Raltegravir (MK-0518) is a novel HIV-1 integrase strand transfer inhibitor with potent in vitro activity against wild-type and multi-class resistant HIV-1 virus (in vitro IC95 for HIV-1 in 50% normal human serum = 33 nM). Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. Raltegravir is administered orally every 12h and does not require boosting with low-dose ritonavir (RTV) to achieve therapeutic concentrations.
| Molecular Weight | 444.42 |
| Formula | C20H21FN6O5 |
| CAS Number | 518048-05-0 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Anton Pozniak, et al. Raltegravir in patients with tuberculosis
[2] Rosa de Miguel, et al. A safety evaluation of raltegravir for the treatment of HIV
[3] Emma D Deeks. Raltegravir Once-Daily Tablet: A Review in HIV-1 Infection
[4] Francois Clavel. HIV resistance to raltegravir
[5] F Cossarini, et al. Raltegravir in treatment naive patients
| Related Integrase Products |
|---|
| Bictegravir Sodium
Bictegravir (GS-9883) Sodium is a novel and potent inhibitor of HIV-1 integrase, specifically targets IN strand transfer activity with an IC50 of 7.5 nM. |
| Lavendustin B
Lavendustin B inhibits HIV-1 integrase (IN) interaction with its cognate cellular cofactor lens epithelium-derived growth factor (LEDGF/p75). Lavendustin B is an inhibitor of Tyrosine Kinase and also a competitive inhibitor of glucose transporter 1 (Glut1). |
| Bictegravir
Bictegravir (GS-9883) is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM. |
| Raltegravir potassium
Raltegravir potassium (MK0518 potassium) is a potent integrase (IN) inhibitor, used to treat HIV infection. |
| Dolutegravir sodium
Dolutegravir sodium is a potent, second generation HIV integrase inhibitor (IC₅₀ = 2.7 nM) that displays potent antiviral activity. |
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