1. Anti-infection
    Metabolic Enzyme/Protease
  2. HIV Protease
    HIV

Ritonavir (Synonyms: A 84538; ABT 538; Abbott 84538; NSC 693184; RTV)

Cat. No.: HY-90001 Purity: 99.25%
Handling Instructions

Ritonavir is an inhibitor of HIV protease used to treat HIV infection and AIDS.

For research use only. We do not sell to patients.
Ritonavir Chemical Structure

Ritonavir Chemical Structure

CAS No. : 155213-67-5

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Description

Ritonavir is an inhibitor of HIV protease used to treat HIV infection and AIDS.

In Vitro

Ritonavir is an inhibitor of CYP3A4 mediated testosterone 6β-hydroxylation with mean Ki of 19 nM and also inhibits tolbutamide hydroxylation with IC50 of 4.2 μM[1]. Ritonavir is found to be a potent inhibitor of CYP3A-mediated biotransformations (nifedipine oxidation with IC50 of 0.07 mM, 17alpha-ethynylestradiol 2-hydroxylation with IC50 of 2 mM; terfenadine hydroxylation with IC50 of 0.14 mM). Ritonavir is also an inhibitor of the reactions mediated by CYP2D6 (IC50=2.5 mM) and CYP2C9/10 (IC50=8.0 mM)[2]. Ritonavir results in an increase in cell viability in uninfected human PBMC cultures. Ritonavir markedly decreases the susceptibility of PBMCs to apoptosis correlated with lower levels of caspase-1 expression, decreases in annexin V staining, and reduces caspase-3 activity in uninfected human PBMC cultures. Ritonavir inhibits induction of tumor necrosis factor (TNF) production by PBMCs and monocytes in a time- and dose-dependent manner at nontoxic concentrations[3]. Ritonavir inhibits p-glycoprotein-mediated extrusion of saquinavir with an IC50 of 0.2 μM, indicating a high affinity of ritonavir for p-glycoprotein[4]. Ritonavir inhibits human liver microsomal metabolism of ABT-378 potently with Ki of 13 nM. Ritonavir combined with ABT-378 (at 3:1 and 29:1 ratios) inhibits CYP3A (IC50=1.1 and 4.6 μM), albeit less potently than Ritonavir (IC50=0.14 μM)[5]

Clinical Trial
Sponsor Condition Start Date Phase
The Huesped Foundation HIV-1 infection 2013-06-30 Phase 4
International Maternal Pediatric Adolescent AIDS Clinical Trials Group HIV-1 infection 2013-11-30 Phase 4
Merck & Co Inc HIV infection 2012-11-01 Phase 4
Janssen Pharmaceutical KK 2008-05-31 Phase 4
HIV-1 infection 2008-12-31 Phase 4
References
M.Wt

720.94

Formula

C₃₇H₄₈N₆O₅S₂

CAS No.

155213-67-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

Purity: 99.25%

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Ritonavir
Cat. No.:
HY-90001
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