Pharmaceutical CAS 1051375-16-6 Dolutegravir Purity Dolutegravir Sodium Powder Intermediate Dolutegravir
Product Description
Product Details
Product Name |
Dolutegravir |
CAS No. |
1051375-16-6 |
MF |
C20H19F2N3O5 |
MW |
419.38 |
Appearance and shape |
White to off-white crystalline powder |
Dolutegravir sodium (Tivicay), developed and marketed by GlaxoSmithKline, was approved by the FDA in August 2013 as a novel integrase inhibitor for the treatment of HIV infection.Dolutegravir was fast-tracked by the FDA in February 2012, and joins an important class of drugs known as Integrase Strand Transfer inhibitors (INSTi's).INSTi's are characterized by their two-metal-chelating scaffolds, which are known to chelate Mg2+ cofactors in the enzyme active site, l interrupting function of HIV-1 integrase, which is essential for replication of viral DNA into host chromatin.Other drugs in this class, raltegravir and elvitegravir, are known to require either high dosages or PK boosting agents, respectively, with raltegravir also exhibiting substantial loss of potency in several major HIV-1 integrase mutation pathways.Dolutegravir was pursued with the goal of developing a novel INSTi with a once-daily, low-dosage treatment with improved resistance profile and without the need for the use of a PK boosting agent.Dolutegravir sodium has been approved for treating a broad population of HIV-infected patients, including adults undergoing their first treatment as well as those who have been treated with other integrase transfer strand inhibiting agents.
Application & Function
1. Dolutegravir (GSK1349572) is a HIV integrase inhibitor with an IC50 of 2.7 nM and is moderately effective against the significant mutants Y143R, Q148K, N155H, and G140S/Q148H against Raltegravir.
2. Dolutegravir is a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir is currently in Phase III clinical trials for the treatment of HIV infection. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.
Specification