Raltegravir
- CAS NO.:518048-05-0
- Empirical Formula: C20H21FN6O5
- Molecular Weight: 444.42
- MDL number: MFCD10698872
- EINECS: 610-733-3
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-03-16 07:03:48
What is Raltegravir?
Absorption
Absorbed from the gastrointestinal tract.
Description
Joining maraviroc as a unique approach to battling HIV-1, raltegravir, an inhibitor of HIV-1 integrase, represents the first in its class to be developed and launched as a combination treatment with other antiretroviral agents (NRTIs, NNRTIs, and PIs). HIV-1 integrase is essential for replication of the virus as a virally encoded enzyme that integrates the viral DNA into the genome of the host cell. Inhibition of HIV-1 integrase prevents the two-step process of endonucleolytic removal of the terminal dinucleotide from each 3′end of the viral DNA followed by the covalent integration of the viral DNA, at these modified 3′ends, into the host DNA, thereby representing a viable intervention in the viral life cycle. In vitro, raltegravir inhibited the strand transfer activity of HIV-1 integrase with an IC50 of 2–7nM with > 1,000-fold selectivity over other phosphoryltransferases. In addition, its in vitro IC95 for HIV-1 in 10% fetal bovine serum and 50% human serum was 19 and 33 nM, respectively. Raltegravir was well tolerated with no dose-related toxicities and a safety profile comparable to placebo. The most common clinical adverse events were diarrhea, nausea, vomiting, fatigue, headache, flushing, pruritus, and injection-site reactions.
The Uses of Raltegravir
Raltegravir (MK-0518, Isentress) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively.
Background
Raltegravir is an antiretroviral drug produced by Merck & Co., used to treat HIV infection. It received approval by the U.S. Food and Drug Administration (FDA) on 12 October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval.
Indications
For the treatment of HIV-1 infection in conjunction with other antiretrovirals.
What are the applications of Application
Raltegravir is Raltegravir is a potent integrase strand transfer inhibitor for (PFV) IN
Metabolism
Hepatic (UGT1A1)
Properties of Raltegravir
Melting point: | 216 °C(Solv: isopropanol (67-63-0)) |
Density | 1.46±0.1 g/cm3(Predicted) |
storage temp. | -20°C Freezer |
solubility | DMSO (Slightly), Methanol (Very Slightly) |
form | Solid |
color | White to Light Beige |
Safety information for Raltegravir
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P332+P313:IF SKIN irritation occurs: Get medical advice/attention. P337+P313:IF eye irritation persists: Get medical advice/attention. |
Computed Descriptors for Raltegravir
Abamectin manufacturer
ShreeGen Pharma Ltd (part of Rumit Group of Companies)
Equilife Laboratories Pvt Ltd
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