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Dolutegravir (DTG) is a second-generation integrase strand transfer inhibitor (INSTI) and INSTIs are the latest class of potent anti-HIV drugs.Compared to the first generation INSTIs, raltegravir, and elvitegravir, Dolutegravir shows a limited cross-resistance profile.More interestingly, clinical resistance mutations to Dolutegravir in treatment-naive patents have not been observed to this date.Dolutegravir is a dominant strategy in the management of TN and TE patients when compared to recommended comparators.Dolutegravir had no effect on NGM/EE PK or PD. NGM/EE can be administered with DTG without dose adjustment.Dolutegravir is the integrase inhibitor of choice for rescue therapy in multiresistant HIV infection, both in integrase inhibitor-naïve patients and in those previously treated with raltegravir or elvitegravir.Treatment with DTG led to less HIV-1 genetic and amino-acid diversification over time, as compared to treatment with RAL or the absence of drug.
| Molecular Weight | 441.36 |
| Formula | C20H18F2N3NaO5 |
| CAS Number | 1051375-19-9 |
| Solubility (25°C) | DMSO 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Mesplède T, et al. AIDS. Dolutegravir inhibits HIV-1 Env evolution in primary human cells.
| Related Integrase Products |
|---|
| BMS-707035
BMS-707035 is an HIV-1 integrase (IN) inhibitor. HIV-1 integrase (IN) represents a therapeutically advantageous viral target to treat HIV/AIDS in the clinic. |
| Elvitegravir
Elvitegravir (EVG) is a HIV integrase inhibitor with IC50 of 0.7 nM, 2.8 nM and 1.4 nM for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD, respectively. |
| Raltegravir
Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively. |
| MK-2048
MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively. |
| Dolutegravir
Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. |
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