67-5(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H225Highly Flammable liquid and vapour

H319Causes serious eye irritation

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PHR1734
Product name
Ritonavir
Packaging
1g
Price
$92.1
Updated
2021/03/22
Sigma-Aldrich
Product number
Y0000706
Product name
Ritonavir for peak identification
Purity
European Pharmacopoeia (EP) Reference Standard
Price
$190
Updated
2021/03/22
Sigma-Aldrich
Product number
1604803
Product name
Ritonavir
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
200mg
Price
$366
Updated
2021/03/22
Cayman Chemical
Product number
13872
Product name
Ritonavir
Purity
≥98%
Packaging
10mg
Price
$44
Updated
2021/03/22
Cayman Chemical
Product number
13872
Product name
Ritonavir
Purity
≥98%
Packaging
50mg
Price
$187
Updated
2021/03/22
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Ritonavir Chemical Properties,Usage,Production

Description

Norvir was launched in Germany, the UK and US for treatment of advanced HIV in combination with antiretroviral nucleoside analogs in a record 72 days by the FDA. It is an inhibitor of HIV aspartic protease which is critical in the processing of a propeptide into the gag, gag-pol gene products and the protease itself. This inhibition results in the release of non-infectous immature virus particles. It is greater than 500-fold more selective for viral aspartic protease than the human version, has good oral bioavailability and may increase the bioavailability of other protease inhibitors. Ritonavir was able to increase the CD4 and CD8 lymphocyte count as well as reduce viral RNA. It is more potent than saqunavir and comparible in potency to zidovudine and lamivudine.

Chemical Properties

White or almost white powder.

Originator

Abbott (USA)

Uses

Protease inhibitor; antiviral (HIV).

Uses

Ritonivir is an HIV protease inhibitor (EC50 = 25 nM) that also inhibits CYP3A4, the primary cytochrome P450 isoform that metabolizes protease inhibitors. Through CYP3A4 inhibition, low doses of ritonivir can reduce the metabolism of concomitantly administered protease inhibitiors, enhancing their bioavailability and efficacy.[Cayman Chemical]

Uses

A selective HIV protease inhibitor

Definition

ChEBI: An L-valine derivative that is an antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.

Indications

Although ritonavir (Norvir) is a potent inhibitor of HIV-1 and HIV-2 protease, it is not well tolerated in higher doses. It is mainly used in low doses to increase blood levels of other protease inhibitors and to extend their dosing interval. Ritonavir is more commonly associated with gastrointestinal side effects, altered taste sensation, paresthesias, and hypertriglyceridemia than are other protease inhibitors. Pancreatitis may occur in the presence or absence of hypertriglyceridemia.

brand name

Norvir (Abbott).

Antimicrobial activity

Ritonavir is active against HIV-1 and, to a lesser extent, HIV-2.

Acquired resistance

At antiretroviral doses resistance is associated with the presence of specific amino acid substitutions in the HIV protease at positions 82 and 84. Concern about the risk for selection of ritonavir resistance when used at a subtherapeutic ‘booster’ dose has so far not been borne out by clinical experience.

Pharmaceutical Applications

A synthetic chemical available for oral use as soft capsules and a liquid formulation. It is now almost exclusively used as a pharmacokinetic enhancer to ‘boost’ the pharmacokinetic properties of HIV protease inhibitors in the treatment of HIV-1 infection in patients over 1 month in age.

Mechanism of action

Because of the strong CYP450-inhibiting effects of ritonavir, the drug has found value when used in fixed-dosage combinations with other PIs to block their metabolism and act as a booster for these drugs (lopinavir/ritonavir and tipranavir/ritonavir). In these cases, ritonavir is used in a subtherapeutic dose but boosts the effectiveness of the coadministered drug. The utilization of ritonavir in a therapeutic dose for treating HIV infections appears to be decreasing, but its utilization as a booster drug is finding favor.

Pharmacokinetics

Oral absorption: Not known/available
Cmax 600 mg twice daily: c. 11.2 mg/L
Cmin 600 mg twice daily: c. 3.7 mg/L
Plasma half-life: c. 3–5 h
Volume of distribution: c. 0.3–0.6 L/kg
Plasma protein binding: c. 97%
Absorption and distribution
Fasting and high-fat meals had no appreciable effect on oral absorption. It penetrates poorly into the CNS. The semen:plasma ratio is <0.04. It is distributed into breast milk.
Metabolism and excretion
Four oxidized metabolites have been identified, the major of which retains antiretroviral activity. Around 11% of the dose is excreted in urine, 4% as unchanged drug. The remainder is found in feces. Metabolites are eliminated primarily via the feces.
No dose adjustment is recommended in mild to moderate hepatic impairment. It should not be given to patients with severe hepatic impairment, nor should it be given as a pharmacokinetic enhancer to patients with decompensated liver disease.

Clinical Use

Treatment of HIV infection in adults and children >1 month old (in combination with other antiretroviral agents)

Side effects

Full (antiretroviral) doses are associated with nausea, vomiting, diarrhea and fatigue in >20% of subjects. The degree to which ritonavir at low dose is associated with specific adverse events is uncertain. In HIV-negative healthy volunteers given ‘booster’ doses of 100 mg every 12 h, the concentration of total cholesterol, low-density cholesterol and triglycerides all increased, and the concentration of high-density cholesterol concentration fell.

Ritonavir Preparation Products And Raw materials

Raw materials

Preparation Products

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Ritonavir Suppliers

TOKYO CHEMICAL INDUSTRY CO., LTD.
Tel
03-3668-0489
Fax
03-3668-0520
Email
Sales-JP@TCIchemicals.com
Country
Japan
ProdList
28438
Advantage
80
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View Lastest Price from Ritonavir manufacturers

Jinan Jianfeng Chemical Co., Ltd
Product
RITONAVIR 155213-67-5
Price
US $1.00/g
Min. Order
1g
Purity
99.99%
Supply Ability
20t
Release date
2021-11-12
Baoji Guokang Bio-Technology Co., Ltd.
Product
Ritonavir 155213-67-5
Price
US $476.00/g/Bag
Min. Order
100g
Purity
99%
Supply Ability
1t
Release date
2021-06-22
Hebei Yirun Sega Biological Technology Co. Ltd
Product
Ritonavir 155213-67-5
Price
US $80.00/KG
Min. Order
100g
Purity
99.99%
Supply Ability
5ton/Month
Release date
2021-11-26

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