Medical uses
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Ritonavir

Medical uses
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
2021/12/16
Sigma-Aldrich
Product number
Y0000706
Product name
Ritonavir for peak identification
Purity
European Pharmacopoeia (EP) Reference Standard
Price
$190
Updated
2021/12/16
Sigma-Aldrich
Product number
1604803
Product name
Ritonavir
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
200mg
Price
$366
Updated
2021/12/16
Sigma-Aldrich
Product number
SML0491
Product name
Ritonavir
Purity
≥98% (HPLC)
Packaging
10mg
Price
$65.5
Updated
2021/03/22
Sigma-Aldrich
Product number
SML0491
Product name
Ritonavir
Purity
≥98% (HPLC)
Packaging
50mg
Price
$264
Updated
2021/03/22
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Ritonavir Chemical Properties,Usage,Production

Medical uses

Ritonavir is indicated in combination with other antiretroviral agents for the treatment of HIV-1-infected patients.

Description

Ritonavir is an HIV protease inhibitor. It inhibits recombinant HIV-1 protease by 79% when used at a concentration of 0.5 nM. It inhibits HIV-13B-induced cell death in MT-4 human T cell leukemia cells (EC50 = 25 nM) as well as cell death induced by HIV-1LAI, HIV-2ROD, and HIV-2EHO in human MT-2 cells (IC50s = 0.045, 0.13, and 0.24 μM, respectively). Ritonavir also inhibits the cytochrome P450 (CYP) isoform CYP3A (IC50 = 0.14 μM). It inhibits CYP-mediated oxidative metabolism of the HIV protease inhibitors saquinavir (Item No. 9001893), indinavir (Item No. 15150), nelfinavir (Item No. 15144), and amprenavir (Item No. 15369) in rat and human liver microsomes in a concentration-dependent manner. Ritonavir (10 mg/kg) also prevents decreases in plasma levels of these four compounds in rats. Formulations containing ritonavir have been used in the treatment of HIV-1 infection.

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.

General Description

Ritonavir belongs to the group of protease inhibitors, which block the part of HIV called protease. Its mode of action involves binding to the protease active site and inhibiting the activity of the enzyme.

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

Shenzhen Shengda Pharmaceutical co Limited
Tel
0755-85269922
Fax
QQ:1799060443
Email
sales@shengdapharm.com
Country
China
ProdList
376
Advantage
58
Aikon International Limited
Tel
025-58859352
Fax
(5)02557626880
Email
cfding@aikonchem.com
Country
China
ProdList
14863
Advantage
58
Wisdom Drugs Co., Ltd.
Tel
Email
527536256@qq.com
Country
China
ProdList
95
Advantage
58
Taizhou Crene Biotechnology Co. Ltd.
Tel
0576-88813233
Email
sales@pharm-intermediates.com
Country
China
ProdList
1963
Advantage
58
Shanghai Dexuan Pharmaceutical Technology Co., Ltd
Tel
1701086315@qq.com
Fax
1701086315@qq.com
Email
1701086315@qq.com
Country
China
ProdList
8174
Advantage
58
wuhan dingxingtong Chemical Technology Co., Ltd Co., Ltd
Tel
027-59207796
Fax
027-59207796
Email
w13429867250@163.com
Country
China
ProdList
1965
Advantage
58
Conier Chem & Pharma Co.,Ltd,
Tel
86-023-62922305
Fax
+86-28-84559521
Email
sales@conier.com
Country
China
ProdList
147
Advantage
56
Guangzhou Belka Biological Technology Co., Ltd.
Tel
Fax
18665676617
Email
11353066@qq.com
Country
China
ProdList
9987
Advantage
58
Wuhan Chujiang Haoyu Chemical Technology Development Co., Ltd.
Tel
Email
371903194@qq.com
Country
China
ProdList
283
Advantage
58
Wuhan Biocar Pharmacy Co.,Ltd
Tel
13343447621
Fax
027-86589876
Email
linkdevil@foxmail.com
Country
China
ProdList
60
Advantage
58
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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
Hong Kong Tiansheng New Material Trading Co., Ltd
Product
Ritonavir 155213-67-5
Price
US $26.99/KG
Min. Order
1KG
Purity
99%
Supply Ability
100KG
Release date
2021-12-27
Hebei Senko Biotechnology Co., Ltd.
Product
Ritonavir 155213-67-5
Price
US $10.00/KG/Tin
Min. Order
1KG
Purity
99%
Supply Ability
10Tons Isonicotinic acid
Release date
2021-07-20

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