Raltegravir
From Proteopedia
(Difference between revisions)
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| - | <applet load="" size="480" color="" frame="true" spin="on" Scene ="" align="right" caption=" | + | <applet load="" size="480" color="" frame="true" spin="on" Scene ="" align="right" caption="Raltegravir, better known as Isentress, ([[___]])"/> |
| - | ===Better Known as:=== | + | ===Better Known as: Isentress=== |
| - | * Marketed By: <br /> | + | * Marketed By: Merck & Co. <br /> |
* Major Indication: [[Human Immunodeficiency Virus]] Infection<br /> | * Major Indication: [[Human Immunodeficiency Virus]] Infection<br /> | ||
| - | * Drug Class: | + | * Drug Class: [[Retroviral Integrase]] Inhibitor |
* Date of FDA Approval (Patent Expiration): <br /> | * Date of FDA Approval (Patent Expiration): <br /> | ||
* 2009 Sales: | * 2009 Sales: | ||
Revision as of 16:57, 7 December 2010
|
Better Known as: Isentress
- Marketed By: Merck & Co.
- Major Indication: Human Immunodeficiency Virus Infection
- Drug Class: Retroviral Integrase Inhibitor
- Date of FDA Approval (Patent Expiration):
- 2009 Sales:
- Importance:
- The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information
Mechanism of Action
Pharmacokinetics
| Retroviral Integrase Inhibitor Pharmacokinetics [1][2] | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Parameter | Raltegravir | Elvitegravir | |||||||||
| Tmax (hr) | 1.8 | 2-4 | |||||||||
| Cmax (ng/ml) | 4253 | 2070 | |||||||||
| Bioavailability (%) | 32 | ~30 | |||||||||
| Protein Binding (%) | 83 | N/A | |||||||||
| T1/2 (hr) | 10.8 | 7.6 | |||||||||
| AUC (ng/ml/hr) | 10168 | 21200 | |||||||||
| Dosage (mg) | 400 | 150 | |||||||||
| Metabolism | Hepatic - (UGT1A1) | Hepatic - (CYP3A4) | |||||||||
References
- ↑ A Gaur, et al. Pharmacokinetics and Safety of Once-Daily Elvitegravir in HIV-Infected Adolescents. 17th Conference on Retroviruses. Poster Number: 874.
- ↑ Iwamoto M, Wenning LA, Petry AS, Laethem M, De Smet M, Kost JT, Breidinger SA, Mangin EC, Azrolan N, Greenberg HE, Haazen W, Stone JA, Gottesdiener KM, Wagner JA. Minimal effects of ritonavir and efavirenz on the pharmacokinetics of raltegravir. Antimicrob Agents Chemother. 2008 Dec;52(12):4338-43. Epub 2008 Oct 6. PMID:18838589 doi:10.1128/AAC.01543-07
