Raltegravir
From Proteopedia
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<applet load="" size="480" color="" frame="true" spin="on" Scene ="" align="right" caption="Raltegravir, better known as Isentress, ([[___]])"/> | <applet load="" size="480" color="" frame="true" spin="on" Scene ="" align="right" caption="Raltegravir, better known as Isentress, ([[___]])"/> | ||
===Better Known as: Isentress=== | ===Better Known as: Isentress=== | ||
| - | * Marketed By: Merck & Co. | + | * Marketed By: Merck & Co. |
| - | * Major Indication: [[Human Immunodeficiency Virus]] Infection | + | * Major Indication: [[Human Immunodeficiency Virus]] Infection |
* Drug Class: [[Retroviral Integrase]] Inhibitor | * Drug Class: [[Retroviral Integrase]] Inhibitor | ||
| - | * | + | * FDA Approval (Patent Expiration): 2007 (2022) |
| - | * 2009 Sales: | + | * 2009 Sales: ~$1.1 Billion |
| - | * Importance: | + | * Importance: It was the first drug of the Integrase Inhibitor class to be approved by the FDA. It offers a powerful new tool to be utilized in combination therapies against [[HIV]] infections.<ref>"FDA approval of Isentress (raltegravir)". U.S. Food and Drug Administration (FDA). June 25, 2009. Retrieved 2010-11-15.</ref> |
* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information | * The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information | ||
Revision as of 17:08, 7 December 2010
|
Better Known as: Isentress
- Marketed By: Merck & Co.
- Major Indication: Human Immunodeficiency Virus Infection
- Drug Class: Retroviral Integrase Inhibitor
- FDA Approval (Patent Expiration): 2007 (2022)
- 2009 Sales: ~$1.1 Billion
- Importance: It was the first drug of the Integrase Inhibitor class to be approved by the FDA. It offers a powerful new tool to be utilized in combination therapies against HIV infections.[1]
- The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information
Mechanism of Action
Pharmacokinetics
| Retroviral Integrase Inhibitor Pharmacokinetics [2][3] | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 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
- ↑ "FDA approval of Isentress (raltegravir)". U.S. Food and Drug Administration (FDA). June 25, 2009. Retrieved 2010-11-15.
- ↑ 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
